PROTACDB ID,PROTAC SMILES,Active/Inactive,Best PROTAC,Cells,cLogP,Comments,Curator,Dc50,Dmax,E3 Binder SMILES,E3 Ligase,Ec50 of Ligand Cells,Ec50 of PROTAC Cells,exit_vector,Hbond acceptors,Hbond donors,Ic50 of Ligand,Ic50 of PROTAC,Ligand Name,Ligand SMILES,Linker,Linker Type,linker_ha,linker_no,linker_rb,MW,Off Targets Reported,PATENT,Ligand PDB,Ligand ID,Pubmed,PROTAC Name,Proteomics Data Available,Secondary Pubmed,Status,Target,Tested A Non Binding E3 Control,Tested Competition With Ligand,Tested Engagement In Cells,Tested Proteaseome Inhibitor,Time,TPSA
1,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CC(=O)N2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Inactive,No,MOLT-4,10.837319999999995,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CC=O,Alkane,6,3,2,1486.2819999999995,No degradation of BCL2,,4QNQ,1XJ,32145645,1a,No,,Reviewed,Q07817,No,No,No,No,48,251.07
2,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCC(=O)N2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Inactive,No,MOLT-4,11.227419999999992,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCC=O,Alkane,7,3,3,1500.3089999999993,No degradation of BCL2,,4QNQ,1XJ,32145645,1b,No,,Reviewed,Q07817,No,No,No,No,48,251.07
3,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCC(=O)N2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Inactive,No,MOLT-4,11.61751999999999,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCCC=O,Alkane,8,3,4,1514.3359999999993,No degradation of BCL2,,4QNQ,1XJ,32145645,1c,No,,Reviewed,Q07817,No,No,No,No,48,251.07
4,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCC(=O)N2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,12.007619999999987,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCCCC=O,Alkane,9,3,5,1528.3629999999994,No degradation of BCL2,,4QNQ,1XJ,32145645,1d,No,,Reviewed,Q07817,No,No,No,No,48,251.07
5,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCC(=O)N2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,12.397719999999985,IC50's are for cell viability assays,Ronen Gabizon,53 nM,~ 100 %,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCCCCC=O,Alkane,10,3,6,1542.3899999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,1e (DT2216),No,,Reviewed,Q07817,No,No,Yes,No,48,251.07
6,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCC(=O)N2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,12.787819999999982,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCCCCCC=O,Alkane,11,3,7,1556.4169999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,1f,No,,Reviewed,Q07817,No,No,No,No,48,251.07
7,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCN2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,12.090919999999986,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NCCCCC=O,Alkane,7,2,4,1500.3529999999994,No degradation of BCL2,,4QNQ,1XJ,32145645,2a,No,,Reviewed,Q07817,No,No,No,No,48,233.99999999999997
8,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,12.481019999999985,IC50's are for cell viability assays,Ronen Gabizon,93 nM,~ 90 %,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NCCCCCC=O,Alkane,8,2,5,1514.3799999999994,No degradation of BCL2,,4QNQ,1XJ,32145645,2b,No,,Reviewed,Q07817,No,No,No,No,48,233.99999999999997
9,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCN2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,12.871119999999982,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NCCCCCCC=O,Alkane,9,2,6,1528.4069999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,2c,No,,Reviewed,Q07817,No,No,No,No,48,233.99999999999997
10,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,13.26121999999998,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NCCCCCCCC=O,Alkane,10,2,7,1542.4339999999993,No degradation of BCL2,,4QNQ,1XJ,32145645,2d,No,,Reviewed,Q07817,No,No,No,No,48,233.99999999999997
11,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCC(=O)N2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,11.244019999999992,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,18,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCOCCC=O,PEG,10,4,6,1544.3619999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,3a,No,,Reviewed,Q07817,No,No,No,No,48,260.3
12,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCC(=O)N2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,10.480419999999997,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,19,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)COCCOCC=O,PEG,11,5,7,1560.3609999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,3b,No,,Reviewed,Q07817,No,No,No,No,48,269.53000000000003
13,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCC(=O)N2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,10.870519999999994,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,19,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)COCCCOCC=O,PEG,12,5,8,1574.3879999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,3c,No,,Reviewed,Q07817,No,No,No,No,48,269.53000000000003
14,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCN2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,10.937219999999995,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,18,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NCCOCC=O,PEG,7,3,4,1502.3249999999994,No degradation of BCL2,,4QNQ,1XJ,32145645,4a,No,,Reviewed,Q07817,No,No,No,No,48,243.22999999999996
15,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCN2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1,Active,No,MOLT-4,10.953819999999993,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,19,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NCCOCCOCC=O,PEG,10,4,7,1546.3779999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,4b,No,,Reviewed,Q07817,No,No,No,No,48,252.46
16,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCC(=O)N(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1,Inactive,No,MOLT-4,12.711919999999981,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,16,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCC=O,Alkane,6,1,3,1487.3099999999993,No degradation of BCL2,,4QNQ,1XJ,32145645,5,No,,Reviewed,Q07817,No,No,No,No,48,247.82999999999998
17,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCN(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1,Active,No,MOLT-4,12.405119999999984,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,16,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCC=O,Alkane,4,1,1,1445.2729999999995,No degradation of BCL2,,4QNQ,1XJ,32145645,6a,No,,Reviewed,Q07817,No,No,No,No,48,230.76
18,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1,Active,No,MOLT-4,12.795219999999983,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,16,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCC=O,Alkane,5,1,2,1459.2999999999995,No degradation of BCL2,,4QNQ,1XJ,32145645,6b,No,,Reviewed,Q07817,No,No,No,No,48,230.76
19,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCN(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1,Active,No,MOLT-4,13.18531999999998,IC50's are for cell viability assays,Ronen Gabizon,71 nM,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,16,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCC=O,Alkane,6,1,3,1473.3269999999993,No degradation of BCL2,,4QNQ,1XJ,32145645,6c,No,,Reviewed,Q07817,No,No,No,No,48,230.76
20,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1,Active,No,MOLT-4,13.575419999999978,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,16,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCC=O,Alkane,7,1,4,1487.3539999999994,No degradation of BCL2,,4QNQ,1XJ,32145645,6d,No,,Reviewed,Q07817,No,No,No,No,48,230.76
21,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCN(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1,Active,No,MOLT-4,13.965519999999977,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,16,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCCC=O,Alkane,8,1,5,1501.3809999999994,No degradation of BCL2,,4QNQ,1XJ,32145645,6e,No,,Reviewed,Q07817,No,No,No,No,48,230.76
22,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1,Active,No,MOLT-4,14.355619999999975,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,16,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCCCC=O,Alkane,9,1,6,1515.4079999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,6f,No,,Reviewed,Q07817,No,No,No,No,48,230.76
23,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCN(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1,Active,No,MOLT-4,11.268019999999993,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,18,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,COCC=O,PEG,5,2,2,1491.2979999999993,No degradation of BCL2,,4QNQ,1XJ,32145645,7a,No,,Reviewed,Q07817,No,No,No,No,48,249.22
24,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCN(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1,Active,No,MOLT-4,11.284619999999993,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,19,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,COCCOCC=O,PEG,8,3,5,1535.3509999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,7b,No,,Reviewed,Q07817,No,No,No,No,48,258.45
25,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCCN(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1,Active,No,MOLT-4,11.301219999999994,IC50's are for cell viability assays,Ronen Gabizon,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,20,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,COCCOCCOCC=O,PEG,11,4,8,1579.4039999999993,No degradation of BCL2,,4QNQ,1XJ,32145645,7c,No,,Reviewed,Q07817,No,No,No,No,48,267.68
26,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(C(=O)CCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,8.938700000000004,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,16,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCC(N)=O,Alkane,6,2,2,1314.9729999999995,No degradation of BCL2,,4QNQ,1XJ,32145645,8a,No,,Reviewed,Q07817,No,No,No,No,48,235.01999999999995
27,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(C(=O)CCCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,9.328800000000003,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,16,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCC(N)=O,Alkane,7,2,3,1328.9999999999993,No degradation of BCL2,,4QNQ,1XJ,32145645,8b,No,,Reviewed,Q07817,No,No,No,No,48,235.01999999999995
28,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(C(=O)CCCCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,9.7189,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,16,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCC(N)=O,Alkane,8,2,4,1343.0269999999991,No degradation of BCL2,,4QNQ,1XJ,32145645,8c,No,,Reviewed,Q07817,No,No,No,No,48,235.01999999999995
29,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(C(=O)CCCCCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Inactive,No,MOLT-4,10.108999999999998,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,16,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCCC(N)=O,Alkane,9,2,5,1357.0539999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,8d,No,,Reviewed,Q07817,No,No,No,No,48,235.01999999999995
30,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(C(=O)CCCCCCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Inactive,No,MOLT-4,10.499099999999997,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,16,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCCCC(N)=O,Alkane,10,2,6,1371.0809999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,8e,No,,Reviewed,Q07817,No,No,No,No,48,235.01999999999995
31,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(CCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,9.022000000000004,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,16,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCN,Alkane,4,1,1,1286.9629999999995,No degradation of BCL2,,4QNQ,1XJ,32145645,9a,No,,Reviewed,Q07817,No,No,No,No,48,217.94999999999996
32,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(CCCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,9.412100000000002,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,16,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCN,Alkane,5,1,2,1300.9899999999993,No degradation of BCL2,,4QNQ,1XJ,32145645,9b,No,,Reviewed,Q07817,No,No,No,No,48,217.94999999999996
33,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(CCCCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,9.8022,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,16,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCN,Alkane,6,1,3,1315.0169999999994,No degradation of BCL2,,4QNQ,1XJ,32145645,9c,No,,Reviewed,Q07817,No,No,No,No,48,217.94999999999996
34,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(C(=O)COCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,8.19170000000001,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,18,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCC(N)=O,PEG,10,4,6,1375.0249999999994,No degradation of BCL2,,4QNQ,1XJ,32145645,10a,No,,Reviewed,Q07817,No,No,No,No,48,253.47999999999996
35,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(C(=O)COCCOCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,8.208300000000008,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,19,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCCOCC(N)=O,PEG,13,5,9,1419.0779999999995,No degradation of BCL2,,4QNQ,1XJ,32145645,10b,No,,Reviewed,Q07817,No,No,No,No,48,262.71
36,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(C(=O)COCCOCCOCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,8.22490000000001,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,20,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCCOCCOCC(N)=O,PEG,16,6,12,1463.1309999999994,No degradation of BCL2,,4QNQ,1XJ,32145645,10c,No,,Reviewed,Q07817,No,No,No,No,48,271.93999999999994
37,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(C(=O)NCCOCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,8.374700000000006,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,18,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCCNC(N)=O,PEG,12,5,7,1404.0669999999996,No degradation of BCL2,,4QNQ,1XJ,32145645,11a,No,,Reviewed,Q07817,No,No,No,No,48,265.51
38,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(C(=S)NCCOCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Inactive,No,MOLT-4,8.539600000000005,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,18,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCCNC(N)=S,PEG,12,4,7,1420.1349999999995,No degradation of BCL2,,4QNQ,1XJ,32145645,11b,No,,Reviewed,Q07817,No,No,No,No,48,248.43999999999997
39,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(CCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,8.648500000000006,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,17,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCN,PEG,6,2,3,1316.9889999999994,No degradation of BCL2,,4QNQ,1XJ,32145645,12a,No,,Reviewed,Q07817,No,No,No,No,48,227.17999999999998
40,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(CCOCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,8.665100000000006,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,18,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCCN,PEG,9,3,6,1361.0419999999992,No degradation of BCL2,,4QNQ,1XJ,32145645,12b,No,,Reviewed,Q07817,No,No,No,No,48,236.40999999999997
41,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@@H](CCN5CCN(CCOCCOCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,Active,No,MOLT-4,8.681700000000006,IC50's are for cell viability assays,Ronen Gabizon,4.5 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,19,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCCOCCN,PEG,12,4,9,1405.0949999999993,No degradation of BCL2,,4QNQ,1XJ,32145645,12c,No,,Reviewed,Q07817,No,No,No,No,48,245.64
42,CN(CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F)C(=O)CCCn1cc(COCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)nn1,Active,No,MOLT-4,9.077800000000003,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,20,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCc1cn(CC)nn1,Other,14,5,7,1429.0770000000005,No degradation of BCL2,,4QNQ,1XJ,32145645,13a,No,,Reviewed,Q07817,No,No,No,No,48,280.94999999999993
43,CN(CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F)C(=O)CCCn1cc(COCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)nn1,Active,No,MOLT-4,9.094400000000004,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,21,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCCOCc1cn(CC)nn1,Other,17,6,10,1473.1300000000006,No degradation of BCL2,,4QNQ,1XJ,32145645,13b,No,,Reviewed,Q07817,No,No,No,No,48,290.17999999999995
44,CN(CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F)C(=O)CCCCCCn1cc(COCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)nn1,Active,No,MOLT-4,10.248099999999999,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,20,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCn1cc(COCCOCC)nn1,Other,17,5,10,1471.1580000000004,No degradation of BCL2,,4QNQ,1XJ,32145645,14a,No,,Reviewed,Q07817,No,No,No,No,48,280.94999999999993
45,CN(CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F)C(=O)CCCCCCn1cc(COCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)nn1,Active,No,MOLT-4,10.2647,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,21,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCn1cc(COCCOCCOCC)nn1,Other,20,6,13,1515.2110000000005,No degradation of BCL2,,4QNQ,1XJ,32145645,14b,No,,Reviewed,Q07817,No,No,No,No,48,290.17999999999995
46,CN(CCCCCCCn1cc(COCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)nn1)CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F,Active,No,MOLT-4,10.721499999999994,IC50's are for cell viability assays,Ronen Gabizon,6.3 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,20,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCn1cc(COCCOCC)nn1,Other,17,5,10,1457.1749999999995,No degradation of BCL2,,4QNQ,1XJ,32145645,15a,No,,Reviewed,Q07817,No,No,No,No,48,263.87999999999994
47,CN(CCCCCCCn1cc(COCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)nn1)CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F,Active,No,MOLT-4,10.738099999999994,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,21,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCn1cc(COCCOCCOCC)nn1,Other,20,6,13,1501.228,No degradation of BCL2,,4QNQ,1XJ,32145645,15b,No,,Reviewed,Q07817,No,No,No,No,48,273.10999999999996
48,CN(CCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F,Active,No,MOLT-4,9.336200000000002,IC50's are for cell viability assays,Ronen Gabizon,10.6 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,C,Alkane,1,0,0,1231.8829999999998,No degradation of BCL2,,4QNQ,1XJ,32145645,16a,No,,Reviewed,Q07817,No,No,No,No,48,214.70999999999998
49,CN(CCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F,Active,No,MOLT-4,9.726299999999998,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CC,Alkane,2,0,0,1245.9099999999999,No degradation of BCL2,,4QNQ,1XJ,32145645,16b,No,,Reviewed,Q07817,No,No,No,No,48,214.70999999999998
50,CN(CCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F,Active,No,MOLT-4,10.116399999999997,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCC,Alkane,3,0,0,1259.937,No degradation of BCL2,,4QNQ,1XJ,32145645,16c,No,,Reviewed,Q07817,No,No,No,No,48,214.70999999999998
51,CN(CCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F,Active,No,MOLT-4,10.506499999999996,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCC,Alkane,4,0,1,1273.9639999999997,No degradation of BCL2,,4QNQ,1XJ,32145645,16d,No,,Reviewed,Q07817,No,No,No,No,48,214.70999999999998
52,CN(CCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F,Inactive,No,MOLT-4,11.28669999999999,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCC,Alkane,6,0,3,1302.0179999999998,No degradation of BCL2,,4QNQ,1XJ,32145645,16e,No,,Reviewed,Q07817,No,No,No,No,48,214.70999999999998
53,CN(CCOCCOCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F,Active,No,MOLT-4,8.979300000000004,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOC,PEG,4,1,1,1305.9619999999998,No degradation of BCL2,,4QNQ,1XJ,32145645,17a,No,,Reviewed,Q07817,No,No,No,No,48,233.17
54,CN(CCOCCOCCOCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F,Active,Yes,MOLT-4,8.995900000000004,IC50's are for cell viability assays,Ronen Gabizon,2.5 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOC,PEG,7,2,4,1350.0149999999999,No degradation of BCL2,,4QNQ,1XJ,32145645,17b (XZ739),No,,Reviewed,Q07817,Yes,Yes,No,Yes,48,242.39999999999998
55,CN(CCOCCOCCOCCOCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)CC[C@@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCN(CC4=C(c5ccc(Cl)cc5)CCC(C)(C)C4)CC3)cc2)cc1S(=O)(=O)C(F)(F)F,Active,No,MOLT-4,9.012500000000005,IC50's are for cell viability assays,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,19,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCCOC,PEG,10,3,7,1394.0679999999995,No degradation of BCL2,,4QNQ,1XJ,32145645,17c,No,,Reviewed,Q07817,No,No,No,No,48,251.62999999999997
56,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCC(=O)Nc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)cc4OC)nc32)c1,Inactive,No,H1975,6.555320000000007,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,14,4,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCCCCCC=O,Alkane,12,1,9,979.1079999999996,No,,5GMP,F62,32171162,14a,No,,Reviewed,P00533,No,No,No,No,16,234.33999999999997
57,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCCNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](O)[C@H](N)Cc6ccccc6)CC5)cc4OC)nc32)c1,Inactive,No,H1975,7.093420000000008,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,,,CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O,Iap,,,aliphatic_CC,13,6,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCCCCCCN,Alkane,12,1,9,999.2709999999996,No,,5GMP,F62,32171162,14b,No,,Reviewed,P00533,No,No,No,No,16,226.14
58,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1,Active,No,H1975,13.49949999999998,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,264 nM,,COc1cc(C(=O)O)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F,Mdm2,,,aliphatic_CC,14,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCCCCCCN,Alkane,12,1,9,1307.3849999999995,No,,5GMP,F62,32171162,14c,No,,Reviewed,P00533,No,No,No,No,16,224.93999999999994
59,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCCCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1,Inactive,No,H1975,13.972899999999978,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,,,COc1cc(C(=O)O)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F,Mdm2,,,aliphatic_CC,14,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCCCCCCN,Alkane,12,1,9,1293.4019999999996,No,,5GMP,F62,32171162,14d,No,,Reviewed,P00533,No,No,No,No,16,207.86999999999995
60,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1,Active,No,H1975,8.756440000000005,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,313 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCCCCCC=O,Alkane,12,1,9,1136.4339999999997,No,,5GMP,F62,32171162,14e,No,,Reviewed,P00533,No,No,No,No,16,233.32
61,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1,Active,No,H1975,9.229840000000005,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,25.3 nM,~ 90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCCCCCC=O,Alkane,12,1,9,1122.4509999999998,"WT EGFR, 50 nM",,5GMP,F62,32171162,14f,No,,Reviewed,P00533,No,No,No,No,16,216.25
62,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1,Active,No,H1975,12.719299999999983,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,77 nM,,COc1cc(C(=O)O)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F,Mdm2,,,aliphatic_CC,14,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCCCCN,Alkane,10,1,7,1279.3309999999997,No,,5GMP,F62,32171162,14g,No,,Reviewed,P00533,No,No,No,No,16,224.93999999999994
63,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1,Inactive,No,H1975,11.939099999999986,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,,,COc1cc(C(=O)O)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F,Mdm2,,,aliphatic_CC,14,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCCN,Alkane,8,1,5,1251.2769999999998,No,,5GMP,F62,32171162,14h,No,,Reviewed,P00533,No,No,No,No,16,224.93999999999994
64,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1,Inactive,No,H1975,11.15889999999999,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,,,COc1cc(C(=O)O)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F,Mdm2,,,aliphatic_CC,14,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCN,Alkane,6,1,3,1223.2229999999997,No,,5GMP,F62,32171162,14i,No,,Reviewed,P00533,No,No,No,No,16,224.93999999999994
65,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1,Active,No,H1975,7.976240000000009,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,69 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCCCC=O,Alkane,10,1,7,1108.3799999999997,No,,5GMP,F62,32171162,14j,No,,Reviewed,P00533,No,No,No,No,16,233.32
66,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1,Active,No,H1975,7.196040000000007,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,235 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCC=O,Alkane,8,1,5,1080.3259999999996,No,,5GMP,F62,32171162,14k,No,,Reviewed,P00533,No,No,No,No,16,233.32
67,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1,Inactive,No,H1975,6.415840000000006,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCC=O,Alkane,6,1,3,1052.2719999999997,No,,5GMP,F62,32171162,14l,No,,Reviewed,P00533,No,No,No,No,16,233.32
68,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1,Active,No,H1975,8.449640000000008,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,132 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCCCC=O,Alkane,10,1,7,1094.3969999999997,No,,5GMP,F62,32171162,14m,No,,Reviewed,P00533,No,No,No,No,16,216.25
69,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1,Active,No,H1975,7.669440000000009,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,466 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCCCC=O,Alkane,8,1,5,1066.3429999999996,No,,5GMP,F62,32171162,14n,No,,Reviewed,P00533,No,No,No,No,16,216.25
70,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1,Active,Yes,H1975,6.889240000000007,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity). EC50 of PROTAC was measured in H1975 cell line",Ronen Gabizon,5.9 nM,100 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCCCC=O,Alkane,6,1,3,1038.2889999999998,No,,5GMP,F62,32171162,14o,No,,Reviewed,P00533,No,Yes,No,Yes,16,216.25
71,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1,Inactive,No,H1975,6.109040000000007,"Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)",Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,< 4 nM,,XTF-262,C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C)CC5)cc4OC)nc32)c1,CCC=O,Alkane,4,1,1,1010.2349999999996,No,,5GMP,F62,32171162,14p,No,,Reviewed,P00533,No,No,No,No,16,216.25
72,COc1cc2c(OC[C@@H]3CCC(=O)N3)ncc(C#CCOCCOCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)c2cc1C(N)=O,Inactive,No,PBMCs,3.032120000000006,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_C,14,5,2.1 nM,0.29 nM,PF-06650833 without fluorine and ethyl groupo,COc1cc2c(OC[C@@H]3CCC(=O)N3)nccc2cc1C(N)=O,C#CCOCCOCCOCCC=O,PEG,14,4,10,942.1049999999999,No,,5UIU,8CG,31312412,2,No,,Reviewed,Q9NWZ3,No,No,No,No,24,242.85999999999999
73,COc1cc2c(OC[C@@H]3CCC(=O)N3)ncc(C#CCCCCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)c2cc1C(N)=O,Active,No,PBMCs,6.493220000000005,,Ronen Gabizon,3 uM,50 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_C,11,5,2.1 nM,0.099 nM,PF-06650833 without fluorine and ethyl groupo,COc1cc2c(OC[C@@H]3CCC(=O)N3)nccc2cc1C(N)=O,C#CCCCCCCCCCCC=O,Alkane,14,1,10,936.1890000000001,No,,5UIU,8CG,31312412,3,No,,Reviewed,Q9NWZ3,Yes,No,No,No,24,215.17
74,COc1cc2c(OC[C@@H]3CCC(=O)N3)ncc(C#CCOCCOCCOCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)c2cc1C(N)=O,Inactive,No,PBMCs,0.8812000000000029,,Ronen Gabizon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_C,13,3,2.1 nM,,PF-06650833 without fluorine and ethyl groupo,COc1cc2c(OC[C@@H]3CCC(=O)N3)nccc2cc1C(N)=O,C#CCOCCOCCOCCO,PEG,13,4,9,757.7530000000002,No,,5UIU,8CG,31312412,4,No,,Reviewed,Q9NWZ3,No,No,No,No,24,224.01000000000002
75,COc1cc2c(OC[C@@H]3CCC(=O)N3)ncc(C#CCCCCCCCCCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)c2cc1C(N)=O,Inactive,No,PBMCs,4.3423000000000025,,Ronen Gabizon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_C,10,3,2.1 nM,2.5 nM,PF-06650833 without fluorine and ethyl groupo,COc1cc2c(OC[C@@H]3CCC(=O)N3)nccc2cc1C(N)=O,C#CCCCCCCCCCCO,Alkane,13,1,9,751.8370000000002,No,,5UIU,8CG,31312412,5,No,,Reviewed,Q9NWZ3,No,No,No,No,24,196.32
76,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)CCOCCOCCOCC#Cc2cnc(OC[C@@H]3CCC(=O)N3)c3cc(OC)c(C(N)=O)cc23)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Inactive,No,PBMCs,2.7436000000000096,,Ronen Gabizon,,,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,aryl_C,13,6,2.1 nM,0.022 nM,PF-06650833 without fluorine and ethyl groupo,COc1cc2c(OC[C@@H]3CCC(=O)N3)nccc2cc1C(N)=O,C#CCOCCOCCOCCC=O,PEG,14,4,10,995.1879999999995,No,,5UIU,8CG,31312412,6,No,,Reviewed,Q9NWZ3,No,No,No,No,24,250.86999999999998
77,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)CCCCCCCCCCC#Cc2cnc(OC[C@@H]3CCC(=O)N3)c3cc(OC)c(C(N)=O)cc23)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Inactive,No,PBMCs,6.204700000000008,,Ronen Gabizon,,,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,aryl_C,10,6,2.1 nM,21 nM,PF-06650833 without fluorine and ethyl groupo,COc1cc2c(OC[C@@H]3CCC(=O)N3)nccc2cc1C(N)=O,C#CCCCCCCCCCCC=O,Alkane,14,1,10,989.2719999999996,No,,5UIU,8CG,31312412,7,No,,Reviewed,Q9NWZ3,No,No,No,No,24,223.17999999999998
78,COc1cc2c(OC[C@@H]3CCC(=O)N3)ncc(C#CCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)c2cc1C(N)=O,Inactive,No,THP-1,3.3724200000000026,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_C,11,5,2.1 nM,0.099 nM,PF-06650833 without fluorine and ethyl groupo,COc1cc2c(OC[C@@H]3CCC(=O)N3)nccc2cc1C(N)=O,C#CCCC=O,Alkane,6,1,2,823.973,No,,5UIU,8CG,31312412,3B,No,,Reviewed,Q9NWZ3,Yes,No,No,No,24,215.17
79,COc1cc2c(OC[C@@H]3CCC(=O)N3)ncc(C#CCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)c2cc1C(N)=O,Inactive,No,THP-1,3.7625200000000047,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_C,11,5,2.1 nM,0.099 nM,PF-06650833 without fluorine and ethyl groupo,COc1cc2c(OC[C@@H]3CCC(=O)N3)nccc2cc1C(N)=O,C#CCCCC=O,Alkane,7,1,3,837.9999999999999,No,,5UIU,8CG,31312412,3C,No,,Reviewed,Q9NWZ3,Yes,No,No,No,24,215.17
80,CC[C@H]1[C@@H](COc2ncc(C#CCCCCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)c3cc(C(N)=O)c(OC)cc23)NC(=O)[C@H]1F,Active,No,PBMCs,7.077320000000007,,Ronen Gabizon,259 nM,90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_C,11,5,2.1 nM,,PF-06650833,CC[C@H]1[C@@H](COc2nccc3cc(C(N)=O)c(OC)cc23)NC(=O)[C@H]1F,C#CCCCCCCCCCCC=O,Alkane,14,1,10,982.2329999999997,No,,5UIU,8CG,31312412,8,No,,Reviewed,Q9NWZ3,No,No,No,No,24,215.17
81,CC[C@H]1[C@@H](COc2ncc(C#CCN3CCC4(CC3)CCN(c3ncc(C(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)cn3)CC4)c3cc(C(N)=O)c(OC)cc23)NC(=O)[C@H]1F,Active,Yes,PBMCs,4.962520000000007,,Ronen Gabizon,151 nM,90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_C,15,5,2.1 nM,,PF-06650833,CC[C@H]1[C@@H](COc2nccc3cc(C(N)=O)c(OC)cc23)NC(=O)[C@H]1F,C#CCN1CCC2(CC1)CCN(c1ncc(C=O)cn1)CC2,Other,22,5,3,1086.3049999999996,No,,5UIU,8CG,31312412,9,No,,Reviewed,Q9NWZ3,Yes,No,No,Yes,24,247.42999999999998
82,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCCCCCOCCOCCOCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,8.732860000000006,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,17,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCOCCOCCOCCCCCC=O,non-PEG polyether,18,4,15,1158.933999999999,No,,2GQG,1N1,31539241,7,No,,Reviewed,P00519,No,No,No,No,24,225.59999999999997
83,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCCOCCOCCOCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,8.259460000000006,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,17,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCOCCOCCOCCCCCC=O,non-PEG polyether,18,4,15,1172.916999999999,No,,2GQG,1N1,31539241,9,No,,Reviewed,P00519,No,No,No,No,24,242.66999999999996
84,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCOCCOCCOCCOCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,5.9520600000000075,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,19,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,COCCOCCOCCOCCOCCC=O,PEG,18,6,15,1176.8609999999992,No,,2GQG,1N1,31539241,10,No,,Reviewed,P00519,No,No,No,No,24,261.12999999999994
85,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCOCCOCCOCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,5.935460000000007,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,18,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,COCCOCCOCCOCCC=O,PEG,15,5,12,1132.8079999999993,No,,2GQG,1N1,31539241,11,No,,Reviewed,P00519,No,No,No,No,24,251.89999999999998
86,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCOCCOCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,5.918860000000006,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,17,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,COCCOCCOCCC=O,PEG,12,4,9,1088.7549999999997,No,,2GQG,1N1,31539241,12,No,,Reviewed,P00519,No,No,No,No,24,242.66999999999996
87,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCOCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,5.9022600000000045,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,16,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,COCCOCCC=O,PEG,9,3,6,1044.7019999999998,No,,2GQG,1N1,31539241,13,No,,Reviewed,P00519,No,No,No,No,24,233.43999999999994
88,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)COCCOCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,5.122060000000004,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,16,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCOCC=O,PEG,6,2,3,1016.6479999999996,No,,2GQG,1N1,31539241,14,No,,Reviewed,P00519,No,No,No,No,24,233.43999999999994
89,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCCCCCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,10.550259999999994,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,14,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCCCCCCCCCCC=O,Alkane,15,1,12,1124.9199999999992,No,,2GQG,1N1,31539241,15,No,,Reviewed,P00519,No,No,No,No,24,214.97999999999996
90,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCCCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,9.770059999999999,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,14,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCCCCCCCCC=O,Alkane,13,1,10,1096.8659999999993,No,,2GQG,1N1,31539241,16,No,,Reviewed,P00519,No,No,No,No,24,214.97999999999996
91,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Active,No,K562,8.209660000000008,,Ronen Gabizon,10.1 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,14,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCCCCC=O,Alkane,9,1,6,1040.7579999999998,No,,2GQG,1N1,31539241,17,No,,Reviewed,P00519,No,No,No,No,24,214.97999999999996
92,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Active,No,K562,7.819560000000009,,Ronen Gabizon,37.9 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,14,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCCCC=O,Alkane,8,1,5,1026.7309999999998,No,,2GQG,1N1,31539241,18,No,,Reviewed,P00519,No,No,No,No,24,214.97999999999996
93,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Active,Yes,K562,7.429460000000008,,Ronen Gabizon,8.5 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,14,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCCC=O,Alkane,7,1,4,1012.7039999999997,"EPHB4, RIPK2, Src, PDGFRβ, BTK",,2GQG,1N1,31539241,19 (SIAIS178),No,,Reviewed,P00519,Yes,Yes,Yes,Yes,24,214.97999999999996
94,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Active,No,K562,7.0393600000000065,,Ronen Gabizon,17.9 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,14,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCC=O,Alkane,6,1,3,998.6769999999997,No,,2GQG,1N1,31539241,20,No,,Reviewed,P00519,No,No,No,No,24,214.97999999999996
95,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Active,No,K562,6.649260000000006,,Ronen Gabizon,34.7 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,14,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCC=O,Alkane,5,1,2,984.6499999999996,No,,2GQG,1N1,31539241,21,No,,Reviewed,P00519,No,No,No,No,24,214.97999999999996
96,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Active,No,K562,6.259160000000006,,Ronen Gabizon,40.2 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,14,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCC=O,Alkane,4,1,1,970.6229999999997,No,,2GQG,1N1,31539241,22,No,,Reviewed,P00519,No,No,No,No,24,214.97999999999996
97,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Active,No,K562,5.869060000000005,,Ronen Gabizon,611 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,14,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CC=O,Alkane,3,1,0,956.5959999999997,No,,2GQG,1N1,31539241,23,No,,Reviewed,P00519,No,No,No,No,24,214.97999999999996
98,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCc3cn(CCCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)nn3)CC2)n1,Inactive,No,K562,6.483460000000005,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,17,5,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCc1cn(CCCC=O)nn1,Other,12,4,5,1079.7549999999997,No,,2GQG,1N1,31539241,24,No,,Reviewed,P00519,No,No,No,No,24,245.68999999999994
99,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CNC(=O)CCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,5.375360000000004,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,15,6,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,NC(=O)CCCC=O,Alkane,8,3,4,1027.6749999999995,No,,2GQG,1N1,31539241,25,No,,Reviewed,P00519,No,No,No,No,24,244.07999999999993
100,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCNC(=O)CCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,8.496160000000007,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,15,6,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCNC(=O)CCCCCCCCC=O,Alkane,16,3,11,1139.8909999999992,No,,2GQG,1N1,31539241,26,No,,Reviewed,P00519,No,No,No,No,24,244.07999999999993
101,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCCCCNC(=O)CCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Inactive,No,K562,8.969560000000005,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,15,6,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCNC(=O)CCCCCCCCC=O,Other,16,3,11,1125.9079999999992,No,,2GQG,1N1,31539241,27,No,,Reviewed,P00519,No,No,No,No,24,227.00999999999993
102,COc1cc(/C=C2\SC(=O)N(Cc3cn(CCCNC(=O)[C@@H](N)CCCNC(=N)N)nn3)C2=O)ccc1Oc1ccc(C#N)cc1C(F)(F)F,Active,No,MCF-7,3.302850000000002,,Ronen Gabizon,5 uM,> 90 %,N=C(N)NCCC[C@H](N)C(=O)O,Ubr1,,,other,12,5,,,29,COc1cc(/C=C2\SC(=O)NC2=O)ccc1Oc1ccc(C#N)cc1C(F)(F)F,Cc1cn(CCCN)nn1,Other,10,4,3,714.7310000000002,No,,3K6P,5FB,31511327,Arg-TERRalpha,No,,Reviewed,P11474,No,Yes,No,Yes,48,227.35999999999996
103,COc1cc(/C=C2\SC(=O)N(Cc3cn(CCCNC(=O)[C@@H](N)Cc4c[nH]cn4)nn3)C2=O)ccc1Oc1ccc(C#N)cc1C(F)(F)F,Active,Yes,MCF-7,4.0053800000000015,,Ronen Gabizon,0.5 uM,~ 90 %,N[C@@H](Cc1c[nH]cn1)C(=O)O,Ubr1,,,other,12,3,,,29,COc1cc(/C=C2\SC(=O)NC2=O)ccc1Oc1ccc(C#N)cc1C(F)(F)F,Cc1cn(CCCN)nn1,Other,10,4,3,695.6840000000002,No,,3K6P,5FB,31511327,His-TERRalpha,No,,Reviewed,P11474,No,Yes,No,Yes,48,194.14
104,CC[C@H](C)[C@H](N)c1cn([C@@H](Cc2ccc(O)cc2)C(=O)N2CCN(c3nc(NCCOCCOCCOCc4cn(CCOCCOCCOCCOCCOCCNC(=O)CN5CCN(C(=O)N6C(c7ccc(OC)cc7OC(C)C)=N[C@@H](c7ccc(Cl)cc7)[C@H]6c6ccc(Cl)cc6)CC5=O)nn4)nc(N4CCN(C(=O)[C@H](Cc5ccc(O)cc5)n5cc([C@@H](N)[C@@H](C)CC)nn5)CC4)n3)CC2)nn1,Active,No,Hs578t,7.887200000000026,,Ronen Gabizon,> 10 uM,,COc1ccc(C2=N[C@@H](c3ccc(Cl)cc3)[C@@H](c3ccc(Cl)cc3)N2C(=O)N2CCNC(=O)C2)c(OC(C)C)c1,Mdm2,,,amine_to_methylamine,35,6,112 nM,,IY-IY,CC[C@H](C)[C@H](N)c1cn([C@@H](Cc2ccc(O)cc2)C(=O)N2CCN(c3nc(N)nc(N4CCN(C(=O)[C@H](Cc5ccc(O)cc5)n5cc([C@@H](N)[C@@H](C)CC)nn5)CC4)n3)CC2)nn1,CCOCCOCCOCc1cn(CCOCCOCCOCCOCCOCCNC(C)=O)nn1,Other,36,13,27,1963.1529999999996,No,,,,31512882,11,No,,Reviewed,Q16288,No,No,No,No,24,460.04999999999984
105,CC[C@H](C)[C@H](N)c1cn([C@@H](Cc2ccc(O)cc2)C(=O)N2CCN(c3nc(NCCOCCOCCOCc4cn(CCCCCC(=O)Nc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)nc(N4CCN(C(=O)[C@H](Cc5ccc(O)cc5)n5cc([C@@H](N)[C@@H](C)CC)nn5)CC4)n3)CC2)nn1,Active,Yes,Hs578t,3.6765000000000114,DC50 is between 0.1uM-1uM,Ronen Gabizon,< 1 uM,100 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,29,7,112 nM,,IY-IY,CC[C@H](C)[C@H](N)c1cn([C@@H](Cc2ccc(O)cc2)C(=O)N2CCN(c3nc(N)nc(N4CCN(C(=O)[C@H](Cc5ccc(O)cc5)n5cc([C@@H](N)[C@@H](C)CC)nn5)CC4)n3)CC2)nn1,CCOCCOCCOCc1cn(CCCCCC=O)nn1,Other,22,7,15,1447.675,No,,,,31512882,4,No,,Reviewed,Q16288,No,No,No,No,24,422.7699999999999
106,CCn1nc(C2CC2)cc1Nc1nc(C(=O)NCCCCNC(=O)COc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)nc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12,Active,No,"RS4;11, MOLM-13",4.335340000000002,"Direct degration studies in this paper only conducted for first and final compounds; during the med chem campaign cell viability was used as the read out. Complex structure with the ligand was modeled based on 4Z93. IC50 of the ligand is between 2nM and 7nM, depending on which BRD. DC50 is between 3nM-10nM.",Ronen Gabizon,< 10 nM,100 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_C,15,5,< 7 nM,,HJB97,CCn1nc(C2CC2)cc1Nc1ncnc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12,O=CNCCCCNC(=O)CO,Alkane,12,5,7,871.9119999999998,No,,,,28339196,9,No,,Reviewed,"O60885, P25440, Q15059",No,No,No,No,3,257.66
107,CCn1nc(C2CC2)cc1Nc1nc(C(=O)NCCCCCCc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)nc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12,Active,No,"RS4;11, MOLM-13",6.522840000000007,"Complex structure with the ligand was modeled based on 4Z93. IC50 of the ligand is between 2nM and 7nM, depending on which BRD",Ronen Gabizon,< 1 nM,100 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_C,12,4,< 7 nM,,HJB97,CCn1nc(C2CC2)cc1Nc1ncnc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12,CCCCCCNC=O,Alkane,9,2,6,812.932,No,,,,28339196,21,No,,Reviewed,"O60885, P25440, Q15059",No,No,No,No,3,202.25999999999996
108,CCn1nc(C2CC2)cc1Nc1nc(C(=O)NCCCCCc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)nc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12,Active,Yes,"RS4;11, MOLM-13",6.132740000000006,"Complex structure with the ligand was modeled based on 4Z93. IC50 of the ligand is between 2nM and 7nM, depending on which BRD",Ronen Gabizon,< 1 nM,100 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_C,12,4,< 7 nM,,HJB97,CCn1nc(C2CC2)cc1Nc1ncnc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12,CCCCCNC=O,Alkane,8,2,5,798.905,No,,,,28339196,23 (BET-d260),No,,Reviewed,"O60885, P25440, Q15059",Yes,Yes,No,Yes,3,202.25999999999996
109,CCn1nc(C2CC2)cc1Nc1nc(C(=O)NCCCCc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)nc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12,Active,No,"RS4;11, MOLM-13",5.742640000000005,"Complex structure with the ligand was modeled based on 4Z93. IC50 of the ligand is between 2nM and 7nM, depending on which BRD",Ronen Gabizon,~ 3 nM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_C,12,4,< 7 nM,,HJB97,CCn1nc(C2CC2)cc1Nc1ncnc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12,CCCCNC=O,Alkane,7,2,4,784.8779999999999,No,,,,28339196,24,No,,Reviewed,"O60885, P25440, Q15059",No,No,No,No,3,202.25999999999996
110,CCn1nc(C2CC2)cc1Nc1nc(C(=O)NCCCc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)nc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12,Active,No,"RS4;11, MOLM-13",5.352540000000005,"Complex structure with the ligand was modeled based on 4Z93. IC50 of the ligand is between 2nM and 7nM, depending on which BRD",Ronen Gabizon,~ 10 nM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_C,12,4,< 7 nM,,HJB97,CCn1nc(C2CC2)cc1Nc1ncnc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12,CCCNC=O,Alkane,6,2,3,770.8509999999999,No,,,,28339196,25,No,,Reviewed,"O60885, P25440, Q15059",No,No,No,No,3,202.25999999999996
111,CC[C@@H]1C(=O)N(C)c2cnc(Nc3ccc(C(=O)NCCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3OC)nc2N1C1CCCC1,Active,Yes,"MV4-11, MOLM-13, KG1",3.009100000000002,They show "dual" degradation but don't do any test that the dual degradation actually made any difference. They make it sound novel but of course we can call our PROTACs "dual" degraders if you can the off-targets "targets". EC50 of ligand is in measured in MV4-11 cell line. EC50 of PROTAC is between 4.5nM-6.94nM (depended on the cell line).,Ronen Gabizon,< 5 nM,~ 100 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_C,14,4,25 nM,,BI2536,CC[C@@H]1C(=O)N(C)c2cnc(Nc3ccccc3OC)nc2N1C1CCCC1,CCOCCOCCNC=O,PEG,11,4,8,811.8969999999998,No,,4O74,R78,31708096,HBL-4,No,,Reviewed,"O60885, P53350",No,No,No,No,24,213.73000000000002
112,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)CCCCCCCCCn2cc(Nc3ncc(Cl)c(NCc4cc(F)ccc4F)n3)cn2)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Active,No,THP,8.033700000000007,Structutre with ligand is modeled in the paper.,Ronen Gabizon,2.5 uM,60 %,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,aliphatic_CC,11,6,< 1 nM,~ 100 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,CCCCCCCCC=O,Alkane,10,1,7,972.6269999999996,No,,,,32001089,7 (JP-2),No,,Reviewed,"O60674, P23458",No,No,No,No,24,187.29999999999998
113,Cc1ncsc1-c1ccc(CNC(=O)[C@H]2C[C@H](O)CN2C(=O)[C@H](NC(=O)CCCCCCCCCn2cc(Nc3ncc(Cl)c(NCc4cc(F)ccc4F)n3)cn2)C(C)(C)C)cc1,Inactive,No,THP,8.322220000000005,Structutre with ligand is modeled in the paper.,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,12,5,< 1 nM,~ 100 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,CCCCCCCCC=O,Alkane,10,1,7,919.544,No,,,,32001089,24,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,179.29000000000002
114,O=C1CCC(N2Cc3c(NC(=O)CCCCCCCCCn4cc(Nc5ncc(Cl)c(NCc6cc(F)ccc6F)n5)cn4)cccc3C2=O)C(=O)N1,Inactive,No,THP,6.480900000000006,Structutre with ligand is modeled in the paper.,Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,4,< 1 nM,< 10 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,CCCCCCCCC=O,Alkane,10,1,7,748.2350000000001,No,,,,32001089,25,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,163.24
115,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)COCCOCCOCCOCCn2cc(Nc3ncc(Cl)c(NCc4cc(F)ccc4F)n3)cn2)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Active,No,THP,4.979300000000013,Structutre with ligand is modeled in the paper.,Ronen Gabizon,> 5 uM,30 %,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,aliphatic_CC,15,6,< 1 nM,~ 10 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,COCCOCCOCCOCC=O,PEG,14,5,11,1036.6229999999998,No,,,,32001089,6 (JP-1),No,,Reviewed,"O60674, P23458",No,No,No,No,24,224.22
116,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCCn2cc(Nc3ncc(Cl)c(NCc4cc(F)ccc4F)n3)cn2)C(C)(C)C)cc1,Inactive,No,THP,5.267820000000005,Structutre with ligand is modeled in the paper.,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,5,< 1 nM,10 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,COCCOCCOCCOCC=O,PEG,14,5,11,983.5399999999997,No,,,,32001089,26,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,216.20999999999998
117,O=C1CCC(N2Cc3c(NC(=O)COCCOCCOCCOCCn4cc(Nc5ncc(Cl)c(NCc6cc(F)ccc6F)n5)cn4)cccc3C2=O)C(=O)N1,Inactive,No,THP,3.4265000000000017,Structutre with ligand is modeled in the paper.,Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,14,4,< 1 nM,10 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,COCCOCCOCCOCC=O,PEG,14,5,11,812.2310000000001,No,,,,32001089,27,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,200.16
118,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)CCCCCCCCCOc2cc(F)cc(CNc3nc(Nc4cnn(C)c4)ncc3Cl)c2F)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Active,No,THP,7.9495000000000084,Structutre with ligand is modeled in the paper.,Ronen Gabizon,> 5 uM,50 %,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,aryl_O,12,6,< 1 nM,~ 100 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,O=CCCCCCCCCCO,Alkane,12,2,9,1002.6529999999995,No,,,,32001089,13 (JP-4),No,,Reviewed,"O60674, P23458",No,No,No,No,24,196.53
119,Cc1ncsc1-c1ccc(CNC(=O)[C@H]2C[C@H](O)CN2C(=O)[C@H](NC(=O)CCCCCCCCCOc2cc(F)cc(CNc3nc(Nc4cnn(C)c4)ncc3Cl)c2F)C(C)(C)C)cc1,Inactive,No,THP,8.238020000000006,Structutre with ligand is modeled in the paper.,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,5,< 1 nM,10 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,O=CCCCCCCCCCO,Alkane,12,2,9,949.5699999999998,No,,,,32001089,28,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,188.51999999999998
120,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)cc(OCCCCCCCCCC(=O)Nc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)c3F)n2)cn1,Inactive,No,THP,6.396700000000006,Structutre with ligand is modeled in the paper.,Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,11,4,< 1 nM,< 10 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,O=CCCCCCCCCCO,Alkane,12,2,9,778.2610000000001,No,,,,32001089,29,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,172.46999999999997
121,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)COCCOCCOCCOCCOc2cc(F)cc(CNc3nc(Nc4cnn(C)c4)ncc3Cl)c2F)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Active,No,THP,4.895100000000013,Structutre with ligand is modeled in the paper.,Ronen Gabizon,~ 5 uM,60 %,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,aryl_O,16,6,< 1 nM,~ 10 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,O=CCOCCOCCOCCOCCO,PEG,16,6,13,1066.6489999999997,No,,,,32001089,10 (JP-3),No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,233.45000000000002
122,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCCOc2cc(F)cc(CNc3nc(Nc4cnn(C)c4)ncc3Cl)c2F)C(C)(C)C)cc1,Inactive,No,THP,5.183620000000005,Structutre with ligand is modeled in the paper.,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,17,5,< 1 nM,~ 10 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,O=CCOCCOCCOCCOCCO,PEG,16,6,13,1013.5659999999997,No,,,,32001089,30,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,225.44
123,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)cc(OCCOCCOCCOCCOCC(=O)Nc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)c3F)n2)cn1,Inactive,No,THP,3.3423000000000007,Structutre with ligand is modeled in the paper.,Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,15,4,< 1 nM,~ 10 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,O=CCOCCOCCOCCOCCO,PEG,16,6,13,842.2570000000001,No,,,,32001089,31,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,209.39
124,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)COCCOCCOCCOCCOCCOCCOc2cc(F)cc(CNc3nc(Nc4cnn(C)c4)ncc3Cl)c2F)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Inactive,No,THP,4.928300000000015,Structutre with ligand is modeled in the paper. IC50 of PROTAC is between 10nM-50nM.,Ronen Gabizon,,,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,aryl_O,18,6,< 1 nM,< 50 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,O=CCOCCOCCOCCOCCOCCOCCO,PEG,22,8,19,1154.755,No,,,,32001089,32,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,251.91
125,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCCOCCOCCOc2cc(F)cc(CNc3nc(Nc4cnn(C)c4)ncc3Cl)c2F)C(C)(C)C)cc1,Inactive,No,THP,5.216820000000007,Structutre with ligand is modeled in the paper. IC50 of PROTAC is between 10nM-50nM.,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,19,5,< 1 nM,< 50 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,O=CCOCCOCCOCCOCCOCCOCCO,PEG,22,8,19,1101.6719999999991,No,,,,32001089,33,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,243.89999999999998
126,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)cc(OCCOCCOCCOCCOCCOCCOCC(=O)Nc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)c3F)n2)cn1,Inactive,No,THP,3.3755000000000006,Structutre with ligand is modeled in the paper.,Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,17,4,< 1 nM,~ 10 nM,Pyrimidine 1,Cn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1,O=CCOCCOCCOCCOCCOCCOCCO,PEG,22,8,19,930.3629999999998,No,,,,32001089,34,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,227.85000000000002
127,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)CCCCCCCCCN2CCN(CCCOc3ccc(-c4cnc5cccc(-c6cc(F)c(CN7CCS(=O)(=O)CC7)c(F)c6)c5n4)cc3OC)CC2)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Active,Yes,THP,8.940800000000008,DC50 is between 1uM-2uM. Dmax is for JAK1.,Ronen Gabizon,< 2 uM,50 %,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,morpholine_to_piperazine,14,4,10 nM,> 100 nM,Quinoxaline,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCOCC1,NCCCCCCCCCC=O,Alkane,12,2,9,1273.6470000000002,No,,3KRR,DQX,32001089,17 (JP-6),No,,Reviewed,"O60674, P23458, P52333",Yes,Yes,No,Yes,24,207.73999999999995
128,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCN(CCCCCCCCCC(=O)N[C@@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1,Inactive,No,THP,9.229320000000003,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,15,3,< 1 nM,100 nM,Quinoxaline,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCOCC1,NCCCCCCCCCC=O,Alkane,12,2,9,1220.5639999999985,No,,3KRR,DQX,32001089,35,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,199.72999999999996
129,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCN(CCCCCCCCCC(=O)Nc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)CC1,Inactive,No,THP,7.388000000000007,IC50 of PROTAC is 10-100 nM,Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,13,2,< 1 nM,< 100 nM,Quinoxaline,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCOCC1,NCCCCCCCCCC=O,Alkane,12,2,9,1049.254999999999,No,,3KRR,DQX,32001089,36,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,183.67999999999998
130,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)COCCOCCOCCOCCN2CCN(CCCOc3ccc(-c4cnc5cccc(-c6cc(F)c(CN7CCS(=O)(=O)CC7)c(F)c6)c5n4)cc3OC)CC2)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Active,No,THP,5.886400000000019,Dmax is for JAK1,Ronen Gabizon,~ 2.5 uM,60 %,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,morpholine_to_piperazine,18,4,< 1 nM,100 nM,Quinoxaline,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCOCC1,NCCOCCOCCOCCOCC=O,PEG,16,6,13,1337.6430000000005,No,,3KRR,DQX,32001089,15 (JP-5),No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,244.65999999999997
131,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCN(CCOCCOCCOCCOCC(=O)N[C@@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1,Inactive,No,THP,6.174920000000011,IC50 of PROTAC is 10-100 nM,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,19,3,< 1 nM,< 100 nM,Quinoxaline,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCOCC1,NCCOCCOCCOCCOCC=O,PEG,16,6,13,1284.5599999999986,No,,3KRR,DQX,32001089,37,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,236.64999999999998
132,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCN(CCOCCOCCOCCOCC(=O)Nc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)CC1,Inactive,No,THP,4.333600000000004,,Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,17,2,< 1 nM,10 nM,Quinoxaline,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCOCC1,NCCOCCOCCOCCOCC=O,PEG,16,6,13,1113.250999999999,No,,3KRR,DQX,32001089,38,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,220.6
133,CN[C@H](C)C(=O)N[C@@H](C(=O)N1C[C@H](NC(=O)COCCOCCOCCOCCOCCOCCN2CCN(CCCOc3ccc(-c4cnc5cccc(-c6cc(F)c(CN7CCS(=O)(=O)CC7)c(F)c6)c5n4)cc3OC)CC2)C[C@@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Inactive,No,THP,5.919600000000017,,Ronen Gabizon,,,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,morpholine_to_piperazine,20,4,< 1 nM,100 nM,Quinoxaline,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCOCC1,NCCOCCOCCOCCOCCOCCOCC=O,PEG,22,8,19,1425.7490000000003,No,,3KRR,DQX,32001089,39,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,263.11999999999995
134,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCN(CCOCCOCCOCCOCCOCCOCC(=O)N[C@@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1,Inactive,No,THP,6.208120000000013,,Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,morpholine_to_piperazine,21,3,< 1 nM,100 nM,Quinoxaline,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCOCC1,NCCOCCOCCOCCOCCOCCOCC=O,PEG,22,8,19,1372.6659999999986,No,,3KRR,DQX,32001089,40,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,255.10999999999996
135,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCN(CCOCCOCCOCCOCCOCCOCC(=O)Nc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)CC1,Inactive,No,THP,4.366800000000008,IC50 of PROTAC is 10-100 nM,Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,19,2,< 1 nM,< 100 nM,Quinoxaline,COc1cc(-c2cnc3cccc(-c4cc(F)c(CN5CCS(=O)(=O)CC5)c(F)c4)c3n2)ccc1OCCCN1CCOCC1,NCCOCCOCCOCCOCCOCCOCC=O,PEG,22,8,19,1201.3569999999993,No,,3KRR,DQX,32001089,41,No,,Reviewed,"O60674, P23458, P52333",No,No,No,No,24,239.05999999999997
136,O=C1CCC(N2Cc3c(NC(=O)CCCCCCCN4CCN(c5ccc(Nc6cc7c(N8CCC(CO)CC8)nc(Nc8ccc(F)cc8)nc7cn6)nc5)CC4)cccc3C2=O)C(=O)N1,Active,Yes,HCC827,6.117100000000006,IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant),Ronen Gabizon,45.2 nM,87 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,5,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,NCCCCCCCC=O,Alkane,10,2,7,913.0719999999998,No,,,,31951960,2,No,,Reviewed,P00533,No,Yes,No,Yes,48,201.14999999999995
137,O=C1CCC(N2Cc3c(NC(=O)CCCCCCN4CCN(c5ccc(Nc6cc7c(N8CCC(CO)CC8)nc(Nc8ccc(F)cc8)nc7cn6)nc5)CC4)cccc3C2=O)C(=O)N1,Active,No,HCC827,5.727000000000005,"Degredation profile isn't concentration dependent, structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant)",Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,5,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,NCCCCCCC=O,Alkane,9,2,6,899.0449999999997,No,,,,31951960,3,No,,Reviewed,P00533,No,No,No,No,48,201.14999999999995
138,O=C1CCC(N2Cc3c(NC(=O)CCCCCN4CCN(c5ccc(Nc6cc7c(N8CCC(CO)CC8)nc(Nc8ccc(F)cc8)nc7cn6)nc5)CC4)cccc3C2=O)C(=O)N1,Active,No,HCC827,5.336900000000004,"Degredation profile isn't concentration dependent, structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant)",Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,5,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,NCCCCCC=O,Alkane,8,2,5,885.0179999999998,No,,,,31951960,4,No,,Reviewed,P00533,No,No,No,No,48,201.14999999999995
139,O=C1CCC(N2Cc3c(NC(=O)CCCCN4CCN(c5ccc(Nc6cc7c(N8CCC(CO)CC8)nc(Nc8ccc(F)cc8)nc7cn6)nc5)CC4)cccc3C2=O)C(=O)N1,Active,No,HCC827,4.946800000000004,"Degredation profile isn't concentration dependent, structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant)",Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,5,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,NCCCCC=O,Alkane,7,2,4,870.9909999999999,No,,,,31951960,5,No,,Reviewed,P00533,No,No,No,No,48,201.14999999999995
140,O=C1CCC(N2Cc3c(NC(=O)CCCCCCCn4cc(CN5CCN(c6ccc(Nc7cc8c(N9CCC(CO)CC9)nc(Nc9ccc(F)cc9)nc8cn7)nc6)CC5)nn4)cccc3C2=O)C(=O)N1,Active,No,HCC827,5.908800000000006,"Degredation profile isn't concentration dependent, structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant)",Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,5,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,NCc1cn(CCCCCCCC=O)nn1,Other,16,5,9,994.1499999999995,No,,,,31951960,6,No,,Reviewed,P00533,No,No,No,No,48,231.85999999999993
141,O=C(CN1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1)NCCC(=O)Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Active,No,HCC827,3.2828000000000017,"Degredation profile isn't concentration dependent, structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant)",Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,6,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,NCC(=O)NCCC=O,Alkane,9,4,4,899.9889999999995,No,,,,31951960,7,No,,Reviewed,P00533,No,No,No,No,48,230.25
142,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCN(CCCCCCCC(=O)Nc6cccc7c6CN(C6CCC(=O)NC6=O)C7=O)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,Active,No,HCC827,6.438800000000006,"Degredation profile isn't concentration dependent, structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant)",Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,4,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,NCCCCCCCC=O,Alkane,10,2,7,926.1149999999997,No,,,,31951960,8,No,,Reviewed,P00533,No,No,No,No,48,184.15999999999997
143,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCN(CC(=O)NCCC(=O)Nc6cccc7c6CN(C6CCC(=O)NC6=O)C7=O)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,Active,No,HCC827,3.6045000000000043,"Degredation profile isn't concentration dependent, structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant)",Ronen Gabizon,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,5,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,NCC(=O)NCCC=O,Alkane,9,4,4,913.0319999999996,No,,,,31951960,9,No,,Reviewed,P00533,No,No,No,No,48,213.26
144,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCN2CCN(c3ccc(Nc4cc5c(N6CCC(CO)CC6)nc(Nc6ccc(F)cc6)nc5cn4)nc3)CC2)C(C)(C)C)cc1,Active,Yes,HCC827,7.568320000000007,Structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant),Ronen Gabizon,34.8 nM,98 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,16,6,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,NCCCCCCC=O,Alkane,9,2,6,1070.3539999999991,No,,,,31951960,10,No,,Reviewed,P00533,No,No,No,No,48,217.2
145,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCN2CCN(c3ccc(Nc4cc5c(N6CCC(CO)CC6)nc(Nc6ccc(F)cc6)nc5cn4)nc3)CC2)C(C)(C)C)cc1,Active,No,HCC827,6.788120000000005,"Degredation profile isn't concentration dependent, structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant)",Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,16,6,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,NCCCCC=O,Alkane,7,2,4,1042.2999999999995,No,,,,31951960,11,No,,Reviewed,P00533,No,No,No,No,48,217.2
146,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NCCOCCOCCOCCN2CCN(c3ccc(Nc4cc5c(N6CCC(CO)CC6)nc(Nc6ccc(F)cc6)nc5cn4)nc3)CC2)C(C)(C)C)cc1,Active,No,HCC827,6.141020000000009,"Degredation profile isn't concentration dependent, structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant)",Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,19,6,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,CCOCCOCCOCCN,PEG,12,4,9,1118.394999999999,No,,,,31951960,12,No,,Reviewed,P00533,No,No,No,No,48,227.82
147,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NCCOCCOCCN2CCN(c3ccc(Nc4cc5c(N6CCC(CO)CC6)nc(Nc6ccc(F)cc6)nc5cn4)nc3)CC2)C(C)(C)C)cc1,Active,No,HCC827,6.124420000000006,"Degredation profile isn't concentration dependent, structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant)",Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,18,6,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,CCOCCOCCN,PEG,9,3,6,1074.3419999999992,No,,,,31951960,13,No,,Reviewed,P00533,No,No,No,No,48,218.58999999999997
148,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NCCOCCOCCn2cc(CN3CCN(c4ccc(Nc5cc6c(N7CCC(CO)CC7)nc(Nc7ccc(F)cc7)nc6cn5)nc4)CC3)nn2)C(C)(C)C)cc1,Active,No,HCC827,5.9161200000000065,"Degredation profile isn't concentration dependent, structure with the ligand was modeled by docking. IC50 of the ligand is between 1nM-34 nM (depends on EGFR mutant). EC50 of ligand is between 0.044uM-1.06 uM (cell line depandant)",Ronen Gabizon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,21,6,< 34 nM,,compound 1,CN(C)C1CCN(c2ccc(Nc3cc4c(N5CCC(CO)CC5)nc(Nc5ccc(F)cc5)nc4cn3)nc2)CC1,CCOCCOCCn1cc(CN)nn1,Other,15,6,8,1155.4199999999992,No,,,,31951960,14,No,,Reviewed,P00533,No,No,No,No,48,249.29999999999995
149,CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl,Active,Yes,"MOLT-4, MOLM14",3.584000000000003,"General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity.",Ronen Gabizon,< 100 nM,> 85 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,16,5,< 1 uM,10.3 nM,TL13-87,CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(C)CC3)cc2)ncc1Cl,COCCOCCNC(C)=O,Other,11,4,6,931.4729999999998,"INCENP, NDUFAB1, CCNH, CCNK, and IKZF1",,2XB7,GUI,29129717,TL12-186,Yes,,Reviewed,"O14976, O75385, P06239, P07332, P11802, P16591, P24941, P30291, P35991, P36888, P42680, P50613, P50750, P51451, P53671, Q00534, Q00537, Q05397, Q08881, Q13131, Q14004, Q14289, Q2M2I8, Q7KZI7, Q91820, Q96GD4, Q96SZ6, Q9NYV4",Yes,No,Yes,Yes,4,233.59999999999997
150,CC(C)(C)/C(O)=C/C(=N)N[N+](=O)Nc1ccc(-c2cn3c(n2)sc2cc(OCCN4CCN(C(=O)CCC(=O)NCCCCNC(=O)COc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)ccc23)cc1,Inactive,No,"MOLM14, MV4-11",4.0876700000000055,IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines,Ronen Gabizon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,16,7,< 1.6 nM,,AC220,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3ccccc34)cc2)no1,O=C(CO)NCCCCNC(=O)CCC(=O)N1CCN(CCO)CC1,Other,25,9,11,1048.1729999999995,No,,4XUF,P30,29129717,JB-4-048,No,,Reviewed,P36888,No,No,No,No,12,289.28
151,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(C(=O)CCC(=O)NCCCOCCOCCOCCCNC(=O)COc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1,Inactive,No,"MOLM14, MV4-11",4.991300000000007,IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines,Ronen Gabizon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_O,19,5,< 1.6 nM,,AC220,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3ccccc34)cc2)no1,O=C(CO)NCCCOCCOCCOCCCNC(=O)CCC(=O)N1CCN(CCO)CC1,Other,34,12,20,1176.3199999999995,No,,4XUF,P30,29129717,JB-4-050,No,,Reviewed,P36888,No,No,No,No,12,295.9099999999999
152,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(CC(=O)NCCCCCCCCNC(=O)COc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1,Inactive,No,"MOLM14, MV4-11",6.195100000000005,IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines,Ronen Gabizon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_O,16,5,< 1.6 nM,,AC220,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3ccccc34)cc2)no1,O=C(CO)NCCCCCCCCNC(=O)CN1CCN(CCO)CC1,Other,26,8,14,1058.2319999999995,No,,4XUF,P30,29129717,JB-4-072,No,,Reviewed,P36888,No,No,No,No,12,251.14999999999998
153,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCOCCOCCNC(=O)CNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)ccc34)cc2)no1,Inactive,No,"MOLM14, MV4-11",5.187000000000003,IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines,Ronen Gabizon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,15,5,< 1.6 nM,,AC220,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3ccccc34)cc2)no1,CC(=O)NCCOCCOCCO,PEG,13,5,8,891.964,No,,4XUF,P30,29129717,TL13-148,No,,Reviewed,P36888,No,No,No,No,12,236.82999999999998
154,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(C(=O)CCC(=O)NCCCCCCCCNC(=O)COc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1,Inactive,No,"MOLM14, MV4-11",6.501900000000006,IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines,Ronen Gabizon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_O,16,5,< 1.6 nM,,AC220,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3ccccc34)cc2)no1,O=C(CO)NCCCCCCCCNC(=O)CCC(=O)N1CCN(CCO)CC1,Other,29,9,15,1100.2689999999996,No,,4XUF,P30,29129717,JB-4-049,No,,Reviewed,P36888,No,No,No,No,12,268.21999999999997
155,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(CC(=O)NCCCCNC(=O)COc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1,Inactive,No,"MOLM14, MV4-11",4.634700000000004,IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines,Ronen Gabizon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_O,16,5,< 1.6 nM,,AC220,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3ccccc34)cc2)no1,O=C(CO)NCCCCNC(=O)CN1CCN(CCO)CC1,Other,22,8,10,1002.1239999999997,No,,4XUF,P30,29129717,JB-4-066,No,,Reviewed,P36888,No,No,No,No,12,251.14999999999998
156,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(CC(=O)NCCCOCCOCCOCCCNC(=O)COc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1,Inactive,No,"MOLM14, MV4-11",4.684500000000006,IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines,Ronen Gabizon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_O,19,5,< 1.6 nM,,AC220,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3ccccc34)cc2)no1,O=C(CO)NCCCOCCOCCOCCCNC(=O)CN1CCN(CCO)CC1,Other,31,11,19,1134.2829999999997,No,,4XUF,P30,29129717,JB-4-073,No,,Reviewed,P36888,No,No,No,No,12,278.84
157,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(CCOCCOCCNC(=O)CNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1,Active,No,"MOLM14, MV4-11",4.804600000000004,Dmax is difficult to quantify because AC220 raises FLT3 expression levels. IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines. EC50 of PROTAC was measured on MOLM-14 cell lines.,Ronen Gabizon,< 10 nM,~ 100 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,17,5,< 1.6 nM,,AC220,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3ccccc34)cc2)no1,CC(=O)NCCOCCOCCN1CCN(CCO)CC1,Other,21,7,11,1004.1399999999998,"No; confirmed that AURKA, BTK and PTK2B are not degraded",,4XUF,P30,29129717,TL13-117,No,,Reviewed,P36888,No,No,No,No,12,243.31
158,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCOCCOCCOCCNC(=O)CNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)ccc34)cc2)no1,Active,No,"MOLM14, MV4-11",5.203600000000003,Dmax is difficult to quantify because AC220 raises FLT3 expression levels. IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines. EC50 of PROTAC was measured on MOLM-14 cell lines.,Ronen Gabizon,< 10 nM,~ 100 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,16,5,< 1.6 nM,,AC220,CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3ccccc34)cc2)no1,CC(=O)NCCOCCOCCOCCO,PEG,16,6,11,936.017,"No; confirmed that AURKA, BTK and PTK2B are not degraded",,4XUF,P30,29129717,TL13-149,No,,Reviewed,P36888,No,No,No,No,12,246.06
159,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(CCOCCOCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)c(OC)cc23)c(Cl)cc1Cl,Active,No,"MOLM14, MV4-11",5.107080000000004,IC50 of ligand is inhibitory - data from Selleckchem. EC50 of the lidand is Src-dependent cell proliferation - data from Selleckchem.,Ronen Gabizon,~ 100 nM,~ 50 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,3,1.2 nM,,Bosutinib,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl,CCOCCOC,Other,7,2,4,903.8209999999998,No,,3UE4,DB8,29129717,CJH-005-067,No,,Reviewed,Q06187,No,No,No,No,4,196.92
160,Cc1cc(C2CC2)cc2ccn(-c3cccc(-c4cc(Nc5ccc(N6CCN(CCOCCOCCNC(=O)CNc7cccc8c7C(=O)N(C7CCC(=O)NC7=O)C8=O)CC6)cn5)c(=O)n(C)c4)c3CO)c(=O)c12,Active,Yes,MOLM14,3.957820000000005,IC50 of ligand is 4 nM (BTK inhibition)/ 0.3 nM (binding). EC50 of ligand is 20-30 nM (B-cell signaling).,Ronen Gabizon,< 40 nM,~ 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,5,< 4 nM,,RN486,CN1CCN(c2ccc(Nc3cc(-c4cccc(-n5ccc6cc(C7CC7)cc(F)c6c5=O)c4CO)cn(C)c3=O)nc2)CC1,COCCOCCNC(C)=O,Other,11,4,6,1033.1559999999997,No,,4OTR,2V3,29129717,DD-04-015,No,,Reviewed,Q06187,No,No,No,No,4,238.76999999999995
161,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Inactive,No,Panc02.13,6.459820000000005,,Paul Gehrtz,> 1000 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCCCO,non-PEG polyether,9,3,6,977.0399999999995,No,,4IM0,1FV,28692295,3a,No,,Reviewed,Q9UHD2,No,No,No,No,16,200.24
162,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Inactive,No,Panc02.13,5.696220000000006,,Paul Gehrtz,> 1000 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,14,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCOCCO,PEG,10,4,7,993.0389999999995,No,,4IM0,1FV,28692295,3b,No,,Reviewed,Q9UHD2,No,No,No,No,16,209.47000000000003
163,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCOCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Inactive,No,Panc02.13,7.240020000000006,,Paul Gehrtz,> 1000 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCCCCCOCCO,non-PEG polyether,11,3,8,1005.0939999999996,No,,4IM0,1FV,28692295,3c,No,,Reviewed,Q9UHD2,No,No,No,No,16,200.24
164,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Inactive,No,Panc02.13,6.476420000000005,,Paul Gehrtz,> 1000 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,14,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCCOCCCO,non-PEG polyether,12,4,9,1021.0929999999995,No,,4IM0,1FV,28692295,3d,No,,Reviewed,Q9UHD2,No,No,No,No,16,209.47000000000003
165,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Inactive,No,Panc02.13,5.712820000000005,,Paul Gehrtz,> 1000 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCOCCOCCO,PEG,13,5,10,1037.0919999999994,No,,4IM0,1FV,28692295,3e,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
166,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,7.256620000000007,,Paul Gehrtz,88 nM,79 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,14,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCCOCCCCCO,non-PEG polyether,14,4,11,1049.1469999999995,No,,4IM0,1FV,28692295,3f,No,,Reviewed,Q9UHD2,No,No,No,No,16,209.47000000000003
167,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,6.493020000000006,,Paul Gehrtz,71 nM,86 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCOCCOCCCCO,non-PEG polyether,15,5,12,1065.1459999999993,No,,4IM0,1FV,28692295,3g,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
168,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,5.729420000000008,,Paul Gehrtz,103 nM,92 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,16,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCOCCOCCOCCO,PEG,16,6,13,1081.144999999999,No,,4IM0,1FV,28692295,3h,No,,Reviewed,Q9UHD2,No,No,No,No,16,227.93
169,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCCOCCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,Yes,"Panc02.13, H23, A549, H1792, H2110, HCC827",7.2732200000000065,,Paul Gehrtz,12 nM,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,4.6 nM,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1093.1999999999991,No,,4IM0,1FV,28692295,3i,No,,Reviewed,Q9UHD2,Yes,No,No,Yes,16,218.7
170,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCOCCCCOCCCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,8.817020000000003,,Paul Gehrtz,95 nM,90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,14,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCCCCCOCCCCOCCCCO,non-PEG polyether,18,4,15,1105.254999999999,No,,4IM0,1FV,28692295,3j,No,,Reviewed,Q9UHD2,No,No,No,No,16,209.47000000000003
171,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCCOCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,5.7460200000000095,,Paul Gehrtz,29 nM,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,17,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCOCCOCCOCCOCCO,PEG,19,7,16,1125.197999999999,No,,4IM0,1FV,28692295,3k,No,,Reviewed,Q9UHD2,No,No,No,No,16,237.15999999999997
172,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCCCOCCCCOCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,7.289820000000007,,Paul Gehrtz,6 nM,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,16,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCOCCCCOCCCCOCCO,non-PEG polyether,20,6,17,1137.2529999999988,No,,4IM0,1FV,28692295,3l,No,,Reviewed,Q9UHD2,No,No,No,No,16,227.93
173,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCCOCCCOCCCOCCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,7.679920000000007,,Paul Gehrtz,25 nM,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,16,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCCOCCCOCCCOCCCOCCCO,non-PEG polyether,21,6,18,1151.279999999999,No,,4IM0,1FV,28692295,3m,No,,Reviewed,Q9UHD2,No,No,No,No,16,227.93
174,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCCOCCOCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,5.762620000000012,,Paul Gehrtz,34 nM,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,18,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCOCCOCCOCCOCCOCCO,PEG,22,8,19,1169.2509999999993,No,,4IM0,1FV,28692295,3n,No,,Reviewed,Q9UHD2,No,No,No,No,16,246.39
175,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCCCOCCCCOCCOCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,7.306420000000007,,Paul Gehrtz,3 nM,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,17,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCOCCCCOCCCCOCCOCCO,non-PEG polyether,23,7,20,1181.3059999999991,No,,4IM0,1FV,28692295,3o,No,,Reviewed,Q9UHD2,No,No,No,No,16,237.15999999999997
176,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCCCOCCCCOCCCCOCCCCOCCCCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,10.427219999999995,,Paul Gehrtz,292 nM,76 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,17,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCCCCOCCCCOCCCCOCCCCOCCCCCO,non-PEG polyether,31,7,28,1293.521999999999,No,,4IM0,1FV,28692295,3p,No,,Reviewed,Q9UHD2,No,No,No,No,16,237.15999999999997
177,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCCOCCCOc2ccc(Nc3nccc(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Inactive,No,Panc02.13,6.510720000000005,,Paul Gehrtz,> 1000 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,725 nM,1b analog,CN(CCCNc1ccnc(Nc2ccccc2)n1)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1014.3039999999994,No,,4IM0,1FV,28692295,5a,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
178,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCCOCCCOc2ccc(Nc3ncc(F)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,6.649820000000005,,Paul Gehrtz,282 nM,74 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,103.5 nM,1b analog,CN(CCCNc1nc(Nc2ccccc2)ncc1F)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1032.2939999999994,No,,4IM0,1FV,28692295,5b,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
179,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCCOCCCOc2ccc(Nc3ncc(Cl)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,7.164120000000007,,Paul Gehrtz,10 nM,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,10.4 nM,1b analog,CN(CCCNc1nc(Nc2ccccc2)ncc1Cl)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1048.7489999999993,No,,4IM0,1FV,28692295,5c,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
180,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCCOCCCOc2ccc(Nc3ncc(I)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,7.115320000000006,,Paul Gehrtz,3 nM,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,4 nM,1b analog,CN(CCCNc1nc(Nc2ccccc2)ncc1I)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1140.1999999999991,No,,4IM0,1FV,28692295,5d,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
181,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCCOCCCOc2ccc(Nc3ncc(C(F)(F)F)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,7.529520000000007,,Paul Gehrtz,29 nM,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,13 nM,1b analog,CN(CCCNc1nc(Nc2ccccc2)ncc1C(F)(F)F)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1082.3009999999992,No,,4IM0,1FV,28692295,5e,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
182,Cc1cnc(Nc2ccc(OCCCOCCCCOCCCOCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)cc2)nc1NCCCN(C)C(=O)C1CCC1,Active,No,Panc02.13,6.81914000000001,,Paul Gehrtz,92 nM,89 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,270 nM,1b analog,Cc1cnc(Nc2ccccc2)nc1NCCCN(C)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1028.3309999999994,No,,4IM0,1FV,28692295,5f,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.70000000000002
183,CCc1cnc(Nc2ccc(OCCCOCCCCOCCCOCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)cc2)nc1NCCCN(C)C(=O)C1CCC1,Active,No,Panc02.13,7.073120000000009,,Paul Gehrtz,121 nM,77 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,275 nM,1b analog,CCc1cnc(Nc2ccccc2)nc1NCCCN(C)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1042.3579999999995,No,,4IM0,1FV,28692295,5g,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.70000000000002
184,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCCOCCCOc2ccc(Nc3ncc(C4CCC4)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,7.778220000000006,,Paul Gehrtz,544 nM,70 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,1035 nM,1b analog,CN(CCCNc1nc(Nc2ccccc2)ncc1C1CCC1)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1068.395999999999,No,,4IM0,1FV,28692295,5h,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
185,C=Cc1cnc(Nc2ccc(OCCCOCCCCOCCCOCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)cc2)nc1NCCCN(C)C(=O)C1CCC1,Active,No,Panc02.13,7.153720000000008,,Paul Gehrtz,48 nM,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,130 nM,1b analog,C=Cc1cnc(Nc2ccccc2)nc1NCCCN(C)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1040.3419999999996,No,,4IM0,1FV,28692295,5i,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.70000000000002
186,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCCOCCCOc2ccc(Nc3ncc(C4CC4)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)(C)C)cc1,Active,No,Panc02.13,7.388120000000006,,Paul Gehrtz,65 nM,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,5,,245 nM,1b analog,CN(CCCNc1nc(Nc2ccccc2)ncc1C1CC1)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1054.3689999999992,No,,4IM0,1FV,28692295,5j,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
187,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)CNC(=O)COCCCOCCCCOCCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)cc1,Inactive,No,Panc02.13,5.858520000000004,,Paul Gehrtz,> 1000 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)CN)cc1,VHL,,,aryl_O,15,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1037.0919999999994,No,,4IM0,1FV,28692295,6a,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
188,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@H](C)NC(=O)COCCCOCCCCOCCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)cc1,Active,No,Panc02.13,6.247020000000005,,Paul Gehrtz,> 1000 nM,34 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@H](C)N)cc1,VHL,,,aryl_O,15,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1051.1189999999995,No,,4IM0,1FV,28692295,6b,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
189,CC[C@H](NC(=O)COCCCOCCCCOCCCOc1ccc(Nc2ncc(Br)c(NCCCN(C)C(=O)C3CCC3)n2)cc1)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1,Active,No,Panc02.13,6.637120000000007,,Paul Gehrtz,864 nM,71 %,CC[C@H](N)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1,VHL,,,aryl_O,15,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1065.1459999999993,No,,4IM0,1FV,28692295,6c,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
190,CCC[C@H](NC(=O)COCCCOCCCCOCCCOc1ccc(Nc2ncc(Br)c(NCCCN(C)C(=O)C3CCC3)n2)cc1)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1,Active,No,Panc02.13,7.027220000000007,,Paul Gehrtz,288 nM,75 %,CCC[C@H](N)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1,VHL,,,aryl_O,15,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1079.172999999999,No,,4IM0,1FV,28692295,6d,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
191,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCCOCCCOc2ccc(Nc3ncc(Br)c(NCCCN(C)C(=O)C4CCC4)n3)cc2)C(C)C)cc1,Active,No,Panc02.13,6.883120000000006,,Paul Gehrtz,44 nM,88 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)C)cc1,VHL,,,aryl_O,15,5,,,1b,CN(CCCNc1nc(Nc2ccccc2)ncc1Br)C(=O)C1CCC1,O=CCOCCCOCCCCOCCCO,non-PEG polyether,17,5,14,1079.1729999999993,No,,4IM0,1FV,28692295,6e,No,,Reviewed,Q9UHD2,No,No,No,No,16,218.7
192,Cc1cc(C)nc(SCC(=O)Nc2ncc(Cc3cccc(OCc4cn(CCCCNC(=O)COc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)c3)s2)n1,Active,Yes,HeLa,3.418640000000001,,Shimrit Azulay,,~ 39 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,16,3,,0.25 uM,sirtuin rearranging ligand,COc1cccc(Cc2cnc(NC(=O)CSc3nc(C)cc(C)n3)s2)c1,O=C(CO)NCCCCn1ccnn1,Other,14,6,6,852.956,No,,,,28379698,Compound 12,No,,Reviewed,Q8IXJ6,No,Yes,No,Yes,"1,3,6",229.58999999999997
193,O=C1CCC(N2C(=O)c3cccc(OCCCCCOc4ccc(CC(=O)Nc5cc(C6CCC6)[nH]n5)cc4)c3C2=O)C(=O)N1,Active,Yes,HCT116,3.8877000000000015,,Rambabu Reddi,,~ 65 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,8,3,,,compound 1,COc1ccc(CC(=O)Nc2cc(C3CCC3)[nH]n2)cc1,CCCCO,Alkane,5,1,2,613.6710000000003,"no off targets. Selective for CDK 9 over CDK2, CDK5, FAK, Akt and IKKβ",,,,28636052,Compound 3,No,,Reviewed,P50750,Yes,Yes,No,No,6,159.79
194,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCCOc2cc3nccc(Nc4ccc5scnc5c4)c3cc2S(=O)(=O)C(C)(C)C)C(C)(C)C)cc1,Active,Yes,Human THP-1 monocytes,6.846520000000008,PROTAC_ERRα is efficacious in mice,Amit Shraga,1.4 nM,> 95 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,17,4,,,Vandetanib,CC(C)(C)S(=O)(=O)c1ccc2nccc(Nc3ccc4scnc4c3)c2c1,O=CCOCCOCCOCCOCCO,PEG,16,6,13,1060.3309999999997,BCR,,5J79,6GE,26075522,PROTAC_RIPK2,Yes,,Reviewed,O43353,Yes,Yes,No,Yes,16,229.72999999999996
195,COc1cc(C=C2SC(=O)N(CCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)C2=O)ccc1Oc1ccc(C#N)cc1C(F)(F)F,Active,Yes,MCF-7 breast cancer cells,7.062000000000007,"protein reduction by nearly 50% was observed as early as 1 h post‐treatment, and almost complete degradation was achieved after 4 h of treatment",Amit Shraga,~ 100 nM,86 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,13,3,,,compound 29 thiazolidinedione-based ligand,COc1cc(/C=C2\SC(=O)N(C)C2=O)ccc1Oc1ccc(C#N)cc1C(F)(F)F,COCCC=O,PEG,6,2,3,949.0429999999999,"RIPK3, NLK, ABL1/BCR-­ABL, TESK2, TGFBR2, TGFBR2",,,,26075522,PROTAC_ERRα,Yes,,Reviewed,P11474,Yes,No,No,Yes,8,200.48999999999995
196,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2C1CCN(CCOCCOCC(=O)Nc2ccc3c(c2)CN(C2CCC(=O)NC2=O)C3=O)CC1,Active,Yes,NAMALWA,3.9376000000000015,"IC50 of ligand is 51.0 nM (WT BTK), 30.7 (C481S)",Amit Shraga,7.9 nM,95 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,3,< 51.0 nM,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,NCCOCCOCC(N)=O,PEG,11,5,7,773.8509999999999,No,,5P9J,"8E8",31879210,SJF620,No,29851337,Reviewed,Q06187,No,No,No,No,24,196.13
197,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2C1CCN(CCCCCCOCCOCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1,Active,No,NAMALWA,5.138200000000003,"IC50 of ligand is 51.0 nM (WT BTK), 30.7 (C481S)",Barr Tivon,80.6 nM,96 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,3,< 51.0 nM,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,NCCCCCCOCCOCC=O,non-PEG polyether,14,4,11,843.942,No,,5P9J,"8E8",29851337,MT-540,No,,Reviewed,Q06187,No,No,No,No,,213.2
198,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2C1CCN(CCCCOCCCCOCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1,Active,No,NAMALWA,5.138200000000003,"IC50 of ligand is 51.0 nM (WT BTK), 30.7 (C481S)",Barr Tivon,90.1 nM,93 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,3,< 51.0 nM,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,NCCCCOCCCCOCC=O,non-PEG polyether,14,4,11,843.942,No,,5P9J,"8E8",29851337,MT-541,No,,Reviewed,Q06187,No,No,No,No,,213.2
199,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2C1CCN(CCCOCCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1,Active,No,NAMALWA,4.748100000000003,"IC50 of ligand is 51.0 nM (WT BTK), 30.7 (C481S)",Barr Tivon,68.3 nM,95 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,3,< 51.0 nM,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,NCCCOCCCOCCC=O,non-PEG polyether,13,4,10,829.9150000000001,No,,5P9J,"8E8",29851337,MT-781,No,,Reviewed,Q06187,No,No,No,No,,213.2
200,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2C1CCN(CCOCCOCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1,Inactive,No,NAMALWA,3.5778000000000008,"IC50 of ligand is 51.0 nM (WT BTK), 30.7 (C481S)",Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,3,< 51.0 nM,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,NCCOCCOCC=O,PEG,10,4,7,787.834,No,,5P9J,"8E8",29851337,MT-797,No,,Reviewed,Q06187,No,No,No,No,,213.2
201,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2C1CCN(CCOCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1,Inactive,No,NAMALWA,3.5612000000000013,"IC50 of ligand is 51.0 nM (WT BTK), 30.7 (C481S)",Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,3,< 51.0 nM,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,NCCOCC=O,PEG,7,3,4,743.781,No,,5P9J,"8E8",29851337,MT-783,No,,Reviewed,Q06187,No,No,No,No,,203.96999999999997
202,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2C1CCN(CCOCCOCC(=O)Nc2ccc3c(c2)C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1,Active,Yes,"NAMALWA, XLA",3.5778000000000008,"DC50 is 9.1 nM (WT BTK, NAMALWA cells), 14.6 nM (WT BTK, XLA cells), 14.9 nM (C481S, XLA cells). IC50 of PROTAC is 46.9 (WT BTK), 20.9 (C481S). IC50 of ligand is 51.0 nM (WT BTK), 30.7 (C481S)",Barr Tivon,< 14.9 nM,> 99 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,3,< 51.0 nM,< 46.9 nM,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,NCCOCCOCC=O,PEG,10,4,7,787.834,"Significant binding to: TEC, ERBB2, ERBB3, HCK, YES, BRK, LCK, BLK, CSK, RIPK2, MEK5, CSNK1E",,5P9J,"8E8",29851337,MT-802,Yes,,Reviewed,Q06187,Yes,Yes,Yes,Yes,"1,2,4,8,16,24",213.2
203,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2C1CCN(CCCCOCCCCOCC(=O)Nc2ccc3c(c2)C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1,Active,No,NAMALWA,5.138200000000003,"IC50 of ligand is 51.0 nM (WT BTK), 30.7 (C481S)",Barr Tivon,11.6 nM,> 99 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,3,< 51.0 nM,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,NCCCCOCCCCOCC=O,non-PEG polyether,14,4,11,843.942,No,,5P9J,"8E8",29851337,MT-809,No,,Reviewed,Q06187,No,No,No,No,,213.2
204,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)NCCCCNC(=O)COc1cccc3c1C(=O)N(C1CCC(=O)NC1=O)C3=O)c1nnc(C)n1-2,Active,Yes,"MV4;11, SUM149, SUM159, MOLM13, MM1.SCRBN−/−, MM1.SW",3.6824600000000025,,Daniel Zaidman,430 nM,95 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,ester_to_amide,12,3,28 nM,20 nM,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCCCNC(=O)CO,Alkane,10,4,5,785.2829999999999,"BRD2, BRD3, BRD4",,3MXF,JQ1,25999370,dBET1,Yes,,Reviewed,O60885,No,Yes,Yes,Yes,"1,2,4,8,16,24",194.05
205,CCC(C)(C)C(=O)C(=O)N1CCCC[C@H]1C(=O)OC(CCc1ccc(OC)c(OC)c1)c1cccc(NC(=O)CCC(=O)NCCCCNC(=O)COc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)c1,Active,Yes,"MV4;11, 293FT, 293FTCRBN−/−",4.518800000000005,,Daniel Zaidman,10 nM,50 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,14,4,,,SLF,CCC(C)(C)C(=O)C(=O)N1CCCC[C@H]1C(=O)OC(CCc1ccc(OC)c(OC)c1)c1cccc(N)c1,O=CCCC(=O)NCCCCNC(=O)CO,Alkane,16,6,9,1009.1229999999994,No,,,,25999370,dFKBP-1,No,,Reviewed,P62942,No,Yes,No,Yes,18,262.21999999999997
206,CCC(C)(C)C(=O)C(=O)N1CCCC[C@H]1C(=O)OC(CCc1ccc(OC)c(OC)c1)c1cccc(NC(=O)CCC(=O)NCCCOCCOCCOCCCNC(=O)COc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)c1,Active,No,"MV4;11, 293FT, 293FTCRBN−/−",4.56860000000001,,Daniel Zaidman,< 10 nM,60 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,17,4,,,SLF,CCC(C)(C)C(=O)C(=O)N1CCCC[C@H]1C(=O)OC(CCc1ccc(OC)c(OC)c1)c1cccc(N)c1,O=CCCC(=O)NCCCOCCOCCOCCCNC(=O)CO,PEG,25,9,18,1141.2819999999992,No,,,,25999370,dFKBP-2,No,,Reviewed,P62942,No,Yes,No,Yes,18,289.90999999999997
207,Cc1ccc(NC(=O)c2ccc(CN3CCN(CCCCCCOCCOCCOCCCCCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,Inactive,No,K562 CML,9.372140000000005,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,5,0.86 nM,4.3 nM,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCCCOCCOCCOCCCCCC=O,non-PEG polyether,19,4,16,1194.558,No,,2HYY,STI,26593377,IMA-6-2-2-6-VHL,No,,Reviewed,P00519,No,No,No,No,24,225.59999999999997
208,Cc1ccc(NC(=O)c2ccc(CN3CCN(CCCCCCOCCOCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,Inactive,No,K562 CML,7.795140000000011,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,0.86 nM,5.8 nM,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCCCOCCOCC=O,non-PEG polyether,12,3,9,1094.397,No,,2HYY,STI,26593377,IMA-6-2-2-VHL,No,,Reviewed,P00519,No,No,No,No,24,216.37
209,Cc1ccc(NC(=O)c2ccc(CN3CCN(CCCCCCOCCOCCOCCOCCOCCOCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,Inactive,No,K562 CML,7.861540000000015,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,19,5,0.86 nM,1.7 nM,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCCCOCCOCCOCCOCCOCCOCC=O,non-PEG polyether,24,7,21,1270.6090000000002,No,,2HYY,STI,26593377,IMA-6-(2-)5-2-VHL,No,,Reviewed,P00519,No,No,No,No,24,253.29000000000002
210,Cc1ccc(NC(=O)c2ccc(CN3CCN(CCCCCCOCCCCCOCCCCCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,Inactive,No,K562 CML,10.525839999999999,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,0.86 nM,19 nM,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCCCOCCCCCOCCCCCC=O,non-PEG polyether,19,3,16,1192.586,No,,2HYY,STI,26593377,IMA-6-5-6-VHL,No,,Reviewed,P00519,No,No,No,No,24,216.37
211,Cc1ccc(NC(=O)c2ccc(CN3CCN(CCCCCCOCCOCCOCCCCCC(=O)Nc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,Inactive,No,K562 CML,7.171020000000007,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,4,0.86 nM,6.2 nM,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCCCOCCOCCOCCCCCC=O,non-PEG polyether,19,4,16,1037.232,No,,2HYY,STI,26593377,IMA-6-2-2-6-CRBN,No,,Reviewed,P00519,No,No,No,No,24,226.61999999999995
212,Cc1ccc(NC(=O)c2ccc(CN3CCN(CCCCCCOCCOCC(=O)Nc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,Inactive,No,K562 CML,5.594020000000004,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,14,4,0.86 nM,4.7 nM,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCCCOCCOCC=O,non-PEG polyether,12,3,9,937.0709999999998,No,,2HYY,STI,26593377,IMA-6-2-2-CRBN,No,,Reviewed,P00519,No,No,No,No,24,217.39
213,Cc1ccc(NC(=O)c2ccc(CN3CCN(CCCCCCOCCOCCOCCOCCOCCOCC(=O)Nc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,Inactive,No,K562 CML,5.660420000000009,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,18,4,0.86 nM,3.0 nM,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCCCOCCOCCOCCOCCOCCOCC=O,non-PEG polyether,24,7,21,1113.283,No,,2HYY,STI,26593377,IMA-6-(2-)5-2-CRBN,No,,Reviewed,P00519,No,No,No,No,24,254.31
214,Cc1ccc(NC(=O)c2ccc(CN3CCN(CCCCCCOCCCCCOCCCCCC(=O)Nc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,Inactive,No,K562 CML,8.324720000000008,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,14,4,0.86 nM,24 nM,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCCCOCCCCCOCCCCCC=O,non-PEG polyether,19,3,16,1035.26,No,,2HYY,STI,26593377,IMA-6-5-6-CRBN,No,,Reviewed,P00519,No,No,No,No,24,217.39
215,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(CCCCCCOCCOCCOCCCCCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CC4)c(OC)cc23)c(Cl)cc1Cl,Inactive,No,K562 CML,9.9722,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,17,4,0.063 nM,1.4 nM,bosutinib,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl,CCCCCOCCOCCOCCCCCC=O,non-PEG polyether,19,4,16,1231.3989999999994,No,,3UE4,DB8,26593377,BOS-6-2-2-6-VHL,No,,Reviewed,P00519,No,No,No,No,24,222.19999999999996
216,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(CCCCCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CC4)c(OC)cc23)c(Cl)cc1Cl,Inactive,No,K562 CML,8.39520000000001,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,4,0.063 nM,1.3 nM,bosutinib,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl,CCCCCOCCOCC=O,non-PEG polyether,12,3,9,1131.2379999999998,No,,3UE4,DB8,26593377,BOS-6-2-2-VHL,No,,Reviewed,P00519,No,No,No,No,24,212.97
217,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(CCCCCCOCCOCCOCCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CC4)c(OC)cc23)c(Cl)cc1Cl,Inactive,No,K562 CML,8.461600000000011,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,20,4,0.063 nM,0.57 nM,bosutinib,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl,CCCCCOCCOCCOCCOCCOCCOCC=O,non-PEG polyether,24,7,21,1307.4499999999991,No,,3UE4,DB8,26593377,BOS-6-(2-)5-2-VHL,No,,Reviewed,P00519,No,No,No,No,24,249.88999999999996
218,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(CCCCCCOCCCCCOCCCCCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CC4)c(OC)cc23)c(Cl)cc1Cl,Inactive,No,K562 CML,11.125899999999994,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,4,0.063 nM,4.6 nM,bosutinib,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl,CCCCCOCCCCCOCCCCCC=O,non-PEG polyether,19,3,16,1229.4269999999995,No,,3UE4,DB8,26593377,BOS-6-5-6-VHL,No,,Reviewed,P00519,No,No,No,No,24,212.97
219,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(CCCCCCOCCOCCOCCCCCC(=O)Nc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)c(OC)cc23)c(Cl)cc1Cl,Active,No,K562 CML,7.771080000000009,c-ABL and BCR-ABL degredation,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,16,3,0.063 nM,0.91 nM,bosutinib,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl,CCCCCOCCOCCOCCCCCC=O,non-PEG polyether,19,4,16,1074.0729999999996,No,,3UE4,DB8,26593377,BOS-6-2-2-6-CRBN,No,,Reviewed,P00519,No,No,No,No,24,223.21999999999997
220,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(CCCCCCOCCOCC(=O)Nc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)c(OC)cc23)c(Cl)cc1Cl,Active,No,K562 CML,6.194080000000006,c-ABL and BCR-ABL degredation,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,3,0.063 nM,0.28 nM,bosutinib,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl,CCCCCOCCOCC=O,non-PEG polyether,12,3,9,973.9119999999999,No,,3UE4,DB8,26593377,BOS-6-2-2-CRBN,No,,Reviewed,P00519,No,No,No,No,24,213.98999999999998
221,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(CCCCCCOCCOCCOCCOCCOCCOCC(=O)Nc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)c(OC)cc23)c(Cl)cc1Cl,Active,No,K562 CML,6.260480000000008,c-ABL and BCR-ABL degredation,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,19,3,0.063 nM,0.38 nM,bosutinib,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl,CCCCCOCCOCCOCCOCCOCCOCC=O,non-PEG polyether,24,7,21,1150.1239999999996,No,,3UE4,DB8,26593377,BOS-6-(2-)5-2-CRBN,No,,Reviewed,P00519,No,No,No,No,24,250.90999999999997
222,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(CCCCCCOCCCCCOCCCCCC(=O)Nc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)c(OC)cc23)c(Cl)cc1Cl,Active,No,K562 CML,8.924780000000005,c-ABL and BCR-ABL degredation,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,3,0.063 nM,2.8 nM,bosutinib,COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl,CCCCCOCCCCCOCCCCCC=O,non-PEG polyether,19,3,16,1072.1009999999997,No,,3UE4,DB8,26593377,BOS-6-5-6-CRBN,No,,Reviewed,P00519,No,No,No,No,24,213.98999999999998
223,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCCCCCOCCOCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Active,No,K562 CML,7.155860000000007,c-ABL degredation,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,16,5,0.030 nM,0.36 nM,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCOCCOCC=O,non-PEG polyether,11,3,8,1058.773,No,,2GQG,1N1,26593377,DAS-6-2-2-VHL,No,,Reviewed,P00519,No,No,No,No,24,216.36999999999995
224,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCCCCCOCCOCCOCCOCCOCCOCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Active,No,K562 CML,7.22226000000001,c-ABL degredation,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,20,5,0.030 nM,0.28 nM,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCOCCOCCOCCOCCOCCOCC=O,non-PEG polyether,23,7,20,1234.984999999999,No,,2GQG,1N1,26593377,DAS-6-(2-)5-2-VHL,No,,Reviewed,P00519,No,No,No,No,24,253.28999999999996
225,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCCCCCOCCCCCOCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1,Active,No,K562 CML,9.886559999999998,c-ABL degredation,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,hydroxyl_to_carbon,16,5,0.030 nM,2.6 nM,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCOCCCCCOCCCCCC=O,non-PEG polyether,18,3,15,1156.961999999999,No,,2GQG,1N1,26593377,DAS-6-5-6-VHL,No,,Reviewed,P00519,No,No,No,No,24,216.36999999999995
226,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCCCCCOCCOCCOCCCCCC(=O)Nc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)n1,Active,No,K562 CML,6.531740000000005,c-ABL and BCR-ABL degredation,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,hydroxyl_to_carbon,16,4,0.030 nM,0.60 nM,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCOCCOCCOCCCCCC=O,non-PEG polyether,18,4,15,1001.6079999999994,No,,2GQG,1N1,26593377,DAS-6-2-2-6-CRBN,No,,Reviewed,P00519,No,No,No,No,24,226.62
227,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCCCCCOCCOCC(=O)Nc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)n1,Active,Yes,K562 CML,4.954740000000003,c-ABL and BCR-ABL degredation,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,hydroxyl_to_carbon,15,4,0.030 nM,0.28 nM,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCOCCOCC=O,non-PEG polyether,11,3,8,901.4469999999998,No,,2GQG,1N1,26593377,DAS-6-2-2-CRBN,No,,Reviewed,P00519,No,No,No,No,24,217.39
228,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCCCCCOCCOCCOCCOCCOCCOCC(=O)Nc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)n1,Active,No,K562 CML,5.021140000000004,c-ABL and BCR-ABL degredation,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,hydroxyl_to_carbon,19,4,0.030 nM,0.26 nM,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCOCCOCCOCCOCCOCCOCC=O,non-PEG polyether,23,7,20,1077.6589999999997,No,,2GQG,1N1,26593377,DAS-6-(2-)5-2-CRBN,No,,Reviewed,P00519,No,No,No,No,24,254.31
229,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCCCCCOCCCCCOCCCCCC(=O)Nc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)n1,Active,No,K562 CML,7.685440000000007,c-ABL and BCR-ABL degredation,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,hydroxyl_to_carbon,15,4,0.030 nM,1.3 nM,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCOCCCCCOCCCCCC=O,non-PEG polyether,18,3,15,999.6359999999993,No,,2GQG,1N1,26593377,DAS-6-5-6-CRBN,No,,Reviewed,P00519,No,No,No,No,24,217.39
230,COc1cc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)ccc1OC(=O)NCCCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,MOLM-13,2.2327700000000004,,Adi Rogel,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,15,5,7.9 nM,13.5 nM,analog of I-BRD9,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OC,NCCCCNC(=O)CO,Alkane,10,4,5,889.9659999999997,No,,,,28418626,1,No,,Reviewed,Q9H8M2,No,No,No,No,4,261.46
231,COc1cc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)ccc1OC(=O)NCCCCCCCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,MOLM-13,3.7931700000000026,,Adi Rogel,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,15,5,7.9 nM,18.9 nM,analog of I-BRD9,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OC,NCCCCCCCCNC(=O)CO,Alkane,14,4,9,946.0739999999994,No,,,,28418626,2,No,,Reviewed,Q9H8M2,No,No,No,No,4,261.46
232,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OCC(=O)NCCCOCCOCCOCCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,MOLM-13,1.6891700000000072,,Adi Rogel,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,18,5,7.9 nM,36.5 nM,analog of I-BRD9,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OC,O=CNCCCOCCOCCOCCCNC(=O)CO,PEG,21,8,16,1036.1519999999994,No,,,,28418626,S1,No,,Reviewed,Q9H8M2,No,No,No,No,4,289.15
233,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OCC(=O)NCCCCCCOc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,MOLM-13,3.303370000000002,,Adi Rogel,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,14,4,7.9 nM,30 nM,analog of I-BRD9,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OC,O=CNCCCCCCO,Alkane,10,3,7,874.9949999999997,No,,,,28418626,3,No,,Reviewed,Q9H8M2,No,No,No,No,4,232.35999999999999
234,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OCC(=O)N1CCC(C2CCN(C(=O)Oc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)CC1,Active,No,MOLM-13,3.697370000000002,,Adi Rogel,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,15,3,7.9 nM,12.5 nM,analog of I-BRD9,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OC,O=CN1CCC(C2CCN(C(=O)O)CC2)CC1,Other,17,5,2,970.0959999999994,No,,,,28418626,S2,No,,Reviewed,Q9H8M2,No,No,No,No,4,243.88
235,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OCC(=O)NCCOCCOCCOCCN[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C,Inactive,No,MOLM-13,4.02699000000001,,Adi Rogel,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,18,6,7.9 nM,26.9 nM,analog of I-BRD9,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OC,CCOCCOCCOCCNC=O,PEG,14,5,11,1107.387999999999,No,,,,28418626,S3,No,,Reviewed,Q9H8M2,No,No,No,No,4,261.83
236,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OCC(=O)NCCOCCOCCN[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C,Inactive,No,MOLM-13,4.010390000000009,,Adi Rogel,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,17,6,7.9 nM,22.7 nM,analog of I-BRD9,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OC,CCOCCOCCNC=O,PEG,11,4,8,1063.3349999999991,No,,,,28418626,S4,No,,Reviewed,Q9H8M2,No,No,No,No,4,252.59999999999997
237,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OCC(=O)NCCCCCCCCNc1ccc2c(c1)C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,MOLM-13,4.116670000000003,,Adi Rogel,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,14,5,7.9 nM,11.5 nM,analog of I-BRD9,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OC,NCCCCCCCCNC=O,Alkane,12,3,9,902.0649999999995,No,,,,28418626,S5,No,,Reviewed,Q9H8M2,No,No,No,No,4,235.16
238,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OCC(=O)NCCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,MOLM-13,4.116670000000003,,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,14,5,7.9 nM,15.5 nM,analog of I-BRD9,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OC,CCCCCCCCNC=O,Alkane,11,2,8,902.0649999999995,No,,,,28418626,4,No,,Reviewed,Q9H8M2,No,No,No,No,4,235.16
239,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OCC(=O)NCCCCCCCCNc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Active,No,MOLM-13,4.476470000000003,,Adi Rogel,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,5,7.9 nM,12.3 nM,analog of I-BRD9,COc1ccc(-c2cn(C)c(=O)c3cc(C(=N)NC4CCS(=O)(=O)CC4)sc23)cc1OC,CCCCCCCCNC=O,Alkane,11,2,8,888.0819999999994,"BET bromodomains (BRD4, BRD7)",,,,28418626,5,Yes,,Reviewed,Q9H8M2,No,Yes,No,Yes,4,218.09
240,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)CC(=O)NCCCCCCNc1ccc2c(c1)C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,MOLM-13,3.2394000000000016,,Adi Rogel,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,12,3,,56.6 nM,BI-7273,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,NCCCCCCNC=O,Alkane,10,3,7,751.8410000000002,No,,5EU1,5SW,28418626,S6,No,,Reviewed,Q9H8M2,No,No,No,No,4,181.27
241,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)CC(=O)NCCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,MOLM-13,4.019600000000002,,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,12,3,,83.1 nM,BI-7273,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CCCCCCCCNC=O,Alkane,11,2,8,779.8950000000002,No,,5EU1,5SW,28418626,S7,No,,Reviewed,Q9H8M2,No,No,No,No,4,181.27
242,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)CC(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C,Inactive,No,MOLM-13,3.456520000000011,,Adi Rogel,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,4,,43.2 nM,BI-7273,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,O=CCOCCOCCOCCNC=O,PEG,15,6,12,999.2009999999999,No,,5EU1,5SW,28418626,S8,No,,Reviewed,Q9H8M2,No,No,No,No,4,225.01
243,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)CC(=O)NCCCCCCCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,MOLM-13,3.1027000000000022,,Adi Rogel,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,13,3,,48 nM,BI-7273,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,O=CNCCCCCCCCNC(=O)CO,Alkane,16,5,11,837.9310000000002,No,,5EU1,5SW,28418626,S9,No,,Reviewed,Q9H8M2,No,No,No,No,4,207.57000000000002
244,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)CC(=O)NCCOCCOCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,Yes,MOLM-13,1.7122000000000035,,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,14,3,,104 nM,BI-7273,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CCOCCOCCNC=O,PEG,11,4,8,783.8390000000002,No,,5EU1,5SW,28418626,6 (dBRD9),No,,Reviewed,Q9H8M2,No,No,No,No,4,199.73000000000002
245,CC(C)(C)c1cnc(CSc2cnc(NC(=O)C3CCN(CC(=O)NCCOCCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)s2)o1,Active,Yes,MOLT4,3.0507000000000044,tested competition with ligand and with thalidomide. EC for ligand and PROTAC was measured in MOLT-4 cell line.,Ella Livnah,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,16,4,,,SNS-032,CC(C)(C)c1cnc(CSc2cnc(NC(=O)C3CCNCC3)s2)o1,CCOCCOCCOCCNC(C)=O,PEG,15,5,10,869.0360000000001,No,,,,29251720,thal-sns-032,Yes,,Reviewed,P50750,No,Yes,No,Yes,6,223.63
246,N#CC1(CNc2cccc(-c3cc(N[C@H]4CC[C@H](NCC(=O)NCCOCCOCCOCCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)ncc3Cl)n2)CCOCC1,Inactive,No,MOLT4,3.9113800000000056,EC50 of ligand is measured on MOLT-4 cell line,Ella Livnah,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,6,< 0.514 nM,,NVP-2,COC[C@@H](C)N[C@H]1CC[C@H](Nc2cc(-c3cccc(NCC4(C#N)CCOCC4)n3)c(Cl)cn2)CC1,CCCOCCOCCOCCN,PEG,13,4,10,943.5029999999997,No,,,,29251720,thal-nvp-2-03-009 (4),No,,Reviewed,P50750,No,No,No,No,6,247.25999999999996
247,N#CC1(CNc2cccc(-c3cc(N[C@H]4CC[C@H](NCCCCCCNc5cccc6c5C(=O)C(C5CCC(=O)NC5=O)C6=O)CC4)ncc3Cl)n2)CCOCC1,Active,No,MOLT4,6.562480000000007,achieved full degradation after 24hrs with addition of off-target CDK10 degradation. EC50 of ligand is measured on MOLT-4 cell line,Ella Livnah,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,5,< 0.514 nM,,NVP-2,COC[C@@H](C)N[C@H]1CC[C@H](Nc2cc(-c3cccc(NCC4(C#N)CCOCC4)n3)c(Cl)cn2)CC1,O=CNC=O,Alkane,5,3,2,795.3849999999999,CDK10 after 24hr treatment,,,,29251720,thal-nvp-2-03-069 (5),No,,Reviewed,P50750,No,No,No,No,"6,24",187.22999999999993
248,N#CC1(CNc2cccc(-c3cc(N[C@H]4CC[C@H](NCCCCCCNC(=O)CNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)ncc3Cl)n2)CCOCC1,Inactive,No,MOLT4,5.031880000000003,EC50 of ligand is measured on MOLT-4 cell line,Ella Livnah,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,6,< 0.514 nM,,NVP-2,COC[C@@H](C)N[C@H]1CC[C@H](Nc2cc(-c3cccc(NCC4(C#N)CCOCC4)n3)c(Cl)cn2)CC1,CCCCNC(C)=O,Alkane,8,2,3,853.4249999999996,No,,,,29251720,thal-nvp-2-03-084 (6),No,,Reviewed,P50750,No,No,No,No,6,219.56999999999996
249,N#CC1(CNc2cccc(-c3cc(N[C@H]4CC[C@H](NCCCC(=O)NCCCCOc5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)ncc3Cl)n2)CCOCC1,Inactive,No,MOLT4,4.9987800000000036,EC50 of ligand is measured on MOLT-4 cell line,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,13,5,< 0.514 nM,,NVP-2,COC[C@@H](C)N[C@H]1CC[C@H](Nc2cc(-c3cccc(NCC4(C#N)CCOCC4)n3)c(Cl)cn2)CC1,CC(=O)NCCCCO,Alkane,9,3,4,854.4089999999997,No,,,,29251720,thal-nvp-2-03-105 (7),No,,Reviewed,P50750,No,No,No,No,6,216.76999999999995
250,Cc1nn(C)c(COc2ccc(N3CCN(S(=O)(=O)N(C)C)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)O)n(CCN3CCN(C(=O)CCC(=O)NCCCOCCOCCOCCCNC(=O)COc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)c12,Active,No,,5.187620000000016,,Barr Tivon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,morpholine_to_piperazine,21,4,19 nM,,A-1210477,Cc1nn(C)c(COc2ccc(N3CCN(S(=O)(=O)N(C)C)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)O)n(CCN3CCOCC3)c12,NC(=O)CCC(=O)NCCCOCCOCCOCCCNC(=O)CO,PEG,26,10,18,1465.695,No,,,,31117518,dMCL1-1,No,,Reviewed,Q07820,No,No,No,No,,324.5899999999999
251,Cc1nn(C)c(COc2ccc(N3CCN(S(=O)(=O)N(C)C)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)O)n(CCN3CCN(C(=O)COc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)c12,Active,Yes,OPM2,5.345020000000006,,Barr Tivon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,morpholine_to_piperazine,16,2,19 nM,30 nM,A-1210477,Cc1nn(C)c(COc2ccc(N3CCN(S(=O)(=O)N(C)C)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)O)n(CCN3CCOCC3)c12,NC(=O)CO,Alkane,5,3,1,1163.3239999999998,No,,,,31117518,dMCL1-2,No,,Reviewed,Q07820,No,No,No,Yes,48,238.69999999999996
252,Cc1nn(C)c(COc2ccc(N3CCN(S(=O)(=O)N(C)C)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)NCCCCNC(=O)COc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)n(CCN3CCOCC3)c12,Inactive,No,,5.461020000000008,,Barr Tivon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,carboxilic_acid_to_amide,17,3,19 nM,,A-1210477,Cc1nn(C)c(COc2ccc(N3CCN(S(=O)(=O)N(C)C)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)O)n(CCN3CCOCC3)c12,NCCCCNC(=O)CO,Alkane,10,4,5,1234.4470000000001,No,,,,31117518,dMCL1-3,No,,Reviewed,Q07820,No,No,No,No,,248.51999999999998
253,Cc1nn(C)c(COc2ccc(N3CCN(C(=O)CCNC(=O)CCCOCCOCCOCCCNC(=O)COc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)O)n(CCN3CCOCC3)c12,Active,No,,6.095820000000015,modest to poor activity,Barr Tivon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,20,4,19 nM,,A-1210477,Cc1nn(C)c(COc2ccc(N3CCN(S(=O)(=O)N(C)C)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)O)n(CCN3CCOCC3)c12,O=CCCNC(=O)CCCOCCOCCOCCCNC(=O)CO,PEG,25,9,18,1359.545,No,,,,31117518,dMCL1-4,No,,Reviewed,Q07820,No,No,No,No,,293.2
254,Cc1nn(C)c(COc2ccc(N3CCN(C(=O)COc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)O)n(CCN3CCOCC3)c12,Active,No,,6.253220000000007,modest to poor activity,Barr Tivon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,15,2,19 nM,,A-1210477,Cc1nn(C)c(COc2ccc(N3CCN(S(=O)(=O)N(C)C)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)O)n(CCN3CCOCC3)c12,O=CCO,Alkane,4,2,1,1057.1739999999998,No,,,,31117518,dMCL1-5,No,,Reviewed,Q07820,No,No,No,No,,207.30999999999997
255,Cc1nn(C)c(COc2ccc(N3CCN(C(=O)CCCNC(=O)COc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)O)n(CCN3CCOCC3)c12,Active,No,,6.149620000000007,modest to poor activity,Barr Tivon,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,16,3,19 nM,,A-1210477,Cc1nn(C)c(COc2ccc(N3CCN(S(=O)(=O)N(C)C)CC3)cc2)c1-c1cccc2c(CCCOc3cccc4ccccc34)c(C(=O)O)n(CCN3CCOCC3)c12,O=CCCCNC(=O)CO,Alkane,10,4,5,1142.2800000000002,No,,,,31117518,dMCL1-6,No,,Reviewed,Q07820,No,No,No,No,,236.40999999999997
256,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOCCOCCN2CCN(c3cc(-c4ccccc4O)nnc3N)CC2)c1,Active,No,MV-4-11,3.7085200000000036,"poor cellular permeability, ternary complex crystal structure: 6HAY (VCB:PROTAC 1:SMARCA2). DC50 is SMARCA2 300nM, SMARCA4 250nM. DCmax isSMARCA2 65%, SMARCA4 70%.",Efrat Resnick,< 300 nM,< 70 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,15,5,,,SMARCABD,Nc1nnc(-c2ccccc2O)cc1N1CCNCC1,CCOCCOCCO,PEG,9,3,6,918.1059999999993,No,,6HAZ,FX5,31178587,PROTAC 1,No,,Reviewed,"P51531, P51532",No,Yes,No,No,,217.83
257,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1,Active,No,,5.418020000000005,"ternary complex crystal structure: 6HAX (VCB:PROTAC 2:SMARCA2BD), 6HAR2 (VCB:PROTAC 2:SMARCA4BD)",Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,13,5,,,SMARCABD,Nc1nnc(-c2ccccc2O)cc1N1CCNCC1,Cc1ccc(CCO)cc1,Other,10,1,2,920.1249999999994,No,,6HAZ,FX5,31178587,PROTAC 2,No,,Reviewed,"P51531, P51532",Yes,Yes,No,No,,199.36999999999998
258,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1,Active,Yes,"MV-4-11 SK-MEL-5, NCI-H1568",5.254320000000003,"EC50 of PROTAC is 28nM in MV-4-11, 68nM in NCI-H1568. DC50 is (SMARCA2 6nM, SMARCA4 11nM, PBRM1 32nM in MV-4-11; SMARCA2 3.3nM, PBRM1 15.6nM in NCI-H1568)",Efrat Resnick,< 32 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,14,5,,,SMARCABD,Nc1nnc(-c2ccccc2O)cc1N1CCNCC1,Cc1ccc(OCCO)cc1,Other,11,2,3,936.1239999999995,No,,6HAZ,FX5,31178587,ACBI1,Yes,,Reviewed,"P51531, P51532",Yes,Yes,No,No,18,208.6
259,C[C@@H]1C[C@@H](O)c2ncnc(C3CCN(C(=O)[C@H](CNCCCCCCCCCCc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)c4ccc(Cl)cc4)CC3)c21,Active,Yes,MDA-MB-468,6.874500000000007,"IC50 of ligand is AKT1 5 nM, AKT2 18 nM, AKT3 8 nM. EC50 of ligand is 0.229-12.9 uM (cell dependant). EC50 of PROTAC is 0.016-1.65 uM (cell dependant). EC50 of PROTAC is AKT1 2 nM, AKT2 6.8 nM, AKT3 3.5 nM.",Rambabu Reddi,2 nM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,8,3,< 18 nM,< 6.8 nM,GDC-0068,CC(C)NC[C@@H](C(=O)N1CCC(c2ncnc3c2[C@H](C)C[C@H]3O)CC1)c1ccc(Cl)cc1,CCCCCCCC,Alkane,8,0,5,797.4410000000001,No,,4EKL,0RF,31859249,INY-03-041,Yes,,Reviewed,P31750,Yes,Yes,No,Yes,12,144.82999999999998
260,O=C(NC1CCNCC1)c1n[nH]cc1NC(=O)c1c(Cl)cccc1Cl,Inactive,No,PC-3,2.4505999999999997,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,4,4,,,AT-7519,O=C(NC1CCNCC1)c1n[nH]cc1NC(=O)c1c(Cl)cccc1Cl,None,Alkane,0,0,0,382.2510000000001,No,,,,31846828,A1,No,,Reviewed,"P24941, P50750",No,No,No,No,12,98.91
261,O=C(COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)NCCCCCC(=O)N1CCC(NC(=O)c2n[nH]cc2NC(=O)c2c(Cl)cccc2Cl)CC1,Active,No,PC-3,2.846400000000002,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,10,5,,,AT-7519,O=C(NC1CCNCC1)c1n[nH]cc1NC(=O)c1c(Cl)cccc1Cl,O=CCCCCCNC(=O)CO,Alkane,12,4,7,809.664,No,,,,31846828,A2,No,,Reviewed,"P24941, P50750",No,No,No,No,12,229.07
262,O=C(CCC(=O)N1CCC(NC(=O)c2n[nH]cc2NC(=O)c2c(Cl)cccc2Cl)CC1)NCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,PC-3,2.099300000000001,,Ella Livnah,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,10,6,,,AT-7519,O=C(NC1CCNCC1)c1n[nH]cc1NC(=O)c1c(Cl)cccc1Cl,CCNC(=O)CCC=O,Alkane,9,3,4,780.626,No,,,,31846828,A3,No,,Reviewed,"P24941, P50750",No,No,No,No,12,231.86999999999998
263,O=C(CCC(=O)N1CCC(NC(=O)c2n[nH]cc2NC(=O)c2c(Cl)cccc2Cl)CC1)NCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,PC-3,2.879500000000001,,Ella Livnah,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,10,6,,,AT-7519,O=C(NC1CCNCC1)c1n[nH]cc1NC(=O)c1c(Cl)cccc1Cl,CCCCNC(=O)CCC=O,Alkane,11,3,6,808.6799999999998,No,,,,31846828,A4,No,,Reviewed,"P24941, P50750",No,No,No,No,12,231.86999999999998
264,O=C(CCC(=O)N1CCC(NC(=O)c2n[nH]cc2NC(=O)c2c(Cl)cccc2Cl)CC1)NCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,PC-3,3.6597000000000017,,Ella Livnah,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,10,6,,,AT-7519,O=C(NC1CCNCC1)c1n[nH]cc1NC(=O)c1c(Cl)cccc1Cl,CCCCCCNC(=O)CCC=O,Alkane,13,3,8,836.7339999999997,No,,,,31846828,A5,No,,Reviewed,"P24941, P50750",No,No,No,No,12,231.86999999999998
265,O=C(CCC(=O)N1CCC(NC(=O)c2n[nH]cc2NC(=O)c2c(Cl)cccc2Cl)CC1)NCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,PC-3,1.182400000000002,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,11,6,,,AT-7519,O=C(NC1CCNCC1)c1n[nH]cc1NC(=O)c1c(Cl)cccc1Cl,O=CCCC(=O)NCCNC(=O)CO,Alkane,14,6,7,838.6619999999999,No,,,,31846828,A6,No,,Reviewed,"P24941, P50750",No,No,No,No,12,258.16999999999996
266,O=C(CCC(=O)N1CCC(NC(=O)c2n[nH]cc2NC(=O)c2c(Cl)cccc2Cl)CC1)NCCCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,PC-3,1.9626000000000006,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,11,6,,,AT-7519,O=C(NC1CCNCC1)c1n[nH]cc1NC(=O)c1c(Cl)cccc1Cl,O=CCCC(=O)NCCCCNC(=O)CO,Alkane,16,6,9,866.7159999999998,No,,,,31846828,A7,No,,Reviewed,"P24941, P50750",No,No,No,No,12,258.16999999999996
267,O=C(CCC(=O)N1CCC(NC(=O)c2n[nH]cc2NC(=O)c2c(Cl)cccc2Cl)CC1)NCCCCCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,PC-3,2.742800000000001,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,11,6,,,AT-7519,O=C(NC1CCNCC1)c1n[nH]cc1NC(=O)c1c(Cl)cccc1Cl,O=CCCC(=O)NCCCCCCNC(=O)CO,Alkane,18,6,11,894.7699999999996,No,,,,31846828,A8,No,,Reviewed,"P24941, P50750",No,No,No,No,12,258.16999999999996
268,O=C(COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)NCCOCCOCC(=O)N1CCC(NC(=O)c2n[nH]cc2NC(=O)c2c(Cl)cccc2Cl)CC1,Active,No,PC-3,1.3192000000000037,Controls were done against CDK2. tested competition with ligand and with pomalidomide,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,12,5,,,AT-7519,O=C(NC1CCNCC1)c1n[nH]cc1NC(=O)c1c(Cl)cccc1Cl,O=CCOCCOCCNC(=O)CO,PEG,14,6,9,841.662,No,,,,31846828,A9,No,,Reviewed,"P24941, P50750",No,Yes,No,Yes,12,247.52999999999997
269,O=C(CCC(=O)N1CCC(NC(=O)c2n[nH]cc2NC(=O)c2c(Cl)cccc2Cl)CC1)NCCCOCCOCCOCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,PC-3,1.622300000000005,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,14,6,,,AT-7519,O=C(NC1CCNCC1)c1n[nH]cc1NC(=O)c1c(Cl)cccc1Cl,O=CCCC(=O)NCCCOCCOCCOCCNC(=O)CO,PEG,24,9,17,984.8479999999995,No,,,,31846828,A10,No,,Reviewed,"P24941, P50750",No,No,No,No,12,285.85999999999996
270,O=C(COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)NCCCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1,Active,No,PC-3,1.697700000000003,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,13,6,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,O=CCCCNC(=O)CO,Alkane,10,4,5,816.8359999999999,No,,,,31846828,F1,No,,Reviewed,"P24941, P50750",No,No,No,No,12,256.81
271,O=C(COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)NCCCCCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1,Active,No,PC-3,2.4779000000000027,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,13,6,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,O=CCCCCCNC(=O)CO,Alkane,12,4,7,844.89,No,,,,31846828,F2,No,,Reviewed,"P24941, P50750",No,No,No,No,12,256.81
272,O=C(CCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1)NCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,Yes,PC-3,1.7308000000000008,"preferentially degrades CDK9 over CDK2. Controls were done against CDK2 and CDK9. tested competition with ligand and with pomalidomide. DC50 is CDK2: 62 nM, CDK9: 33 nM.",Ella Livnah,< 62 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,13,7,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,CCNC(=O)CCC=O,Alkane,9,3,4,815.8519999999997,No,,,,31846828,F3,No,,Reviewed,"P24941, P50750",No,Yes,No,Yes,12,259.61
273,O=C(CCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1)NCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,PC-3,2.511000000000001,,Ella Livnah,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,13,7,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,CCCCNC(=O)CCC=O,Alkane,11,3,6,843.9059999999996,No,,,,31846828,F4,No,,Reviewed,"P24941, P50750",No,No,No,No,12,259.61
274,O=C(CCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1)NCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,PC-3,3.291200000000001,,Ella Livnah,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,13,7,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,CCCCCCNC(=O)CCC=O,Alkane,13,3,8,871.9599999999995,No,,,,31846828,F5,No,,Reviewed,"P24941, P50750",No,No,No,No,12,259.61
275,O=C(CCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1)NCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,PC-3,0.8139000000000034,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,14,7,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,O=CCCC(=O)NCCNC(=O)CO,Alkane,14,6,7,873.8879999999997,No,,,,31846828,F6,No,,Reviewed,"P24941, P50750",No,No,No,No,12,285.90999999999997
276,O=C(CCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1)NCCCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,PC-3,1.5941000000000027,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,14,7,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,O=CCCC(=O)NCCCCNC(=O)CO,Alkane,16,6,9,901.9419999999996,No,,,,31846828,F7,No,,Reviewed,"P24941, P50750",No,No,No,No,12,285.90999999999997
277,O=C(CCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1)NCCCCCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,PC-3,2.3743000000000025,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,14,7,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,O=CCCC(=O)NCCCCCCNC(=O)CO,Alkane,18,6,11,929.9959999999994,No,,,,31846828,F8,No,,Reviewed,"P24941, P50750",No,No,No,No,12,285.90999999999997
278,O=C(COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)NCCOCCOCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1,Active,No,PC-3,0.9507000000000062,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,15,6,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,O=CCOCCOCCNC(=O)CO,PEG,14,6,9,876.8879999999998,No,,,,31846828,F9,No,,Reviewed,"P24941, P50750",No,No,No,No,12,275.27
279,O=C(CCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1)NCCCOCCOCCOCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,PC-3,1.2538000000000065,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,17,7,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,O=CCCC(=O)NCCCOCCOCCOCCNC(=O)CO,PEG,24,9,17,1020.0739999999993,No,,,,31846828,F10,No,,Reviewed,"P24941, P50750",No,No,No,No,12,313.5999999999999
280,O=C(CCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1)NCCNc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Active,No,PC-3,2.0906000000000016,,Ella Livnah,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,12,7,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,CCNC(=O)CCC=O,Alkane,9,3,4,801.8689999999997,No,,,,31846828,F11,No,,Reviewed,"P24941, P50750",Yes,No,No,No,12,242.54
281,O=C(CCC(=O)N1CCN(Cc2ccc(NC(=O)c3n[nH]cc3Nc3ncnc4[nH]ccc34)cc2)CC1)NCCNc1ccc2c(c1)C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,PC-3,1.7308000000000008,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_amide,13,7,,,FN-1501,O=C(Nc1ccc(CN2CCNCC2)cc1)c1n[nH]cc1Nc1ncnc2[nH]ccc12,NCCNC(=O)CCC=O,Alkane,10,4,5,815.8519999999997,No,,,,31846828,F12,No,,Reviewed,"P24941, P50750",No,No,No,No,12,259.61
282,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCNC(=O)c2ccc(-c3cnc(NCc4ccco4)n4cnnc34)cc2)C(C)(C)C)cc1,Active,No,HeLa,4.357320000000003,,Shimrit Azulay,,47 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,13,5,45 nM,275 nM,EED226,CS(=O)(=O)c1ccc(-c2cnc(NCc3ccco3)n3cnnc23)cc1,O=CCCNC=O,Alkane,7,3,4,818.9609999999999,No,,5WUK,73K,31831267,UNC6851,No,,Reviewed,"O75530, Q15022, Q15910",No,No,No,No,24,208.98000000000002
283,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCNC(=O)c2ccc(-c3cnc(NCc4ccco4)n4cnnc34)cc2)C(C)(C)C)cc1,Active,Yes,"HeLa, DLBCL",4.7474200000000035,DC50 value is for HeLa cells. DC50 is 0.61 uM for DLBCL cells. DMAX value is for HeLa cells. DMAX is 96 % for DLBCL cells.,Shimrit Azulay,0.79 uM,92 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,13,5,45 nM,247 nM,EED226,CS(=O)(=O)c1ccc(-c2cnc(NCc3ccco3)n3cnnc23)cc1,O=CCCCNC=O,Alkane,8,3,5,832.9879999999998,"EZH2, SUZ12",,5WUK,73K,31831267,UNC6852,Yes,,Reviewed,"O75530, Q15022, Q15910",Yes,No,No,Yes,24,208.98000000000002
284,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCNC(=O)c2ccc(-c3cnc(NCc4ccco4)n4cnnc34)cc2)C(C)(C)C)cc1,Inactive,No,HeLa,5.137520000000003,,Shimrit Azulay,,24 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,13,5,45 nM,368 nM,EED226,CS(=O)(=O)c1ccc(-c2cnc(NCc3ccco3)n3cnnc23)cc1,O=CCCCCNC=O,Alkane,9,3,6,847.0149999999999,No,,5WUK,73K,31831267,UNC6853,No,,Reviewed,"O75530, Q15022, Q15910",No,No,No,No,24,208.98000000000002
285,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOCCNC(=O)c2ccc(-c3cnc(NCc4ccco4)n4cnnc34)cc2)C(C)(C)C)cc1,Inactive,No,HeLa,4.390520000000003,,Shimrit Azulay,,0.03 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,15,5,45 nM,82 nM,EED226,CS(=O)(=O)c1ccc(-c2cnc(NCc3ccco3)n3cnnc23)cc1,O=CCCOCCOCCNC=O,PEG,13,5,10,907.0669999999999,No,,5WUK,73K,31831267,UNC6845,No,,Reviewed,"O75530, Q15022, Q15910",No,No,No,No,24,227.44
286,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCNC(=O)c2ccc(-c3cnc(NCc4ccco4)n4cnnc34)cc2)C(C)(C)C)cc1,Inactive,No,HeLa,4.017020000000005,,Shimrit Azulay,,0.04 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,16,5,45 nM,613 nM,EED226,CS(=O)(=O)c1ccc(-c2cnc(NCc3ccco3)n3cnnc23)cc1,O=CCOCCOCCOCCNC=O,PEG,15,6,12,937.0929999999998,No,,5WUK,73K,31831267,UNC6846,No,,Reviewed,"O75530, Q15022, Q15910",No,No,No,No,24,236.67000000000002
287,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOCCOCCOCCNC(=O)c2ccc(-c3cnc(NCc4ccco4)n4cnnc34)cc2)C(C)(C)C)cc1,Inactive,No,HeLa,4.4237200000000065,,Shimrit Azulay,,29 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,17,5,45 nM,241 nM,EED226,CS(=O)(=O)c1ccc(-c2cnc(NCc3ccco3)n3cnnc23)cc1,O=CCCOCCOCCOCCOCCNC=O,PEG,19,7,16,995.1729999999997,No,,5WUK,73K,31831267,UNC6847,No,,Reviewed,"O75530, Q15022, Q15910",No,No,No,No,24,245.89999999999998
288,O=C1CCC(N2C(=O)c3cccc(NCCOCCOCCNC(=O)c4ccc(CN(CC5CCCCC5)S(=O)(=O)c5ccc(S(=O)(=O)N(Cc6ccc(Cl)cc6)C6CCCC6)cc5)cc4)c3C2=O)C(=O)N1,Active,No,Jurkat,6.521000000000007,"proteomics of PDEdelta degradation show upregulation of enzymes involved in lipid metabolism - deltasonamide 1 also causes this. IC50 Deltasonamide 1 is 203 pM, and of the Bn derivative is 8 nM.",Paul Gehrtz,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,carboxilic_acid_to_amide,12,3,8 nM,14.8 nM,deltasonamide 1 Bn derivative,O=C(O)c1ccc(CN(CC2CCCCC2)S(=O)(=O)c2ccc(S(=O)(=O)N(Cc3ccc(Cl)cc3)C3CCCC3)cc2)cc1,NCCOCCOCCN,PEG,10,4,7,1045.678,ferritin light chain,,5ML8,V98,31829492,1,Yes,,Reviewed,O43924,No,No,No,No,"24,48",217.89999999999998
289,O=C1CCC(N2C(=O)c3cccc(NCCOCCOCCOCCNC(=O)c4ccc(CN(CC5CCCCC5)S(=O)(=O)c5ccc(S(=O)(=O)N(Cc6ccc(Cl)cc6)C6CCCC6)cc5)cc4)c3C2=O)C(=O)N1,Active,No,Jurkat,6.537600000000007,"proteomics of PDEdelta degradation show upregulation of enzymes involved in lipid metabolism - deltasonamide 1 also causes this. IC50 Deltasonamide 1 is 203 pM, and of the Bn derivative is 8 nM.",Paul Gehrtz,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,carboxilic_acid_to_amide,13,3,8 nM,27.0 nM,deltasonamide 1 Bn derivative,O=C(O)c1ccc(CN(CC2CCCCC2)S(=O)(=O)c2ccc(S(=O)(=O)N(Cc3ccc(Cl)cc3)C3CCCC3)cc2)cc1,NCCOCCOCCOCCN,PEG,13,5,10,1089.731,ferritin light chain,,5ML8,V98,31829492,2,Yes,,Reviewed,O43924,No,No,No,No,"24,48",227.13
290,O=C1CCC(N2C(=O)c3cccc(NCCOCCOCCOCCOCCNC(=O)c4ccc(CN(CC5CCCCC5)S(=O)(=O)c5ccc(S(=O)(=O)N(Cc6ccc(Cl)cc6)C6CCCC6)cc5)cc4)c3C2=O)C(=O)N1,Active,Yes,Jurkat and Panc Tu‐I,6.554200000000007,"proteomics of PDEdelta degradation show upregulation of enzymes involved in lipid metabolism - deltasonamide 1 also causes this. Dmax was measured in Panc-Tu-1 cell line. DC50 is 83.4% (24 h, Panc-Tu-1), 85% (24 h, 1 uM, Jurkat). IC50 Deltasonamide 1 is 203 pM, and of the Bn derivative is 8 nM.",Paul Gehrtz,48 nM,> 83.4 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,carboxilic_acid_to_amide,14,3,8 nM,64.3 nM,deltasonamide 1 Bn derivative,O=C(O)c1ccc(CN(CC2CCCCC2)S(=O)(=O)c2ccc(S(=O)(=O)N(Cc3ccc(Cl)cc3)C3CCCC3)cc2)cc1,NCCOCCOCCOCCOCCN,PEG,16,6,13,1133.7839999999997,ferritin light chain,,5ML8,V98,31829492,3,Yes,,Reviewed,O43924,Yes,No,No,Yes,"24,48",236.35999999999999
291,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@H](NC(=O)COCCOCCOCCOCCNC(=O)c2ccc(CN(CC3CCCCC3)S(=O)(=O)c3ccc(S(=O)(=O)N(Cc4ccc(Cl)cc4)C4CCCC4)cc3)cc2)C(C)C)cc1,Active,No,Jurkat and Panc Tu‐I,7.891820000000014,"proteomics of PDEdelta degradation show upregulation of enzymes involved in lipid metabolism - deltasonamide 1 also causes this. IC50 Deltasonamide 1 is 203 pM, and of the Bn derivative is 8 nM.",Paul Gehrtz,,,CC(=O)N[C@@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)C,VHL,,,carboxilic_acid_to_amide,15,4,8 nM,57.1 nM,deltasonamide 1 Bn derivative,O=C(O)c1ccc(CN(CC2CCCCC2)S(=O)(=O)c2ccc(S(=O)(=O)N(Cc3ccc(Cl)cc3)C3CCCC3)cc2)cc1,NCCOCCOCCOCCO,PEG,13,5,10,1291.0659999999996,ferritin light chain,,5ML8,V98,31829492,5,Yes,,Reviewed,O43924,No,No,No,No,"24,48",252.40999999999997
292,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LNCaP,9.255720000000004,,Adi Rogel,7.2 nM,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(-c2scnc2C)cc1,VHL,,,aryl_C,12,3,8 nM,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC1CCN(C(C)C)CC1,Other,11,1,1,1095.8079999999995,No,,,,31804827,1 (ARD-61),No,,Reviewed,P10275,No,No,No,No,"0.5,1,3,6,12,24",194.22999999999996
293,C#Cc1ccc([C@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)CC2)NC(=O)[C@H]2C[C@H](O)CN2C(=O)[C@@H](c2cc(C)no2)C(C)C)cc1,Active,No,LNCaP,7.80510000000001,,Adi Rogel,,> 99 %,C#Cc1ccc([C@H](CC(=O)NC)NC(=O)[C@H]2C[C@H](O)CN2C(=O)[C@@H](c2cc(C)no2)C(C)C)cc1,VHL,,,aryl_C,10,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC1CCN(C(C)C)CC1,Other,11,1,1,1022.6879999999995,No,,,,31804827,2,No,,Reviewed,P10275,No,No,No,No,6,181.33999999999997
294,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)CC2)c2ccc(C#N)cc2)C(C)C)on1,Active,No,LNCaP,7.69548000000001,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(C#N)cc1,VHL,,,aryl_C,11,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC1CCN(C(C)C)CC1,Other,11,1,1,1023.6759999999996,No,,,,31804827,3,No,,Reviewed,P10275,No,No,No,No,6,205.12999999999994
295,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)CC2)c2ccc(Br)cc2)C(C)C)on1,Active,No,LNCaP,8.586300000000007,,Adi Rogel,,> 95 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(Br)cc1,VHL,,,aryl_C,10,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC1CCN(C(C)C)CC1,Other,11,1,1,1077.5619999999997,No,,,,31804827,4,No,,Reviewed,P10275,No,No,No,No,6,181.33999999999997
296,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)CC2)c2ccc(Cl)cc2)C(C)C)on1,Active,No,LNCaP,8.477200000000007,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(Cl)cc1,VHL,,,aryl_C,10,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC1CCN(C(C)C)CC1,Other,11,1,1,1033.1109999999996,No,,,,31804827,5,No,,Reviewed,P10275,No,No,No,No,6,181.33999999999997
297,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)CC2)c2ccc(F)cc2)C(C)C)on1,Active,No,LNCaP,7.96290000000001,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(F)cc1,VHL,,,aryl_C,10,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC1CCN(C(C)C)CC1,Other,11,1,1,1016.6559999999997,No,,,,31804827,6,No,,Reviewed,P10275,No,No,No,No,6,181.33999999999997
298,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)CC2)c2ccccc2)C(C)C)on1,Active,No,LNCaP,7.82380000000001,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccccc1,VHL,,,aryl_C,10,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC1CCN(C(C)C)CC1,Other,11,1,1,998.6659999999997,No,,,,31804827,7,No,,Reviewed,P10275,No,No,No,No,6,181.33999999999997
299,CC(=O)NC[C@H](C(=O)N1C[C@@H](O)C[C@@H]1C(=O)N[C@@H](CC(=O)N1CCC(N2CCC(C#Cc3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)CC1)c1ccccc1)C(C)C,Inactive,No,LNCaP,6.4958800000000085,,Adi Rogel,,11 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](CNC(C)=O)C(C)C)c1ccccc1,VHL,,,aryl_C,9,4,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC1CCN(C(C)C)CC1,Other,11,1,1,988.6709999999997,No,,,,31804827,8,No,,Reviewed,P10275,No,No,No,No,6,184.40999999999997
300,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)C3)CC2)c2ccccc2)C(C)C)on1,Active,No,LNCaP,7.0436000000000085,,Adi Rogel,,86 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccccc1,VHL,,,aryl_C,10,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC1CN(C(C)C)C1,Other,9,1,1,970.6119999999997,No,,,,31804827,9,No,,Reviewed,P10275,No,No,No,No,6,181.33999999999997
301,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CC(N3CCC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)C2)c2ccccc2)C(C)C)on1,Active,No,LNCaP,7.0436000000000085,,Adi Rogel,,68 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccccc1,VHL,,,aryl_C,10,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC1CCN(C)CC1,Other,9,1,0,970.6119999999997,No,,,,31804827,10,No,,Reviewed,P10275,No,No,No,No,6,181.33999999999997
302,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(C#Cc3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)c2ccccc2)C(C)C)on1,Active,Yes,LNCaP,7.359400000000009,,Adi Rogel,0.5352 nM,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccccc1,VHL,,,aryl_C,9,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC(C)C,Other,5,0,0,915.5319999999999,No,,,,31804827,11 (ARD-266),No,,Reviewed,P10275,No,Yes,No,Yes,"0.5,1,3,6,12,24",178.09999999999997
303,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(C3CN(c4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)C3)CC2)c2ccccc2)C(C)C)on1,Active,No,LNCaP,7.444100000000009,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccccc1,VHL,,,aryl_N,10,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,CC(C)C1CNC1,Other,7,1,1,946.5899999999998,No,,,,31804827,12,No,,Reviewed,P10275,No,No,No,No,6,181.33999999999997
304,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CC(c4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)C3)CC2)c2ccccc2)C(C)C)on1,Active,No,LNCaP,7.159500000000008,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccccc1,VHL,,,aryl_C,10,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,CC(C)N1CCC1,Other,7,1,1,946.5899999999998,No,,,,31804827,13,No,,Reviewed,P10275,No,No,No,No,6,181.33999999999997
305,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(c3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)c2ccccc2)C(C)C)on1,Active,No,LNCaP,7.475300000000009,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccccc1,VHL,,,aryl_C,9,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,CCC,Other,3,0,0,891.5099999999999,No,,,,31804827,14,No,,Reviewed,P10275,No,No,No,No,6,178.09999999999997
306,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCN(c3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)c2ccccc2)C(C)C)on1,Active,No,LNCaP,6.4179000000000075,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccccc1,VHL,,,aryl_N,10,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,CNC,Other,3,1,0,892.4979999999998,No,,,,31804827,15,No,,Reviewed,P10275,No,No,No,No,6,181.33999999999997
307,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(C#Cc3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LNCaP,8.791320000000006,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(-c2scnc2C)cc1,VHL,,,aryl_C,11,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC(C)C,Other,5,0,0,1012.6739999999998,No,,,,31804827,16,No,,Reviewed,P10275,No,No,No,No,6,190.98999999999995
308,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(C#Cc3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)c2ccc(F)cc2)C(C)C)on1,Active,No,LNCaP,7.49850000000001,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(F)cc1,VHL,,,aryl_C,9,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC(C)C,Other,5,0,0,933.5219999999999,No,,,,31804827,17,No,,Reviewed,P10275,No,No,No,No,6,178.09999999999997
309,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(C#Cc3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)c2ccc(Cl)cc2)C(C)C)on1,Active,No,LNCaP,8.01280000000001,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(Cl)cc1,VHL,,,aryl_C,9,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC(C)C,Other,5,0,0,949.9769999999999,No,,,,31804827,18,No,,Reviewed,P10275,No,No,No,No,6,178.09999999999997
310,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(C#Cc3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)c2ccc(Br)cc2)C(C)C)on1,Active,No,LNCaP,8.121900000000009,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(Br)cc1,VHL,,,aryl_C,9,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC(C)C,Other,5,0,0,994.4279999999999,No,,,,31804827,19,No,,Reviewed,P10275,No,No,No,No,6,178.09999999999997
311,Cc1cc([C@H](C(=O)N2C[C@@H](O)C[C@@H]2C(=O)N[C@@H](CC(=O)N2CCC(C#Cc3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)c2ccc(C#N)cc2)C(C)C)on1,Active,No,LNCaP,7.231080000000009,,Adi Rogel,,> 99 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(C#N)cc1,VHL,,,aryl_C,10,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC(C)C,Other,5,0,0,940.5419999999998,No,,,,31804827,20,No,,Reviewed,P10275,No,No,No,No,6,201.89
312,C#Cc1ccc([C@H](CC(=O)N2CCC(C#Cc3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)NC(=O)[C@H]2C[C@H](O)CN2C(=O)[C@@H](c2cc(C)no2)C(C)C)cc1,Active,No,LNCaP,7.340700000000009,,Adi Rogel,,> 99 %,C#Cc1ccc([C@H](CC(=O)NC)NC(=O)[C@H]2C[C@H](O)CN2C(=O)[C@@H](c2cc(C)no2)C(C)C)cc1,VHL,,,aryl_C,9,3,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC(C)C,Other,5,0,0,939.5539999999997,No,,,,31804827,21,No,,Reviewed,P10275,No,No,No,No,6,178.09999999999997
313,CC(=O)N[C@H](C(=O)N1C[C@@H](O)C[C@@H]1C(=O)N[C@@H](CC(=O)N1CCC(C#Cc2ccc(C(=O)N[C@H]3C(C)(C)[C@H](Oc4ccc(C#N)c(Cl)c4)C3(C)C)cc2)CC1)c1ccccc1)C(C)C,Inactive,No,LNCaP,5.783880000000007,,Adi Rogel,,< 5 %,CNC(=O)C[C@H](NC(=O)[C@H]1C[C@H](O)CN1C(=O)[C@@H](CNC(C)=O)C(C)C)c1ccccc1,VHL,,,aryl_C,8,4,,,Apalutamide analog,CC1(C)[C@H](NC(=O)c2ccccc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,C#CC(C)C,Other,5,0,0,891.5099999999999,No,,,,31804827,22,No,,Reviewed,P10275,No,No,No,No,6,181.17
314,CCN(CCOCCOCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF7,7.7630200000000125,also tested degradation for two common mutants of ERa. EC50 of PROTAC was measured in MCF-7 cell line.,Adi Rogel,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,15,5,,,RALOXIFENE,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,O=CCOCCOCCO,PEG,10,4,7,1050.31,No,,2JFA,RAL,32067153,ERD56,No,30990042,Reviewed,P03372,No,No,No,No,24,209.31999999999996
315,CC/C(=C(\c1ccccc1)c1ccc(OCCN(CC)CCCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)cc1)c1ccccc1,Active,No,MCF7,10.118819999999998,also tested degradation for two common mutants of ERa. EC50 of PROTAC was measured in MCF-7 cell line.,Adi Rogel,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,8,3,,,GW5638,CC/C(=C(\c1ccccc1)c1ccc(/C=C/C(=O)O)cc1)c1ccccc1,CCN(CCO)CCCCCC=O,Alkane,13,3,9,912.254,No,,1R5K,GW5,32067153,ERD32,No,30990042,Reviewed,P03372,No,No,No,No,24,124.10000000000001
316,CCCCN(Cc1ccc(C(=O)NO)cc1)C(=O)Nc1ccc(NC(=O)CCCc2cn(CCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nn2)cc1,Active,Yes,"HeLa, Mino, Jeko-1, HUVEC, MDA-MB-231, MM.1S",3.7226000000000026,,"Daniel Zaidman, Yangwode Jing",3.2 nM,~ 100 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_N,13,6,,,Nex A,CCCCN(Cc1ccc(C(=O)NO)cc1)C(=O)Nc1ccccc1,CCOCCn1cc(CCCC(N)=O)nn1,non-PEG polyether,16,6,8,836.907,No,,5G0J,N4R,31769449,NH2,No,30796636,Reviewed,Q9UBN7,Yes,Yes,No,Yes,"1,18,24",246.28999999999996
317,O=C1CCC(N2C(=O)c3cccc(NCCOCCOCCn4cc(CCCCN(Cc5ccc(C(=O)NO)cc5)C(=O)Nc5ccccc5)nn4)c3C2=O)C(=O)N1,Active,No,"Hela, MM.1S",3.0006000000000004,,"Daniel Zaidman, Yangwode Jing",3.8 nM,~ 100 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,5,,,Nex A,CCCCN(Cc1ccc(C(=O)NO)cc1)C(=O)Nc1ccccc1,CCOCCOCCn1ccnn1,non-PEG polyether,13,5,7,795.8540000000004,No,,5G0J,N4R,31769449,NP8,No,30796636,Reviewed,Q9UBN7,Yes,Yes,No,Yes,"2,24",226.42
318,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)NCCOCCOCCNc1cccc3nnn(C4CCC(=O)NC4=O)c(=O)c13)c1nnc(C)n1-2,Active,No,22Rv1,3.533760000000002,,Daniel Zaidman,,36 %,Nc1cccc2nnn(C3CCC(=O)NC3=O)c(=O)c12,Cereblon,,,ester_to_amide,15,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,CCOCCOCCN,Alkane,9,3,6,787.3029999999998,No,,,,30684871,TD-230,No,,Reviewed,O60885,No,No,No,No,24,196.60999999999996
319,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)NCCCCCCCCNc1cccc3nnn(C4CCC(=O)NC4=O)c(=O)c13)c1nnc(C)n1-2,Active,No,22Rv1,5.841160000000005,,Daniel Zaidman,,63 %,Nc1cccc2nnn(C3CCC(=O)NC3=O)c(=O)c12,Cereblon,,,ester_to_amide,13,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,CCCCCCCCN,PEG,9,1,6,783.3589999999999,No,,,,30684871,TD-207,No,,Reviewed,O60885,No,No,No,No,24,178.14999999999998
320,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)Nc1ccc(OCCOCCOCCNc3cccc4nnn(C5CCC(=O)NC5=O)c(=O)c34)cc1)c1nnc(C)n1-2,Active,No,22Rv1,5.435060000000005,,Daniel Zaidman,3.3 nM,100 %,Nc1cccc2nnn(C3CCC(=O)NC3=O)c(=O)c12,Cereblon,,,ester_to_amide,16,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,CCOCCOCCOc1ccc(N)cc1,PEG,16,4,8,879.3999999999999,No,,,,30684871,TD-188,No,,Reviewed,O60885,No,No,No,No,24,205.83999999999997
321,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)Nc1cccc(OCCOCCOCCNc3cccc4nnn(C5CCC(=O)NC5=O)c(=O)c34)c1)c1nnc(C)n1-2,Active,Yes,22Rv1,5.435060000000005,,Daniel Zaidman,0.32 nM,100 %,Nc1cccc2nnn(C3CCC(=O)NC3=O)c(=O)c12,Cereblon,,,ester_to_amide,16,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,CCOCCOCCOc1cccc(N)c1,PEG,16,4,8,879.3999999999997,No,,,,30684871,TD-428,No,,Reviewed,O60885,No,Yes,No,Yes,24,205.83999999999997
322,COc1ccc(C2=NC(c3ccc(Cl)cc3)C(c3ccc(Cl)cc3)N2C(=O)N2CCN(CC(=O)NCCOCCOCCOCC(=O)Nc3ccc(OCC(C)(O)C(=O)Nc4ccc([N+](=O)[O-])c(C(F)(F)F)c4)cc3)C(=O)C2)c(OC(C)C)c1,Active,Yes,HeLa,8.098400000000012,,Daniel Zaidman,,,COc1ccc(C2=NC(c3ccc(Cl)cc3)C(c3ccc(Cl)cc3)N2C(=O)N2CCNC(=O)C2)c(OC(C)C)c1,Mdm2,,,aliphatic_CO,15,4,4 nM,,SARM,CC(=O)Nc1ccc(OCC(C)(O)C(=O)Nc2ccc([N+](=O)[O-])c(C(F)(F)F)c2)cc1,CC(=O)NCCOCCOCCO,PEG,13,5,8,1210.0569999999996,No,,,,18752944,SARM-nutlin PROTAC,No,,Reviewed,P10275,No,No,No,Yes,7,262.27
323,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2[C@@H](F)[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCNC(=O)C[C@@H]2N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc32)C(C)(C)C)cc1,Active,Yes,"HeLa, MV4;11, A549",5.544680000000006,DC50 is 1-3nM,Daniel Zaidman,< 3 nM,100 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2[C@@H](F)[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,15,4,,249 nM,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCOCCOCCOCC=O,PEG,13,5,10,1020.6509999999995,"BRD2, BRD3",,,,29949369,15a,No,,Reviewed,O60885,No,No,No,No,24,211.48999999999995
324,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2[C@H](F)[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCNC(=O)C[C@@H]2N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc32)C(C)(C)C)cc1,Active,No,"HeLa, MV4;11, A549",5.544680000000006,DC50 is 10-30nM,Daniel Zaidman,< 30 nM,99 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2[C@H](F)[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,15,4,,603 nM,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCOCCOCCOCC=O,PEG,13,5,10,1020.6509999999995,"BRD2, BRD3",,,,29949369,15b,No,,Reviewed,O60885,No,No,No,No,24,211.48999999999995
325,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CC(=O)NCCOCCOCCOCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,AML cells,2.3575200000000027,,Daniel Zaidman,,~ 100 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,18,4,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCCOCCNC(C)=O,PEG,15,5,10,936.0399999999996,"CDK4, IKZF1, IKZF3",,5L2I,LQQ,30595531,YKL-06-102,Yes,,Reviewed,"P11802, Q00534",No,Yes,No,Yes,4,248.62
326,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CCOCCOCCOCCNC(=O)COc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,Yes,"AML cells, CRBN-/-",2.3244200000000035,,Daniel Zaidman,,~ 100 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,18,3,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCCOCCNC(=O)CO,PEG,16,6,11,937.0239999999997,No,,5L2I,LQQ,30595531,BSJ-03-123,Yes,,Reviewed,Q00534,Yes,Yes,Yes,No,4,245.82
327,Cc1cc(Nc2ncc(Cl)c(Nc3ccccc3S(=O)(=O)C(C)C)n2)c(OC(C)C)cc1C1CCN(CC(=O)NCCOCCOCCOCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1,Active,No,SU-DHL-1 and NCI-H2228,5.786820000000006,"competition with ligand only slightly rescued protein degradation. EC50 of ligand and PROTAC is measured on SUDHL-1 cell line. DC50 is SU-DHL-1: 3 ± 1 nM, NCI-H2228: 34 ± 9 nM.","Ella Livnah, Yangwode Jing",< 34 nM,> 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,19,5,1.3 nM,37 nM,Ceritinib,Cc1cc(Nc2ncc(Cl)c(Nc3ccccc3S(=O)(=O)C(C)C)n2)c(OC(C)C)cc1C1CCNCC1,CCOCCOCCOCCOCCOCCNC(C)=O,PEG,21,7,16,1134.7509999999993,No,,4MKC,4MK,29627725,5,No,,Reviewed,Q9UM73,Yes,Yes,No,Yes,16,267.28
328,Cc1cc(Nc2ncc(Cl)c(Nc3ccccc3S(=O)(=O)C(C)C)n2)c(OC(C)C)cc1C1CCN(CC(=O)NCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1,Active,Yes,SU-DHL-1 and NCI-H2228,5.703820000000005,"competition with ligand only slightly rescued protein degradation. EC50 of ligand and PROTAC is measured on SUDHL-1 cell line. DC50 is SU-DHL-1: 11 ± 2 nM, NCI-H2228: 59 ± 16 nM.","Ella Livnah, Yangwode Jing",< 59 nM,> 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,14,5,1.3 nM,19 nM,Ceritinib,Cc1cc(Nc2ncc(Cl)c(Nc3ccccc3S(=O)(=O)C(C)C)n2)c(OC(C)C)cc1C1CCNCC1,CCNC(C)=O,Alkane,6,2,1,914.4859999999995,No,,4MKC,4MK,29627725,6,No,,Reviewed,Q9UM73,Yes,Yes,No,Yes,16,221.13
329,O=C(CCCCCCC(=O)N/N=C/c1ccc(OCCn2cc(CNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nn2)cc1)NO,Active,No,MCF-7,1.6665000000000023,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,5,,,compound 2c,COc1ccc(/C=N/NC(=O)CCCCCCC(=O)NO)cc1,Cc1cn(C)nn1,PEG,7,3,0,687.7140000000004,No,,,,29871848,9a,No,,Reviewed,Q9UBN7,No,Yes,No,No,12,226.30999999999995
330,O=C(CCCCCCC(=O)N/N=C/c1ccc(OCCOCCn2cc(CNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nn2)cc1)NO,Active,No,MCF-7,1.6831000000000025,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,14,5,,,compound 2c,COc1ccc(/C=N/NC(=O)CCCCCCC(=O)NO)cc1,COCCn1cc(C)nn1,PEG,10,4,3,731.7670000000003,No,,,,29871848,9b,No,,Reviewed,Q9UBN7,No,Yes,No,No,12,235.53999999999996
331,O=C(CCCCCCC(=O)N/N=C/c1ccc(OCCOCCOCCn2cc(CNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nn2)cc1)NO,Active,Yes,"MCF-7, MM.1S",1.6997000000000018,DC50 and Dmax are for MCF-7 cells,Barr Tivon,34 nM,70.5 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,5,,,compound 2c,COc1ccc(/C=N/NC(=O)CCCCCCC(=O)NO)cc1,COCCOCCn1cc(C)nn1,PEG,13,5,6,775.8200000000003,No,,,,29871848,dHDAC6 (or 9c),No,,Reviewed,Q9UBN7,No,Yes,No,Yes,12,244.76999999999998
332,O=C(CCCCCCC(=O)N/N=C/c1ccc(OCCOCCOCCOCCn2cc(CNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nn2)cc1)NO,Active,No,MCF-7,1.716300000000003,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,16,5,,,compound 2c,COc1ccc(/C=N/NC(=O)CCCCCCC(=O)NO)cc1,COCCOCCOCCn1cc(C)nn1,PEG,16,6,9,819.8730000000003,No,,,,29871848,9d,No,,Reviewed,Q9UBN7,No,Yes,No,No,12,254.0
333,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)NCCn1cc(COc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nn1)c1nnc(C)n1-2,Active,No,H661,3.577760000000003,,Ella Livnah,0.49 uM,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,ester_to_amide,14,2,,,JQ-1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCn1cc(CO)nn1,PEG,10,5,3,781.2549999999998,No,,,,28378579,11a,No,,Reviewed,O60885,No,No,Yes,No,4,195.65999999999997
334,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)NCCn1cc(COCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nn1)c1nnc(C)n1-2,Inactive,No,H661,3.5943600000000018,,Ella Livnah,> 5 uM,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,ester_to_amide,15,2,,,JQ-1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCn1cc(COCCO)nn1,PEG,13,6,6,825.3079999999998,No,,,,28378579,11b,No,,Reviewed,O60885,No,No,Yes,No,4,204.89
335,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)NCCn1cc(COCCOCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nn1)c1nnc(C)n1-2,Inactive,No,H661,3.6109600000000013,,Ella Livnah,> 5 uM,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,ester_to_amide,16,2,,,JQ-1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCn1cc(COCCOCCO)nn1,PEG,16,7,9,869.3609999999999,No,,,,28378579,11c,No,,Reviewed,O60885,No,No,Yes,No,4,214.11999999999995
336,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)NCCn1cc(COCCOCCOCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nn1)c1nnc(C)n1-2,Active,No,H661,3.6275600000000017,,Ella Livnah,0.45 uM,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,ester_to_amide,17,2,,,JQ-1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCn1cc(COCCOCCOCCO)nn1,PEG,19,8,12,913.4139999999998,No,,,,28378579,11d,No,,Reviewed,O60885,No,No,Yes,No,4,223.34999999999997
337,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)NCCn1cc(COCCOCCOCCOCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nn1)c1nnc(C)n1-2,Active,Yes,H661,3.644160000000003,,Ella Livnah,0.20 uM,> 90 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,ester_to_amide,18,2,,,JQ-1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCn1cc(COCCOCCOCCOCCO)nn1,PEG,22,9,15,957.4669999999996,No,,,,28378579,11e,No,,Reviewed,O60885,No,Yes,Yes,Yes,4,232.57999999999998
338,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCc2cn(CCNC(=O)C[C@@H]3N=C(c4ccc(Cl)cc4)c4c(sc(C)c4C)-n4c(C)nnc43)nn2)C(C)(C)C)cc1,Active,No,H661,5.355180000000006,,Ella Livnah,0.059 uM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,16,4,,,JQ-1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCn1cc(COCC=O)nn1,PEG,13,6,6,995.6329999999995,No,,,,28378579,12a,No,,Reviewed,O60885,No,Yes,Yes,Yes,4,223.73999999999995
339,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCc2cn(CCNC(=O)C[C@@H]3N=C(c4ccc(Cl)cc4)c4c(sc(C)c4C)-n4c(C)nnc43)nn2)C(C)(C)C)cc1,Active,No,H661,5.371780000000006,,Ella Livnah,0.083 uM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,17,4,,,JQ-1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCn1cc(COCCOCC=O)nn1,PEG,16,7,9,1039.6859999999995,No,,,,28378579,12b,No,,Reviewed,O60885,No,No,Yes,No,4,232.96999999999997
340,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCc2cn(CCNC(=O)C[C@@H]3N=C(c4ccc(Cl)cc4)c4c(sc(C)c4C)-n4c(C)nnc43)nn2)C(C)(C)C)cc1,Active,No,H661,5.388380000000007,,Ella Livnah,0.24 uM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,18,4,,,JQ-1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCn1cc(COCCOCCOCC=O)nn1,PEG,19,8,12,1083.7389999999991,No,,,,28378579,12c,No,,Reviewed,O60885,No,No,Yes,No,4,242.19999999999993
341,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCc2cn(CCNC(=O)C[C@@H]3N=C(c4ccc(Cl)cc4)c4c(sc(C)c4C)-n4c(C)nnc43)nn2)C(C)(C)C)cc1,Active,No,H661,5.404980000000009,,Ella Livnah,0.46 uM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,19,4,,,JQ-1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCn1cc(COCCOCCOCCOCC=O)nn1,PEG,22,9,15,1127.791999999999,No,,,,28378579,12d,No,,Reviewed,O60885,No,No,Yes,No,4,251.42999999999995
342,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCCOCc2cn(CCNC(=O)C[C@@H]3N=C(c4ccc(Cl)cc4)c4c(sc(C)c4C)-n4c(C)nnc43)nn2)C(C)(C)C)cc1,Active,No,H661,5.421580000000009,,Ella Livnah,0.63 uM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,20,4,,,JQ-1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCn1cc(COCCOCCOCCOCCOCC=O)nn1,PEG,25,10,18,1171.8449999999991,No,,,,28378579,12e,No,,Reviewed,O60885,No,No,Yes,No,4,260.6599999999999
343,COc1ccc(OC)c2c1c(OC)cc1c(=O)cc(-c3ccc(-c4cn(CCOc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)cc3)oc12,Active,No,DU145/Cy,4.3777000000000035,"Tested reversal of docetaxel resistance by degradation of CYP, followed by lysis and WB, model with the ligand is available in previous publication",Paul Gehrtz,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_C,13,1,1.4 nM,101.2 nM,Compound 2,COc1ccc(OC)c2c1c(OC)cc1c(=O)cc(-c3ccccc3)oc12,OCCn1ccnn1,Other,8,4,2,729.7020000000001,No,,,,31945665,6A,No,,Reviewed,Q16678,No,No,No,No,48,181.39
344,COc1ccc(OC)c2c1c(OC)cc1c(=O)cc(-c3ccc(-c4cn(CCCCCOc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)cc3)oc12,Active,No,DU145/Cy,5.548000000000006,"Tested reversal of docetaxel resistance by degradation of CYP, followed by lysis and WB, model with the ligand is available in previous publication",Paul Gehrtz,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_C,13,1,1.4 nM,152.7 nM,Compound 2,COc1ccc(OC)c2c1c(OC)cc1c(=O)cc(-c3ccccc3)oc12,OCCCCCn1ccnn1,Other,11,4,5,771.7830000000001,No,,,,31945665,6B,No,,Reviewed,Q16678,No,No,No,No,48,181.39
345,COc1ccc(OC)c2c1c(OC)cc1c(=O)cc(-c3ccc(-c4cn(CCCCCCOc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)cc3)oc12,Active,Yes,DU145/Cy,5.938100000000007,"Tested reversal of docetaxel resistance by degradation of CYP, followed by lysis and WB, model with the ligand is available in previous publication",Paul Gehrtz,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_C,13,1,1.4 nM,95.1 nM,Compound 2,COc1ccc(OC)c2c1c(OC)cc1c(=O)cc(-c3ccccc3)oc12,OCCCCCCn1ccnn1,Other,12,4,6,785.8100000000001,No,,,,31945665,6C,No,,Reviewed,Q16678,No,No,No,No,48,181.39
346,COc1ccc(OC)c2c1c(OC)cc1c(=O)cc(-c3ccc(-c4cn(CCCCCCCCOc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)cc3)oc12,Inactive,No,DU145/Cy,6.718300000000006,"Tested reversal of docetaxel resistance by degradation of CYP, followed by lysis and WB, model with the ligand is available in previous publication",Paul Gehrtz,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_C,13,1,1.4 nM,166.2 nM,Compound 2,COc1ccc(OC)c2c1c(OC)cc1c(=O)cc(-c3ccccc3)oc12,OCCCCCCCCn1ccnn1,Other,14,4,8,813.8640000000001,No,,,,31945665,6D,No,,Reviewed,Q16678,No,No,No,No,48,181.39
347,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCNC(=O)C[C@@H]2N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc32)C(C)(C)C)cc1,Active,No,Hela,5.596680000000006,,Daniel Zaidman,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,15,4,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCOCCOCCOCC=O,PEG,13,5,10,1002.6609999999996,"BRD2, BRD3",,3MXF,JQ1,28288108,MZ1,No,,Reviewed,O60885,Yes,No,Yes,No,24,211.48999999999995
348,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCCNC(=O)C[C@@H]2N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc32)C(C)(C)C)cc1,Active,No,Hela,5.613280000000007,,Daniel Zaidman,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,16,4,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCOCCOCCOCCOCC=O,PEG,16,6,13,1046.7139999999995,"BRD2, BRD3",,3MXF,JQ1,28288108,MZ2,No,,Reviewed,O60885,No,No,Yes,No,24,220.71999999999997
349,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)[C@@H](Cc2ccccc2)NC(=O)COCCOCCOCCNC(=O)C[C@@H]2N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc32)C(C)(C)C)cc1,Active,No,Hela,6.324180000000008,,Daniel Zaidman,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,16,5,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCOCCOCCOCC(=O)N[C@@H](C=O)Cc1ccccc1,PEG,24,7,14,1149.8379999999988,"BRD2, BRD3",,3MXF,JQ1,28288108,MZ3,No,,Reviewed,O60885,No,No,Yes,No,24,240.58999999999992
350,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCNC(=O)C[C@@H]2N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc32)C(C)(C)C)cc1,Active,No,Hela,5.580080000000006,,Daniel Zaidman,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,14,4,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCOCCOCC=O,PEG,10,4,7,958.6079999999996,"BRD2, BRD3",,3MXF,JQ1,28288108,MZ4,No,,Reviewed,O60885,No,No,Yes,No,24,202.26
351,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)SCCCCCCNC(=O)C[C@@H]1N=C(c2ccc(Cl)cc2)c2c(sc(C)c2C)-n2c(C)nnc21,Active,Yes,Hela,7.592880000000009,,Daniel Zaidman,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,13,4,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCCCCCS,Alkane,8,1,5,972.7039999999993,"BRD2, BRD3",,3MXF,JQ1,28288108,AT1,No,,Reviewed,O60885,No,No,Yes,No,24,183.8
352,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)SCCCCNC(=O)C[C@@H]1N=C(c2ccc(Cl)cc2)c2c(sc(C)c2C)-n2c(C)nnc21,Active,No,Hela,6.812680000000008,,Daniel Zaidman,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,13,4,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCCCS,Alkane,6,1,3,944.6499999999994,"BRD2, BRD3",,3MXF,JQ1,28288108,AT2,No,,Reviewed,O60885,No,No,Yes,No,24,183.8
353,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)SCCOCCNC(=O)C[C@@H]1N=C(c2ccc(Cl)cc2)c2c(sc(C)c2C)-n2c(C)nnc21,Active,No,Hela,6.049080000000007,,Daniel Zaidman,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,14,4,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCOCCS,PEG,7,2,4,960.6489999999994,"BRD2, BRD3",,3MXF,JQ1,28288108,AT3,No,,Reviewed,O60885,No,No,Yes,No,24,193.02999999999997
354,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)SCCCOCCCNC(=O)C[C@@H]1N=C(c2ccc(Cl)cc2)c2c(sc(C)c2C)-n2c(C)nnc21,Active,No,Hela,6.829280000000009,,Daniel Zaidman,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,14,4,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCCOCCCS,non-PEG polyether,9,2,6,988.7029999999993,"BRD2, BRD3",,3MXF,JQ1,28288108,AT4,No,,Reviewed,O60885,No,No,Yes,No,24,193.02999999999997
355,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)SCCCCOCCNC(=O)C[C@@H]1N=C(c2ccc(Cl)cc2)c2c(sc(C)c2C)-n2c(C)nnc21,Active,No,Hela,6.829280000000009,,Daniel Zaidman,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,14,4,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCOCCCCS,non-PEG polyether,9,2,6,988.7029999999993,"BRD2, BRD3",,3MXF,JQ1,28288108,AT5,No,,Reviewed,O60885,No,No,Yes,No,24,193.02999999999997
356,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)SCCOCCOCCNC(=O)C[C@@H]1N=C(c2ccc(Cl)cc2)c2c(sc(C)c2C)-n2c(C)nnc21,Active,No,Hela,6.065680000000007,,Daniel Zaidman,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,15,4,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCOCCOCCS,PEG,10,3,7,1004.7019999999993,"BRD2, BRD3",,3MXF,JQ1,28288108,AT6,No,,Reviewed,O60885,No,No,Yes,No,24,202.26
357,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOc2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2)C(C)(C)C)cc1,Active,No,VCaP,6.163400000000006,,Daniel Zaidman,,47 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,13,3,70 nM,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,O=CCOCCOCCOCCO,PEG,13,5,10,1008.155,No,,,,30271980,2a,No,,Reviewed,P10275,No,No,No,No,20,195.89
358,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOCCCCCOc2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2)C(C)(C)C)cc1,Active,No,VCaP,7.707200000000009,,Daniel Zaidman,15 nM,76 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,3,70 nM,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,O=CCOCCCOCCCCCO,non-PEG polyether,14,4,11,1020.2099999999999,No,,,,30271980,2b,No,,Reviewed,P10275,No,No,No,No,20,186.66
359,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCCOc2ccc(-c3ccc(N4C(=S)N(c5ccc(C#N)c(C(F)(F)F)c5)C(=O)C4(C)C)cc3)cc2)C(C)(C)C)cc1,Active,Yes,VCaP,8.577400000000006,,Daniel Zaidman,5 nM,98 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,11,3,70 nM,36 nM,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,cc-c(cc)OCCCCOCC=O,Other,14,3,9,1024.2009999999998,No,,,,30271980,2c (ARCC-4),No,,Reviewed,P10275,Yes,No,No,Yes,20,177.43
360,CN1CC(Nc2cnn(C)c(=O)c2Br)CC(c2ccc(C(=O)N(C)CCCN(C)c3ccc(CCCOc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3)cc2)C1,Active,No,THP1,4.453900000000003,DC50 is 1.5nM/3nM. DCmax is 97%/91%.,Daniel Zaidman,< 3 nM,> 91 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_C,12,2,60 nM,,GSK4027,CN1C[C@H](Nc2cnn(C)c(=O)c2Br)C[C@H](c2ccccc2)C1,CN(C=O)CCCN(C)c1ccc(CCCO)cc1,Other,19,4,9,895.8559999999998,No,,,,30200762,GSK983,No,,Reviewed,"Q92830, Q92831",No,No,No,No,18,166.48999999999998
361,CN1C[C@H](Nc2cnn(C)c(=O)c2Br)C[C@H](c2ccc(C(=O)N(C)CCCN(C)c3ccc(CCCOc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3)cc2)C1,Active,Yes,THP1,4.453900000000003,,Daniel Zaidman,,97 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_C,12,2,60 nM,,GSK4027,CN1C[C@H](Nc2cnn(C)c(=O)c2Br)C[C@H](c2ccccc2)C1,CN(C=O)CCCN(C)c1ccc(CCCO)cc1,Other,19,4,9,895.8559999999998,No,,,,30200762,GSK699,No,,Reviewed,"Q92830, Q92831",No,No,No,Yes,18,166.48999999999998
362,CN1C[C@@H](Nc2cnn(C)c(=O)c2Br)C[C@@H](c2ccc(C(=O)N(C)CCCN(C)c3ccc(CCCOc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3)cc2)C1,Active,No,THP1,4.453900000000003,only slightly active,Daniel Zaidman,,38 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_C,12,2,60 nM,,GSK4027,CN1C[C@H](Nc2cnn(C)c(=O)c2Br)C[C@H](c2ccccc2)C1,CN(C=O)CCCN(C)c1ccc(CCCO)cc1,Other,19,4,9,895.8559999999998,No,,,,30200762,GSK702,No,,Reviewed,"Q92830, Q92831",No,No,No,No,18,166.48999999999998
363,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOc2ccc(Nc3ncc(C(F)(F)F)c(NCc4cccc(N(C)S(C)(=O)=O)c4)n3)cc2)C(C)(C)C)cc1,Active,No,PC3,5.883320000000005,,Daniel Zaidman,23.2 nM,99 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,3.9 nM,10.7 nM,defactinib analog,CNC(=O)c1ccc(Nc2ncc(C(F)(F)F)c(NCc3ccccc3N(C)S(C)(=O)=O)n2)cc1,O=CCOCCO,PEG,7,3,4,982.121,No,,,,30444612,PROTAC-1,No,,Reviewed,Q05397,No,No,No,No,24,217.31
364,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCOc2ccc(Nc3ncc(C(F)(F)F)c(NCc4cccc(N(C)S(C)(=O)=O)c4)n3)cc2)C(C)(C)C)cc1,Active,No,PC3,6.273420000000005,,Daniel Zaidman,7.6 nM,99 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,3.9 nM,14.7 nM,defactinib analog,CNC(=O)c1ccc(Nc2ncc(C(F)(F)F)c(NCc3ccccc3N(C)S(C)(=O)=O)n2)cc1,O=CCOCCCO,non-PEG polyether,8,3,5,996.1479999999999,No,,,,30444612,PROTAC-2,No,,Reviewed,Q05397,No,No,No,No,24,217.31
365,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOc2ccc(Nc3ncc(C(F)(F)F)c(NCc4cccc(N(C)S(C)(=O)=O)c4)n3)cc2)C(C)(C)C)cc1,Active,Yes,"PC3, MDA-MB-231",6.273420000000005,,Daniel Zaidman,3.0 nM,99 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,3.9 nM,6.5 nM,defactinib analog,CNC(=O)c1ccc(Nc2ncc(C(F)(F)F)c(NCc3ccccc3N(C)S(C)(=O)=O)n2)cc1,O=CCCOCCO,PEG,8,3,5,996.1479999999999,Other kinases,,,,30444612,PROTAC-3,No,,Reviewed,Q05397,Yes,No,No,No,24,217.31
366,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCCOc2ccc(Nc3ncc(C(F)(F)F)c(NCc4cccc(N(C)S(C)(=O)=O)c4)n3)cc2)C(C)(C)C)cc1,Active,No,PC3,6.663520000000006,,Daniel Zaidman,4.0 nM,99 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,3.9 nM,14.5 nM,defactinib analog,CNC(=O)c1ccc(Nc2ncc(C(F)(F)F)c(NCc3ccccc3N(C)S(C)(=O)=O)n2)cc1,O=CCCOCCCO,non-PEG polyether,9,3,6,1010.175,No,,,,30444612,PROTAC-4,No,,Reviewed,Q05397,No,No,No,No,24,217.31
367,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOCCOc2ccc(Nc3ncc(C(F)(F)F)c(NCc4cccc(N(C)S(C)(=O)=O)c4)n3)cc2)C(C)(C)C)cc1,Active,No,PC3,6.2900200000000055,,Daniel Zaidman,20.8 nM,99 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,15,5,3.9 nM,12.7 nM,defactinib analog,CNC(=O)c1ccc(Nc2ncc(C(F)(F)F)c(NCc3ccccc3N(C)S(C)(=O)=O)n2)cc1,O=CCCOCCOCCO,PEG,11,4,8,1040.201,No,,,,30444612,PROTAC-5,No,,Reviewed,Q05397,No,No,No,No,24,226.54000000000002
368,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOCCOCCOCCOc2ccc(Nc3ncc(C(F)(F)F)c(NCc4cccc(N(C)S(C)(=O)=O)c4)n3)cc2)C(C)(C)C)cc1,Active,No,PC3,6.323220000000006,,Daniel Zaidman,48.1 nM,91 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,17,5,3.9 nM,6.1 nM,defactinib analog,CNC(=O)c1ccc(Nc2ncc(C(F)(F)F)c(NCc3ccccc3N(C)S(C)(=O)=O)n2)cc1,O=CCCOCCOCCOCCOCCO,PEG,17,6,14,1128.3069999999996,No,,,,30444612,PROTAC-6,No,,Reviewed,Q05397,No,No,No,No,24,245.0
369,CN(c1cccc(CNc2nc(Nc3ccc(OCCCOCCC(=O)NCCOc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3)ncc2C(F)(F)F)c1)S(C)(=O)=O,Active,No,PC3,4.018900000000002,,Daniel Zaidman,8.2 nM,98 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,4,3.9 nM,11.3 nM,defactinib analog,CNC(=O)c1ccc(Nc2ncc(C(F)(F)F)c(NCc3ccccc3N(C)S(C)(=O)=O)n2)cc1,O=C(CCOCCCO)NCCO,non-PEG polyether,13,5,8,896.9020000000003,No,,,,30444612,PROTAC-8,No,,Reviewed,Q05397,No,No,No,No,24,227.56
370,CN(c1cccc(CNc2nc(Nc3ccc(OCCOCCOCCC(=O)NCCOc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3)ncc2C(F)(F)F)c1)S(C)(=O)=O,Active,No,PC3,3.6454000000000013,,Daniel Zaidman,26.7 nM,99 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,15,4,3.9 nM,4.7 nM,defactinib analog,CNC(=O)c1ccc(Nc2ncc(C(F)(F)F)c(NCc3ccccc3N(C)S(C)(=O)=O)n2)cc1,O=C(CCOCCOCCO)NCCO,PEG,15,6,10,926.9280000000002,No,,,,30444612,PROTAC-9,No,,Reviewed,Q05397,No,No,No,No,24,236.79000000000002
371,CN(c1cccc(CNc2nc(Nc3ccc(OCCOCCOCCOCCOCCC(=O)NCCOc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3)ncc2C(F)(F)F)c1)S(C)(=O)=O,Active,No,PC3,3.678600000000003,,Daniel Zaidman,< 10 nM,87 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,17,4,3.9 nM,9.7 nM,defactinib analog,CNC(=O)c1ccc(Nc2ncc(C(F)(F)F)c(NCc3ccccc3N(C)S(C)(=O)=O)n2)cc1,O=C(CCOCCOCCOCCOCCO)NCCO,PEG,21,8,16,1015.0340000000002,No,,,,30444612,PROTAC-10,No,,Reviewed,Q05397,No,No,No,No,24,255.25
372,Cc1ncsc1-c1ccc2c(c1)OCCOCCOC[C@@H](NC(=O)C[C@@H]1N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc31)COCCOCCOCC(=O)N[C@@H](C(C)(C)C)C(=O)N1C[C@H](O)C[C@H]1C(=O)NC2,Active,Yes,hela,5.3908800000000054,they heva a ternary complex crystal structure but dont give PDB. DC50 is between 25-125nM,Efrat Resnick,< 125 nM,90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,ester_to_amide,18,4,,189 nM,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,N[C@H](COCCOCCO)COCCOCCOCC=O,Other,21,8,17,1118.7769999999994,Brd2 and Brd3 (DC50 >125nM),,,,31746102,macroPROTAC-1,No,,Reviewed,O60885,No,No,No,No,"4,18",239.17999999999998
373,Cc1nc(CCC(=O)NCCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1-c1cnc(NCc2c(F)ccc3c2CCO3)n2cnnc12,Active,No,Karpas422,5.640940000000007,,Adi Rogel,,~ 100 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,14,5,< 1 nM,< 1 nM,EED ligand,CNC(=O)CCc1ccc(-c2cnc(NCc3c(F)ccc4c3CCO4)n3cnnc23)c(C)n1,CCCC=O,Alkane,5,1,2,960.1499999999994,"SUZ12, EZH2 (also members of the PRC2 complex)",,,,31786184,PROTAC 1,Yes,,Reviewed,O75530,Yes,Yes,No,Yes,"1,2,6,8,24,48",217.95999999999998
374,Cc1nc(CCC(=O)NCCOc2ccc(OCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)cc2)ccc1-c1cnc(NCc2c(F)ccc3c2CCO3)n2cnnc12,Active,Yes,Karpas422,5.928440000000008,,Adi Rogel,,~ 100 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,5,< 1 nM,~ 1 nM,EED ligand,CNC(=O)CCc1ccc(-c2cnc(NCc3c(F)ccc4c3CCO4)n3cnnc23)c(C)n1,COc1ccc(OCC=O)cc1,Other,12,3,4,1054.2189999999996,"SUZ12, EZH2 (also members of the PRC2 complex)",,,,31786184,PROTAC 2,Yes,,Reviewed,O75530,Yes,Yes,No,Yes,"1,2,6,8,24,48",236.41999999999996
375,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)Nc1ccc(OCCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)cc1)c1nnc(C)n1-2,Active,Yes,"Namalwa, CA-46, Ramos",5.770260000000006,"tested also biological effects - proliferation and caspase activity on BL cells. IC50 of ligand is 14 nM (BD1), 3.5 nM (BD2). IC50 of PROTAC is 90 nM (BD1), 28 nM (BD2).",Adi Rogel,< 1 nM,~ 100 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,3,< 14 nM,< 90 nM,OTX015,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)Nc1ccc(O)cc1)c1nnc(C)n1-2,CCOCCOCCOCC,PEG,11,3,8,923.4489999999997,No,,,,26051217,ARV-825,No,,Reviewed,O60885,No,No,No,Yes,"0.5,1,2,4,7,24",204.67000000000002
376,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2[C@@H]1CCCN(C(=O)c2cn(CCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nn2)C1,Active,Yes,"HBL1, Ramos, Mino, IgE MM",3.4997000000000007,"also degrades ibrutinib-resistant C481S BTK. DC50 is 6.3 nM (HBL1), 8.5 nM (Ramos), 9.2 nM (Mino), 11.4 nM (IgE MM)",Adi Rogel,< 11.4 nM,94 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,3,,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,cn(CCOCCOCCOCC)nn,Other,15,6,10,912.9649999999997,No,,5P9J,"8E8",29875397,P13I,No,,Reviewed,Q06187,No,Yes,No,Yes,"4,8,12,24",253.14
377,N#CC1=C(NCCC(=O)NCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)c2ccc(Sc3ccc(Br)cc3)c3cccc(c23)C1=O,Inactive,No,hela,4.793680000000003,"IC50 error: for ligand ± 0.87 uM, for PROTAC ± 3.66 uM",Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,10,4,2.31 uM,10.48 uM,S1-6,N#CC1=C(C#N)c2ccc(Sc3ccc(Br)cc3)c3cccc(c23)C1=O,CCNC(=O)CCN,Alkane,8,3,3,777.6570000000002,No,,,,31389699,H1,No,,Reviewed,"Q07820, Q92934",No,No,No,No,12,177.57
378,N#CC1=C(NCCC(=O)NCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)c2ccc(Sc3ccc(Br)cc3)c3cccc(c23)C1=O,Inactive,No,hela,5.573880000000004,"IC50 error: for ligand ± 0.87 uM, for PROTAC ± 2.13 uM",Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,10,4,2.31 uM,9.71 uM,S1-6,N#CC1=C(C#N)c2ccc(Sc3ccc(Br)cc3)c3cccc(c23)C1=O,CCCCNC(=O)CCN,Alkane,10,3,5,805.7110000000001,No,,,,31389699,H2,No,,Reviewed,"Q07820, Q92934",No,No,No,No,12,177.57
379,N#CC1=C(NCCC(=O)NCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)c2ccc(Sc3ccc(Br)cc3)c3cccc(c23)C1=O,Inactive,No,hela,6.354080000000006,"IC50 error: for ligand ± 0.87 uM, for PROTAC ± 0.58 uM",Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,10,4,2.31 uM,1.94 uM,S1-6,N#CC1=C(C#N)c2ccc(Sc3ccc(Br)cc3)c3cccc(c23)C1=O,CCCCCCNC(=O)CCN,Alkane,12,3,7,833.7650000000001,No,,,,31389699,H3,No,,Reviewed,"Q07820, Q92934",No,No,No,No,12,177.57
380,N#CC1=C(NCCC(=O)NCCCCCC(=O)NCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)c2ccc(Sc3ccc(Br)cc3)c3cccc(c23)C1=O,Inactive,No,hela,7.030680000000006,"IC50 error: for ligand ± 0.87 uM, for PROTAC ± 4.44 uM",Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,11,5,2.31 uM,11.65 uM,S1-6,N#CC1=C(C#N)c2ccc(Sc3ccc(Br)cc3)c3cccc(c23)C1=O,CCCCCCNC(=O)CCCCCNC(=O)CCN,Other,20,5,13,946.9250000000002,No,,,,31389699,H4,No,,Reviewed,"Q07820, Q92934",No,No,No,No,12,206.67
381,N#CC1=C(NCCC(=O)NCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)c2ccc(Sc3ccc(Br)cc3)c3cccc(c23)C1=O,Inactive,No,hela,4.826880000000005,"IC50 error: for ligand ± 0.87 uM, for PROTAC ± 0.89 uM",Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,4,2.31 uM,2.24 uM,S1-6,N#CC1=C(C#N)c2ccc(Sc3ccc(Br)cc3)c3cccc(c23)C1=O,CCOCCOCCNC(=O)CCN,PEG,14,5,9,865.763,No,,,,31389699,H5,No,,Reviewed,"Q07820, Q92934",No,No,No,No,12,196.03
382,O=C(CCCCC(=O)NCCN1C(=O)c2cccc3c(Sc4ccc(Br)cc4)ccc(c23)C1=O)NCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,hela,4.6556000000000015,"IC50 error: for ligand ± 1.39 uM, for PROTAC ± 4.33 uM",Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,10,4,3.18 uM,15.21 uM,Nap-1,CC(C)(C)c1ccc(C(=O)NCCN2C(=O)c3cccc4c(Sc5ccc(Br)cc5)ccc(c34)C2=O)cc1,CCN,Alkane,3,1,0,853.7519999999997,No,,,,31389699,C1,No,,Reviewed,"Q07820, Q92934",No,No,No,No,12,191.16
383,O=C(CCCCC(=O)NCCN1C(=O)c2cccc3c(Sc4ccc(Br)cc4)ccc(c23)C1=O)NCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,hela,5.435800000000003,"IC50 error: for ligand ± 1.39 uM, for PROTAC ± 2.90 uM",Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,10,4,3.18 uM,10.02 uM,Nap-1,CC(C)(C)c1ccc(C(=O)NCCN2C(=O)c3cccc4c(Sc5ccc(Br)cc5)ccc(c34)C2=O)cc1,CCCCN,Alkane,5,1,2,881.8059999999996,No,,,,31389699,C2,No,,Reviewed,"Q07820, Q92934",No,No,No,No,12,191.16
384,O=C(CCCCC(=O)NCCN1C(=O)c2cccc3c(Sc4ccc(Br)cc4)ccc(c23)C1=O)NCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,Yes,hela,6.216000000000005,"IC50 error: for ligand ± 1.39 uM, for PROTAC ± 0.27 uM",Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,10,4,3.18 uM,0.54 uM,Nap-1,CC(C)(C)c1ccc(C(=O)NCCN2C(=O)c3cccc4c(Sc5ccc(Br)cc5)ccc(c34)C2=O)cc1,CCCCCCN,Alkane,7,1,4,909.8599999999994,No,,,,31389699,C3,No,,Reviewed,"Q07820, Q92934",Yes,Yes,Yes,Yes,12,191.16
385,O=C(CCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)NCCCCCCNC(=O)CCCCC(=O)NCCN1C(=O)c2cccc3c(Sc4ccc(Br)cc4)ccc(c23)C1=O,Inactive,No,hela,6.892600000000007,"IC50 error: for ligand ± 1.39 uM, for PROTAC ± 4.57 uM",Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,11,5,3.18 uM,13.47 uM,Nap-1,CC(C)(C)c1ccc(C(=O)NCCN2C(=O)c3cccc4c(Sc5ccc(Br)cc5)ccc(c34)C2=O)cc1,CCCCCC(=O)NCCCCCCN,Other,15,3,10,1023.0199999999998,No,,,,31389699,C4,No,,Reviewed,"Q07820, Q92934",No,No,No,No,12,220.26
386,O=C(CCCCC(=O)NCCN1C(=O)c2cccc3c(Sc4ccc(Br)cc4)ccc(c23)C1=O)NCCOCCOCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,Yes,hela,4.688800000000002,"IC50 error: for ligand ± 1.39 uM, for PROTAC ± 1.36 uM",Efrat Resnick,3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,4,3.18 uM,4.94 uM,Nap-1,CC(C)(C)c1ccc(C(=O)NCCN2C(=O)c3cccc4c(Sc5ccc(Br)cc5)ccc(c34)C2=O)cc1,CCOCCOCCN,Other,9,3,6,941.8579999999995,No,,,,31389699,C5,No,,Reviewed,"Q07820, Q92934",Yes,Yes,Yes,Yes,12,209.62
387,O=C(CCCCC(=O)NCCN1C(=O)c2cccc3c(Sc4ccc(Br)cc4)ccc(c23)C1=O)NCCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Inactive,No,hela,6.996200000000006,"IC50 error: for ligand ± 1.39 uM, for PROTAC ± 2.28 uM",Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,10,4,3.18 uM,7.66 uM,Nap-1,CC(C)(C)c1ccc(C(=O)NCCN2C(=O)c3cccc4c(Sc5ccc(Br)cc5)ccc(c34)C2=O)cc1,CCCCCCCCN,Other,9,1,6,937.9139999999993,No,,,,31389699,C6,No,,Reviewed,"Q07820, Q92934",No,No,No,No,12,191.16
388,NC(=O)c1c(-c2ccc(Oc3ccc(F)cc3F)cc2)nn([C@H]2CCCN(C(=O)OCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)c1N,Inactive,No,"Ramos, THP-1",3.5885000000000007,Ligand name is from PMID 24068666,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,4,0.5 nM,735 nM,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCO,PEG,3,1,0,756.7229999999998,No,,,,30012605,1,No,,Reviewed,Q06187,No,No,No,No,24,221.28000000000003
389,NC(=O)c1c(-c2ccc(Oc3ccc(F)cc3F)cc2)nn([C@H]2CCCN(C(=O)COCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)c1N,Inactive,No,"Ramos, THP-1",2.995099999999999,Ligand name is from PMID 24068666,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,4,0.5 nM,1400 nM,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOC,PEG,4,1,1,770.7499999999999,No,,,,30012605,2,No,,Reviewed,Q06187,No,No,No,No,24,221.28000000000003
390,NC(=O)c1c(-c2ccc(Oc3ccc(F)cc3F)cc2)nn([C@H]2CCCN(C(=O)OCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)c1N,Active,No,"Ramos, THP-1",3.605100000000001,Ligand name is from PMID 24068666. DCmax is 18-33%,Adi Rogel,,< 33 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,4,0.5 nM,1535 nM,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOCCO,PEG,6,2,3,800.7759999999998,No,,,,30012605,3,No,,Reviewed,Q06187,No,No,No,No,24,230.51000000000002
391,NC(=O)c1c(-c2ccc(Oc3ccc(F)cc3F)cc2)nn([C@H]2CCCN(C(=O)COCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)c1N,Active,No,"Ramos, THP-1",3.0116999999999994,Ligand name is from PMID 24068666. DCmax is 15-34%,Adi Rogel,,< 34 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,4,0.5 nM,489 nM,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOCCOC,PEG,7,2,4,814.8029999999999,No,,,,30012605,4,No,,Reviewed,Q06187,No,No,No,No,24,230.51000000000002
392,NC(=O)c1c(-c2ccc(Oc3ccc(F)cc3F)cc2)nn([C@H]2CCCN(C(=O)OCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)c1N,Active,No,"Ramos, THP-1",3.6217000000000006,Ligand name is from PMID 24068666. DCmax is 36-64%. DC50 is 1487 - 1994.5 nM.,Adi Rogel,< 1994.5 nM,< 64 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,4,0.5 nM,1150 nM,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOCCOCCO,PEG,9,3,6,844.8289999999997,No,,,,30012605,5,No,,Reviewed,Q06187,No,No,No,No,24,239.74
393,NC(=O)c1c(-c2ccc(Oc3ccc(F)cc3F)cc2)nn([C@H]2CCCN(C(=O)OCCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)c1N,Active,No,"Ramos, THP-1",3.638300000000001,Ligand name is from PMID 24068666. DCmax is 68-85%. DC50 is 36.9 - 398.5 nM.,Adi Rogel,< 398.5 nM,> 68 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,4,0.5 nM,71 nM,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOCCOCCOCCO,PEG,12,4,9,888.8819999999996,No,,,,30012605,6,No,,Reviewed,Q06187,No,No,No,No,24,248.97000000000003
394,NC(=O)c1c(-c2ccc(Oc3ccc(F)cc3F)cc2)nn([C@H]2CCCN(C(=O)COCCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)c1N,Active,No,"Ramos, THP-1",3.044900000000001,Ligand name is from PMID 24068666. DCmax is 63-84%. DC50 is 21.8 - 469.9 nM.,Adi Rogel,< 469.9 nM,> 63 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,4,0.5 nM,79 nM,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOCCOCCOCCOC,PEG,13,4,10,902.9089999999997,No,,,,30012605,7,No,,Reviewed,Q06187,No,No,No,No,24,248.97000000000003
395,NC(=O)c1c(-c2ccc(Oc3ccc(F)cc3F)cc2)nn([C@H]2CCCN(C(=O)OCCOCCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)c1N,Active,No,"Ramos, THP-1",3.6549000000000014,Ligand name is from PMID 24068666. DCmax is 75-87%. DC50 is 4.5 - 90.5 nM.,Adi Rogel,< 90.5 nM,> 75 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,4,0.5 nM,80 nM,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOCCOCCOCCOCCO,PEG,15,5,12,932.9349999999995,No,,,,30012605,8,No,,Reviewed,Q06187,No,No,No,No,24,258.2
396,NC(=O)c1c(-c2ccc(Oc3ccc(F)cc3F)cc2)nn([C@H]2CCCN(C(=O)COCCOCCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)c1N,Active,No,"Ramos, THP-1",3.0615000000000014,Ligand name is from PMID 24068666. DCmax is 71-85%. DC50 is 5.9 - 217.7 nM.,Adi Rogel,< 217.7 nM,> 71 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,4,0.5 nM,74 nM,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOCCOCCOCCOCCOC,PEG,16,5,13,946.9619999999995,"TEC, ZFP91, IKZF1, IKZF3, ZNF827",,,,30012605,9,Yes,,Reviewed,Q06187,No,Yes,No,No,"0.02,0.5,1,2,4,6,8,24,32,48",258.2
397,NC(=O)c1c(-c2ccc(Oc3ccc(F)cc3F)cc2)nn([C@H]2CCCN(C(=O)OCCOCCOCCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)c1N,Active,Yes,"Ramos, THP-1",3.6715000000000018,Ligand name is from PMID 24068666. DCmax is 80-87%. DC50 is 1.1 - 37.4 nM.,Adi Rogel,< 37.4 nM,> 80 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,4,0.5 nM,61 nM,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOCCOCCOCCOCCOCCO,PEG,18,6,15,976.9879999999994,"ZFP91, IKZF1, IKZF3, ZNF827",,,,30012605,10,Yes,,Reviewed,Q06187,No,No,No,No,24,267.43
398,NC(=O)c1c(-c2ccc(Oc3ccc(F)cc3F)cc2)nn([C@H]2CCCN(C(=O)COCCOCCOCCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)c1N,Active,No,"Ramos, THP-1",3.078100000000002,Ligand name is from PMID 24068666. DCmax is 70-85%. DC50 is 9.7 - 184.1 nM.,Adi Rogel,< 184.1 nM,> 70 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,4,0.5 nM,138 nM,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOCCOCCOCCOCCOCCOC,PEG,19,6,16,991.0149999999994,No,,,,30012605,11,No,,Reviewed,Q06187,No,No,No,No,24,267.43
399,Cc1nc[nH]c1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOCCOCCOCCOCCC(=O)N2CCC[C@@H](n3nc(-c4ccc(Oc5ccc(F)cc5F)cc4)c(C(N)=O)c3N)C2)C(C)(C)C)cc1,Inactive,No,"Ramos, THP-1",4.836020000000009,Ligand name is from PMID 24068666,Adi Rogel,,,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2[nH]cnc2C)cc1)C(C)(C)C,VHL,,,other,16,6,,,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOCCOCCOCCOCCOC,PEG,16,5,13,1129.2729999999992,No,,,,30012605,12,No,,Reviewed,Q06187,No,No,No,No,24,290.0399999999999
400,Cc1nc[nH]c1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOCCOCCOCCOCCOCCC(=O)N2CCC[C@@H](n3nc(-c4ccc(Oc5ccc(F)cc5F)cc4)c(C(N)=O)c3N)C2)C(C)(C)C)cc1,Inactive,No,"Ramos, THP-1",4.8526200000000115,Ligand name is from PMID 24068666,Adi Rogel,,,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2[nH]cnc2C)cc1)C(C)(C)C,VHL,,,other,17,6,,,PF-06250112,N#CN1CCC[C@H](n2nc(-c3ccc(Oc4ccc(F)cc4F)cc3)c(C(N)=O)c2N)C1,CCOCCOCCOCCOCCOCCOC,PEG,19,6,16,1173.3259999999993,No,,,,30012605,13,No,,Reviewed,Q06187,No,No,No,No,24,299.2699999999999
401,C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCC(=O)Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,K562,2.8121,Covalent Protac,Paul Gehrtz,,~ 50 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_ester,16,3,,,1 (Ibrutinib analogue),C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)O,CCOCCOCC=O,PEG,9,3,6,871.8639999999998,BLK (proven for cmpd 7),,5P9J,"8E8",31922153,3a,No,,Reviewed,Q06187,No,Yes,No,Yes,24,256.57
402,C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCCOCC(=O)Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,K562,2.8287000000000004,Covalent Protac,Paul Gehrtz,,~ 50 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_ester,17,3,,,1 (Ibrutinib analogue),C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)O,CCOCCOCCOCC=O,PEG,12,4,9,915.9169999999997,BLK (proven for cmpd 7),,5P9J,"8E8",31922153,3b,No,,Reviewed,Q06187,No,Yes,No,Yes,24,265.79999999999995
403,C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCCOCCOCC(=O)Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,K562,2.845300000000001,Covalent Protac,Paul Gehrtz,,~ 50 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_ester,18,3,,,1 (Ibrutinib analogue),C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)O,CCOCCOCCOCCOCC=O,PEG,15,5,12,959.9699999999996,BLK (proven for cmpd 7),,5P9J,"8E8",31922153,3c,No,,Reviewed,Q06187,No,Yes,No,Yes,24,275.03
404,C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCCOCCOCCOCC(=O)Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,K562,2.861900000000004,Covalent Protac,Paul Gehrtz,,~ 50 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_ester,19,3,,,1 (Ibrutinib analogue),C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)O,CCOCCOCCOCCOCCOCC=O,PEG,18,6,15,1004.0229999999995,BLK (proven for cmpd 7),,5P9J,"8E8",31922153,3d,No,,Reviewed,Q06187,No,Yes,No,Yes,24,284.25999999999993
405,C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)NCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,K562,3.605500000000001,Covalent Protac,Paul Gehrtz,,~ 50 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,13,4,,,1 (Ibrutinib analogue),C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)O,CCCCN,Alkane,5,1,2,796.845,BLK (proven for cmpd 7),,5P9J,"8E8",31922153,4a,No,,Reviewed,Q06187,No,Yes,No,Yes,24,223.83999999999997
406,C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)NCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,K562,4.385700000000002,Covalent Protac,Paul Gehrtz,,~ 50 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,13,4,,,1 (Ibrutinib analogue),C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)O,CCCCCCN,Alkane,7,1,4,824.8989999999999,BLK (proven for cmpd 7),,5P9J,"8E8",31922153,4b,No,,Reviewed,Q06187,No,Yes,No,Yes,24,223.83999999999997
407,C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)NCCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,K562,5.165900000000003,Covalent Protac,Paul Gehrtz,,~ 50 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,13,4,,,1 (Ibrutinib analogue),C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)O,CCCCCCCCN,Alkane,9,1,6,852.9529999999997,BLK (proven for cmpd 7),,5P9J,"8E8",31922153,4c,No,,Reviewed,Q06187,No,Yes,No,Yes,24,223.83999999999997
408,C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)NCCCCCCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Active,No,K562,6.7263000000000055,Covalent Protac,Paul Gehrtz,,~ 50 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,13,4,,,1 (Ibrutinib analogue),C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)O,CCCCCCCCCCCCN,Alkane,13,1,10,909.0609999999995,BLK (proven for cmpd 7),,5P9J,"8E8",31922153,4d,No,,Reviewed,Q06187,No,Yes,No,Yes,24,223.83999999999997
409,C=CC(=O)N[C@@H](CCC(=O)OCCOCCOCC(=O)Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,Inactive,No,K562,4.347440000000008,Covalent Protac,Paul Gehrtz,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_ester,16,7,,,2 (PLS-123 analogue),C=CC(=O)N[C@@H](CCC(=O)O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,CCOCCOCC=O,PEG,9,3,6,1037.0559999999998,BLK (proven for cmpd 7),,,,31922153,5a,No,,Reviewed,Q06187,No,Yes,No,Yes,24,311.61999999999995
410,C=CC(=O)N[C@@H](CCC(=O)OCCOCCOCCOCCOCC(=O)Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,Inactive,No,K562,4.38064000000001,Covalent Protac,Paul Gehrtz,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_ester,18,7,,,2 (PLS-123 analogue),C=CC(=O)N[C@@H](CCC(=O)O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,CCOCCOCCOCCOCC=O,PEG,15,5,12,1125.1619999999998,BLK (proven for cmpd 7),,,,31922153,5b,No,,Reviewed,Q06187,No,Yes,No,Yes,24,330.0799999999999
411,C=CC(=O)N[C@@H](CCC(=O)NCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,Active,No,K562,5.140840000000003,Covalent Protac,Paul Gehrtz,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,13,8,,,2 (PLS-123 analogue),C=CC(=O)N[C@@H](CCC(=O)O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,CCCCN,Alkane,5,1,2,962.0369999999999,BLK (proven for cmpd 7),,,,31922153,6a,No,,Reviewed,Q06187,No,Yes,No,Yes,24,278.89
412,C=CC(=O)N[C@@H](CCC(=O)NCCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,Active,No,K562,6.701240000000003,Covalent Protac,Paul Gehrtz,< 300 nM,~ 75 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,13,8,,186 nM,2 (PLS-123 analogue),C=CC(=O)N[C@@H](CCC(=O)O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,CCCCCCCCN,Alkane,9,1,6,1018.1449999999998,BLK (proven for cmpd 7),,,,31922153,6b,No,,Reviewed,Q06187,No,Yes,No,Yes,24,278.89
413,C=CC(=O)N1C[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C,Active,Yes,K562,5.013220000000006,Covalent Protac,Paul Gehrtz,136 nM,88 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,carboxilic_acid_to_ester,17,4,,39 nM,1 (Ibrutinib analogue),C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)O,CCOCCOCC=O,PEG,9,3,6,1029.1899999999996,BLK (proven for cmpd 7),,5P9J,"8E8",31922153,7,No,,Reviewed,Q06187,No,Yes,No,Yes,24,255.54999999999995
414,C=CC(=O)N[C@H](CCC(=O)NCCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)CC1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,Active,No,K562,8.428960000000007,Covalent Protac,Paul Gehrtz,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,carboxilic_acid_to_amide,14,9,,,2 (PLS-123 analogue),C=CC(=O)N[C@@H](CCC(=O)O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,NCCCCCCCC=O,Alkane,10,2,7,1189.4539999999995,BLK (proven for cmpd 7),,,,31922153,8,No,,Reviewed,Q06187,No,Yes,No,Yes,24,294.93999999999994
415,CCC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)CC1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C,Active,No,K562,5.237220000000007,Non covalent control,Paul Gehrtz,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,17,4,,2657 nM,1 (Ibrutinib analogue),C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)O,CCOCCOCC=O,PEG,9,3,6,1031.2059999999994,BLK (proven for cmpd 7),,5P9J,"8E8",31922153,9,No,,Reviewed,Q06187,No,Yes,No,Yes,24,255.54999999999995
416,CCC(=O)N[C@@H](CCC(=O)NCCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,Active,No,K562,6.925240000000003,Non covalent control,Paul Gehrtz,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,8,,415 nM,2 (PLS-123 analogue),C=CC(=O)N[C@@H](CCC(=O)O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1,CCCCCCCCN,Alkane,9,1,6,1020.1609999999997,BLK (proven for cmpd 7),,,,31922153,10,No,,Reviewed,Q06187,No,Yes,No,Yes,24,278.89
417,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,3.016420000000002,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,19,3,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCCn1cc(C)nn1,Other,14,5,7,916.0129999999995,No,,2EUF,LQQ,31330105,CP-2,No,,Reviewed,Q00534,Yes,No,No,No,,240.99999999999994
418,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCOCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,3.033020000000004,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,20,3,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCCOCCn1cc(C)nn1,Other,17,6,10,960.0659999999995,No,,2EUF,LQQ,31330105,CP-3,No,,Reviewed,Q00534,No,No,No,No,,250.22999999999996
419,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCOCCOCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,3.0496200000000036,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,21,3,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCCOCCOCCn1cc(C)nn1,Other,20,7,13,1004.1189999999996,No,,2EUF,LQQ,31330105,CP-4,No,,Reviewed,Q00534,No,No,No,No,,259.46
420,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CC(=O)NCCOCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,2.324320000000002,DC50 for CDK4 > 100 nM,Efrat Resnick,1.1 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,16,4,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCNC(C)=O,Other,9,3,4,847.9339999999995,No,,2EUF,LQQ,31330105,CP-5,No,,Reviewed,Q00534,No,No,No,No,,230.15999999999997
421,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CC(=O)NCCOCCOCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,2.3409200000000014,DC50 for CDK4 > 100 nM,Efrat Resnick,24.2 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,17,4,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCCNC(C)=O,Other,12,4,7,891.9869999999995,No,,2EUF,LQQ,31330105,CP-6,No,,Reviewed,Q00534,No,No,No,No,,239.39
422,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CC(=O)NCCOCCOCCOCCOCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,2.374120000000006,DC50 for CDK4 > 100 nM,Efrat Resnick,31 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,19,4,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCCOCCOCCNC(C)=O,Other,18,6,13,980.0929999999995,No,,2EUF,LQQ,31330105,CP-8,No,,Reviewed,Q00534,No,No,No,No,,257.85
423,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,Yes,U251,2.9998200000000015,DC50 for CDK4 > 100 nM. EC50 of PROTAC is 10nM in MM.lS 8nM in Mino.,Efrat Resnick,2.1 nM,89 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,18,3,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCn1cc(C)nn1,Other,11,4,4,871.9599999999995,No,,2EUF,LQQ,31330105,CP-10,Yes,,Reviewed,Q00534,Yes,Yes,No,Yes,,231.76999999999998
424,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCCCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,4.153520000000002,DC50 for CDK4 > 100 nM,Efrat Resnick,5.3 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,17,3,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCCCCn1cc(C)nn1,Other,11,3,4,869.9879999999995,No,,2EUF,LQQ,31330105,CP-13,No,,Reviewed,Q00534,No,No,No,No,,222.53999999999996
425,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCCCCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,4.543620000000002,DC50 for CDK4 > 100 nM,Efrat Resnick,10.6 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,17,3,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCCCCCn1cc(C)nn1,Other,12,3,5,884.0149999999995,No,,2EUF,LQQ,31330105,CP-14,No,,Reviewed,Q00534,No,No,No,No,,222.53999999999996
426,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CCOCCOCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,3.2247200000000014,DC50 for CDK4 > 100 nM,Efrat Resnick,1.6 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,16,3,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCC,Other,8,2,5,834.9349999999996,No,,2EUF,LQQ,31330105,CP-15,No,,Reviewed,Q00534,No,No,No,No,,210.28999999999996
427,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCCCCCc6cccc7c6CN(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,5.0340200000000035,DC50 for CDK4 > 50 nM,Efrat Resnick,1.7 nM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,15,2,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCCCCCn1cc(C)nn1,Other,12,3,5,855.0169999999996,No,,2EUF,LQQ,31330105,CP-16,No,,Reviewed,Q00534,No,No,No,No,,193.43999999999994
428,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCCCC#Cc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,4.093120000000002,DC50 for CDK4 > 100 nM,Efrat Resnick,81.6 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,16,2,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,C#CCCCCn1cc(C)nn1,Other,12,3,4,864.9679999999995,No,,2EUF,LQQ,31330105,CP-21,No,,Reviewed,Q00534,No,No,No,No,,210.50999999999993
429,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCCCCC#Cc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,,4.483220000000003,DC50 for CDK4 > 100 nM,Efrat Resnick,86.8 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,16,2,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,C#CCCCCCn1cc(C)nn1,Other,13,3,5,878.9949999999995,No,,2EUF,LQQ,31330105,CP-22,No,,Reviewed,Q00534,No,No,No,No,,210.50999999999993
430,COc1ccc(C2=N[C@H](c3ccc(Cl)cc3)[C@H](c3ccc(Cl)cc3)N2C(=O)N2CCN(CC(=O)NCCOCCn3cc(CN4CCN(c5ccc(Nc6ncc7c(C)c(C(C)=O)c(=O)n(C8CCCC8)c7n6)nc5)CC4)nn3)C(=O)C2)c(OC(C)C)c1,Inactive,No,,8.214520000000011,,Efrat Resnick,,,COc1ccc(C2=N[C@H](c3ccc(Cl)cc3)[C@H](c3ccc(Cl)cc3)N2C(=O)N2CCNC(=O)C2)c(OC(C)C)c1,Mdm2,,,amine_to_methylamine,19,2,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CC(=O)NCCOCCn1cc(C)nn1,Other,15,6,6,1237.263999999999,No,,2EUF,LQQ,31330105,MP-1,No,,Reviewed,Q00534,No,No,No,No,,239.96999999999994
431,COc1ccc(C2=N[C@H](c3ccc(Cl)cc3)[C@H](c3ccc(Cl)cc3)N2C(=O)N2CCN(CC(=O)NCCOCCOCCn3cc(CN4CCN(c5ccc(Nc6ncc7c(C)c(C(C)=O)c(=O)n(C8CCCC8)c7n6)nc5)CC4)nn3)C(=O)C2)c(OC(C)C)c1,Inactive,No,,8.23112000000001,,Efrat Resnick,,,COc1ccc(C2=N[C@H](c3ccc(Cl)cc3)[C@H](c3ccc(Cl)cc3)N2C(=O)N2CCNC(=O)C2)c(OC(C)C)c1,Mdm2,,,amine_to_methylamine,20,2,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CC(=O)NCCOCCOCCn1cc(C)nn1,Other,18,7,9,1281.3169999999993,No,,2EUF,LQQ,31330105,MP-2,No,,Reviewed,Q00534,No,No,No,No,,249.1999999999999
432,COc1ccc(C2=N[C@H](c3ccc(Cl)cc3)[C@H](c3ccc(Cl)cc3)N2C(=O)N2CCN(CC(=O)NCCOCCOCCOCCn3cc(CN4CCN(c5ccc(Nc6ncc7c(C)c(C(C)=O)c(=O)n(C8CCCC8)c7n6)nc5)CC4)nn3)C(=O)C2)c(OC(C)C)c1,Inactive,No,,8.24772000000001,,Efrat Resnick,,,COc1ccc(C2=N[C@H](c3ccc(Cl)cc3)[C@H](c3ccc(Cl)cc3)N2C(=O)N2CCNC(=O)C2)c(OC(C)C)c1,Mdm2,,,amine_to_methylamine,21,2,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CC(=O)NCCOCCOCCOCCn1cc(C)nn1,Other,21,8,12,1325.3699999999994,No,,2EUF,LQQ,31330105,MP-3,No,,Reviewed,Q00534,No,No,No,No,,258.42999999999995
433,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCNC(=O)CCC(=O)NC(C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Inactive,No,,4.623940000000008,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,20,5,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,Cc1cn(CCOCCNC(=O)CCC=O)nn1,Other,18,7,9,1128.3749999999998,No,,2EUF,LQQ,31330105,VP-1,No,,Reviewed,Q00534,No,No,No,No,,276.91999999999996
434,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCOCCNC(=O)CCC(=O)NC(C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Inactive,No,,4.64054000000001,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,21,5,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,Cc1cn(CCOCCOCCNC(=O)CCC=O)nn1,Other,21,8,12,1172.4279999999999,No,,2EUF,LQQ,31330105,VP-2,No,,Reviewed,Q00534,No,No,No,No,,286.1499999999999
435,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCOCCOCCNC(=O)CCC(=O)NC(C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Inactive,No,,4.657140000000011,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,22,5,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,Cc1cn(CCOCCOCCOCCNC(=O)CCC=O)nn1,Other,24,9,15,1216.4810000000002,No,,2EUF,LQQ,31330105,VP-3,No,,Reviewed,Q00534,No,No,No,No,,295.37999999999994
436,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCOCCOCCOCCNC(=O)CCC(=O)NC(C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O,Inactive,No,,4.673740000000012,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,23,5,,,palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,Cc1cn(CCOCCOCCOCCOCCNC(=O)CCC=O)nn1,Other,27,10,18,1260.5340000000003,No,,2EUF,LQQ,31330105,VP-4,No,,Reviewed,Q00534,No,No,No,No,,304.60999999999996
437,CN(C)C(=O)c1cc2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n1C1CCCC1,Inactive,No,,2.830400000000002,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,17,3,,,ribociclib,CN(C)C(=O)c1cc2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n1C1CCCC1,CCOCCn1cc(C)nn1,Other,11,4,4,858.9649999999993,No,,5L2T,6ZZ,31330105,CP-R1,No,,Reviewed,Q00534,No,No,No,No,,217.93999999999994
438,CN(C)C(=O)c1cc2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n1C1CCCC1,Inactive,No,,2.8470000000000013,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,18,3,,,ribociclib,CN(C)C(=O)c1cc2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n1C1CCCC1,CCOCCOCCn1cc(C)nn1,Other,14,5,7,903.0179999999993,No,,5L2T,6ZZ,31330105,CP-R2,No,,Reviewed,Q00534,No,No,No,No,,227.16999999999996
439,CN(C)C(=O)c1cc2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCOCCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n1C1CCCC1,Inactive,No,,2.8636000000000026,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,19,3,,,ribociclib,CN(C)C(=O)c1cc2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n1C1CCCC1,CCOCCOCCOCCn1cc(C)nn1,Other,17,6,10,947.0709999999995,No,,5L2T,6ZZ,31330105,CP-R3,No,,Reviewed,Q00534,No,No,No,No,,236.39999999999998
440,Cc1nc2c(F)cc(-c3nc(Nc4ccc(CN5CCN(c6cn(CCOCCNc7cccc8c7C(=O)N(C7CCC(=O)NC7=O)C8=O)nn6)CC5)cn4)ncc3F)cc2n1C(C)C,Active,No,,4.243020000000002,DC50 for CDK4 > 500 nM,Efrat Resnick,8.6 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,3,,,Abemaciclib,CCN1CCN(Cc2ccc(Nc3ncc(F)c(-c4cc(F)c5nc(C)n(C(C)C)c5c4)n3)nc2)CC1,CCOCCnnn,Other,8,4,4,888.9409999999997,No,,5L2S,6ZZ,31330105,CP-A1,No,,Reviewed,Q00534,No,No,No,No,,210.51999999999998
441,Cc1nc2c(F)cc(-c3nc(Nc4ccc(CN5CCN(c6cn(CCOCCOCCNc7cccc8c7C(=O)N(C7CCC(=O)NC7=O)C8=O)nn6)CC5)cn4)ncc3F)cc2n1C(C)C,Active,No,,4.259620000000002,DC50 for CDK4 > 500 nM,Efrat Resnick,129.7 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,3,,,Abemaciclib,CCN1CCN(Cc2ccc(Nc3ncc(F)c(-c4cc(F)c5nc(C)n(C(C)C)c5c4)n3)nc2)CC1,CCOCCOCCnnn,Other,11,5,7,932.9939999999997,No,,5L2S,6ZZ,31330105,CP-A2,No,,Reviewed,Q00534,No,No,No,No,,219.74999999999994
442,Cc1nc2c(F)cc(-c3nc(Nc4ccc(CN5CCN(c6cn(CCOCCOCCOCCNc7cccc8c7C(=O)N(C7CCC(=O)NC7=O)C8=O)nn6)CC5)cn4)ncc3F)cc2n1C(C)C,Active,No,,4.276220000000003,DC50 for CDK4 > 500 nM,Efrat Resnick,271.9 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,19,3,,,Abemaciclib,CCN1CCN(Cc2ccc(Nc3ncc(F)c(-c4cc(F)c5nc(C)n(C(C)C)c5c4)n3)nc2)CC1,CCOCCOCCOCCnnn,Other,14,6,10,977.0469999999998,No,,5L2S,6ZZ,31330105,CP-A3,No,,Reviewed,Q00534,No,No,No,No,,228.97999999999996
443,Cc1nc2c(F)cc(-c3nc(Nc4ccc(CN5CCN(c6cn(CCOCCOCCOCCOCCNc7cccc8c7C(=O)N(C7CCC(=O)NC7=O)C8=O)nn6)CC5)cn4)ncc3F)cc2n1C(C)C,Active,No,,4.292820000000003,DC50 for CDK4 > 500 nM,Efrat Resnick,145.5 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,20,3,,,Abemaciclib,CCN1CCN(Cc2ccc(Nc3ncc(F)c(-c4cc(F)c5nc(C)n(C(C)C)c5c4)n3)nc2)CC1,CCOCCOCCOCCOCCnnn,Other,17,7,13,1021.0999999999997,No,,5L2S,6ZZ,31330105,CP-A4,No,,Reviewed,Q00534,No,No,No,No,,238.20999999999998
444,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Inactive,No,,1.773920000000004,,"Efrat Resnick, Yangwode Jing",,< 20 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,13,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCOCCOCC=O,PEG,9,3,6,831.949,No,,4CI3,Y70,30672516,CRBN-2-2-2-VHL,No,,Reviewed,Q96SW2,No,No,No,No,,225.67
445,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Inactive,No,,1.7905200000000052,,"Efrat Resnick, Yangwode Jing",,< 20 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,14,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCOCCOCCOCC=O,PEG,12,4,9,876.002,No,,4CI3,Y70,30672516,CRBN-2-2-2-2-VHL,No,,Reviewed,Q96SW2,No,No,No,No,,234.89999999999998
446,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCOCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Inactive,No,,2.9608200000000044,,"Efrat Resnick, Yangwode Jing",,< 20 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,14,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCOCCOCCOCCCCC=O,non-PEG polyether,15,4,12,918.0829999999999,No,,4CI3,Y70,30672516,CRBN-2-2-2-5-VHL,No,,Reviewed,Q96SW2,No,No,No,No,,234.89999999999998
447,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCOCCCCCOCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Active,Yes,MM1S,5.674920000000003,,"Efrat Resnick, Yangwode Jing",1.5 nM,> 90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,13,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCCCCCOCCCCCOCCCCC=O,non-PEG polyether,19,3,16,972.2189999999996,No,,4CI3,Y70,30672516,CRBN-6-5-5-VHL,No,,Reviewed,Q96SW2,Yes,Yes,No,Yes,24,225.67
448,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCOCCCCCCOCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Active,No,,6.455120000000004,,"Efrat Resnick, Yangwode Jing",,> 90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,13,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCCCCCOCCCCCCOCCCCCC=O,non-PEG polyether,21,3,18,1000.2729999999995,No,,4CI3,Y70,30672516,CRBN-6-6-6-VHL,No,,Reviewed,Q96SW2,No,No,No,No,,225.67
449,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCOCCCCOCCCCOCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Active,No,,5.691520000000005,,"Efrat Resnick, Yangwode Jing",,> 90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,14,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCCCOCCCCOCCCCOCCCCCC=O,non-PEG polyether,22,4,19,1016.2719999999995,No,,4CI3,Y70,30672516,CRBN-4-4-4-6-VHL,No,,Reviewed,Q96SW2,No,No,No,No,,234.89999999999998
450,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCOCCOCCOCCOCCOCCOCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Active,No,,4.961120000000009,,"Efrat Resnick, Yangwode Jing",,> 90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,17,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCCCCCOCCOCCOCCOCCOCCOCCCCCC=O,non-PEG polyether,29,7,26,1120.3769999999988,No,,4CI3,Y70,30672516,CRBN-6-(2)5-6-VHL,No,,Reviewed,Q96SW2,No,No,No,No,,262.59
451,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCOCCCCOCCCCOCCCCOCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Active,No,,7.268520000000008,,"Efrat Resnick, Yangwode Jing",,> 90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,15,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCCCCCOCCCCOCCCCOCCCCOCCCCCC=O,non-PEG polyether,29,5,26,1116.4329999999986,No,,4CI3,Y70,30672516,CRBN-6-(4)3-6-VHL,No,,Reviewed,Q96SW2,No,No,No,No,,244.12999999999997
452,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2[C@@H]1CCCN(CC(=O)NCCOCCOCC(=O)NCCOCCOc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C1,Active,Yes,Ramos,2.2671000000000037,,Ella Livnah,,85 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,17,4,,0.159 uM,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,NCCOCCOCC(=O)NCCOCCO,PEG,17,7,12,932.9919999999997,No,,,,30601480,8c,No,,Reviewed,Q06187,No,No,No,No,16,260.76
453,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2[C@@H]1CCCN(CC(=O)NCCOCCOc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C1,Inactive,No,Ramos,3.1177,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,3,,0.102 uM,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,NCCOCCO,PEG,7,3,4,787.8340000000001,No,,,,30601480,10,No,,Reviewed,Q06187,No,No,No,No,16,213.2
454,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2[C@@H]1CCCN(CC(=O)NCCOCCOCCC(=O)NCCOCCOCC(=O)NCCOCCOc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C1,Active,No,Ramos,1.8066000000000084,,Ella Livnah,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,20,5,,0.108 uM,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,NCCOCCOCCC(=O)NCCOCCOCC(=O)NCCOCCO,PEG,28,11,21,1092.1769999999995,No,,,,30601480,12,No,,Reviewed,Q06187,No,No,No,No,16,308.31999999999994
461,COc1cc(C(=O)NCCOCCOCCOCCNC(=O)C[C@@H]2N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc32)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F,Active,No,HCT116,10.339739999999995,,Adi Rogel,32 nM,98 %,COc1cc(C(N)=O)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F,Mdm2,,,ester_to_amide,14,4,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,CCOCCOCCOCCN,PEG,12,4,9,1173.6119999999994,No,,,,30385614,A1874,No,,Reviewed,O60885,Yes,No,No,No,24,203.10999999999999
462,NC(=O)c1cccc2cn(-c3ccc(-c4cn(CCOCCOCCOCCOCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)cc3)nc12,Inactive,No,MDA-MB-231,1.9626,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_C,15,3,,,Niraparib derivative,NC(=O)c1cccc2cn(-c3ccccc3)nc12,CCOCCOCCOCCOCCn1ccnn1,Other,19,7,13,779.811,No,,4R6E,3JD,30540295,1,No,,Reviewed,P09874,No,No,No,No,,224.12
463,Cc1ncsc1-c1ccc(CNC(=O)[C@H]2C[C@H](O)CN2C(=O)C(NC(=O)CCC(=O)NCCOCCOCCOCCn2cc(-c3ccc(-n4cc5cccc(C(N)=O)c5n4)cc3)nn2)C(C)(C)C)cc1,Inactive,No,MDA-MB-231,3.5701200000000055,,Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_C,16,5,,,Niraparib derivative,NC(=O)c1cccc2cn(-c3ccccc3)nc12,O=CCCC(=O)NCCOCCOCCOCCn1ccnn1,Other,23,9,15,992.1729999999994,No,,4R6E,3JD,30540295,2,No,,Reviewed,P09874,No,No,No,No,,260.03999999999996
464,COc1ccc(C2=N[C@@H](c3ccc(Cl)cc3)[C@@H](c3ccc(Cl)cc3)N2C(=O)N2CCN(CC(=O)NCCOCCOCCOCCOCCn3cc(-c4ccc(-n5cc6cccc(C(N)=O)c6n5)cc4)nn3)C(=O)C2)cc1OC(C)C,Active,Yes,MDA-MB-231,7.17730000000001,"EC50 of PROTAC is 8.45 ± 0.54uM (24h treatment), 6.12 ± 0.204uM (48h treatment)",Efrat Resnick,,,COc1ccc(C2=N[C@H](c3ccc(Cl)cc3)[C@H](c3ccc(Cl)cc3)N2C(=O)N2CCNC(=O)C2)c(OC(C)C)c1,Mdm2,,,aryl_C,16,2,,,Niraparib derivative,NC(=O)c1cccc2cn(-c3ccccc3)nc12,CC(=O)NCCOCCOCCOCCOCCn1ccnn1,Other,23,9,15,1145.114999999999,No,,4R6E,3JD,30540295,3,No,,Reviewed,P09874,No,Yes,No,Yes,"24,48",232.31999999999996
465,O=C1CCC(N2C(=O)c3cccc(NCCOCCOCCOCCOCCn4cc(CCCC(=O)N5CCN(C(=O)c6cc(Cc7n[nH]c(=O)c8ccccc78)ccc6F)CC5)nn4)c3C2=O)C(=O)N1,Inactive,No,MDA-MB-231,2.1315000000000057,,Efrat Resnick,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,3,,,Olaparib derivative,C=Cc1c(Cc2ccc(F)c(C(=O)N3CCN(C(=O)CCC)CC3)c2)n[nH]c(=O)c1C,CCOCCOCCOCCOCCn1ccnn1,Other,19,7,13,979.0359999999997,No,,,,30540295,4,No,,Reviewed,P09874,No,No,No,No,,249.57999999999996
466,COc1ccc(C2=N[C@H](c3ccc(Cl)cc3)[C@H](c3ccc(Cl)cc3)N2C(=O)N2CCN(CC(=O)NCCOCCOCCOCCOCCn3cc(CCCC(=O)N4CCN(C(=O)c5cc(Cc6n[nH]c(=O)c7ccccc67)ccc5F)CC4)nn3)C(=O)C2)cc1OC(C)C,Inactive,No,MDA-MB-231,7.346200000000011,,Efrat Resnick,,,COc1ccc(C2=N[C@H](c3ccc(Cl)cc3)[C@H](c3ccc(Cl)cc3)N2C(=O)N2CCNC(=O)C2)c(OC(C)C)c1,Mdm2,,,other,17,2,,,Olaparib derivative,C=Cc1c(Cc2ccc(F)c(C(=O)N3CCN(C(=O)CCC)CC3)c2)n[nH]c(=O)c1C,CC(=O)NCCOCCOCCOCCOCCn1ccnn1,Other,23,9,15,1344.3399999999988,No,,,,30540295,5,No,,Reviewed,P09874,No,No,No,No,,257.78000000000003
467,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOCCOc2ccc3c(c2)sc2nc(-c4ccc(NC(=O)Nc5cc(C(C)(C)C)on5)cc4)cn23)C(C)(C)C)cc1,Active,Yes,"MV4-11, MOLM-14",8.188620000000007,"IC50 of ligand is FLT-3 ITD 10.3± 0.3nM, FLT-3 WT 7.4± 0.3nM. IC50 of PROTAC is FLT-3 ITD 43± 3.2nM, FLT-3 WT 36± 3nM.",Efrat Resnick,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CO,15,5,< 10.3 nM,< 43 nM,quizartinib,CCOc1ccc2c(c1)sc1nc(-c3ccc(NC(=O)Nc4cc(C(C)(C)C)on4)cc3)cn12,O=CCCOCCO,PEG,8,3,5,1020.2479999999998,other kinases,,,,30427680,FLT-3 PROTAC,No,,Reviewed,P36888,Yes,No,No,No,,223.77999999999994
468,Cc1cc(C(C(=O)N2C[C@H](O)CC2C(=O)NC(CC(=O)N2CCC(N3CCC(C#Cc4ccc(C(=O)NC5C(C)(C)C(Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,Yes,LnCap,9.255720000000004,,Paul Gehrtz,8.0 nM,,Cc1cc(C(C(=O)N2C[C@H](O)CC2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)C)on1,VHL,,,other,12,3,,,ARI-16,CC1(C)C(NC(=O)c2cnn(CCO)c2)C(C)(C)C1Oc1ccc(C#N)c(Cl)c1,cc(-c)C#CC1CCN(C2CCN(C(C)=O)CC2)CC1,Alkane,20,3,1,1095.8079999999995,No,,,,31931431,ARD-61-HXC (7),Yes,,Reviewed,P10275,No,Yes,No,Yes,6,194.22999999999996
469,Cc1cc(C(C(=O)N2C[C@H](O)CC2C(=O)NC(CC(=O)N2CCC(N3CCC(C#Cc4ccc(N5C(=S)N(c6cnc(C#N)c(C(F)(F)F)c6)C(=O)C56CCC6)cc4)CC3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LnCap,8.464920000000008,,Paul Gehrtz,,,Cc1cc(C(C(=O)N2C[C@H](O)CC2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)C)on1,VHL,,,other,13,2,,,Apalutamide,CNC(=O)c1ccc(N2C(=S)N(c3cnc(C#N)c(C(F)(F)F)c3)C(=O)C23CCC3)cc1F,CC(=O)N1CCC(N2CCC(C)CC2)CC1,Alkane,16,3,1,1115.3179999999993,No,,,,31931431,ARD-77-HXC (8),No,,Reviewed,P10275,No,Yes,No,Yes,6,192.33999999999997
470,Cc1cc(C(C(=O)N2C[C@H](O)CC2C(=O)NC(CC(=O)N2CCC(N3CCC(C#Cc4ccc(N5C(=S)N(c6ccc(C#N)c(C(F)(F)F)c6)C(=O)C5(C)C)cc4)CC3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LnCap,8.925820000000005,,Paul Gehrtz,,,Cc1cc(C(C(=O)N2C[C@H](O)CC2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)C)on1,VHL,,,other,12,2,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CC(=O)N1CCC(N2CCC(C)CC2)CC1,Alkane,16,3,1,1102.3189999999995,No,,,,31931431,ARD-86-HXC (9),No,,Reviewed,P10275,No,Yes,No,Yes,6,179.44999999999993
471,Cc1cc(C(C(=O)N2C[C@H](O)CC2C(=O)NC(CC(=O)N2CCC(N3CCC(C#Cc4ccc(S(=O)(=O)CC(C)(O)C(=O)Nc5ccc(C#N)c(C(F)(F)F)c5)cc4)CC3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Inactive,No,LnCap,7.17252000000001,,Paul Gehrtz,,,Cc1cc(C(C(=O)N2C[C@H](O)CC2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)C)on1,VHL,,,other,14,4,,,Bicalutamide,CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc1ccc(C#N)c(C(F)(F)F)c1,C#CC1CCN(C2CCN(C(C)=O)CC2)CC1,Alkane,17,3,1,1125.3059999999996,No,,,,31931431,ARD-111-HXC (10),No,,Reviewed,P10275,No,Yes,No,Yes,6,239.36999999999995
472,COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1OCCCCOCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C,Active,Yes,"MDA-MB-231, HeLa",8.884720000000003,DC50 error ± 1.0 nM. DMAX error ± 1.1 %.,Ella Livnah,9.5 nM,99.6 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,foretinib,COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1O,CCCCOCCCCOCC=O,PEG,13,3,10,1120.2859999999987,No,,,,30631068,SJFα,No,,Reviewed,"O15264, Q16539",No,No,Yes,Yes,"0.5,1.5,3,6,24",228.87
473,COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1OCCOCCOCCOc1cc(-c2scnc2C)ccc1CNC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@H](C(C)C)N1Cc2ccccc2C1=O,Active,No,"MDA-MB-231, HeLa",8.852820000000005,DC50 error ± 81.3 nM. DMAX error ± 10.1 %.,Ella Livnah,45.9 nM,34.5 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@H](C(C)C)N2Cc3ccccc3C2=O)c(O)c1,VHL,,,other,15,4,,,foretinib,COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1O,CCOCCOCC,PEG,8,2,5,1168.2859999999994,No,,,,30631068,SJFδ,No,,Reviewed,"O15264, Q16539",No,No,Yes,Yes,"0.5,1.5,3,6,24",229.31
474,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCNC(=O)c2cccc(-c3cc(Nc4ccc(OC(F)(F)F)cc4)ncn3)c2)C(C)(C)C)cc1,Active,No,K562,5.773220000000006,,Adi Rogel,2 uM,85 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,GNF-5,O=C(NCCO)c1cccc(-c2cc(Nc3ccc(OC(F)(F)F)cc3)ncn2)c1,CC=O,PEG,3,1,0,888.9700000000001,No,,3K5V,STJ,31311809,GMB-101,No,,Reviewed,P00519,No,No,No,No,18,196.99999999999994
475,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOc2cccc(-c3cc(Nc4ccc(OC(F)(F)F)cc4)ncn3)c2)C(C)(C)C)cc1,Active,Yes,K562,6.4222200000000065,,Adi Rogel,340 nM,95 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,4,,,GNF-5 analog,Oc1cccc(-c2cc(Nc3ccc(OC(F)(F)F)cc3)ncn2)c1,CCOCC=O,PEG,6,2,3,861.9440000000002,No,,3K5V,STJ,31311809,GMB-475,Yes,,Reviewed,P00519,Yes,No,No,Yes,18,177.13
476,COc1c(O)cc(O)c2c(=O)cc(-c3ccc(OCCCCCC(=O)Nc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3)oc12,Inactive,No,MCF-7,3.858900000000001,EC50 of ligand and PROTAC was measured in MCF-7 cell line,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,11,4,,,Wogonin,COc1c(O)cc(O)c2c(=O)cc(-c3ccccc3)oc12,O=CCCCCCO,Alkane,8,2,5,669.6430000000003,No,,,,30196207,8a,No,,Reviewed,P50750,No,No,No,No,24,201.77999999999997
477,COc1c(O)cc(O)c2c(=O)cc(-c3ccc(OCCCCCCC(=O)Nc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3)oc12,Inactive,No,MCF-7,4.249000000000001,EC50 of ligand and PROTAC was measured in MCF-7 cell line,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,11,4,,,Wogonin,COc1c(O)cc(O)c2c(=O)cc(-c3ccccc3)oc12,O=CCCCCCCO,Alkane,9,2,6,683.6700000000002,No,,,,30196207,8b,No,,Reviewed,P50750,No,No,No,No,24,201.77999999999997
478,COc1c(O)cc(O)c2c(=O)cc(-c3ccc(OCCCCCCCC(=O)Nc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3)oc12,Active,No,MCF-7,4.639100000000003,EC50 of ligand and PROTAC was measured in MCF-7 cell line,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,11,4,,,Wogonin,COc1c(O)cc(O)c2c(=O)cc(-c3ccccc3)oc12,O=CCCCCCCCO,Alkane,10,2,7,697.6970000000002,No,,,,30196207,8c,No,,Reviewed,P50750,No,No,No,No,24,201.77999999999997
479,COc1c(O)cc(O)c2c(=O)cc(-c3ccc(OCCCCCCCCCC(=O)Nc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3)oc12,Active,No,MCF-7,5.419300000000004,EC50 of ligand and PROTAC was measured in MCF-7 cell line,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,11,4,,,Wogonin,COc1c(O)cc(O)c2c(=O)cc(-c3ccccc3)oc12,O=CCCCCCCCCCO,Alkane,12,2,9,725.7510000000002,No,,,,30196207,8d,No,,Reviewed,P50750,No,No,No,No,24,201.77999999999997
480,COc1c(O)cc(O)c2c(=O)cc(-c3ccc(OCc4cn(CCCCCC(=O)Nc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)cc3)oc12,Active,No,MCF-7,3.6506000000000007,EC50 of ligand and PROTAC was measured in MCF-7 cell line,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,14,4,,,Wogonin,COc1c(O)cc(O)c2c(=O)cc(-c3ccccc3)oc12,O=CCCCCCn1cc(CO)nn1,Other,14,5,7,750.721,No,,,,30196207,11a,No,,Reviewed,P50750,No,No,No,No,24,232.48999999999995
481,COc1c(O)cc(O)c2c(=O)cc(-c3ccc(OCc4cn(CCCCCCC(=O)Nc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)cc3)oc12,Active,No,MCF-7,4.040700000000001,EC50 of ligand and PROTAC was measured in MCF-7 cell line,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,14,4,,,Wogonin,COc1c(O)cc(O)c2c(=O)cc(-c3ccccc3)oc12,O=CCCCCCCn1cc(CO)nn1,Other,15,5,8,764.748,No,,,,30196207,11b,No,,Reviewed,P50750,No,No,No,No,24,232.48999999999995
482,COc1c(O)cc(O)c2c(=O)cc(-c3ccc(OCc4cn(CCCCCCCC(=O)Nc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)cc3)oc12,Active,Yes,MCF-7,4.430800000000001,EC50 of ligand and PROTAC was measured in MCF-7 cell line,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,14,4,,,Wogonin,COc1c(O)cc(O)c2c(=O)cc(-c3ccccc3)oc12,O=CCCCCCCCn1cc(CO)nn1,Other,16,5,9,778.7750000000001,No,,,,30196207,11c,No,,Reviewed,P50750,No,No,No,No,24,232.48999999999995
483,COc1c(O)cc(O)c2c(=O)cc(-c3ccc(OCc4cn(CCCCCCCCCC(=O)Nc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)cc3)oc12,Active,No,MCF-7,5.211000000000004,EC50 of ligand and PROTAC was measured in MCF-7 cell line,Adi Rogel,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,14,4,,,Wogonin,COc1c(O)cc(O)c2c(=O)cc(-c3ccccc3)oc12,O=CCCCCCCCCCn1cc(CO)nn1,Other,18,5,11,806.8290000000001,No,,,,30196207,11d,No,,Reviewed,P50750,No,No,No,Yes,24,232.48999999999995
484,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4cn[nH]c4n3)cc2)c1,Active,No,HEK293,4.638640000000008,,"Ella Livnah, Yangwode Jing",,77 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,17,5,,,Sanofi 308-R,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4cn[nH]c4n3)cc2)c1,CCOCCOCCOCC=O,PEG,12,4,9,1101.2939999999999,No,,,,31461270,DAT1,No,,Reviewed,Q96BR1,No,No,No,Yes,"8,16,48",261.65000000000003
485,COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4c(C)n[nH]c4n3)cc2)c1,Inactive,No,HEK293,5.161540000000008,,"Ella Livnah, Yangwode Jing",,16 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,18,5,,,Sanofi 290-R,COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4c(C)n[nH]c4n3)cc2)c1,CCOCCOCCOCC=O,PEG,12,4,9,1147.7749999999999,No,,,,31461270,DAT2,No,,Reviewed,Q96BR1,No,No,No,No,48,270.88
486,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCOCCOCCOCC(=O)NCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CCO4)c4cn[nH]c4n3)cc2)c1,Inactive,No,HEK293,2.027120000000004,,"Ella Livnah, Yangwode Jing",,30 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,17,5,,,Sanofi 308-R,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4cn[nH]c4n3)cc2)c1,CCNC(=O)COCCOCCOCC,PEG,15,5,10,987.0369999999998,No,,,,31461270,DAT3,No,,Reviewed,Q96BR1,No,No,No,No,48,274.7
487,COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCOCCOCCOCC(=O)NCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CCO4)c4c(C)n[nH]c4n3)cc2)c1,Inactive,No,HEK293,2.5500200000000044,,"Ella Livnah, Yangwode Jing",,16 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,18,5,,,Sanofi 290-R,COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4c(C)n[nH]c4n3)cc2)c1,CCNC(=O)COCCOCCOCC,PEG,15,5,10,1033.5179999999998,No,,,,31461270,DAT4,No,,Reviewed,Q96BR1,No,No,No,No,48,283.93
488,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4cn[nH]c4n3)cc2)c1,Active,No,HEK293,4.622040000000006,,"Ella Livnah, Yangwode Jing",,64 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,16,5,,,Sanofi 308-R,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4cn[nH]c4n3)cc2)c1,CCOCCOCC=O,PEG,9,3,6,1057.2409999999998,No,,,,31461270,DAT5,No,,Reviewed,Q96BR1,No,No,No,No,48,252.42000000000002
489,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCOCCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4cn[nH]c4n3)cc2)c1,Active,No,HEK293,4.65524000000001,,"Ella Livnah, Yangwode Jing",,80 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,18,5,,,Sanofi 308-R,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4cn[nH]c4n3)cc2)c1,CCOCCOCCOCCOCC=O,PEG,15,5,12,1145.347,No,,,,31461270,DAT6,No,,Reviewed,Q96BR1,No,No,No,No,48,270.88
490,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCOCCOCCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4cn[nH]c4n3)cc2)c1,Active,No,HEK293,4.67184000000001,,"Ella Livnah, Yangwode Jing",,63 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,19,5,,,Sanofi 308-R,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4cn[nH]c4n3)cc2)c1,CCOCCOCCOCCOCCOCC=O,PEG,18,6,15,1189.4,No,,,,31461270,DAT7,No,,Reviewed,Q96BR1,No,No,No,No,48,280.11
491,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCCCCCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4cn[nH]c4n3)cc2)c1,Active,Yes,"HEK293, CAMA-1, ZR-75-1",6.199040000000008,,"Ella Livnah, Yangwode Jing",< 100 nM,81 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,17,5,,,Sanofi 308-R,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4cn[nH]c4n3)cc2)c1,CCCCCCOCCOCCOCC=O,PEG,16,4,13,1157.402,No,,,,31461270,"DAT8, SGK3-PROTAC1",Yes,,Reviewed,Q96BR1,Yes,No,No,No,"2,48",261.65000000000003
492,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCCCCCOCCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4cn[nH]c4n3)cc2)c1,Active,No,HEK293,6.215640000000009,,"Ella Livnah, Yangwode Jing",,88 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,18,5,,,Sanofi 308-R,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4cn[nH]c4n3)cc2)c1,CCCCCCOCCOCCOCCOCC=O,PEG,19,5,16,1201.4550000000002,No,,,,31461270,DAT9,No,,Reviewed,Q96BR1,No,No,No,No,48,270.88
493,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCCCCCOCCCCCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4cn[nH]c4n3)cc2)c1,Active,No,HEK293,7.742840000000009,,"Ella Livnah, Yangwode Jing",,91 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,16,5,,,Sanofi 308-R,Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4cn[nH]c4n3)cc2)c1,CCCCCCOCCCCCCOCC=O,non-PEG polyether,17,3,14,1169.4570000000003,No,,,,31461270,DAT10,No,,Reviewed,Q96BR1,No,No,No,No,48,252.42000000000002
494,COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCCCCCOCCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4c(C)n[nH]c4n3)cc2)c1,Active,No,HEK293,6.73854000000001,,"Ella Livnah, Yangwode Jing",,71 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,19,5,,,Sanofi 290-R,COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4c(C)n[nH]c4n3)cc2)c1,CCCCCCOCCOCCOCCOCC=O,PEG,19,5,16,1247.9359999999997,No,,,,31461270,DAT11,No,,Reviewed,Q96BR1,No,No,No,No,48,280.11
495,COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCCCCCOCCCCCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4cn[nH]c4n3)cc2)c1,Active,No,HEK293,7.957320000000008,,"Ella Livnah, Yangwode Jing",,71 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,17,5,,,Sanofi 290-R,COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CNCCO4)c4c(C)n[nH]c4n3)cc2)c1,CCCCCCOCCCCCCOCC=O,non-PEG polyether,17,3,14,1201.911,No,,,,31461270,DAT12,No,,Reviewed,Q96BR1,No,No,No,No,48,261.65000000000003
496,O=C1CCC(N2C(=O)c3cccc(NCCOCCOCc4cn(CCCC(=O)N5CCN(CC#Cc6ccc(OCCCc7sc(N8CCc9cccc(C(=O)Nc%10nc%11ccccc%11s%10)c9C8)nc7C(=O)O)c(F)c6)CC5)nn4)c3C2=O)C(=O)N1,Active,Yes,MOLT4,6.030800000000005,"Selective BCLXL degradation: only in MOLT4 cells, not platelets",Paul Gehrtz,50 nM,85 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,20,4,0.005 nM,0.009 nM,A-1155463,CN(C)CC#Cc1ccc(OCCCc2sc(N3CCc4cccc(C(=O)Nc5nc6ccccc6s5)c4C3)nc2C(=O)O)c(F)c1,CCOCCOCc1cn(CCCC(=O)N(C)C)nn1,non-PEG polyether,20,7,10,1221.364,No,,4QVX,3CQ,31754664,XZ424,No,,Reviewed,Q07817,Yes,No,No,Yes,16,272.94999999999993
497,COc1cc(/C=C(\C#N)C(=O)NCCN[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Active,No,MDA-MB-231,7.049400000000009,DCmax was measured in 100nM,Amit Shraga,,50 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,10,4,5.67 nM,7.33 nM,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CC,Alkane,2,0,0,900.9430000000002,No,,3K6P,5FB,31097997,6a,No,,Reviewed,P62508,No,No,No,No,4,165.91
498,COc1cc(/C=C(\C#N)C(=O)NCCCN[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Active,No,MDA-MB-231,7.4395000000000095,DCmax was measured in 100nM,Amit Shraga,,85 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,10,4,5.67 nM,6.33 nM,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCC,Alkane,3,0,0,914.9700000000001,No,,3K6P,5FB,31097997,6b,No,,Reviewed,P62508,No,No,No,No,4,165.91
499,COc1cc(/C=C(\C#N)C(=O)NCCCCN[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Active,Yes,MDA-MB-231,7.829600000000012,"selective towards ERRa (tested also against ERRb, ERRg). DCmax was measured in 100nM",Amit Shraga,,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,10,4,5.67 nM,12.67 nM,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCCC,Alkane,4,0,1,928.9970000000002,No,,3K6P,5FB,31097997,6c,No,,Reviewed,P62508,Yes,Yes,Yes,Yes,4,165.91
500,COc1cc(/C=C(\C#N)C(=O)NCCCCCN[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Active,No,MDA-MB-231,8.21970000000001,DCmax was measured in 100nM,Amit Shraga,,78 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,10,4,5.67 nM,5.67 nM,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCCCC,Alkane,5,0,2,943.0240000000001,No,,3K6P,5FB,31097997,6d,No,,Reviewed,P62508,No,No,No,No,4,165.91
501,COc1cc(/C=C(\C#N)C(=O)NCCCCCCN[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Active,No,MDA-MB-231,8.609800000000007,DCmax was measured in 100nM,Amit Shraga,,71 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,10,4,5.67 nM,12.33 nM,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCCCCC,Alkane,6,0,3,957.051,No,,3K6P,5FB,31097997,6e,No,,Reviewed,P62508,No,No,No,No,4,165.91
502,COc1cc(/C=C(\C#N)C(=O)NCCCCCCCN[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Active,No,MDA-MB-231,8.999900000000004,DCmax was measured in 100nM,Amit Shraga,,9 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,10,4,5.67 nM,7.67 nM,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCCCCCC,Alkane,7,0,4,971.0780000000001,No,,3K6P,5FB,31097997,6f,No,,Reviewed,P62508,No,No,No,No,4,165.91
503,COc1cc(/C=C(\C#N)C(=O)NCCOCN[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Active,No,MDA-MB-231,7.023500000000009,DCmax was measured in 100nM,Amit Shraga,,92 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,11,4,5.67 nM,11.33 nM,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCOC,PEG,4,1,1,930.969,No,,3K6P,5FB,31097997,6g,No,,Reviewed,P62508,No,No,No,No,4,175.13999999999996
504,COc1cc(/C=C(\C#N)C(=O)NCCOCCN[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Active,No,MDA-MB-231,7.06600000000001,DCmax was measured in 100nM,Amit Shraga,,89 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,11,4,5.67 nM,9.33 nM,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCOCC,PEG,5,1,2,944.9960000000001,No,,3K6P,5FB,31097997,6h,No,,Reviewed,P62508,No,No,No,No,4,175.13999999999996
505,COc1cc(/C=C(\C#N)C(=O)NCCOCCOCCN[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Active,No,MDA-MB-231,7.082600000000011,DCmax was measured in 100 nM,Amit Shraga,,19 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,4,5.67 nM,5.33 nM,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCOCCOCC,PEG,8,2,5,989.0490000000001,No,,3K6P,5FB,31097997,6i,No,,Reviewed,P62508,No,No,No,No,4,184.36999999999998
506,COc1cc(/C=C(\C#N)C(=O)NCCOCCOCCOCCN[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Active,No,MDA-MB-231,7.099200000000011,DCmax was measured in 100 nM,Amit Shraga,,10 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,13,4,5.67 nM,7.00 nM,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCOCCOCCOCC,PEG,11,3,8,1033.1019999999999,No,,3K6P,5FB,31097997,6j,No,,Reviewed,P62508,No,No,No,No,4,193.6
507,COc1cc(/C=C(\C#N)C(=O)NCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Inactive,No,MDA-MB-231,5.628480000000005,,Amit Shraga,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,9,3,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCCC,Alkane,4,0,1,771.6710000000004,No,,3K6P,5FB,31097997,7a,No,,Reviewed,P62508,No,No,No,No,,166.92999999999998
508,COc1cc(/C=C(\C#N)C(=O)NCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Inactive,No,MDA-MB-231,6.408680000000006,,Amit Shraga,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,9,3,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCCCCC,Alkane,6,0,3,799.7250000000003,No,,3K6P,5FB,31097997,7b,No,,Reviewed,P62508,No,No,No,No,,166.92999999999998
509,COc1cc(/C=C(\C#N)C(=O)NCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Inactive,No,MDA-MB-231,4.881480000000003,,Amit Shraga,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,11,3,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCOCCOCC,PEG,8,2,5,831.7230000000003,No,,3K6P,5FB,31097997,7c,No,,Reviewed,P62508,No,No,No,No,,185.39
510,COc1cc(/C=C(\C#N)C(=O)NCCOCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Inactive,No,MDA-MB-231,4.898080000000004,,Amit Shraga,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,3,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCOCCOCCOCC,PEG,11,3,8,875.7760000000004,No,,3K6P,5FB,31097997,7d,No,,Reviewed,P62508,No,No,No,No,,194.61999999999998
511,COc1cc(/C=C(\C#N)C(=O)NCCCOCCCCOCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Inactive,No,MDA-MB-231,6.4418800000000065,,Amit Shraga,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,11,3,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCCOCCCCOCCC,PEG,12,2,9,887.8310000000005,No,,3K6P,5FB,31097997,7e,No,,Reviewed,P62508,No,No,No,No,,185.39
512,COc1cc(/C=C(\C#N)C(=O)NCCCOCCOCCOCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Inactive,No,MDA-MB-231,5.678280000000005,,Amit Shraga,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,3,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCCOCCOCCOCCC,PEG,13,3,10,903.8300000000004,No,,3K6P,5FB,31097997,7f,No,,Reviewed,P62508,No,No,No,No,,194.61999999999998
513,COc1cc(/C=C(\C#N)C(=O)NCCOCCOCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Inactive,No,MDA-MB-231,4.914680000000005,,Amit Shraga,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,3,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCOCCOCCOCCOCC,PEG,14,4,11,919.8290000000003,No,,3K6P,5FB,31097997,7g,No,,Reviewed,P62508,No,No,No,No,,203.85
514,COc1cc(/C=C(\C#N)C(=O)NCCOCCOCCOCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Inactive,No,MDA-MB-231,4.931280000000007,,Amit Shraga,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,3,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCOCCOCCOCCOCCOCC,PEG,17,5,14,963.8820000000003,No,,3K6P,5FB,31097997,7h,No,,Reviewed,P62508,No,No,No,No,,213.07999999999998
515,COc1cc(/C=C(\C#N)C(=O)NCCCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](O)[C@H](N)Cc2ccccc2)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Inactive,No,MDA-MB-231,5.693180000000007,,Amit Shraga,,,CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O,Iap,,,other,8,5,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCCCN,Alkane,5,1,2,805.8170000000003,No,,3K6P,5FB,31097997,8a,No,,Reviewed,P62508,No,No,No,No,,175.79999999999998
516,COc1cc(/C=C(\C#N)C(=O)NCCOCCOCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](O)[C@H](N)Cc2ccccc2)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,Inactive,No,MDA-MB-231,4.946180000000005,,Amit Shraga,,,CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O,Iap,,,other,10,5,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCOCCOCCN,PEG,9,3,6,865.8690000000004,No,,3K6P,5FB,31097997,8b,No,,Reviewed,P62508,No,No,No,No,,194.26
517,COc1ccc(C2=N[C@@H](c3ccc(Cl)cc3)[C@@H](c3ccc(Cl)cc3)N2C(=O)N2CCN(CC(=O)CCNC(=O)/C(C#N)=C/c3ccc(OCc4ccc(C(F)(F)F)cc4C(F)(F)F)c(OC)c3)C(=O)C2)c(OC(C)C)c1,Inactive,No,MDA-MB-231,10.905979999999994,,Amit Shraga,,,COc1ccc(C2=N[C@H](c3ccc(Cl)cc3)[C@H](c3ccc(Cl)cc3)N2C(=O)N2CCNC(=O)C2)c(OC(C)C)c1,Mdm2,,,other,10,1,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCC(C)=O,Alkane,5,1,1,1093.9059999999997,No,,3K6P,5FB,31097997,9a,No,,Reviewed,P62508,No,No,No,No,,163.1
518,COc1ccc(C2=N[C@@H](c3ccc(Cl)cc3)[C@@H](c3ccc(Cl)cc3)N2C(=O)N2CCN(CC(=O)NCCCCCNC(=O)/C(C#N)=C/c3ccc(OCc4ccc(C(F)(F)F)cc4C(F)(F)F)c(OC)c3)C(=O)C2)c(OC(C)C)c1,Inactive,No,MDA-MB-231,11.233279999999993,,Amit Shraga,,,COc1ccc(C2=N[C@H](c3ccc(Cl)cc3)[C@H](c3ccc(Cl)cc3)N2C(=O)N2CCNC(=O)C2)c(OC(C)C)c1,Mdm2,,,other,10,2,,,XCT790 4a with thiadiazoloacylamide removed,COc1cc(/C=C(\C#N)C(N)=O)ccc1OCc1ccc(C(F)(F)F)cc1C(F)(F)F,CCCCCNC(C)=O,Alkane,9,2,4,1151.0019999999995,No,,3K6P,5FB,31097997,9b,No,,Reviewed,P62508,No,No,No,No,,175.12999999999997
519,CCN(CCOCCOCCOCC#Cc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Inactive,No,MCF-7,5.773700000000007,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM,Amit Shraga,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,3,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,C#CCOCCOCCO,PEG,10,3,6,845.9710000000003,No,,1ERR,RAL,30990042,12,No,,Reviewed,P03372,No,No,No,No,4,164.17
520,CCN(CCCCCCC#Cc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Inactive,No,MCF-7,7.67440000000001,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,9,3,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,C#CCCC,Alkane,5,0,1,783.9470000000003,No,,1ERR,RAL,30990042,13,No,,Reviewed,P03372,No,No,No,No,4,136.48000000000002
521,CCN(CCOCCOCCOCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF-7,8.153120000000012,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 99.4 %).,Amit Shraga,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,15,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,O=CCCOCCOCCO,PEG,11,4,8,1064.3369999999998,No,,1ERR,RAL,30990042,14,No,,Reviewed,P03372,No,No,No,No,4,209.31999999999996
522,CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF-7,10.053819999999996,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 99.6 %).,Amit Shraga,,79 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,1002.3129999999999,No,,1ERR,RAL,30990042,15,No,,Reviewed,P03372,No,No,No,No,4,181.63
523,CCN(CCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Inactive,No,MCF-7,8.493420000000006,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,37 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,C=O,Alkane,2,1,0,946.2049999999999,No,,1ERR,RAL,30990042,16,No,,Reviewed,P03372,No,No,No,No,4,181.63
524,CCN(CCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Inactive,No,MCF-7,8.883520000000003,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,10 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CC=O,Alkane,3,1,0,960.2319999999999,No,,1ERR,RAL,30990042,17,No,,Reviewed,P03372,No,No,No,No,4,181.63
525,CCN(CCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF-7,9.273620000000001,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,74 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCC=O,Alkane,4,1,1,974.2589999999999,No,,1ERR,RAL,30990042,18,No,,Reviewed,P03372,No,No,No,No,4,181.63
526,CCN(CCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF-7,9.663719999999998,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,68 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCC=O,Alkane,5,1,2,988.286,No,,1ERR,RAL,30990042,19,No,,Reviewed,P03372,No,No,No,No,4,181.63
527,CCN(CCCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF-7,10.443919999999993,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,77 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCCC=O,Alkane,7,1,4,1016.3399999999998,No,,1ERR,RAL,30990042,20,No,,Reviewed,P03372,No,No,No,No,4,181.63
528,CCN(CCCCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF-7,10.83401999999999,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,75 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCCCC=O,Alkane,8,1,5,1030.367,No,,1ERR,RAL,30990042,21,No,,Reviewed,P03372,No,No,No,No,4,181.63
529,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(C)CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C(C)(C)C)cc1,Inactive,No,MCF-7,9.663720000000001,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 0 %).,Amit Shraga,,73 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCC=O,Alkane,5,1,2,988.2860000000001,No,,1ERR,RAL,30990042,22,No,,Reviewed,P03372,No,No,No,No,4,181.62999999999997
530,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C(C)C)C(C)(C)C)cc1,Active,No,MCF-7,10.442319999999995,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).,Amit Shraga,,72 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,1016.34,No,,1ERR,RAL,30990042,23,No,,Reviewed,P03372,No,No,No,No,4,181.62999999999997
531,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C(C)(C)C)C(C)(C)C)cc1,Active,No,MCF-7,10.832419999999992,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).,Amit Shraga,,79 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,1030.367,No,,1ERR,RAL,30990042,24,No,,Reviewed,P03372,No,No,No,No,4,181.62999999999997
532,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C2CC2)C(C)(C)C)cc1,Active,No,MCF-7,10.196319999999996,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).,Amit Shraga,,80 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,1014.324,No,,1ERR,RAL,30990042,25,No,,Reviewed,P03372,No,No,No,No,4,181.62999999999997
533,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C2CCC2)C(C)(C)C)cc1,Active,No,MCF-7,10.586419999999993,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).,Amit Shraga,,85 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,1028.3509999999999,No,,1ERR,RAL,30990042,26,No,,Reviewed,P03372,No,No,No,No,4,181.62999999999997
534,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C2CCCC2)C(C)(C)C)cc1,Active,No,MCF-7,10.976519999999988,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).,Amit Shraga,,25 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,1042.378,No,,1ERR,RAL,30990042,27,No,,Reviewed,P03372,No,No,No,No,4,181.62999999999997
535,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C2CCCCC2)C(C)(C)C)cc1,Active,No,MCF-7,11.366619999999987,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).,Amit Shraga,,32 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,1056.4049999999997,No,,1ERR,RAL,30990042,28,No,,Reviewed,P03372,No,No,No,No,4,181.62999999999997
536,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)CC2CCC2)C(C)(C)C)cc1,Active,No,MCF-7,10.834019999999992,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).,Amit Shraga,,24 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,1042.378,No,,1ERR,RAL,30990042,29,No,,Reviewed,P03372,No,No,No,No,4,181.62999999999997
537,CCN(CCOCCOCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF-7,8.136520000000012,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 97.6 %).,Amit Shraga,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,O=CCCOCCO,PEG,8,3,5,1020.2839999999998,No,,1ERR,RAL,30990042,30,No,,Reviewed,P03372,No,No,No,No,4,200.08999999999995
538,CCN(CCOCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF-7,7.746420000000012,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99.6 %).,Amit Shraga,,6 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,O=CCOCCO,PEG,7,3,4,1006.2569999999998,No,,1ERR,RAL,30990042,31,No,,Reviewed,P03372,No,No,No,No,4,200.08999999999995
539,CCN(CCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,Yes,MCF-7,8.900120000000005,"EC50 of PROTAC was measured in MCF7 cell line. DC50 is 0.17 nM MCF-7, 0.43 T47D. EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 5 nM > 95 %).",Amit Shraga,< 0.43 nM,92 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,13,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCOCC=O,Alkane,6,2,3,1004.2849999999999,No,,1ERR,RAL,30990042,32 / ERD-308,No,,Reviewed,P03372,No,Yes,No,Yes,"1,3,4",190.85999999999999
540,CCN(CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1)CCC1CCN(CCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1,Inactive,No,MCF-7,9.595520000000002,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,13,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCN(CC)CCCC=O,Other,10,2,6,1057.3929999999996,No,,1ERR,RAL,30990042,33,No,,Reviewed,P03372,No,No,No,No,4,184.87
541,CCN(CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1)CCN1CCN(CCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1,Active,No,MCF-7,8.11102000000001,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 50 %).,Amit Shraga,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,O=CCCCN1CCNCC1,Other,11,3,4,1058.3809999999996,No,,1ERR,RAL,30990042,34,No,,Reviewed,P03372,No,No,No,No,4,188.10999999999996
542,CCN(CCCC#Cc1cnn(CCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)c1)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF-7,9.131720000000003,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 99.5 %).,Amit Shraga,,30 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,C#Cc1cnn(CCC=O)c1,Other,11,3,3,1064.3439999999998,No,,1ERR,RAL,30990042,35,No,,Reviewed,P03372,No,No,No,No,4,199.44999999999996
543,CCN(CCC#Cc1cnn(CC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)c1)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF-7,8.35152000000001,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 55 %).,Amit Shraga,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,Cc1cnn(CC=O)c1,Other,9,3,2,1036.29,No,,1ERR,RAL,30990042,36,No,,Reviewed,P03372,No,No,No,No,4,199.44999999999996
544,CCN(CCCCc1cnn(CC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)c1)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Active,No,MCF-7,8.932620000000005,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 80 %).,Amit Shraga,,1 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,Cc1cnn(CC=O)c1,Other,9,3,2,1040.322,No,,1ERR,RAL,30990042,37,No,,Reviewed,P03372,No,No,No,No,4,199.44999999999996
545,CC/C(=C(\c1ccc(O)cc1)c1ccc(OCCN(CC)CCCCCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)cc1)c1ccccc1,Active,No,MCF-7,10.604619999999995,DCmax was measured in 1 nM (at 76 nM 80 %).,Amit Shraga,,45 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,9,4,,,tamoxifen,CC[N]CCOc1ccc(/C(=C(/CC)c2ccccc2)c2ccc(O)cc2)cc1,CCCCCC=O,Alkane,7,1,4,956.307,No,,,,30990042,38,No,,Reviewed,P03372,No,No,No,No,4,144.32999999999998
546,CC/C(=C(\c1ccccc1)c1ccc(OCCN(CC)CCCCCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)cc1)c1ccccc1,Active,No,MCF-7,10.899019999999993,DCmax was measured in 1 nM (at 10 nM 3 %).,Amit Shraga,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,8,3,,,4-hydroxytamoxifen,CC[N]CCOc1ccc(/C(=C(/CC)c2ccccc2)c2ccccc2)cc1,CCCCCC=O,Alkane,7,1,4,940.308,No,,,,30990042,39,No,,Reviewed,P03372,No,No,No,No,4,124.10000000000001
547,CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(Cn2c(-c3ccc(O)cc3)c(C)c3cc(O)ccc32)cc1,Active,No,MCF-7,9.919539999999998,DCmax was measured in 1 nM (at 90 nM 3 %).,Amit Shraga,,26 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,11,5,,,bazedoxifene,CC[N]CCOc1ccc(Cn2c(-c3ccc(O)cc3)c(C)c3cc(O)ccc32)cc1,CCCCCC=O,Alkane,7,1,4,985.3049999999997,No,,,,30990042,40,No,,Reviewed,P03372,No,No,No,No,4,169.49
548,CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc([C@@H]2c3ccc(O)cc3CC[C@@H]2c2ccccc2)cc1,Active,No,MCF-7,10.097419999999998,DCmax was measured in 1 nM (at 10 nM 95 %).,Amit Shraga,,26 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,9,4,,,lasofoxifene,CC[N]CCOc1ccc([C@@H]2c3ccc(O)cc3CC[C@@H]2c2ccccc2)cc1,CCCCCC=O,Alkane,7,1,4,956.3069999999998,No,,,,30990042,41,No,,Reviewed,P03372,No,No,No,No,4,144.33
549,CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Inactive,No,MCF-7,9.49282,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 29 %).,Amit Shraga,,21 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,988.286,No,,1ERR,RAL,30990042,42,No,,Reviewed,P03372,No,No,No,No,4,181.63
550,CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(Cl)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Inactive,No,MCF-7,9.275300000000001,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,1 %,C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](N)C(C)(C)C)c1ccc(Cl)cc1,VHL,,,other,10,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,939.616,No,,1ERR,RAL,30990042,43,No,,Reviewed,P03372,No,No,No,No,4,168.74
551,CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(C#N)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Inactive,No,MCF-7,8.493580000000007,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,,C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](N)C(C)(C)C)c1ccc(C#N)cc1,VHL,,,other,11,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,930.181,No,,1ERR,RAL,30990042,44,No,,Reviewed,P03372,No,No,No,No,4,192.52999999999997
552,C#Cc1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CC)CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C(C)(C)C)cc1,Active,No,MCF-7,8.603200000000006,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 76 %).,Amit Shraga,,10 %,C#Cc1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,10,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,929.1930000000003,No,,1ERR,RAL,30990042,45,No,,Reviewed,P03372,No,No,No,No,4,168.73999999999998
553,CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(C2CC2)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Inactive,No,MCF-7,9.499300000000002,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,,C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](N)C(C)(C)C)c1ccc(C2CC2)cc1,VHL,,,other,10,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,945.236,No,,1ERR,RAL,30990042,46,No,,Reviewed,P03372,No,No,No,No,4,168.74
554,CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(C(C)C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Inactive,No,MCF-7,9.7453,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,,CC(C)c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,10,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,947.252,No,,1ERR,RAL,30990042,47,No,,Reviewed,P03372,No,No,No,No,4,168.74
555,CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(C(C)(C)C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1,Inactive,No,MCF-7,9.9194,EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.,Amit Shraga,,,C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](N)C(C)(C)C)c1ccc(C(C)(C)C)cc1,VHL,,,other,10,5,,,raloxifene,O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12,CCCCC=O,Alkane,6,1,3,961.279,No,,1ERR,RAL,30990042,48,No,,Reviewed,P03372,No,No,No,No,4,168.74
556,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(C(=O)NCCCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,MiaPaCa2,3.681320000000002,,Amit Shraga,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,14,4,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCCCNC=O,Alkane,7,2,4,817.9079999999996,No,,5L2I,LQQ,30935795,2,No,,Reviewed,Q00534,No,No,No,No,"4,24",220.93
557,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(C(=O)NCCCCCCCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,MiaPaCa2,5.2417200000000035,,Amit Shraga,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,14,4,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCCCCCCCNC=O,Alkane,11,2,8,874.0159999999996,No,,5L2I,LQQ,30935795,3,No,,Reviewed,Q00534,No,No,No,No,"4,24",220.93
558,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CCCCCC(=O)Nc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,MiaPaCa2,4.278520000000002,,Amit Shraga,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,14,3,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCCCCC=O,Alkane,7,1,4,816.9199999999997,No,,5L2I,LQQ,30935795,4,No,,Reviewed,Q00534,No,No,No,No,"4,24",208.89999999999998
559,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CCOCCOCCONc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,MiaPaCa2,3.156320000000002,,Amit Shraga,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,17,3,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCCO,PEG,9,3,6,850.9339999999996,No,,5L2I,LQQ,30935795,5,No,,Reviewed,Q00534,No,No,No,No,"4,24",219.51999999999998
560,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CC(=O)NCCCOCCOCCOCCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,Yes,"MiaPaCa2, HPNE",3.1377200000000034,,Amit Shraga,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,18,4,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCCOCCOCCOCCCNC(C)=O,PEG,17,5,12,964.0939999999996,No,,5L2I,LQQ,30935795,6,No,,Reviewed,Q00534,No,Yes,No,Yes,"4,24",248.62
561,COc1cc(OC)c(/C=C/S(=O)(=O)Cc2ccc(OC)c(CC(=O)NCC(=O)Nc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)c2)c(OC)c1,Active,Yes,"MCF-7, MDA-MB-231, HepG2, LO2, B16",2.0053,Dmax is measured in 10uM. EC50 of PROTAC is MCF-7: 2.70 ± 0.19 MDA-MB-231: 21.21 ± 1.95 HepG2: 18.70 ± 1.65 LO2: 41.11 ± 3.70 B16: 22.68 ± 2.03 uM. EC50 of ligand is MCF-7: 4.17 ± 0.31 MDA-MB-231: 21.33 ± 1.96 HepG2: 10.59 ± 0.94 LO2: 35.57 ± 2.81 B16: 14.49 ± 1.28 uM.,Amit Shraga,~ 0.5 uM,81 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,3,,,RGS,CNc1cc(CS(=O)(=O)/C=C/c2c(OC)cc(OC)cc2OC)ccc1OC,CC(=O)NCC=O,Alkane,7,3,2,748.767,No,,,,30901674,2,No,,Reviewed,P15056,No,Yes,No,Yes,"24,72",212.80999999999997
562,CN1C(=O)CCc2cc3cc(c21)OCCOC[C@H]1CN(C(=O)CCC(=O)NCCCOCCOCCOc2cccc4c2C(=O)N(C2CCC(=O)NC2=O)C4=O)CCN1c1ncc(Cl)c(n1)N3,Active,Yes,"Karpas 422,ULA, SUDHL4, OCI-Ly1, Ramos",2.0087000000000046,"half the paper develops the ligand and checks its selectivity. Dmax is 76% Karpas 422, 59% ULA, 84% SUDHL4, 82% OCI-Ly1, 82% Ramos.",Amit Shraga,~ 1 uM,> 76 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,16,3,0.063 uM,0.12 uM,14,CC(C)CCC(=O)N1CCN2c3ncc(Cl)c(n3)Nc3cc4c(c(c3)OCCOC[C@H]2C1)N(C)C(=O)CC4,NCCCOCCOCCO,PEG,11,4,8,946.4149999999997,No,,6EW8,C0Q,30335946,15,Yes,,Reviewed,P41182,No,Yes,No,Yes,4,240.47
563,COc1cc(N2CCN(C(=O)CCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,Active,No,SR,8.104020000000009,"EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).","Daniel Zaidman, Yangwode Jing",> 50 uM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,Brigatinib,COc1cc(N2CCC(N3CCN(C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,NC(=O)CCCCCCC=O,Alkane,11,3,7,1055.6839999999995,No,,6MX8,6GY,32179332,compound 8,No,,Reviewed,Q9UM73,No,No,No,No,,211.32000000000005
564,COc1cc(N2CCN(C(=O)CCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,Active,No,SR,8.494120000000006,"EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).","Daniel Zaidman, Yangwode Jing",15 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,Brigatinib,COc1cc(N2CCC(N3CCN(C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,NC(=O)CCCCCCCC=O,Alkane,12,3,8,1069.7109999999996,No,,6MX8,6GY,32179332,compound 9,No,,Reviewed,Q9UM73,No,No,No,No,,211.32000000000005
565,COc1cc(N2CCN(C(=O)CCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,Active,No,SR,8.884220000000003,"EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).","Daniel Zaidman, Yangwode Jing",> 50 uM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,Brigatinib,COc1cc(N2CCC(N3CCN(C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,NC(=O)CCCCCCCCC=O,Alkane,13,3,9,1083.7379999999996,No,,6MX8,6GY,32179332,compound 10,No,,Reviewed,Q9UM73,No,No,No,No,,211.32000000000005
566,COc1cc(N2CCC(NC(=O)CCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,Active,No,SR,8.540420000000006,"EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).","Daniel Zaidman, Yangwode Jing",9.1 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,6,,,Brigatinib,COc1cc(N2CCC(N3CCN(C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,CCCCCC=O,Alkane,7,1,4,1069.7109999999996,No,,6MX8,6GY,32179332,compound 15,No,,Reviewed,Q9UM73,No,No,No,No,,220.11
567,COc1cc(N2CCC(NC(=O)CCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,Active,No,SR,8.930520000000005,"EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).","Daniel Zaidman, Yangwode Jing",20.9 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,6,,,Brigatinib,COc1cc(N2CCC(N3CCN(C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,CCCCCCC=O,Alkane,8,1,5,1083.7379999999996,No,,6MX8,6GY,32179332,compound 16,No,,Reviewed,Q9UM73,No,No,No,No,,220.11
568,COc1cc(N2CCC(NC(=O)CCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,Active,No,SR,9.320620000000003,"EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).","Daniel Zaidman, Yangwode Jing",7.2 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,6,,,Brigatinib,COc1cc(N2CCC(N3CCN(C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,CCCCCCCC=O,Alkane,9,1,6,1097.7649999999994,No,,6MX8,6GY,32179332,compound 17,No,,Reviewed,Q9UM73,No,No,No,No,,220.11
569,COc1cc(N2CCC(N3CCN(C(=O)CCCCCCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,Active,No,SR,8.568420000000007,"EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).","Daniel Zaidman, Yangwode Jing",11.4 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,,,Brigatinib,COc1cc(N2CCC(N3CCN(C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,CCCCCCC=O,Alkane,8,1,5,1138.817999999999,No,,6MX8,6GY,32179332,compound 23,No,,Reviewed,Q9UM73,No,No,No,No,,214.56
570,COc1cc(N2CCC(N3CCN(C(=O)CCCCCCCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,Active,No,SR,8.958520000000004,"EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).","Daniel Zaidman, Yangwode Jing",25.1 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,,,Brigatinib,COc1cc(N2CCC(N3CCN(C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,CCCCCCCC=O,Alkane,9,1,6,1152.8449999999991,No,,6MX8,6GY,32179332,compound 24,No,,Reviewed,Q9UM73,No,No,No,No,,214.56
571,COc1cc(N2CCC(N3CCN(C(=O)CCCCCCCCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,Active,No,SR,9.348620000000002,"EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).","Daniel Zaidman, Yangwode Jing",7.5 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,5,,,Brigatinib,COc1cc(N2CCC(N3CCN(C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,CCCCCCCCC=O,Alkane,10,1,7,1166.8719999999992,No,,6MX8,6GY,32179332,compound 25,No,,Reviewed,Q9UM73,No,No,No,No,,214.56
572,COc1cc(N2CCC(NC(=O)CCCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,Active,Yes,"SR, H2228, NCI–H69, NCI–H1688, NCI–H446",9.710720000000004,"EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells). EC50 of PROTAC is 1.7 ± 1 nM (SF cells), 46nM ± 16 nM (H2228 cells).","Daniel Zaidman, Yangwode Jing",7.0 nM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,6,,,Brigatinib,COc1cc(N2CCC(N3CCN(C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1,CCCCCCCCC=O,Alkane,10,1,7,1111.7919999999992,No,,6MX8,6GY,32179332,compound 18 (SIAIS117),No,,Reviewed,Q9UM73,Yes,No,No,Yes,,220.11
573,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOc2ccc(-c3ccc4ncnc(Nc5ccc(OCc6cccc(F)c6)c(Cl)c5)c4c3)cc2)C(C)(C)C)cc1,Active,Yes,"OVCAR8 (WT EGFR), HeLa (EGFR Exon 20 Ins), SKBr3 (HER2)",9.064920000000003,DC50 is for WT EGFR. DC50 for EGFR Exon 20 Ins is 736.2 nM. DMAX is for WT EGFR. DMAX for EGFR Exon 20 Ins is 68.8 %.,Barr Tivon,39.2 nM,97.6 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,13,4,,,lapatinib-based,CS(=O)(=O)CCNCc1ccc(-c2ccc3ncnc(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)c3c2)o1,CCOCCOCC=O,PEG,9,3,6,1030.62,No,,1XKK,FMM,29129716,compound 1,No,,Reviewed,"P00533, P04626",Yes,No,No,No,24,186.35999999999996
574,COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1OCCCCCOCCOCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C,Active,No,"HCC827 (Exon 19 del), H3255 (L858R)",7.387920000000008,DC50 is for EGFR (Exon 19 del). DC50 for EGFR (L858R) 22.3 nM. DMAX is for EGFR (Exon 19 del). DMAX for EGFR (L858R) 96.6 %.,Barr Tivon,11.7 nM,98.9 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,13,4,,,gefitinib-based,COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1OCCCN1CCOCC1,CCOCCOCCC=O,PEG,10,3,7,934.532,No,,4WKQ,IRE,29129716,compound 3,No,,Reviewed,P00533,No,No,No,No,24,186.36
575,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCOCCCCOCCCCOc2cc3ncnc(Nc4ccc(F)c(Cl)c4)c3cc2NC(=O)/C=C/CN(C)C)C(C)(C)C)cc1,Active,No,H1975,8.996020000000001,,Barr Tivon,215.8 nM,79.1 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,afatinib-based,CN(C)C/C=C/C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1OC1CCOC1,COCCCCOCCCCCC=O,non-PEG polyether,14,3,11,1086.7729999999992,No,,4G5J,0WN,29129716,compound 4,No,,Reviewed,P00533,No,No,No,No,24,209.46999999999997
576,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOc2ccc(-c3ccc4ncnc(Nc5ccc(OCc6cccc(F)c6)c(Cl)c5)c4c3)cc2)C(C)(C)C)cc1,Active,No,OVCAR8,9.081520000000003,,Barr Tivon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,4,,,lapatinib-based,CS(=O)(=O)CCNCc1ccc(-c2ccc3ncnc(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)c3c2)o1,CCOCCOCCOCC=O,PEG,12,4,9,1074.6729999999998,No,,1XKK,FMM,29129716,compound 5,No,,Reviewed,P00533,Yes,No,No,No,24,195.58999999999997
577,COc1cc2c(Oc3ccc(N(C(=O)C4(C(N)=O)CC4)c4ccc(F)cc4)cc3F)ccnc2cc1OCCCOCCCOCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C,Active,Yes,"MDA-MB-231, GTL16",8.06742000000001,,Barr Tivon,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,4,,,foretinib-based,COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1OCCCN1CCOCC1,O=CCCOCCCO,non-PEG polyether,9,3,6,1106.2589999999989,No,,6SD9,88Z,29129716,compound 7,No,,Reviewed,P08581,Yes,No,Yes,Yes,24,234.07
578,Cc1nnc2n1-c1sc(C#Cc3cnn(-c4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)c(Cc3ccccc3)c1COC2,Inactive,No,"RS4;11, MV4;11, MOLM-13,",3.2449200000000022,EC50 of ligand is 55.8-207 nM.,Daniel Zaidman,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,11,1,10.7 nM,,QCA276,Cc1nnc2n1-c1sc(C#Cc3cnn(C)c3)c(Cc3ccccc3)c1COC2,None,Other,0,0,0,643.6850000000003,"BRD2, BRD3",,,,30019901,26,No,,Reviewed,O60885,No,No,No,No,"3,24,96",141.30999999999997
579,Cc1nnc2n1-c1sc(C#Cc3cnn(COc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)c(Cc3ccccc3)c1COC2,Active,No,"RS4;11, MV4;11, MOLM-13,",3.292220000000002,EC50 of PROTAC is 19.7nM-311nM. EC50 of ligand is 55.8-207 nM.,Daniel Zaidman,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CO,12,1,10.7 nM,,QCA276,Cc1nnc2n1-c1sc(C#Cc3cnn(C)c3)c(Cc3ccccc3)c1COC2,O,PEG,1,1,0,673.7110000000001,"BRD2, BRD3",,,,30019901,27,No,,Reviewed,O60885,No,No,No,No,"3,24,96",150.54
580,Cc1nnc2n1-c1sc(C#Cc3cnn(CCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)c(Cc3ccccc3)c1COC2,Active,No,"RS4;11, MV4;11, MOLM-13,",3.367820000000002,EC50 of PROTAC is 0.379nM-2.23nM. EC50 of ligand is 55.8-207 nM.,Daniel Zaidman,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,12,2,10.7 nM,,QCA276,Cc1nnc2n1-c1sc(C#Cc3cnn(C)c3)c(Cc3ccccc3)c1COC2,CN,Alkane,2,1,0,686.754,"BRD2, BRD3",,,,30019901,28,No,,Reviewed,O60885,No,No,No,No,"3,24,96",153.33999999999997
581,Cc1nnc2n1-c1sc(C#Cc3cnn(CCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)c(Cc3ccccc3)c1COC2,Active,No,"RS4;11, MV4;11, MOLM-13,",3.757920000000002,EC50 of PROTAC is 0.038nM-0.56nM. EC50 of ligand is 55.8-207 nM.,Daniel Zaidman,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,12,2,10.7 nM,,QCA276,Cc1nnc2n1-c1sc(C#Cc3cnn(C)c3)c(Cc3ccccc3)c1COC2,CCN,Alkane,3,1,0,700.7810000000001,"BRD2, BRD3",,,,30019901,29,No,,Reviewed,O60885,No,No,No,No,"3,24,96",153.33999999999997
582,Cc1nnc2n1-c1sc(C#Cc3cnn(CCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)c(Cc3ccccc3)c1COC2,Active,No,"RS4;11, MV4;11, MOLM-13,",4.1480200000000025,EC50 of PROTAC is 0.02nM-0.19nM. EC50 of ligand is 55.8-207 nM.,Daniel Zaidman,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,12,2,10.7 nM,,QCA276,Cc1nnc2n1-c1sc(C#Cc3cnn(C)c3)c(Cc3ccccc3)c1COC2,CCCN,Alkane,4,1,1,714.808,"BRD2, BRD3",,,,30019901,30,No,,Reviewed,O60885,No,No,No,No,"3,24,96",153.33999999999997
583,Cc1nnc2n1-c1sc(C#Cc3cnn(CCCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)c(Cc3ccccc3)c1COC2,Active,No,"RS4;11, MV4;11, MOLM-13,",4.538120000000004,EC50 of PROTAC is 0.02nM-0.19nM. EC50 of ligand is 55.8-207 nM.,Daniel Zaidman,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,12,2,10.7 nM,,QCA276,Cc1nnc2n1-c1sc(C#Cc3cnn(C)c3)c(Cc3ccccc3)c1COC2,CCCCN,Alkane,5,1,2,728.835,"BRD2, BRD3",,,,30019901,31,No,,Reviewed,O60885,No,No,No,No,"3,24,96",153.33999999999997
584,Cc1nnc2n1-c1sc(C#Cc3cnn(CCCC#Cc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)c3)c(Cc3ccccc3)c1COC2,Active,Yes,"RS4;11, MV4;11, MOLM-13,",4.447420000000004,EC50 of PROTAC is 0.0083nM-0.062nM. EC50 of ligand is 55.8-207 nM.,Daniel Zaidman,< 0.5 nM,100 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,10,1,10.7 nM,,QCA276,Cc1nnc2n1-c1sc(C#Cc3cnn(C)c3)c(Cc3ccccc3)c1COC2,C#CCC,Other,4,0,0,695.8050000000001,"BRD2, BRD3",,,,30019901,35 (QCA570),No,,Reviewed,O60885,Yes,Yes,No,Yes,"3,24,96",124.24
585,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)COCCOCCOCCOCCN2CCN(C/C=C/C(=O)N3CCC[C@@H](n4nc(-c5ccc(-c6ccccc6)cc5)c5c(N)ncnc54)C3)CC2)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Inactive,No,THP-1,5.098700000000015,,Daniel Zaidman,,,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,other,17,5,,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,CN1CCN(CCOCCOCCOCCOCC=O)CC1,PEG,22,7,14,1222.547,No,,5P9J,"8E8",30807093,2,Yes,,Reviewed,Q06187,Yes,No,No,No,16,252.97000000000006
586,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)COCCOCCOCCOCCN2CCN(CCCC(=O)N3CCC[C@@H](n4nc(-c5ccc(-c6ccccc6)cc5)c5c(N)ncnc54)C3)CC2)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Active,Yes,THP-1,5.3227000000000135,,Daniel Zaidman,~ 200 nM,,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)N[C@@H]1CCCc2ccccc21)C1CCCCC1,Iap,,,other,17,5,,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,CCN1CCN(CCOCCOCCOCCOCC=O)CC1,PEG,23,7,15,1224.5629999999999,No,,5P9J,"8E8",30807093,3,Yes,,Reviewed,Q06187,Yes,No,No,No,16,252.97000000000006
587,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2[C@@H]1CCCN(C(=O)/C=C/CN2CCN(CCNC(=O)CCCCn3cc(COCCC(=O)Nc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)nn3)CC2)C1,Inactive,No,Ramos,4.089700000000003,covalent,Daniel Zaidman,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,18,4,,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,CN1CCN(CCNC(=O)CCCCn2cc(COCCC=O)nn2)CC1,Other,27,9,13,1076.2329999999995,CSK and LYN,,5P9J,"8E8",30807093,4,Yes,,Reviewed,Q06187,No,No,No,No,24,270.25999999999993
588,Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2[C@@H]1CCCN(C(=O)CCCNC(=O)CCCCn2cc(COCCC(=O)Nc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)nn2)C1,Active,No,Ramos,4.696100000000002,,Daniel Zaidman,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,4,,,Ibrutinib,C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1,CCNC(=O)CCCCn1cc(COCCC=O)nn1,Other,20,7,11,966.0729999999994,"CSK, LYN, and LAT2",,5P9J,"8E8",30807093,5,Yes,,Reviewed,Q06187,No,No,No,No,24,263.78
589,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCCOC(=O)NC(Nc2ncccn2)C(Cl)(Cl)Cl)C(C)(C)C)cc1,Active,Yes,"MCF-7, U2OS, MDA-MB-231, MDA-MB-435, Flag-Cdc20, MDA-MB-231, 22Rv1, LNCaP",3.9215200000000072,EC50 of PROTAC is 2.6 uM for MDA-MB-231 and 1.99 uM for MDA-MB-435,Daniel Zaidman,1.6 uM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,17,6,,,Apcin,Cc1ncc([N+](=O)[O-])n1CCOC(=O)NC(Nc1ncccn1)C(Cl)(Cl)Cl,CNC(=O)CCOCCOCCOCCOCCOCCC=O,PEG,23,8,18,1075.5109999999993,No,,4N14,WR7,31669221,CP5V,No,,Reviewed,Q12834,Yes,No,No,Yes,10,263.0199999999999
590,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1,Inactive,No,Hella,4.009520000000007,Engagment was tested in-vitro,"Daniel Zaidman, Yangwode Jing",,32 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCOCC=O,PEG,12,4,8,953.1759999999998,No,,5EU1,5SW,30540463,5,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,Yes,No,"4,16",189.92000000000002
591,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1,Inactive,No,Hella,4.042720000000011,,"Daniel Zaidman, Yangwode Jing",,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,17,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCOCCOCCOCC=O,PEG,18,6,14,1041.2820000000002,No,,5EU1,5SW,30540463,6,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"4,16",208.38
592,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1,Active,No,Hella,4.059320000000011,,"Daniel Zaidman, Yangwode Jing",,46 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,18,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCOCCOCCOCCOCC=O,PEG,21,7,17,1085.3349999999996,No,,5EU1,5SW,30540463,22,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"4,16",217.61
593,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCCCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1,Active,No,Hella,5.179820000000008,,"Daniel Zaidman, Yangwode Jing",,20 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCCCCOCCOCC=O,Alkane,15,4,11,995.257,No,,5EU1,5SW,30540463,23,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"4,16",189.92000000000002
594,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1,Inactive,No,Hella,4.026120000000009,,"Daniel Zaidman, Yangwode Jing",,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCOCCOCC=O,PEG,15,5,11,997.2289999999999,No,,5EU1,5SW,30540463,24,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"4,16",199.15000000000003
595,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(C(=O)COCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1,Inactive,No,Hella,3.5527200000000096,,"Daniel Zaidman, Yangwode Jing",,5 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)C(=O)COCCOCCOCC=O,PEG,16,6,10,1011.2119999999998,No,,5EU1,5SW,30540463,25,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"4,16",216.22000000000003
596,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1,Active,No,Hella,4.890420000000005,Engagment was tested in-vitro,"Daniel Zaidman, Yangwode Jing",560 nM,10 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCOCCO,PEG,12,4,8,1041.257,No,,5EU1,5SW,30540463,26,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,Yes,No,"4,16",199.15
597,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(C#N)CC2)C(C)(C)C)CC1,Active,No,Hella,4.692100000000006,,"Daniel Zaidman, Yangwode Jing",,12 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(C#N)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,17,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCOCCO,PEG,12,4,8,1048.2769999999998,No,,5EU1,5SW,30540463,27,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"4,16",222.94
598,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(C)=O)C(C)(C)C)CC1,Inactive,No,Hella,4.408220000000005,,"Daniel Zaidman, Yangwode Jing",,5 %,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C,VHL,,,aliphatic_CC,16,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCOCCO,PEG,12,4,8,997.2289999999998,No,,5EU1,5SW,30540463,28,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"4,16",199.15
599,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOCCOCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1,Active,No,Hella,4.9236200000000085,,"Daniel Zaidman, Yangwode Jing",,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,18,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCOCCOCCOCCO,PEG,18,6,14,1129.3629999999998,No,,5EU1,5SW,30540463,29,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"4,16",217.61
600,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOCCOCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(C#N)CC2)C(C)(C)C)CC1,Inactive,No,Hella,4.725300000000008,,"Daniel Zaidman, Yangwode Jing",,11 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(C#N)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,19,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCOCCOCCOCCO,PEG,18,6,14,1136.3829999999996,No,,5EU1,5SW,30540463,30,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"4,16",241.4
601,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOCCOCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(C)=O)C(C)(C)C)CC1,Inactive,No,Hella,4.441420000000008,,"Daniel Zaidman, Yangwode Jing",,2 %,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C,VHL,,,aliphatic_CC,18,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCOCCOCCOCCO,PEG,18,6,14,1085.3349999999996,No,,5EU1,5SW,30540463,31,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"4,16",217.61
602,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1,Active,No,"Hella, RI-1",4.873820000000006,,"Daniel Zaidman, Yangwode Jing",,92 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCO,PEG,9,3,5,997.2039999999997,No,,5EU1,5SW,30540463,46,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",189.92000000000002
603,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN1CCN(CCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1,Active,No,"Hella, RI-1",4.873820000000006,,"Daniel Zaidman, Yangwode Jing",,97 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,other,15,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCO,PEG,9,3,5,997.2039999999997,No,,5EU1,5SW,30540463,47,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",189.92000000000002
604,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN1CCN(CCOCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1,Active,No,"Hella, RI-1",4.890420000000005,,"Daniel Zaidman, Yangwode Jing",,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,3,,,1b,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN(C)C,CN(C)CCOCCOCCO,PEG,12,4,8,1041.257,No,,5F1H,5U6,30540463,48,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",199.15
605,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCOCCOCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1,Active,No,"Hella, RI-1",4.907020000000008,,"Daniel Zaidman, Yangwode Jing",,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,other,17,3,,,1b,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN(C)C,CN(C)CCOCCOCCOCCO,PEG,15,5,11,1085.3099999999997,No,,5F1H,5U6,30540463,49,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",208.38000000000002
606,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN1CCN(CCOCCOCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1,Active,No,"Hella, RI-1",4.907020000000008,,"Daniel Zaidman, Yangwode Jing",,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,other,17,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCOCCOCCOCCO,PEG,15,5,11,1085.3099999999997,No,,5EU1,5SW,30540463,50,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",208.38000000000002
607,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCCCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1,Active,Yes,"Hella, RI-1, EOL-1, A-204",6.027520000000005,DC50 is 1.76 nM and 4.5 nM,"Daniel Zaidman, Yangwode Jing",< 4.5 nM,90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,other,14,3,,,1b,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN(C)C,CN(C)CCCCCO,Alkane,9,2,5,995.2319999999997,No,,5F1H,5U6,30540463,51 (VZ185),Yes,28418626,Reviewed,"Q9H8M2, Q9NPI1",Yes,Yes,Yes,Yes,"2,4",180.69
608,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN1CCN(CCCCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1,Active,No,"Hella, RI-1",6.027520000000005,,"Daniel Zaidman, Yangwode Jing",,35 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,other,14,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCCCCO,Alkane,9,2,5,995.2319999999997,No,,5EU1,5SW,30540463,52,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",180.69
609,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCCCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1,Active,No,"Hella, RI-1",6.044120000000006,,"Daniel Zaidman, Yangwode Jing",,17 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,3,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CN(C)CCCCCOCCO,Alkane,12,3,8,1039.2849999999999,No,,5EU1,5SW,30540463,53,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",189.92000000000002
610,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN1CCN(CCCCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1,Inactive,No,"Hella, RI-1",6.044120000000006,,"Daniel Zaidman, Yangwode Jing",,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,3,,,1b,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN(C)C,CN(C)CCCCCOCCO,Alkane,12,3,8,1039.2849999999999,No,,5F1H,5U6,30540463,54,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",189.92000000000002
611,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CC(NC(=O)COCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)C1,Active,No,"Hella, RI-1",4.056620000000003,,"Daniel Zaidman, Yangwode Jing",,71 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,4,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CNC(=O)COCCO,PEG,9,4,4,997.1599999999997,No,,5EU1,5SW,30540463,55,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",215.77999999999997
612,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN1CC(NC(=O)COCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)C1,Active,No,"Hella, RI-1",4.056620000000003,,"Daniel Zaidman, Yangwode Jing",,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,4,,,1b,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN(C)C,CNC(=O)COCCO,PEG,9,4,4,997.1599999999997,No,,5F1H,5U6,30540463,56,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",215.77999999999997
613,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CC(NC(=O)COCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)C1,Active,No,"Hella, RI-1",4.073220000000005,,"Daniel Zaidman, Yangwode Jing",,47 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,4,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CNC(=O)COCCOCCO,PEG,12,5,7,1041.2129999999997,No,,5EU1,5SW,30540463,57,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",225.01
614,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN1CC(NC(=O)COCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)C1,Active,No,"Hella, RI-1",4.073220000000005,,"Daniel Zaidman, Yangwode Jing",,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,4,,,1b,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN(C)C,CNC(=O)COCCOCCO,PEG,12,5,7,1041.2129999999997,No,,5F1H,5U6,30540463,58,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",225.01
615,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CC(NC(=O)COCCOCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)C1,Active,No,"Hella, RI-1",4.089820000000008,,"Daniel Zaidman, Yangwode Jing",,2 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,17,4,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CNC(=O)COCCOCCOCCO,PEG,15,6,10,1085.2659999999994,No,,5EU1,5SW,30540463,59,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",234.23999999999998
616,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN1CC(NC(=O)COCCOCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)C1,Active,No,"Hella, RI-1",4.089820000000008,,"Daniel Zaidman, Yangwode Jing",,15 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,17,4,,,1b,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN(C)C,CNC(=O)COCCOCCOCCO,PEG,15,6,10,1085.2659999999994,No,,5F1H,5U6,30540463,60,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",234.23999999999998
617,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CC(NC(=O)CCCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)C1,Active,No,"Hella, RI-1",5.210320000000005,,"Daniel Zaidman, Yangwode Jing",,75 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,14,4,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CNC(=O)CCCCO,Alkane,9,3,4,995.1879999999998,No,,5EU1,5SW,30540463,61,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",206.54999999999998
618,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN1CC(NC(=O)CCCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)C1,Active,No,"Hella, RI-1",5.210320000000005,,"Daniel Zaidman, Yangwode Jing",,46 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,14,4,,,1b,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN(C)C,CNC(=O)CCCCO,Alkane,9,3,4,995.1879999999998,No,,5F1H,5U6,30540463,62,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",206.54999999999998
619,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CC(NC(=O)CCCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)C1,Active,No,"Hella, RI-1",5.226920000000005,,"Daniel Zaidman, Yangwode Jing",,69 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,4,,,1a,COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN(C)C,CNC(=O)CCCCOCCO,non-PEG polyether,12,4,7,1039.2409999999998,No,,5EU1,5SW,30540463,63,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",215.77999999999997
620,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN1CC(NC(=O)CCCCOCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)C1,Active,No,"Hella, RI-1",5.226920000000005,,"Daniel Zaidman, Yangwode Jing",,3 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,4,,,1b,COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN(C)C,CNC(=O)CCCCOCCO,non-PEG polyether,12,4,7,1039.2409999999998,No,,5F1H,5U6,30540463,64,No,28418626,Reviewed,"Q9H8M2, Q9NPI1",No,No,No,No,"2,4",215.77999999999997
621,O=C1CCC(N2C(=O)c3cccc(NCCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3C2=O)C(=O)N1,Active,Yes,"MM1S, HEK293T, CRBNY384A/W386A",0.04620000000000346,,"Daniel Zaidman, Yangwode Jing",,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,12,4,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCOCCOCC,PEG,8,2,5,660.6400000000003,"IKZF1, IKZF3",,4CI3,Y70,30118587,15a,Yes,,Reviewed,Q96SW2,Yes,Yes,No,Yes,16,209.61999999999998
622,O=C1CCC(N2C(=O)c3cccc(NCCCOCCOCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3C2=O)C(=O)N1,Active,No,MM1S,0.8264000000000018,,"Daniel Zaidman, Yangwode Jing",,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,12,4,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCCOCCOCCC,non-PEG polyether,10,2,7,688.6940000000003,IKZF1,,4CI3,Y70,30118587,15b,No,,Reviewed,Q96SW2,No,No,No,No,16,209.61999999999998
623,O=C1CCC(N2C(=O)c3cccc(NCCCOCCCCOCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3C2=O)C(=O)N1,Active,No,MM1S,1.6066000000000018,,"Daniel Zaidman, Yangwode Jing",,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,12,4,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCCOCCCCOCCC,non-PEG polyether,12,2,9,716.7480000000002,IKZF1,,4CI3,Y70,30118587,15c,No,,Reviewed,Q96SW2,No,No,No,No,16,209.61999999999998
624,O=C1CCC(N2C(=O)c3cccc(NCCCOCCOCCOCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3C2=O)C(=O)N1,Active,No,MM1S,0.8430000000000031,,"Daniel Zaidman, Yangwode Jing",,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,13,4,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCCOCCOCCOCCC,non-PEG polyether,13,3,10,732.7470000000002,IKZF1,,4CI3,Y70,30118587,15d,No,,Reviewed,Q96SW2,No,No,No,No,16,218.85
625,O=C1CCC(N2C(=O)c3cccc(NCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3C2=O)C(=O)N1,Active,No,MM1S,0.02960000000000218,,"Daniel Zaidman, Yangwode Jing",,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,11,4,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCOCC,PEG,5,1,2,616.5870000000002,IKZF1,,4CI3,Y70,30118587,15e,No,,Reviewed,Q96SW2,No,No,No,No,16,200.39
626,O=C1CCC(N2C(=O)c3cccc(OCCOCCOCCOc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3C2=O)C(=O)N1,Inactive,No,MM1S,-0.01999999999999702,,"Daniel Zaidman, Yangwode Jing",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_O,12,2,,,Thalidomide,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,OCCOCCOCCO,PEG,10,4,7,662.6080000000003,No,,4CI1,EF2,30118587,18,No,,Reviewed,Q96SW2,No,No,No,No,16,204.01999999999998
627,O=C1CCC(N2C(=O)c3ccc(C(=O)NCCOCCOCCNC(=O)c4ccc5c(c4)C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3C2=O)C(=O)N1,Inactive,No,MM1S,-1.3179999999999932,,"Daniel Zaidman, Yangwode Jing",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_C,12,4,,,Thalidomide,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,O=CNCCOCCOCCNC=O,PEG,14,6,11,716.6600000000002,No,,4CI1,EF2,30118587,19,No,,Reviewed,Q96SW2,No,No,No,No,16,243.76
628,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",3.724300000000005,,Daniel Zaidman,2.63 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCC,Other,4,0,0,1130.1120000000003,No,,6NUQ,KQV,31747516,12,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",310.80999999999995
629,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",4.114400000000006,,Daniel Zaidman,0.26 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCC,Other,5,0,1,1144.1390000000004,No,,6NUQ,KQV,31747516,13,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",310.80999999999995
630,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,Yes,"Molm-16, SU-DHL-1",4.504500000000006,EC50 of PROTAC is 10nM-35nM,Daniel Zaidman,0.06 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,8,,< 35 nM,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCCC,Other,6,0,2,1158.1660000000004,No,,6NUQ,KQV,31747516,14 (SD-36),Yes,31715132,Reviewed,P40763,Yes,No,No,No,"4,16",310.80999999999995
631,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",4.894600000000006,,Daniel Zaidman,0.09 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCCCC,Other,7,0,3,1172.1930000000004,No,,6NUQ,KQV,31747516,15,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",310.80999999999995
632,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",5.674800000000006,,Daniel Zaidman,0.15 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCCCCCC,Other,9,0,5,1200.2470000000003,No,,6NUQ,KQV,31747516,16,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",310.80999999999995
633,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(CCCCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",4.977900000000005,,Daniel Zaidman,0.65 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amide_to_amine,10,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCCC,Other,6,0,2,1144.1830000000004,No,,6NUQ,KQV,31747516,17,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",293.7399999999999
634,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)OCCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",4.334300000000006,,Daniel Zaidman,0.24 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,11,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCCCO,Other,7,1,3,1160.1380000000004,No,,6NUQ,KQV,31747516,18,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",320.0399999999999
635,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)NCCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",3.907300000000009,,Daniel Zaidman,0.05 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,10,9,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCCCN,Other,7,1,3,1159.1540000000005,No,,6NUQ,KQV,31747516,19,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",322.84
636,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)c3cnn(CCCC#Cc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)c3)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",3.8445000000000062,,Daniel Zaidman,0.18 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCCn(-c)nc,Other,9,2,3,1196.1750000000002,No,,6NUQ,KQV,31747516,20,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",328.62999999999994
637,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCn3cc(C#Cc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)cn3)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",3.5790000000000077,,Daniel Zaidman,0.25 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,12,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#Cc1cnn(CC)c1,Other,9,2,1,1196.1750000000004,No,,6NUQ,KQV,31747516,21,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",328.63
638,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)N3CCC(CCC#Cc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)CC3)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",4.639600000000007,,Daniel Zaidman,0.18 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,10,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCC1CCNCC1,Other,10,1,2,1199.2190000000003,No,,6NUQ,KQV,31747516,22,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",314.0499999999999
639,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCN3CCC(C#Cc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)CC3)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",3.6561000000000092,,Daniel Zaidman,2.47 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,11,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CC1CCN(C)CC1,Other,9,1,0,1199.2190000000003,No,,6NUQ,KQV,31747516,23,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",314.0499999999999
640,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CC(=O)N3CCC(C#Cc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)CC3)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",3.1827000000000076,,Daniel Zaidman,0.38 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,11,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CC1CCN(C=O)CC1,Other,10,2,1,1213.2020000000002,No,,6NUQ,KQV,31747516,24,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",331.11999999999995
641,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCCCc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",5.085600000000007,,Daniel Zaidman,0.16 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,CCCCCC,Alkane,6,0,3,1162.1980000000005,No,,6NUQ,KQV,31747516,25,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",310.80999999999995
642,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCCNc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",4.564900000000007,,Daniel Zaidman,0.09 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,11,9,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,CCCCC,Alkane,5,0,2,1163.1860000000004,No,,6NUQ,KQV,31747516,26,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",322.84
643,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCC#Cc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",4.144700000000006,,Daniel Zaidman,3.54 uM,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,11,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCCC,Other,6,0,2,1172.1490000000003,No,,6NUQ,KQV,31747516,27,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",327.87999999999994
644,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCC#Cc3ccc4c(c3)CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",4.5045000000000055,,Daniel Zaidman,0.41 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCCC,Other,6,0,2,1158.1660000000004,No,,6NUQ,KQV,31747516,28,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",310.80999999999995
645,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCC#Cc3ccc4c(c3)C(=O)N(C3CCC(=O)NC3=O)C4)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Active,No,"Molm-16, SU-DHL-1",4.504500000000006,,Daniel Zaidman,0.36 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,8,,,SI-109,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCCC,Other,6,0,2,1158.1660000000004,No,,6NUQ,KQV,31747516,29,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",310.80999999999995
646,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NCc1ccccc1,Active,No,"Molm-16, SU-DHL-1",2.915100000000005,,Daniel Zaidman,0.22 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,8,,,SI-109 analog,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NCc3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(C(F)(F)P(=O)(O)O)ccc3[nH]2)C1,C#CCCCC,Other,6,0,2,1082.0680000000004,No,,6NUQ,KQV,31747516,30,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",310.80999999999995
647,CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12,Active,No,"Molm-16, SU-DHL-1",1.3447000000000042,,Daniel Zaidman,0.64 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,8,,,SI-109 analog,CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CC[C@@H]2CCN(C(C)=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12,C#CCCCC,Other,6,0,2,1005.9700000000003,No,,6NUQ,KQV,31747516,31,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",310.81
648,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(OP(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Inactive,No,"Molm-16, SU-DHL-1",3.749000000000006,,Daniel Zaidman,> 10 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,11,8,,,SI-109 analog,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(OP(=O)(O)O)ccc3[nH]2)C1,C#CCCCC,Other,6,0,2,1124.1580000000004,No,,6NUQ,KQV,31747516,32,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",320.0399999999999
649,NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(CP(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1,Inactive,No,"Molm-16, SU-DHL-1",3.9552000000000076,,Daniel Zaidman,> 10 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,8,,,SI-109 analog,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)c2cc3cc(CP(=O)(O)O)ccc3[nH]2)C1,C#CCCCC,Other,6,0,2,1122.1860000000004,No,,6NUQ,KQV,31747516,33,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",310.80999999999995
650,C/C(=C\C(=O)N[C@H]1CN(C(=O)CCCCCC#Cc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C1=O)c1ccc(C(F)(F)P(=O)(O)O)cc1,Active,No,"Molm-16, SU-DHL-1",4.812900000000009,,Daniel Zaidman,4.45 uM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,7,,,SI-109 analog,CC(=O)N1CC[C@H]2CC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c3ccccc3)c3ccccc3)N2C(=O)[C@@H](NC(=O)/C=C(\C)c2ccc(C(F)(F)P(=O)(O)O)cc2)C1,C#CCCCC,Other,6,0,2,1159.1939999999997,No,,6NUQ,KQV,31747516,34,No,31715132,Reviewed,P40763,No,No,No,No,"4,16",295.02
651,O=C1CCC(N2C(=O)c3cccc(NCCCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)c3C2=O)C(=O)N1,Active,No,RS4;11,6.442900000000005,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,9,6,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,CCC,Alkane,3,0,0,908.8150000000002,No,,5TRF,7HC,30525597,1,No,,Reviewed,Q00987,No,No,No,No,2,194.91
652,O=C1CCC(N2C(=O)c3cccc(NCCOCCOCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)c3C2=O)C(=O)N1,Active,No,RS4;11,5.695900000000004,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,97 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,11,6,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,CCOCCOC,PEG,7,2,4,968.8669999999998,No,,5TRF,7HC,30525597,2,No,,Reviewed,Q00987,No,No,No,No,2,213.36999999999998
653,O=C1CCC(N2Cc3c(NC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)cccc3C2=O)C(=O)N1,Inactive,No,RS4;11,6.4329000000000045,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,10 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,7,5,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,None,Other,0,0,0,823.7090000000003,No,,5TRF,7HC,30525597,3,No,,Reviewed,Q00987,No,No,No,No,2,165.81
654,O=C1CCC(N2C(=O)c3cccc(NCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)c3C2=O)C(=O)N1,Active,No,RS4;11,5.662700000000003,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,60 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,9,6,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,C,Alkane,1,0,0,880.7610000000002,No,,5TRF,7HC,30525597,4,No,,Reviewed,Q00987,No,No,No,No,2,194.91
655,O=C1CCC(N2C(=O)c3cccc(NCCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)c3C2=O)C(=O)N1,Active,No,RS4;11,6.052800000000005,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,70 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,9,6,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,CC,Alkane,2,0,0,894.7880000000001,No,,5TRF,7HC,30525597,5,No,,Reviewed,Q00987,No,No,No,No,2,194.91
656,O=C1CCC(N2C(=O)c3cccc(NCCCCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)c3C2=O)C(=O)N1,Active,No,RS4;11,6.8330000000000055,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,80 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,9,6,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,CCCC,Alkane,4,0,1,922.8420000000001,No,,5TRF,7HC,30525597,6,No,,Reviewed,Q00987,No,No,No,No,2,194.91
657,O=C1CCC(N2C(=O)c3cccc(NCCCCCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)c3C2=O)C(=O)N1,Active,No,RS4;11,7.223100000000006,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,40 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,9,6,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,CCCCC,Alkane,5,0,2,936.869,No,,5TRF,7HC,30525597,7,No,,Reviewed,Q00987,No,No,No,No,2,194.91
658,O=C1CCC(N2C(=O)c3cccc(NCCCCCCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)c3C2=O)C(=O)N1,Inactive,No,RS4;11,7.613200000000006,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,30 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,9,6,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,CCCCCC,Alkane,6,0,3,950.896,No,,5TRF,7HC,30525597,8,No,,Reviewed,Q00987,No,No,No,No,2,194.91
659,O=C1CCC(N2C(=O)c3cccc(NCCOCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)c3C2=O)C(=O)N1,Active,No,RS4;11,5.679300000000005,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,70 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,10,6,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,CCOC,PEG,4,1,1,924.8140000000001,No,,5TRF,7HC,30525597,9,No,,Reviewed,Q00987,No,No,No,No,2,204.14
660,O=C1CCC(N2C(=O)c3cccc(NCCOCCOCCOCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)c3C2=O)C(=O)N1,Active,No,RS4;11,5.712500000000004,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,70 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,12,6,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,CCOCCOCCOC,PEG,10,3,7,1012.9199999999997,No,,5TRF,7HC,30525597,10,No,,Reviewed,Q00987,No,No,No,No,2,222.6
661,O=C1CCC(N2Cc3c(CCCCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)cccc3C2=O)C(=O)N1,Active,No,"RS4;11, MV4;11",7.323400000000007,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,98 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,7,5,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,CCCC,Alkane,4,0,1,893.8440000000002,No,,5TRF,7HC,30525597,13 (MD-222),No,,Reviewed,Q00987,No,No,No,No,2,165.81
662,O=C1CCC(N2Cc3c(C#CCCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)cccc3C2=O)C(=O)N1,Active,Yes,"RS4;11, MV4;11",6.7423000000000055,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,99 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,7,5,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,C#CCC,Other,4,0,0,889.8120000000002,No,,5TRF,7HC,30525597,14 (MD-224),No,,Reviewed,Q00987,Yes,No,No,Yes,2,165.81
663,O=C1CCC(N2Cc3cc(C#CCCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)ccc3C2=O)C(=O)N1,Active,No,RS4;11,6.7423000000000055,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,80 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,7,5,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,C#CCC,Other,4,0,0,889.8120000000001,No,,5TRF,7HC,30525597,16,No,,Reviewed,Q00987,No,No,No,No,2,165.81
664,O=C1CCC(N2Cc3ccc(C#CCCCNC(=O)c4ccc(NC(=O)[C@@H]5NC6(CCCCC6)[C@@]6(C(=O)Nc7cc(Cl)ccc76)[C@H]5c5cccc(Cl)c5F)cc4)cc3C2=O)C(=O)N1,Active,No,RS4;11,6.742300000000005,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,80 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,7,5,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,C#CCC,Other,4,0,0,889.8120000000001,No,,5TRF,7HC,30525597,17,No,,Reviewed,Q00987,No,No,No,No,2,165.81
665,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOCCOCCNC(=O)c2ccc(NC(=O)[C@@H]3NC4(CCCCC4)[C@@]4(C(=O)Nc5cc(Cl)ccc54)[C@H]3c3cccc(Cl)c3F)cc2)C(C)(C)C)cc1,Inactive,No,RS4;11,7.830320000000009,EC50 of ligand and PROTAC was measured in RS4;11 cell line.,Daniel Zaidman,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,13,7,2.7 nM,,MI-1242,CNC(=O)c1ccc(NC(=O)[C@@H]2NC3(CCCCC3)[C@@]3(C(=O)Nc4cc(Cl)ccc43)[C@H]2c2cccc(Cl)c2F)cc1,COCCOCCOCCC=O,PEG,12,4,9,1198.2559999999992,No,,5TRF,7HC,30525597,20,No,,Reviewed,Q00987,No,No,No,No,2,238.64999999999998
666,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1,Active,No,LNCaP,5.993800000000006,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,35 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,10,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CC=O,Alkane,3,1,0,935.039,No,,,,30629437,8,No,,Reviewed,P10275,No,No,No,No,6,188.07
667,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1,Active,No,LNCaP,6.383900000000006,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,33 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,10,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CCC=O,Alkane,4,1,1,949.0659999999999,No,,,,30629437,9,No,,Reviewed,P10275,No,No,No,No,6,188.07
668,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1,Inactive,No,LNCaP,6.774000000000006,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,25 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,10,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CCCC=O,Alkane,5,1,2,963.093,No,,,,30629437,10,No,,Reviewed,P10275,No,No,No,No,6,188.07
669,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1,Inactive,No,LNCaP,7.1641000000000075,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,29 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,10,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CCCCC=O,Alkane,6,1,3,977.12,No,,,,30629437,11,No,,Reviewed,P10275,No,No,No,No,6,188.07
670,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1,Active,No,LNCaP,7.554200000000007,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,84 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,10,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CCCCCC=O,Alkane,7,1,4,991.1469999999999,No,,,,30629437,12,No,,Reviewed,P10275,No,No,No,No,6,188.07
671,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1,Active,No,LNCaP,7.944300000000007,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,65 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,10,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CCCCCCC=O,Alkane,8,1,5,1005.174,No,,,,30629437,13,No,,Reviewed,P10275,No,No,No,No,6,188.07
672,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1,Active,No,LNCaP,8.334400000000006,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,87 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,10,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CCCCCCCC=O,Alkane,9,1,6,1019.201,No,,,,30629437,14,No,,Reviewed,P10275,No,No,No,No,6,188.07
673,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1,Active,No,LNCaP,8.724500000000004,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,88 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,10,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CCCCCCCCC=O,Alkane,10,1,7,1033.228,No,,,,30629437,15,No,,Reviewed,P10275,No,No,No,No,6,188.07
674,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1,Active,No,LNCaP,9.114600000000001,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,86 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,10,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CCCCCCCCCC=O,Alkane,11,1,8,1047.255,No,,,,30629437,16,No,,Reviewed,P10275,No,No,No,No,6,188.07
675,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1,Active,No,LNCaP,9.5047,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,75 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,10,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CCCCCCCCCCC=O,Alkane,12,1,9,1061.282,No,,,,30629437,17,No,,Reviewed,P10275,No,No,No,No,6,188.07
676,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1,Active,No,LNCaP,6.0270000000000055,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,40 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,12,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,COCCOCCC=O,PEG,9,3,6,1023.145,No,,,,30629437,18,No,,Reviewed,P10275,No,No,No,No,6,206.53
677,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCc2ccc(C#Cc3ccc(N4C(=S)N(c5ccc(C#N)c(C(F)(F)F)c5)C(=O)C4(C)C)cc3)cn2)C(C)(C)C)cc1,Active,No,LNCaP,9.022600000000002,,Daniel Zaidman,,96 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,10,3,,,Enzalutamide (-F analog),CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,Cc1ccc(CCCCCCC=O)nc1,Other,15,2,7,1031.24,No,,,,30629437,19,No,,Reviewed,P10275,No,No,No,No,6,171.85999999999996
678,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCN2CCN(c3ccc(C#Cc4ccc(N5C(=S)N(c6ccc(C#N)c(C(F)(F)F)c6)C(=O)C5(C)C)cc4)cn3)CC2)C(C)(C)C)cc1,Active,No,LNCaP,7.431800000000008,,Daniel Zaidman,,80 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,3,,,Enzalutamide (-F analog),CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,Cc1ccc(N2CCN(CCCC=O)CC2)nc1,Other,18,4,5,1073.2809999999995,No,,,,30629437,20,No,,Reviewed,P10275,No,No,No,No,6,178.33999999999997
679,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCN2CCN(c3ccc(C#Cc4ccc(N5C(=S)N(c6ccc(C#N)c(C(F)(F)F)c6)C(=O)C5(C)C)cc4)cn3)CC2)C(C)(C)C)cc1,Active,No,LNCaP,7.99280000000001,,Daniel Zaidman,,92 %,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,3,,,Enzalutamide (-F analog),CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,Cc1ccc(N2CCN(CCCC=O)CC2)nc1,Other,18,4,5,1087.3079999999993,No,,,,30629437,21,No,,Reviewed,P10275,No,No,No,No,6,178.33999999999997
680,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCN2CCN(c3ccc(C#Cc4ccc(N5C(=S)N(c6ccc(C#N)c(C(F)(F)F)c6)C(=O)C5(C)C)cc4)cn3)CC2)C(C)(C)C)cc1,Active,No,LNCaP,8.382900000000006,,Daniel Zaidman,,89 %,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,3,,,Enzalutamide (-F analog),CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,Cc1ccc(N2CCN(CCCCC=O)CC2)nc1,Other,19,4,6,1101.3349999999994,No,,,,30629437,22,No,,Reviewed,P10275,No,No,No,No,6,178.33999999999997
681,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCN2CCN(c3ccc(C#Cc4ccc(N5C(=S)N(c6ccc(C#N)c(C(F)(F)F)c6)C(=O)C5(C)C)cc4)cn3)CC2)C(C)(C)C)cc1,Active,No,LNCaP,7.602700000000009,,Daniel Zaidman,,78 %,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,3,,,Enzalutamide (-F analog),CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,Cc1ccc(N2CCN(CCC=O)CC2)nc1,Other,17,4,4,1073.2809999999995,No,,,,30629437,23,No,,Reviewed,P10275,No,No,No,No,6,178.33999999999997
682,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CN2CCN(c3ccc(C#Cc4ccc(N5C(=S)N(c6ccc(C#N)c(C(F)(F)F)c6)C(=O)C5(C)C)cc4)cn3)CC2)C(C)(C)C)cc1,Active,No,LNCaP,7.212600000000009,,Daniel Zaidman,,31 %,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,12,3,,,Enzalutamide (-F analog),CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,Cc1ccc(N2CCN(CC=O)CC2)nc1,Other,16,4,3,1059.2539999999997,No,,,,30629437,24,No,,Reviewed,P10275,No,No,No,No,6,178.33999999999997
683,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)N2CCN(c3ccc(C#Cc4ccc(N5C(=S)N(c6ccc(C#N)c(C(F)(F)F)c6)C(=O)C5(C)C)cc4)cn3)CC2)C(C)(C)C)cc1,Inactive,No,LNCaP,7.806000000000009,,Daniel Zaidman,,12 %,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,11,3,,,Enzalutamide (-F analog),CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,Cc1ccc(N2CCN(C=O)CC2)nc1,Other,15,4,2,1045.2269999999996,No,,,,30629437,25,No,,Reviewed,P10275,No,No,No,No,6,178.33999999999997
684,Cc1cc([C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](CC(=O)NCCCCCCCCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LNCaP,9.587119999999999,"EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM",Daniel Zaidman,,87 %,CNC(=O)C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(-c2scnc2C)cc1,VHL,,,aliphatic_CC,12,4,,,Enzalutamide,CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CCCCCCC,Alkane,7,0,4,1114.302,No,,,,30629437,26,No,,Reviewed,P10275,No,No,No,No,6,214.09999999999997
685,Cc1cc([C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](CC(=O)NCCCN2CCN(c3ccc(C#Cc4ccc(N5C(=S)N(c6ccc(C#N)c(C(F)(F)F)c6)C(=O)C5(C)C)cc4)cn3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LNCaP,8.294420000000008,,Daniel Zaidman,,94 %,CNC(=O)C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(-c2scnc2C)cc1,VHL,,,other,14,3,,,Enzalutamide (-F analog),CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CCN1CCN(c2ccc(C)cn2)CC1,Other,15,3,2,1154.3549999999996,No,,,,30629437,27,No,,Reviewed,P10275,No,No,No,No,6,204.36999999999995
686,Cc1cc([C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](CC(=O)N2CCN(c3ccc(C#Cc4ccc(N5C(=S)N(c6ccc(C#N)c(C(F)(F)F)c6)C(=O)C5(C)C)cc4)cn3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LNCaP,8.314720000000007,,Daniel Zaidman,,93 %,CNC(=O)C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(-c2scnc2C)cc1,VHL,,,other,13,2,,,Enzalutamide (-F analog),CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,Cc1ccc(N(C)C)nc1,Other,10,2,1,1097.2589999999996,No,,,,30629437,28,No,,Reviewed,P10275,No,No,No,No,6,192.33999999999992
687,Cc1cc([C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(N5C(=S)N(c6ccc(C#N)c(C(F)(F)F)c6)C(=O)C5(C)C)cc4)CC3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LNCaP,8.925820000000005,,Daniel Zaidman,,97 %,CNC(=O)C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(-c2scnc2C)cc1,VHL,,,other,12,2,,,Enzalutamide (-F analog),CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F,CC1CCN(C(C)C)CC1,Other,10,1,1,1102.3189999999995,No,,,,30629437,29,No,,Reviewed,P10275,No,No,No,No,6,179.44999999999993
688,Cc1cc([C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(N5C(=S)N(c6cnc(C#N)c(C(F)(F)F)c6)C(=O)C56CCC6)cc4)CC3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LNCaP,8.464920000000008,,Daniel Zaidman,,95 %,CNC(=O)C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(-c2scnc2C)cc1,VHL,,,other,13,2,,,Enzalutamide (analog),Cc1ccc(N2C(=S)N(c3cnc(C#N)c(C(F)(F)F)c3)C(=O)C23CCC3)cc1,CC1CCN(C(C)C)CC1,Other,10,1,1,1115.3179999999993,No,,,,30629437,30,No,,Reviewed,P10275,No,No,No,No,6,192.33999999999997
689,Cc1cc([C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(S(=O)CC(C)(O)C(=O)Nc5ccc(C#N)c(C(F)(F)F)c5)cc4)CC3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LNCaP,7.50642000000001,,Daniel Zaidman,,35 %,CNC(=O)C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(-c2scnc2C)cc1,VHL,,,other,13,4,,,Enzalutamide (analog),Cc1ccc(S(=O)CC(C)(O)C(=O)Nc2ccc(C#N)c(C(F)(F)F)c2)cc1,CC1CCN(C(C)C)CC1,Other,10,1,1,1109.3069999999996,No,,,,30629437,31,No,,Reviewed,P10275,No,No,No,No,6,222.29999999999995
690,Cc1cc([C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LNCaP,9.255720000000004,,Daniel Zaidman,,99 %,CNC(=O)C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(-c2scnc2C)cc1,VHL,,,other,12,3,,,Enzalutamide (analog),Cc1ccc(C(=O)N[C@H]2C(C)(C)[C@H](Oc3ccc(C#N)c(Cl)c3)C2(C)C)cc1,CC1CCN(C(C)C)CC1,Other,10,1,1,1095.8079999999995,No,,,,30629437,32,No,,Reviewed,P10275,No,No,No,No,6,194.22999999999996
691,Cc1cc([C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(Cc5c(C)nn(-c6ccc(C#N)c(Cl)c6)c5C)cc4)CC3)CC2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LNCaP,9.037060000000006,,Daniel Zaidman,,93 %,CNC(=O)C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(-c2scnc2C)cc1,VHL,,,other,12,2,,,Enzalutamide (analog),Cc1ccc(Cc2c(C)nn(-c3ccc(C#N)c(Cl)c3)c2C)cc1,CC1CCN(C(C)C)CC1,Other,10,1,1,1034.7279999999996,No,,,,30629437,33,No,,Reviewed,P10275,No,No,No,No,6,173.71999999999997
692,Cc1ncsc1-c1ccc([C@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)CC2)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,Active,Yes,"LNCaP, VCaP, and 22Rv",8.552500000000006,"DC50 is 0.86nM in LNCaP, 0.76 in VCaP and 10.4 nM at 1uM in 22Rv1. EC50 in cells is 0.25nM for LNCaP, 0.34 nM for VCaP, 183nM for 22Rv1.",Daniel Zaidman,< 10.4 nM,> 95 %,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)cc1,VHL,,,other,11,4,,,Enzalutamide (analog),Cc1ccc(C(=O)N[C@H]2C(C)(C)[C@H](Oc3ccc(C#N)c(Cl)c3)C2(C)C)cc1,CC1CCN(C2CCN(C=O)CC2)CC1,Other,15,3,2,1129.8409999999992,No,,,,30629437,34 (ARD-69),No,,Reviewed,P10275,Yes,Yes,No,Yes,"6,24",197.29999999999998
693,Cc1ncsc1-c1ccc([C@H](CC(=O)N2CCC(N3CCC(C#Cc4ccc(C(=O)N[C@H]5C(C)(C)[C@H](Oc6ccc(C#N)c(Cl)c6)C5(C)C)cc4)CC3)CC2)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(C#N)CC2)C(C)(C)C)cc1,Active,No,LNCaP,8.354180000000007,,Daniel Zaidman,,100 %,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(C#N)CC2)C(C)(C)C)cc1,VHL,,,other,12,4,,,Enzalutamide (analog),Cc1ccc(C(=O)N[C@H]2C(C)(C)[C@H](Oc3ccc(C#N)c(Cl)c3)C2(C)C)cc1,CC1CCN(C2CCN(C=O)CC2)CC1,Other,15,3,2,1136.8609999999992,No,,,,30629437,35,No,,Reviewed,P10275,No,No,No,No,6,221.08999999999997
694,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](CC(=O)N1CCC(N2CCC(C#Cc3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)CC1)c1ccc(-c2scnc2C)cc1)C(C)(C)C,Active,No,LNCaP,8.07030000000001,,Daniel Zaidman,,99 %,CC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C,VHL,,,other,11,4,,,Enzalutamide (analog),Cc1ccc(C(=O)N[C@H]2C(C)(C)[C@H](Oc3ccc(C#N)c(Cl)c3)C2(C)C)cc1,CC1CCN(C2CCN(C=O)CC2)CC1,Other,15,3,2,1085.8129999999992,No,,,,30629437,36,No,,Reviewed,P10275,No,No,No,No,6,197.29999999999995
695,Cc1cc([C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](CC(=O)NCCCCCCCCCNC(=O)c2ccc(C(=O)N[C@H]3C(C)(C)[C@H](Oc4ccc(C#N)c(Cl)c4)C3(C)C)cc2)c2ccc(-c3scnc3C)cc2)C(C)C)on1,Active,No,LNCaP,9.777919999999998,,Daniel Zaidman,,96 %,CNC(=O)C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](c1cc(C)no1)C(C)C)c1ccc(-c2scnc2C)cc1,VHL,,,other,12,5,,,Enzalutamide (analog),Cc1ccc(C(=O)N[C@H]2C(C)(C)[C@H](Oc3ccc(C#N)c(Cl)c3)C2(C)C)cc1,CCCCCCCCN,Alkane,9,1,6,1089.801,No,,,,30629437,39,No,,Reviewed,P10275,No,No,No,No,6,228.87999999999994
696,CC1(C)[C@H](NC(=O)c2ccc(C(=O)NCCCCCCCCCCc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)cc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,Inactive,No,LNCaP,7.318180000000008,,Daniel Zaidman,,20 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,8,3,,,Enzalutamide (analog),Cc1ccc(C(=O)N[C@H]2C(C)(C)[C@H](Oc3ccc(C#N)c(Cl)c3)C2(C)C)cc1,CCCCCCCCCCN,Alkane,11,1,8,822.4030000000001,No,,,,30629437,40,No,,Reviewed,P10275,No,No,No,No,6,174.76999999999998
697,CC1(C)[C@H](NC(=O)c2ccc(C#CC3CCN(C4CCN(c5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)cc2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1,Inactive,No,LNCaP,5.957380000000006,,Daniel Zaidman,,25 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,9,2,,,Enzalutamide (analog),Cc1ccc(C(=O)N[C@H]2C(C)(C)[C@H](Oc3ccc(C#N)c(Cl)c3)C2(C)C)cc1,CCC(CC)N1CCC(C)CC1,Other,12,1,3,829.3979999999998,No,,,,30629437,41,No,,Reviewed,P10275,No,No,No,No,6,152.14999999999998
698,C=CC(=O)N1CCN(c2nc(NCCC(=O)NCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,4.247400000000006,,Efrat Resnick,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,14,5,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCOCCOCCNC(=O)CCN,non-PEG polyether,15,6,10,936.3979999999999,No,,5V9O,91G,31883964,2,No,,Reviewed,P01116,No,No,No,No,16,224.73
699,C=CC(=O)N1CCN(c2nc(NCCC(=O)NCCOCCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,4.280600000000008,,Efrat Resnick,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,16,5,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCOCCOCCOCCOCCNC(=O)CCN,non-PEG polyether,21,8,16,1024.504,No,,5V9O,91G,31883964,3,No,,Reviewed,P01116,No,No,No,No,16,243.19000000000003
700,C=CC(=O)N1CCN(c2nc(NCCCc3cn(CCOCCOCCOCCC(=O)Nc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)nn3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,5.258500000000006,,Efrat Resnick,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,16,4,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCCc1cn(CCOCCOCCOCCC(N)=O)nn1,non-PEG polyether,23,9,15,1032.531,No,,5V9O,91G,31883964,4,No,,Reviewed,P01116,No,No,No,No,16,235.56999999999996
701,C=CC(=O)N1CCN(c2nc(NCCOCCOCCOCCc3cn(CCOCCOCCOCCC(=O)Nc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)nn3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,4.91820000000001,,Efrat Resnick,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,19,4,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCOCCOCCOCCc1cn(CCOCCOCCOCCC(N)=O)nn1,non-PEG polyether,31,12,23,1150.663,No,,5V9O,91G,31883964,5,No,,Reviewed,P01116,No,No,No,No,16,263.26
702,C=CC(=O)N1CCN(c2nc(NCCOCCOCCOCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,4.724600000000005,,Efrat Resnick,,7 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,14,3,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCOCCOCCOCCO,PEG,13,5,10,910.356,No,,5V9O,91G,31883964,6,No,,Reviewed,P01116,No,No,No,No,16,202.05999999999997
703,C=CC(=O)N1CCN(c2nc(NCCOCCOCCOCCOCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,4.741200000000006,,Efrat Resnick,,6 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,15,3,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCOCCOCCOCCOCCO,PEG,16,6,13,954.4089999999999,No,,5V9O,91G,31883964,7,No,,Reviewed,P01116,No,No,No,No,16,211.29
704,C=CC(=O)N1CCN(c2nc(NCCOCCOCCOCCOCCOCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,4.757800000000006,,Efrat Resnick,,3 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,16,3,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCOCCOCCOCCOCCOCCO,PEG,19,7,16,998.4619999999999,No,,5V9O,91G,31883964,8,No,,Reviewed,P01116,No,No,No,No,16,220.52
705,C=CC(=O)N1CCN(c2nc(NCCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,4.757700000000006,Engagment was tested in-vitro,Efrat Resnick,,19 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,14,4,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCOCCOCCOCCN,PEG,13,5,10,909.372,No,,5V9O,91G,31883964,9,No,,Reviewed,P01116,Yes,No,Yes,No,16,204.85999999999999
706,C=CC(=O)N1CCN(c2nc(NCCCCCCCCCCCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,8.608900000000006,,Efrat Resnick,,1 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,11,4,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCCCCCCCCCCCN,Alkane,14,2,11,917.4830000000001,No,,5V9O,91G,31883964,10,No,,Reviewed,P01116,No,No,No,No,16,177.17
707,C=CC(=O)N1CCN(c2nc(NCCCN(C)CCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,5.4199000000000055,Engagment was tested in-vitro,Efrat Resnick,,25 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,12,4,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,CN(CCCN)CCCN,Other,10,3,6,862.3629999999999,No,,5V9O,91G,31883964,11,No,,Reviewed,P01116,No,No,Yes,No,16,180.41
708,C=CC(=O)N1CCN(c2nc(NCCN3CCN(CCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,4.325500000000005,,Efrat Resnick,,24 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,13,4,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCN1CCN(CCN)CC1,Other,12,4,4,889.3889999999998,No,,5V9O,91G,31883964,12,No,,Reviewed,P01116,No,No,No,No,16,183.65
709,C=CC(=O)N1CCN(c2nc(NCCCN3CCN(CCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Active,Yes,GFP-KRASG12C reporter cell line in Flp-In 293,5.105700000000006,Engagment was tested in-vitro,Efrat Resnick,,32 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,13,4,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCCN1CCN(CCCN)CC1,Other,14,4,6,917.4429999999999,No,,5V9O,91G,31883964,13 (XY-4-88),Yes,,Reviewed,P01116,Yes,Yes,Yes,Yes,16,183.65
710,C=CC(=O)N1CCN(c2nc(NCCCCN3CCN(CCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,5.885900000000007,,Efrat Resnick,,17 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,13,4,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCCCN1CCN(CCCCN)CC1,Other,16,4,8,945.4969999999998,No,,5V9O,91G,31883964,14,No,,Reviewed,P01116,No,No,No,No,16,183.65
711,C=CC(=O)N1CCN(c2nc(NCCOCCCN3CCN(CCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,4.748800000000006,,Efrat Resnick,,10 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,15,4,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCOCCCN1CCN(CCOCCN)CC1,Other,19,6,11,991.5219999999997,No,,5V9O,91G,31883964,15,No,,Reviewed,P01116,No,No,No,No,16,202.10999999999999
712,C=CC(=O)N1CCN(c2nc(NCCOCCOCCNc3ccc4c(c3)C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Inactive,No,GFP-KRASG12C reporter cell line in Flp-In 293,4.741100000000003,,Efrat Resnick,,4 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,13,4,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCOCCOCCN,PEG,10,4,7,865.319,No,,5V9O,91G,31883964,16,No,,Reviewed,P01116,No,No,No,No,16,195.62999999999997
713,C=CC(=O)N1CCN(c2nc(NCCCN3CCN(CCCNc4ccc5c(c4)C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,Active,No,GFP-KRASG12C reporter cell line in Flp-In 293,5.105700000000006,,Efrat Resnick,,35 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aryl_N,13,4,,,Compound 1,C=CC(=O)N1CCN(c2ncnc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1,NCCCN1CCN(CCCN)CC1,Other,14,4,6,917.4429999999999,No,,5V9O,91G,31883964,17,No,,Reviewed,P01116,No,No,No,No,16,183.65
714,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Active,No,HEK293T,4.471420000000002,,"Paul Gehrtz, Yangwode Jing",44.5 nM,97.1 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,11,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCCCCCCCC=O,Alkane,10,1,7,842.032,CNIH1 and LMBRD2,,4CI3,Y70,31873151,6a (TD158),Yes,,Reviewed,Q96SW2,No,Yes,Yes,Yes,24,207.20999999999998
715,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Active,Yes,HEK293T,5.251620000000002,,"Paul Gehrtz, Yangwode Jing",20.4 nM,99.6 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,11,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCCCCCCCCCC=O,Alkane,12,1,9,870.086,No,,4CI3,Y70,31873151,6b (TD165),No,,Reviewed,Q96SW2,No,No,Yes,No,24,207.20999999999998
716,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Active,No,HEK293T,3.6912200000000013,,"Paul Gehrtz, Yangwode Jing",100.6 nM,96.9 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,11,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CCCCCCC=O,Alkane,8,1,5,813.978,No,,4CI3,Y70,31873151,6d (TD-156),No,,Reviewed,Q96SW2,No,No,Yes,No,24,207.20999999999998
717,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNC(=O)CNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Active,No,HEK293T,4.367820000000004,,"Paul Gehrtz, Yangwode Jing",28.8 nM,98.4 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,12,6,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,CC(=O)NCCCCCCCCCCC=O,Alkane,16,3,11,927.1379999999999,No,,4CI3,Y70,31873151,6e (TD-759),No,,Reviewed,Q96SW2,Yes,No,Yes,No,24,236.30999999999997
718,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNC(=O)COc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Active,No,HEK293T,4.3347200000000035,,"Paul Gehrtz, Yangwode Jing",367.7 nM,82 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_ether,12,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,O=CCCCCCCCCCCNC(=O)CO,Alkane,17,4,12,928.122,No,,4CI3,Y70,31873151,6f (TD-760),No,,Reviewed,Q96SW2,No,No,Yes,No,24,233.50999999999996
719,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1,Active,No,HEK293T,3.2178200000000006,,"Paul Gehrtz, Yangwode Jing",2546.1 nM,77.9 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_amide,11,5,,,Pomalidomide,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,O=CCCCCCC=O,Alkane,9,2,6,827.961,No,,4CI3,Y70,31873151,12 (TD-033),No,,Reviewed,Q96SW2,No,No,Yes,No,24,224.27999999999997
720,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CCCCCCCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)(C)C)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,Jurkat,7.820840000000009,,Daniel Zaidman,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,15,4,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCCCCCCC=O,Alkane,9,1,6,1016.3269999999995,No,,5L2I,LQQ,32184044,4,No,,Reviewed,"P11802, Q00534",No,No,No,Yes,24,207.88
721,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)(C)C)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,Jurkat,5.530040000000008,,Daniel Zaidman,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,18,4,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCCOCC=O,PEG,12,4,9,1064.3239999999996,No,,5L2I,LQQ,32184044,5,No,,Reviewed,"P11802, Q00534",No,No,No,No,24,235.57
722,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CC(=O)NCCOCCOCCOCCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)(C)C)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,Jurkat,5.036340000000011,"inactive for CDK4, active for CDK6",Daniel Zaidman,,,Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,19,5,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CC(=O)NCCOCCOCCOCCC=O,PEG,17,6,12,1135.403,No,,5L2I,LQQ,32184044,6,No,,Reviewed,"P11802, Q00534",No,No,No,No,24,264.66999999999996
723,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)COCCOCCOCCN2CCN(c3ccc(Nc4ncc5c(C)c(C(C)=O)c(=O)n(C6CCCC6)c5n4)nc3)CC2)C[C@H]1C(=O)Nc1c(F)cccc1F)C(C)(C)C,Active,No,Jurkat,3.8694200000000105,,Daniel Zaidman,,,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)Nc1c(F)cccc1F)C(C)(C)C,Iap,,,amine_to_methylamine,17,5,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCCOCC=O,Alkane,12,4,9,1059.229999999999,No,,5L2I,LQQ,32184044,7,No,,Reviewed,"P11802, Q00534",No,No,No,Yes,24,243.57999999999996
724,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](NC(=O)CCOCCOCCOCCNC(=O)CN2CCN(c3ccc(Nc4cc5c(cn4)c(C)c(C(C)=O)c(=O)n5C4CCCC4)nc3)CC2)C[C@H]1C(=O)Nc1c(F)cccc1F)C(C)(C)C,Inactive,No,Jurkat,3.980720000000013,,Daniel Zaidman,,,CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@@H](N)C[C@H]1C(=O)Nc1c(F)cccc1F)C(C)(C)C,Iap,,,other,17,6,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CC(=O)NCCOCCOCCOCCC=O,PEG,17,6,12,1129.3209999999992,No,,5L2I,LQQ,32184044,9,No,,Reviewed,"P11802, Q00534",No,No,No,No,24,259.78999999999996
725,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CCCCNC(=O)CNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,Yes,Jurkat,3.0879200000000013,,Daniel Zaidman,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,15,4,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCCCNC(C)=O,Alkane,8,2,3,831.9349999999996,No,,5L2I,LQQ,32184044,10,No,,Reviewed,"P11802, Q00534",No,No,No,Yes,24,220.93
726,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CCOCCOCCNC(=O)CNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O,Active,No,Jurkat,2.3409200000000023,,Daniel Zaidman,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,17,4,,,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCOCCOCCNC(C)=O,PEG,12,4,7,891.9869999999995,No,,5L2I,LQQ,32184044,11,No,,Reviewed,"P11802, Q00534",No,No,No,No,24,239.39
727,COc1ccccc1S(=O)(=O)Nc1ccc2c3c(cc(CCC(=O)NCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc13)C(=O)N2C,Inactive,No,"MV4-11, Molm-13",2.8012999999999995,"EC50 of ligand is 0.370 uM for MV4- 11, 3.369 uM for Molm-13. EC50 of PROTAC is 1.648uM for MV4-11, >10uM for Molm-13",Daniel Zaidman,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_C,10,4,49.5 nM,,compound 6,COc1ccccc1S(=O)(=O)Nc1ccc2c3c(cccc13)C(=O)N2C,CCNC(=O)CC,Alkane,7,2,2,738.779,No,,,,31767403,13,No,,Reviewed,"O60885, P25440",No,No,No,No,"1,2,4,6,16,24",200.39
728,COc1ccccc1S(=O)(=O)Nc1ccc2c3c(cc(CCC(=O)NCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc13)C(=O)N2C,Active,No,"MV4-11, Molm-13",3.1914000000000007,"EC50 of ligand is 0.370 uM for MV4- 11, 3.369 uM for Molm-13. EC50 of PROTAC is 0.025uM for MV4-11, 0.18uM for Molm-13",Daniel Zaidman,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_C,10,4,49.5 nM,,compound 6,COc1ccccc1S(=O)(=O)Nc1ccc2c3c(cccc13)C(=O)N2C,CCCNC(=O)CC,Alkane,8,2,3,752.806,No,,,,31767403,14,No,,Reviewed,"O60885, P25440",No,No,No,No,"1,2,4,6,16,24",200.39
729,COc1ccccc1S(=O)(=O)Nc1ccc2c3c(cc(CCC(=O)NCCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc13)C(=O)N2C,Active,Yes,Big sellection of cacer cell lines,3.581500000000001,"EC50 of ligand is 0.370 uM for MV4- 11, 3.369 uM for Molm-13. EC50 of PROTAC is 0.012uM for MV4-11, 0.052uM for Molm-13.",Daniel Zaidman,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_C,10,4,49.5 nM,,compound 6,COc1ccccc1S(=O)(=O)Nc1ccc2c3c(cccc13)C(=O)N2C,CCCCNC(=O)CC,Alkane,9,2,4,766.8330000000001,No,,,,31767403,15,No,,Reviewed,"O60885, P25440",No,No,No,No,"1,2,4,6,16,24",200.39
730,COc1ccccc1S(=O)(=O)Nc1ccc2c3c(cc(CCC(=O)NCCCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc13)C(=O)N2C,Active,No,"MV4-11, Molm-13",3.9716000000000014,"EC50 of ligand is 0.370 uM for MV4- 11, 3.369 uM for Molm-13. EC50 of PROTAC is 0.032uM for MV4-11, 0.177uM for Molm-13.",Daniel Zaidman,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_C,10,4,49.5 nM,,compound 6,COc1ccccc1S(=O)(=O)Nc1ccc2c3c(cccc13)C(=O)N2C,CCCCCNC(=O)CC,Alkane,10,2,5,780.86,No,,,,31767403,16,No,,Reviewed,"O60885, P25440",No,No,No,No,"1,2,4,6,16,24",200.39
731,COc1ccccc1S(=O)(=O)Nc1ccc2c3c(cc(CCC(=O)NCCCCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc13)C(=O)N2C,Inactive,No,"MV4-11, Molm-13",4.361700000000003,"EC50 of ligand is 0.370 uM for MV4- 11, 3.369 uM for Molm-13. EC50 of PROTAC is 3.429uM for MV4-11, >10uM for Molm-13.",Daniel Zaidman,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_C,10,4,49.5 nM,,compound 6,COc1ccccc1S(=O)(=O)Nc1ccc2c3c(cccc13)C(=O)N2C,CCCCCCNC(=O)CC,Alkane,11,2,6,794.8870000000001,No,,,,31767403,17,No,,Reviewed,"O60885, P25440",No,No,No,No,"1,2,4,6,16,24",200.39
732,ClC1=CC=C(C2=N[C@@H](CNC(C3=CC(F)=C(/N=N/C4=C(F)C=C(C(N[C@@H](C(C)(C)C)C(N5[C@H](C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)C[C@@H](O)C5)=O)=O)C=C4F)C(F)=C3)=O)C8=NN=C(C)N8C9=C2C(C)=C(C)S9)C=C1,Active,Yes,RAMOS,10.055979999999995,,"Shimrit Azulay, Daniel Zaidman",,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,4,,,JQ1,O=C(C[C@H]1C2=NN=C(N2C3=C(C(C4=CC=C(C=C4)Cl)=N1)C(C)=C(S3)C)C)OC(C)(C)C,NC(=O)c1cc(F)c(/N=N/c2c(F)cc(C=O)cc2F)c(F)c1,Other,23,5,4,1108.6449999999998,,,,,31660436,trans-photoPROTAC-1,No,,Reviewed,O15155,No,No,No,No,,208.51999999999998
733,ClC1=CC=C(C=C1)C2=N[C@H](C3=NN=C(N3C4=C2C(C)=C(S4)C)C)CNC(C5=CC(F)=C(C(F)=C5)/N=N\C6=C(C=C(C=C6F)C(N[C@H](C(N7[C@@H](C[C@H](C7)O)C(NCC8=CC=C(C=C8)C9=C(N=CS9)C)=O)=O)C(C)(C)C)=O)F)=O,Inactive,No,RAMOS,10.055979999999998,,"Shimrit Azulay, Daniel Zaidman",,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,4,,,JQ1,O=C(C[C@H]1C2=NN=C(N2C3=C(C(C4=CC=C(C=C4)Cl)=N1)C(C)=C(S3)C)C)OC(C)(C)C,NC(=O)c1cc(F)c(/N=N\c2c(F)cc(C=O)cc2F)c(F)c1,Other,23,5,4,1108.6449999999993,,,,,31660436,cis-photoPROTAC-1,No,,Reviewed,O15155,No,No,No,No,,208.51999999999998
736,FC1=CC(I)=CC=C1NC(N2C)=C(NS(C3=CC=C(CCC(NCCOCOCOCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)=O)=O)=O)C=C3)(=O)=O)C=C(C)C2=O,Active,No,A375,5.797440000000005,IC50 value of PROTAC tested with MEK1,"Shimrit Azulay, Daniel Zaidman",,,N[C@H](C(N1C[C@@H](C[C@H]1C(N[C@@H](C)C2=CC=C(C=C2)C3=C(N=CS3)C)=O)O)=O)C(C)(C)C,VHL,,,aryl_C,15,6,0.4 uM,0.1 uM,Compound 2,FC1=CC(I)=CC=C1NC(N2C)=C(NS(C3=CC=CC=C3)(=O)=O)C=C(C)C2=O,CCC(=O)NCCOCOCOCC=O,PEG,15,6,10,1173.1379999999995,,,,VRA,31804822,Compound 3,No,,Reviewed,"P36507, Q02750",No,No,No,Yes,16,248.61999999999995
737,FC1=CC(I)=CC=C1NC(N2C)=C(NS(C3=CC=C(CCC(NCCOCOCOCOCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)=O)=O)=O)C=C3)(=O)=O)C=C(C)C2=O,Active,Yes,A375,5.771540000000005,IC50 value of PROTAC tested with MEK1,"Shimrit Azulay, Daniel Zaidman",,,N[C@H](C(N1C[C@@H](C[C@H]1C(N[C@@H](C)C2=CC=C(C=C2)C3=C(N=CS3)C)=O)O)=O)C(C)(C)C,VHL,,,aryl_C,16,6,0.4 uM,0.1 uM,Compound 2,FC1=CC(I)=CC=C1NC(N2C)=C(NS(C3=CC=CC=C3)(=O)=O)C=C(C)C2=O,CCC(=O)NCCOCOCOCOCC=O,PEG,17,7,12,1203.1639999999995,,,,VRA,31804822,Compound 4,No,,Reviewed,"P36507, Q02750",No,No,No,Yes,16,257.84999999999997
738,FC1=CC(I)=CC=C1NC(N2C)=C(NS(C3=CC=C(OCC(NCCOCOCOCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)=O)=O)=O)C=C3)(=O)=O)C=C(C)C2=O,Active,No,A375,5.243640000000004,IC50 value of PROTAC tested with MEK1,"Shimrit Azulay, Daniel Zaidman",,,N[C@H](C(N1C[C@@H](C[C@H]1C(N[C@@H](C)C2=CC=C(C=C2)C3=C(N=CS3)C)=O)O)=O)C(C)(C)C,VHL,,,aryl_O,16,6,0.4 uM,0.16 uM,Compound 2,FC1=CC(I)=CC=C1NC(N2C)=C(NS(C3=CC=CC=C3)(=O)=O)C=C(C)C2=O,O=CCOCOCOCCNC(=O)CO,PEG,15,7,10,1175.1099999999994,,,,VRA,31804822,Compound 5,No,,Reviewed,"P36507, Q02750",No,No,No,Yes,16,257.84999999999997
739,O=C(N1CCC[C@H](N2C3=C(C(N)=NC=N3)C(C4=CC=C(OC5=CC=CC=C5)C=C4)=N2)C1)/C(C#N)=C/C(C)(CCCOCCOCCOCCOCCOC6=CC=CC(C(N7C8CCC(NC8=O)=O)=O)=C6C7=O)C,Active,Yes,"Mino, Ramos",5.834280000000005,,Amit Shraga,6 nM,85 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,17,2,,,Ibrutinib,C=CC(=O)N1CCC[C@H](C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N,CC(C)CCCOCCOCCOCCOCCO,PEG,19,5,15,998.1069999999994,BLK,,,,32369353,RC-3,Yes,,Reviewed,Q06187,Yes,Yes,No,Yes,"1,2,4,6,24",252.64999999999995
740,O=C(N1CCC[C@H](N2C3=C(C(N)=NC=N3)C(C4=CC=C(OC5=CC=CC=C5)C=C4)=N2)C1)CCCCCCOCCOCCOCCOCCOC6=CC=CC(C(N7C8CCC(NC8=O)=O)=O)=C6C7=O,Active,Yes,"Mino, Ramos",5.528400000000005,,Amit Shraga,2.2 nM,97 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,16,2,,,Ibrutinib,C=CC(=O)N1CCC[C@H](C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N,CCCCCOCCOCCOCCOCCO,PEG,18,5,15,947.0589999999996,,,,,32369353,NC-1,Yes,,Reviewed,Q06187,Yes,Yes,No,Yes,"1,2,4,6,24",228.85999999999999
741,O=C(N1CCC[C@H](N2C3=C(C(N)=NC=N3)C(C4=CC=C(OC5=CC=CC=C5)C=C4)=N2)C1)/C=C/CCCCOCCOCCOCCOCCOC6=CC=CC(C(N7C8CCC(NC8=O)=O)=O)=C6C7=O,Active,No,"Mino, Ramos",5.304400000000005,,Amit Shraga,1.9 nM,88 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,16,2,,,Ibrutinib,C=CC(=O)N1CCC[C@H](C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N,CCCCOCCOCCOCCOCCO,PEG,17,5,14,945.0429999999996,,,,,32369353,IR-2,Yes,,Reviewed,Q06187,Yes,Yes,No,Yes,"1,2,4,6,24",228.85999999999999
742,O=C1N(C2CCC(NC2=O)=O)C(C3=CC=CC(OCCOCCOCCOCCOCCOC/C=C/C(N4CCC[C@H](C4)N5C6=C(C(C7=CC=C(C=C7)OC8=CC=CC=C8)=N5)C(N)=NC=N6)=O)=C31)=O,Active,No,"Mino, Ramos",4.150700000000004,,Amit Shraga,8.6 nM,91 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,17,2,,,Ibrutinib,C=CC(=O)N1CCC[C@H](C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N,COCCOCCOCCOCCOCCO,Other,17,6,14,947.0149999999999,,,,,32369353,IR-1,Yes,,Reviewed,Q06187,Yes,Yes,No,Yes,"1,2,4,6,24",238.09000000000003
743,O=C(/C(C#N)=C/CCCCOCCOCCOCCOCCOC1=CC=CC(C(N2C3CCC(NC3=O)=O)=O)=C1C2=O)N4CCC[C@@H](C4)N5C6=C(C(C7=CC=C(C=C7)OC8=CC=CC=C8)=N5)C(N)=NC=N6,Active,No,"Mino, Ramos",5.198180000000003,,Amit Shraga,35 nM,66 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,17,2,,,Ibrutinib,C=CC(=O)N1CCC[C@H](C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N,CCCCOCCOCCOCCOCCO,Other,17,5,14,970.0529999999995,,,,,32369353,RC-2,Yes,,Reviewed,Q06187,Yes,Yes,No,Yes,"1,2,4,6,24",252.65000000000003
744,O=C(CC1)NC(C1N2C(C(C=CC=C3OCCOCCOCCOCCOCCOC/C=C(C#N)/C(N(CCC4)C[C@@H]4N5N=C(C6=CC=C(C=C6)OC7=CC=CC=C7)C(C5=NC=N8)=C8N)=O)=C3C2=O)=O)=O,Inactive,No,"Mino, Ramos",4.044480000000004,,Amit Shraga,10 nM,68 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,18,2,,,Ibrutinib,C=CC(=O)N1CCC[C@H](C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N,COCCOCCOCCOCCOCCO,Other,17,6,14,972.0249999999997,,,,,32369353,RC-1,Yes,,Reviewed,Q06187,Yes,Yes,No,Yes,"1,2,4,6,24",261.88
745,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC(NCCC(NC5=C6C(C(N(C7CCC(NC7=O)=O)C6)=O)=CC=C5)=O)=O)C(N3C)=O)=C2,Active,No,,3.8256400000000026,IC50 of PROTAC with error of ± 13.8 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,8,3,46.4 nM,132.2 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,CC(=O)NCCC=O,Alkane,8,3,3,703.7560000000003,,,,,31813613,Compound 8,No,,Reviewed,O60885,No,No,No,No,,174.26
746,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC(NCCCC(NC5=C6C(C(N(C7CCC(NC7=O)=O)C6)=O)=CC=C5)=O)=O)C(N3C)=O)=C2,Active,No,,4.215740000000004,IC50 of PROTAC with error of ± 15.4 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,8,3,46.4 nM,138.4 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,CC(=O)NCCCC=O,Alkane,9,3,4,717.7830000000004,,,,,31813613,Compound 9,No,,Reviewed,O60885,No,No,No,No,,174.26
747,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC(NCCCCC(NC5=C6C(C(N(C7CCC(NC7=O)=O)C6)=O)=CC=C5)=O)=O)C(N3C)=O)=C2,Active,No,,4.605840000000004,IC50 of PROTAC with error of ± 14.2 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,8,3,46.4 nM,133.6 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,CC(=O)NCCCCC=O,Alkane,10,3,5,731.8100000000004,,,,,31813613,Compound 10,No,,Reviewed,O60885,No,No,No,No,,174.26
748,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC(NCCCCCC(NC5=C6C(C(N(C7CCC(NC7=O)=O)C6)=O)=CC=C5)=O)=O)C(N3C)=O)=C2,Active,No,,4.9959400000000045,IC50 of PROTAC with error of ± 8.7 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,8,3,46.4 nM,99.1 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,CC(=O)NCCCCCC=O,Alkane,11,3,6,745.8370000000004,,,,,31813613,Compound 11,No,,Reviewed,O60885,No,No,No,No,,174.26
749,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC(NCCCCCCC(NC5=C6C(C(N(C7CCC(NC7=O)=O)C6)=O)=CC=C5)=O)=O)C(N3C)=O)=C2,Active,No,,5.386040000000006,IC50 of PROTAC with error of ± 6.5 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,8,3,46.4 nM,80.6 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,CC(=O)NCCCCCCC=O,Alkane,12,3,7,759.8640000000004,,,,,31813613,Compound 12,No,,Reviewed,O60885,No,No,No,No,,174.26
750,CC%11(C)CC/C(c1ccc(Cl)cc1)=C(CN%10CCN(c9ccc(C(=O)NS(=O)(=O)c8ccc(NC(CCN6CCN(C(=O)CCCn5cc(COCCOCCNc3cccc4c(=O)n(C2CCC(=O)NC2=O)c(=O)c34)nn5)CC6)CSc7ccccc7)c(S(=O)(=O)C(F)(F)F)c8)cc9)CC%10)\C%11,Active,Yes,WI38 platelets,8.763600000000006,,Barr Tivon,46 nM,96.2 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,21,4,,,ABT-263,C1(=CC=C(C=C1)C2=C(CC(CC2)(C)C)CN3CCN(CC3)C4=CC=C(C=C4)C(=O)N[S](C5=CC=C(C(=C5)[S](C(F)(F)F)(=O)=O)NC(CCN6CCNCC6)CSC7=CC=CC=C7)(=O)=O)Cl,CCOCCOCc1cn(CCCC=O)nn1,Other,17,6,10,1484.1569999999995,,,6QGH,1XJ,32332723,PZ15227,No,,Reviewed,Q07817,Yes,Yes,No,Yes,16,284.18999999999994
751,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC(NCCCCCCCC(NC5=C6C(C(N(C7CCC(NC7=O)=O)C6)=O)=CC=C5)=O)=O)C(N3C)=O)=C2,Active,No,,5.776140000000006,IC50 of PROTAC with error of ± 7.1 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,8,3,46.4 nM,68.3 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,CC(=O)NCCCCCCCC=O,Alkane,13,3,8,773.8910000000003,,,3MXF,,31813613,Compound 13,No,,Reviewed,O60885,No,No,No,No,,174.26
752,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CCCCC(NC5=C6C(C(N(C7CCC(NC7=O)=O)C6)=O)=CC=C5)=O)C(N3C)=O)=C2,Active,No,,5.489640000000006,IC50 of PROTAC with error of ± 13.6 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 nM,,other,7,2,46.4 nM,143.7 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,CCCCC=O,Alkane,6,1,3,674.7580000000004,,,3MXF,,31813613,Compound 14,No,,Reviewed,O60885,No,No,No,No,,145.16
753,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CCCCCC(NC5=C6C(C(N(C7CCC(NC7=O)=O)C6)=O)=CC=C5)=O)C(N3C)=O)=C2,Active,No,,5.879740000000006,IC50 of PROTAC with error of ± 14.0 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,7,2,46.4 nM,135.1 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,CCCCCC=O,Alkane,7,1,4,688.7850000000004,,,3MXF,,31813613,Compound 15,No,,Reviewed,O60885,No,No,No,No,,145.16
754,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CCCCCCC(NC5=C6C(C(N(C7CCC(NC7=O)=O)C6)=O)=CC=C5)=O)C(N3C)=O)=C2,Active,No,,6.2698400000000065,IC50 of PROTAC with error of ± 12.6 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,7,2,46.4 nM,118.2 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,CCCCCCC=O,Alkane,8,1,5,702.8120000000005,,,3MXF,,31813613,Compound 16,No,,Reviewed,O60885,No,No,No,No,,145.16
755,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC5=CN(COCC(NC6=C7C(C(N(C8CCC(NC8=O)=O)C7)=O)=CC=C6)=O)N=N5)C(N3C)=O)=C2,Active,No,THP-1,4.0851400000000035,IC50 of PROTAC with error of ± 1.6 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 nM,1.83 uM,other,11,2,46.4 nM,14.2 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,Cc1cn(COCC=O)nn1,PEG,11,5,4,743.7810000000003,,,3MXF,,31813613,Compound 17,No,,Reviewed,O60885,No,No,No,No,,185.09999999999997
756,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC5=CN(CCOCCOCC(NC6=C7C(C(N(C8CCC(NC8=O)=O)C7)=O)=CC=C6)=O)N=N5)C(N3C)=O)=C2,Active,No,,4.1442400000000035,IC50 of PROTAC with error of ± 2.3 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,12,2,46.4 nM,15.4 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,Cc1cn(CCOCCOCC=O)nn1,PEG,15,6,8,801.8610000000001,,,3MXF,,31813613,Compound 18,No,,Reviewed,O60885,No,No,No,No,,194.32999999999998
757,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC5=CN(COCC(NC6=C7C(C(N(C8CCC(NC8=O)=O)C7=O)=O)=CC=C6)=O)N=N5)C(N3C)=O)=C2,Active,Yes,THP-1,3.7253400000000028,IC50 of PROTAC with error of ± 7.8 nM,"Shimrit Azulay, Daniel Zaidman",,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,0.81 uM,other,12,2,46.4 nM,41.8 nM,Compound 21,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,Cc1cn(COCC=O)nn1,PEG,11,5,4,757.7640000000004,,,3MXF,,31813613,Compound 21,No,,Reviewed,O60885,No,Yes,No,No,,202.16999999999996
758,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC5=CN(CCOCOCCOCC(NC6=C7C(C(N(C8CCC(NC8=O)=O)C7)=O)=CC=C6)=O)N=N5)C(N3C)=O)=C2,Active,No,,4.1183400000000026,IC50 of PROTAC with error of ± 2.9 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,13,2,46.4 nM,22.1 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,Cc1cn(CCOCOCCOCC=O)nn1,PEG,17,7,10,831.8870000000001,,,3MXF,,31813613,Compound 19,No,,Reviewed,O60885,No,No,No,No,,203.56
759,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC5=CN(CCOCOCOCCOCC(NC6=C7C(C(N(C8CCC(NC8=O)=O)C7)=O)=CC=C6)=O)N=N5)C(N3C)=O)=C2,Active,No,,4.0924400000000025,IC50 of PROTAC with error of ± 3.7 nM,Shimrit Azulay,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,14,2,46.4 nM,22.6 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,Cc1cn(CCOCOCOCCOCC=O)nn1,PEG,19,8,12,861.913,,,3MXF,,31813613,Compound 20,No,,Reviewed,O60885,No,No,No,No,,212.78999999999996
760,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC5=CN(CCOCCOCC(NC6=C7C(C(N(C8CCC(NC8=O)=O)C7=O)=O)=CC=C6)=O)N=N5)C(N3C)=O)=C2,Active,No,THP-1,3.7844400000000027,IC50 of PROTAC with error of ± 9.0 nM,Shimrit Azulay,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,1.66 uM,other,13,2,46.4 nM,67.7 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,Cc1cn(CCOCCOCC=O)nn1,PEG,15,6,8,815.8440000000002,,,3MXF,,31813613,Compound 22,No,,Reviewed,O60885,No,No,No,No,,211.39999999999998
761,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC5=CN(CCOCOCCOCC(NC6=C7C(C(N(C8CCC(NC8=O)=O)C7=O)=O)=CC=C6)=O)N=N5)C(N3C)=O)=C2,Active,No,THP-1,3.7585400000000027,IC50 of PROTAC with error of ± 8.5 nM,Shimrit Azulay,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,1.75 uM,other,14,2,46.4 nM,68.5 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,Cc1cn(CCOCOCCOCC=O)nn1,PEG,17,7,10,845.8700000000001,,,3MXF,,31813613,Compound 23,No,,Reviewed,O60885,No,No,No,No,,220.63
762,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)N(CC5=CN(CCOCOCOCCOCC(NC6=C7C(C(N(C8CCC(NC8=O)=O)C7=O)=O)=CC=C6)=O)N=N5)C(N3C)=O)=C2,Active,No,,3.7326400000000017,IC50 of PROTAC with error of ± 23.2 nM,Shimrit Azulay,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,3.26 uM,,other,15,2,46.4 nM,173.4 nM,compound 6,CC1=NOC(C)=C1C2=CC=C3C(C(C4=CC=CC=C4)NC(N3C)=O)=C2,Cc1cn(CCOCOCOCCOCC=O)nn1,PEG,19,8,12,875.8960000000001,,,3MXF,,31813613,Compound 24,No,,Reviewed,O60885,No,No,No,No,,229.85999999999996
763,O=C(C(CC1)N(C2=O)C(C(C2=CC=C3)=C3NCCOCCOC(C=C4)=CC=C4NC5=NC(NC6=CC7=C(C=CC=C7)C=N6)=CC=N5)=O)NC1=O,Inactive,No,"MCF7, A549",4.420700000000002,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,4,,,"2,4-bis-arylamino-1,3-pyrimidine",OC(C=C1)=CC=C1NC2=NC(NC3=CC4=C(C=CC=C4)C=N3)=CC=N2,CCOCC,PEG,5,1,2,672.7020000000002,,,3QQU,,32340152,10a,No,,Reviewed,"P08069, P12931",No,No,No,No,72,176.77
764,O=C(C(CC1)N(C2=O)C(C(C2=CC=C3)=C3NCCOCCOCCOC(C=C4)=CC=C4NC5=NC(NC6=CC7=C(C=CC=C7)C=N6)=CC=N5)=O)NC1=O,Inactive,No,"MCF7, A549",4.437300000000001,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,4,,,"2,4-bis-arylamino-1,3-pyrimidine",OC(C=C1)=CC=C1NC2=NC(NC3=CC4=C(C=CC=C4)C=N3)=CC=N2,CCOCCOCC,PEG,8,2,5,716.7550000000002,,,3QQU,,32340152,10b,No,,Reviewed,"P08069, P12931",No,No,No,No,72,186.0
765,O=C(C(CC1)N(C2=O)C(C(C2=CC=C3)=C3NCCOCCOCCOCCOC(C=C4)=CC=C4NC5=NC(NC6=CC7=C(C=CC=C7)C=N6)=CC=N5)=O)NC1=O,Inactive,No,"MCF7, A549",4.453900000000002,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,4,,,"2,4-bis-arylamino-1,3-pyrimidine",OC(C=C1)=CC=C1NC2=NC(NC3=CC4=C(C=CC=C4)C=N3)=CC=N2,CCOCCOCCOCC,PEG,11,3,8,760.8080000000002,,,3QQU,,32340152,10c,No,,Reviewed,"P08069, P12931",No,No,No,No,72,195.23
766,O=C(C(CC1)N(C2=O)C(C(C2=CC=C3)=C3NCCOCCOC(C=C4)=CC=C4NC5=NC(NC6=NNC(C)=C6)=CC=N5)=O)NC1=O,Active,Yes,"MCF7, A549",2.904020000000001,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,5,,< 4.2 uM,"N2-phenyl-N4-(1H-pyrazol-3-yl)pyrimidine-2,4-diamine",OC(C=C1)=CC=C1NC2=NC(NC3=NNC(C)=C3)=CC=N2,CCOCC,PEG,5,1,2,625.6460000000002,,,,,32340152,12a,No,,Reviewed,"P08069, P12931",No,No,No,No,24,192.55999999999997
767,O=C(C(CC1)N(C2=O)C(C(C2=CC=C3)=C3NCCOCCOCCOC(C=C4)=CC=C4NC5=NC(NC6=NNC(C)=C6)=CC=N5)=O)NC1=O,Active,Yes,"MCF7, A549",2.9206199999999995,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,5,,< 7.6 uM,"N2-phenyl-N4-(1H-pyrazol-3-yl)pyrimidine-2,4-diamine",OC(C=C1)=CC=C1NC2=NC(NC3=NNC(C)=C3)=CC=N2,CCOCCOCC,PEG,8,2,5,669.6990000000002,,,,,32340152,"12b, CPR4",No,,Reviewed,"P08069, P12931",No,No,No,No,24,201.79
768,O=C(C(CC1)N(C2=O)C(C(C2=CC=C3)=C3NCCOCCOCCOC(C=C4)=CC=C4NC5=NC(NC6=NNC(C)=C6)=C(Cl)C=N5)=O)NC1=O,Inactive,No,"MCF7, A549",3.574019999999999,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,5,,,"N2-phenyl-N4-(1H-pyrazol-3-yl)pyrimidine-2,4-diamine",OC(C=C1)=CC=C1NC2=NC(NC3=NNC(C)=C3)=CC=N2,CCOCCOCC,PEG,8,2,5,704.1440000000001,,,,,32340152,12d,No,,Reviewed,"P08069, P12931",No,No,No,No,72,201.79
769,O=C(C(CC1)N(C2=O)C(C(C2=CC=C3)=C3NCCOCCOC(C=C4)=CC=C4NC5=NC(NC6=NNC(C)=C6)=C(Cl)C=N5)=O)NC1=O,Inactive,No,"MCF7, A549",3.5574200000000005,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,12,5,,,"N2-phenyl-N4-(1H-pyrazol-3-yl)pyrimidine-2,4-diamine",OC(C=C1)=CC=C1NC2=NC(NC3=NNC(C)=C3)=CC=N2,CCOCC,PEG,5,1,2,660.0910000000001,,,,,32340152,12c,No,,Reviewed,"P08069, P12931",No,No,No,No,72,192.55999999999997
770,NC1=C2C(N(CC3=CN(CC(NC4=CC=C(OCCOCCNC5=C(C(N(C6CCC(NC6=O)=O)C7=O)=O)C7=CC=C5)C=C4)=O)N=N3)N=C2C8=CC=C(Cl)C=C8)=NC=N1,Inactive,No,"MCF7, A549",2.916100000000002,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,4,,,"aminopyrazolo [3,4-d]pyrimidine",NC1=C2C(NN=C2C3=CC=CC=C3)=NC=N1,CCOCCOc1ccc(NC(=O)Cn2cc(C)nn2)cc1,Other,22,7,8,819.239,,,,,32340152,16a,No,,Reviewed,"P08069, P12931",No,No,No,No,72,243.4699999999999
771,O=C([C@H]1N(C([C@@H](NC([C@@H](NC)C)=O)C(C)(C)C)=O)CC(C=C(OCCOCCOCCOCCOC(C(S(C(C)(C)C)(=O)=O)=C2)=CC3=C2C(NC(C=C4)=CC5=C4SC=N5)=CC=N3)C=C6)=C6C1)N[C@H]7CCCC8=CC=CC=C87,Active,No,THPT1,8.253800000000007,,"Amit Shraga, Daniel Zaidman",< 1 uM,> 80 %,O=C([C@H]1N(C([C@@H](NC([C@@H](NC)C)=O)C(C)(C)C)=O)CC(C=CC=C2)=C2C1)N[C@H]3CCCC4=CC=CC=C43,Iap,,,aryl_O,15,4,,,RIP-2 kinase,O=S(C1=CC2=C(C=C1)N=CC=C2NC(C=C3)=CC4=C3SC=N4)(C(C)(C)C)=O,OCCOCCOCCOCCO,PEG,13,5,10,1092.395,,US10336744B2,,,,7a,No,,Reviewed,O43353,No,No,No,No,,208.64000000000001
772,CC/C(C1=CC=CC=C1)=C(C2=CC=C(O)C=C2)/C(C=C3)=CC=C3OCCN(C)CCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)=O,Active,No,MCF-7,7.36272000000001,,"Amit Shraga, Daniel Zaidman",< 1 uM,,N[C@H](C(N1[C@@H](C[C@H](C1)O)C(N[C@H](C2=CC=C(C=C2)C3=C(N=CS3)C)C)=O)=O)C(C)(C)C.Cl,VHL,,,other,12,4,,,tamoxifen,CC[N]CCOc1ccc(/C(c2ccc(O)cc2)=C(c3ccccc3)/CC)cc1,O=CCOCCOCCO,PEG,10,4,7,976.2499999999999,,ES2717436T3,2JF9,,,"(25.4R) -1 - ((S) -2- (tert -Butyl) -17- (4 - ((Z) -1,2-diphenylbut-1-en-1-yl) phenoxy) -15- methyl-4-oxo-6,9,12-trioxa-3,15-diazaheptadecan-I-oil) -4-hydroxy-M- (4- (4-methylthiazol-5-yl) benzyl) pyrrolidine-2-carboxamide N26699-42",No,,Reviewed,P03372,No,No,No,No,24,172.01999999999998
773,CC/C(C1=CC=CC=C1)=C(C2=CC=C(O)C=C2)/C(C=C3)=CC=C3OCCN(C)CCOCCOCCOCC(N[C@@H](C(C)C)C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)=O,Active,No,MCF-7,6.97262000000001,,"Amit Shraga, Daniel Zaidman",< 1 uM,,N[C@H](C(N1[C@@H](C[C@H](C1)O)C(N[C@H](C2=CC=C(C=C2)C3=C(N=CS3)C)C)=O)=O)C(C)(C)C.Cl,VHL,,,other,12,4,,,tamoxifen,CC[N]CCOc1ccc(/C(c2ccc(O)cc2)=C(c3ccccc3)/CC)cc1,O=CCOCCOCCO,Other,10,4,7,962.223,,ES2717436T3,2JF9,,,"(2S, 4R) -1 - ((S) -17- (4 - ((Z) 2-Diphenylbut-1-en-I-yl) phenoxy) -2-isopropyl-15-methyl-4-oxo-6 , 9,12-trioxa-3,15-diazaheptadecan-I-oil) -4-hydroxy-N- (4- (4-methylthiazol-5-yl) benzyl) pyrrolidine-2-carboxamide N26699-42",No,,Reviewed,P03372,No,No,No,No,24,172.01999999999998
774,NC1=C2C(N(CC3=CN(CC(NC4=CC=C(OCCOCCOCCNC5=C(C(N(C6CCC(NC6=O)=O)C7=O)=O)C7=CC=C5)C=C4)=O)N=N3)N=C2C8=CC=C(Cl)C=C8)=NC=N1,Inactive,No,"MCF7, A549",2.9327000000000023,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,4,,,"aminopyrazolo [3,4-d]pyrimidine",NC1=C2C(NN=C2C3=CC=CC=C3)=NC=N1,CCOCCOCCOc1ccc(NC(=O)Cn2cc(C)nn2)cc1,Other,25,8,11,863.292,,,,,32340152,16b,No,,Reviewed,"P08069, P12931",No,No,No,No,72,252.69999999999993
775,NC1=C2C(N(CCCNC3=CC=C(OCCOCCOCCNC4=C(C(N(C5CCC(NC5=O)=O)C6=O)=O)C6=CC=C4)C=C3)N=C2C7=CC=C(Cl)C=C7)=NC=N1,Inactive,No,"MCF7, A549",4.156400000000003,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,4,,,"aminopyrazolo [3,4-d]pyrimidine",NC1=C2C(NN=C2C3=CC=CC=C3)=NC=N1,CCCNc1ccc(OCCOCCOCC)cc1,Other,19,4,11,782.2580000000002,,,,,32340152,18b,No,,Reviewed,"P08069, P12931",No,No,No,No,72,204.91999999999996
776,NC1=C2C(N(CCCNC3=CC=C(OCCOCCNC4=C(C(N(C5CCC(NC5=O)=O)C6=O)=O)C6=CC=C4)C=C3)N=C2C7=CC=C(Cl)C=C7)=NC=N1,Inactive,No,"MCF7, A549",4.139800000000004,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,4,,,"aminopyrazolo [3,4-d]pyrimidine",NC1=C2C(NN=C2C3=CC=CC=C3)=NC=N1,CCCNc1ccc(OCCOCC)cc1,Other,16,3,8,738.2050000000002,,,,,32340152,18a,No,,Reviewed,"P08069, P12931",No,No,No,No,72,195.68999999999994
777,NC1=C2C(N(CCCN3N=NC(CNC4=CC=C(OCCOCCOCCNC5=C(C(N(C6CCC(NC6=O)=O)C7=O)=O)C7=CC=C5)C=C4)=C3)N=C2C8=CC=C(Cl)C=C8)=NC=N1,Inactive,No,"MCF7, A549",3.948100000000003,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,4,,,"aminopyrazolo [3,4-d]pyrimidine",NC1=C2C(NN=C2C3=CC=CC=C3)=NC=N1,CCCn1cc(CNc2ccc(OCCOCCOCC)cc2)nn1,Other,25,7,13,863.3360000000004,,,,,32340152,21b,No,,Reviewed,"P08069, P12931",No,No,No,No,72,235.62999999999994
778,NC1=C2C(N(CCCN3N=NC(CNC4=CC=C(OCCOCCNC5=C(C(N(C6CCC(NC6=O)=O)C7=O)=O)C7=CC=C5)C=C4)=C3)N=C2C8=CC=C(Cl)C=C8)=NC=N1,Inactive,No,"MCF7, A549",3.9315000000000033,,Barr Tivon,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,4,,,"aminopyrazolo [3,4-d]pyrimidine",NC1=C2C(NN=C2C3=CC=CC=C3)=NC=N1,CCCn1cc(CNc2ccc(OCCOCC)cc2)nn1,Other,22,6,10,819.2830000000002,,,,,32340152,21a,No,,Reviewed,"P08069, P12931",No,No,No,No,72,226.39999999999998
779,O=C(C1=C2C(OCCOCCOCCOCCOCCOC/C=C\C(N3C[C@H](N(CC3)C4=NC(N(C5=C4C=C(C(C6=C(C=CC=C6F)O)=N5)F)C7=C(C=CN=C7C(C)C)C)=O)C)=O)=CC=C1)N(C(C(N8)=O)CCC8=O)C2=O,Inactive,No,HOP62/INC-H23,4.414820000000002,Inactive PROTAC for KRAS based on AMG-510.,Ronen Gabizon,,,O=C(N(C1=O)C(CC2)C(NC2=O)=O)C3=C1C=CC=C3,Cereblon,68 nM,,aliphatic_CC,18,2,~ 50 nM,,AMG-510,C=CC(N1C[C@H](N(CC1)C2=NC(N(C3=C2C=C(C(C4=C(C=CC=C4F)O)=N3)F)C5=C(C=CN=C5C(C)C)C)=O)C)=O,COCCOCCOCCOCCOCCO,PEG,17,6,14,1067.1129999999998,,,6OIM,MOV,,RG40,No,,Reviewed,P01116,No,No,No,No,24,243.37999999999997
780,NC(C1=CC(C(N(C2=O)CC(NCCNc3c(C4=O)c(C(N4C(CC5)C(NC5=O)=O)=O)ccc3)=O)=O)=C(N=C1N)N2C6CC6)=O,Inactive,No,MDA-MB-231,-1.7962999999999956,"There was no reported structure for full-length eEF2K. The structure of target-ligand complex was generated using homology modelling (PDB code 5E4H); IC50 of this ligand (A484954) was reported as 0.42uM in another paper (10.1016/j.bmc.2014.06.050), which can be accounted for by the difference in ATP concentration in assays.","Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,13,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCN,Alkane,4,2,1,617.579,No,,,,32717479,9a,No,25047940,Reviewed,O00418,No,No,No,No,24,250.67999999999998
781,NC(C1=CC(C(N(CC(NCCCNc2cccc(C(N3C(C(N4)=O)CCC4=O)=O)c2C3=O)=O)C5=O)=O)=C(N5C6CC6)N=C1N)=O,Inactive,No,MDA-MB-231,-1.4061999999999961,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,13,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCCN,Alkane,5,2,2,631.606,No,,,,32717479,9b,No,25047940,Reviewed,O00418,No,No,No,No,24,250.67999999999998
782,NC(C1=CC(C(N(CC(NCCCCNc2cccc(C(N3C(C(N4)=O)CCC4=O)=O)c2C3=O)=O)C5=O)=O)=C(N5C6CC6)N=C1N)=O,Inactive,No,MDA-MB-231,-1.0160999999999965,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,13,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCCCN,Alkane,6,2,3,645.633,No,,,,32717479,9c,No,25047940,Reviewed,O00418,No,No,No,No,24,250.67999999999998
783,NC(C1=CC(C(N(CC(NCCCCCNc2cccc(C(N3C(C(N4)=O)CCC4=O)=O)c2C3=O)=O)C5=O)=O)=C(N5C6CC6)N=C1N)=O,Inactive,No,MDA-MB-231,-0.6259999999999968,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,13,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCCCCN,Alkane,7,2,4,659.66,No,,,,32717479,9d,No,25047940,Reviewed,O00418,No,No,No,No,24,250.67999999999998
784,NC(C1=CC(C(N2CC(NCCCCCCNc3c(C4=O)c(C(N4C(CC5)C(NC5=O)=O)=O)ccc3)=O)=O)=C(N=C1N)N(C6CC6)C2=O)=O,Inactive,No,MDA-MB-231,-0.235899999999996,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,13,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCCCCCN,Alkane,8,2,5,673.6869999999999,No,,,,32717479,9e,No,25047940,Reviewed,O00418,No,No,No,No,24,250.67999999999998
785,NC(C1=CC(C(N2CC(NCCOCCNc3c(C4=O)c(C(N4C(CC5)C(NC5=O)=O)=O)ccc3)=O)=O)=C(N=C1N)N(C6CC6)C2=O)=O,Inactive,No,MDA-MB-231,-1.7796999999999952,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCOCCN,Other,7,3,4,661.632,No,,,,32717479,9f,No,25047940,Reviewed,O00418,No,No,No,No,24,259.91
786,NC(C1=CC(C(N2CC(NCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)C6CC6)N=C1N)=O,Inactive,No,MDA-MB-231,-2.7131999999999943,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCNC(=O)CO,Alkane,8,4,3,675.6149999999999,No,,,,32717479,11a,No,25047940,Reviewed,O00418,No,No,No,No,24,276.9799999999999
787,NC(C1=CC(C(N2CC(NCCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)C6CC6)N=C1N)=O,Inactive,No,MDA-MB-231,-2.323099999999994,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCCNC(=O)CO,Alkane,9,4,4,689.6419999999999,No,,,,32717479,11b,No,25047940,Reviewed,O00418,No,No,No,No,24,276.9799999999999
788,NC(C1=CC(C(N2CC(NCCCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)C6CC6)N=C1N)=O,Inactive,No,MDA-MB-231,-1.9329999999999936,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCCCNC(=O)CO,Alkane,10,4,5,703.669,No,,,,32717479,11c,No,25047940,Reviewed,O00418,No,No,No,No,24,276.9799999999999
789,NC(C1=CC(C(N2CC(NCCCCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)C6CC6)N=C1N)=O,Inactive,No,MDA-MB-231,-1.5428999999999944,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCCCCNC(=O)CO,Alkane,11,4,6,717.696,No,,,,32717479,11d,No,25047940,Reviewed,O00418,No,No,No,No,24,276.9799999999999
790,NC(C1=CC(C(N2CC(NCCCCCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)C6CC6)N=C1N)=O,Inactive,No,MDA-MB-231,-1.1527999999999947,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCCCCCNC(=O)CO,Alkane,12,4,7,731.7230000000001,No,,,,32717479,11e,No,25047940,Reviewed,O00418,No,No,No,No,24,276.9799999999999
791,NC(C1=CC(C(N2CC(NCCOCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)C6CC6)N=C1N)=O,Inactive,No,MDA-MB-231,-2.696599999999993,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,15,5,0.28 uM,,A484954,O=C(N(CC)C1=O)N(C2CC2)C3=C1C=C(C(N)=O)C(N)=N3,NCCOCCNC(=O)CO,Other,11,5,6,719.668,No,,,,32717479,11f,No,25047940,Reviewed,O00418,No,No,No,No,24,286.2099999999999
792,NC(C1=CC(C(N2CC(NCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Active,No,MDA-MB-231,-3.028199999999994,,"Yangwode Jing, Daniel Zaidman",,10.0 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCNC(=O)CO,Alkane,8,4,3,663.6039999999999,No,,,,32717479,11g,No,25047940,Reviewed,O00418,No,No,No,No,24,276.9799999999999
793,NC(C1=CC(C(N2CC(NCCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Active,No,MDA-MB-231,-2.6380999999999935,,"Yangwode Jing, Daniel Zaidman",,15.4 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCCNC(=O)CO,Alkane,9,4,4,677.631,No,,,,32717479,11h,No,25047940,Reviewed,O00418,No,No,No,No,24,276.9799999999999
794,NC(C1=CC(C(N2CC(NCCCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Active,No,MDA-MB-231,-2.247999999999993,,"Yangwode Jing, Daniel Zaidman",,26.0 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCCCNC(=O)CO,Alkane,10,4,5,691.658,No,,,,32717479,11i,No,25047940,Reviewed,O00418,No,No,No,No,24,276.9799999999999
795,NC(C1=CC(C(N2CC(NCCCCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Active,No,MDA-MB-231,-1.8578999999999937,,"Yangwode Jing, Daniel Zaidman",,32.0 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCCCCNC(=O)CO,Alkane,11,4,6,705.6850000000001,No,,,,32717479,11j,No,25047940,Reviewed,O00418,No,No,No,No,24,276.9799999999999
796,NC(C1=CC(C(N2CC(NCCCCCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Active,No,MDA-MB-231,-1.4677999999999936,,"Yangwode Jing, Daniel Zaidman",,35.3 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCCCCCNC(=O)CO,Alkane,12,4,7,719.7120000000001,No,,,,32717479,11k,No,25047940,Reviewed,O00418,No,No,No,No,24,276.9799999999999
797,NC(C1=CC(C(N2CC(NCCOCCNC(COc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Active,Yes,MDA-MB-231,-3.0115999999999925,,"Yangwode Jing, Daniel Zaidman",,56.7 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,15,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCOCCNC(=O)CO,Other,11,5,6,707.657,No,,,,32717479,11l,No,25047940,Reviewed,O00418,No,No,No,Yes,24,286.2099999999999
798,NC(C1=CC(C(N2CC(NCCNc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Inactive,No,MDA-MB-231,-2.1112999999999955,,"Yangwode Jing, Daniel Zaidman",,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,13,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCN,Alkane,4,2,1,605.5680000000001,No,,,,32717479,9g,No,25047940,Reviewed,O00418,No,No,No,No,24,250.67999999999998
799,NC(C1=CC(C(N2CC(NCCCNc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Active,No,MDA-MB-231,-1.7211999999999952,,"Yangwode Jing, Daniel Zaidman",,20.0 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,13,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCCN,Alkane,5,2,2,619.595,No,,,,32717479,9h,No,25047940,Reviewed,O00418,No,No,No,No,24,250.67999999999998
800,NC(C1=CC(C(N2CC(NCCCCNc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Active,No,MDA-MB-231,-1.3310999999999953,,"Yangwode Jing, Daniel Zaidman",,35.0 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,13,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCCCN,Alkane,6,2,3,633.6220000000001,No,,,,32717479,9i,No,25047940,Reviewed,O00418,No,No,No,No,24,250.67999999999998
801,NC(C1=CC(C(N2CC(NCCCCCNc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Active,No,MDA-MB-231,-0.940999999999995,,"Yangwode Jing, Daniel Zaidman",,24.0 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,13,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCCCCN,Alkane,7,2,4,647.649,No,,,,32717479,9j,No,25047940,Reviewed,O00418,No,No,No,No,24,250.67999999999998
802,NC(C1=CC(C(N2CC(NCCCCCCNc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Active,No,MDA-MB-231,-0.5508999999999953,,"Yangwode Jing, Daniel Zaidman",,20.0 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,13,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCCCCCN,Alkane,8,2,5,661.6759999999999,No,,,,32717479,9k,No,25047940,Reviewed,O00418,No,No,No,No,24,250.67999999999998
803,NC(C1=CC(C(N2CC(NCCOCCNc3c(C(N(C4=O)C5C(NC(CC5)=O)=O)=O)c4ccc3)=O)=O)=C(N(C2=O)CC)N=C1N)=O,Active,No,MDA-MB-231,-2.0946999999999942,,"Yangwode Jing, Daniel Zaidman",,15.0 %,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,other,14,5,~ 1 uM,,Ethyl-substituted A484954,CCN(C(N1CC)=O)C(C2=C1N=C(C(C(N)=O)=C2)N)=O,NCCOCCN,Other,7,3,4,649.621,No,,,,32717479,9l,No,25047940,Reviewed,O00418,No,No,No,No,24,259.90999999999997
804,O=C(NC1=O)CCC1N(C2=O)CC3=C2C=CC=C3NC(COCCOCCNCCNC4=NON=C4/C(NC5=CC(Br)=C(F)C=C5)=N/O)=O,Inactive,No,HeLa,1.6535000000000026,EC50 for ligand Epa was also reported as 7.1nM; Cytotoxicity IC50 (CC50) for PROTAC 1a: >40uM,Yangwode Jing,,,NC1=CC=CC2=C1CN(C2=O)C3CCC(NC3=O)=O,Cereblon,12 nM,,other,13,6,72 nM,,Epacadostat,O=S(NCCNC1=NON=C1/C(NC2=CC(Br)=C(F)C=C2)=N/O)(N)=O,CCOCCOCC=O,PEG,9,3,6,746.5510000000004,No,,5WN8,BBJ,33163345,1a,No,,Reviewed,P14902,No,No,No,No,24,221.63999999999996
805,O=C(NC1=O)CCC1N(C2=O)CC3=C2C=CC=C3NC(COCCOCCOCCNCCNC4=NON=C4/C(NC5=CC(Br)=C(F)C=C5)=N/O)=O,Inactive,No,HeLa,1.6701000000000037,Cytotoxicity IC50 (CC50): >40uM,Yangwode Jing,,,NC1=CC=CC2=C1CN(C2=O)C3CCC(NC3=O)=O,Cereblon,12 nM,,other,14,6,72 nM,,Epacadostat,O=S(NCCNC1=NON=C1/C(NC2=CC(Br)=C(F)C=C2)=N/O)(N)=O,CCOCCOCCOCC=O,PEG,12,4,9,790.6040000000003,No,,5WN8,BBJ,33163345,1b,No,,Reviewed,P14902,No,No,No,No,24,230.86999999999998
806,O=C(NC1=O)CCC1N(C2=O)CC3=C2C=CC=C3NC(COCCOCCOCCOCCNCCNC4=NON=C4/C(NC5=CC(Br)=C(F)C=C5)=N/O)=O,Inactive,No,HeLa,1.6867000000000036,Cytotoxicity IC50 (CC50): >40uM,Yangwode Jing,,,NC1=CC=CC2=C1CN(C2=O)C3CCC(NC3=O)=O,Cereblon,12 nM,,other,15,6,72 nM,,Epacadostat,O=S(NCCNC1=NON=C1/C(NC2=CC(Br)=C(F)C=C2)=N/O)(N)=O,CCOCCOCCOCCOCC=O,PEG,15,5,12,834.6570000000004,No,,5WN8,BBJ,33163345,1c,No,,Reviewed,P14902,No,No,No,No,24,240.09999999999994
807,O=C(CCC1N(C(C2=C3C=CC=C2NC(COCCOCCOCCNCCNC4=NON=C4/C(NC5=CC(Br)=C(C=C5)F)=N/O)=O)=O)C3=O)NC1=O,Inactive,No,HeLa,1.310300000000002,Cytotoxicity IC50 (CC50): 34.27uM,Yangwode Jing,,,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,Cereblon,12 nM,,other,15,6,72 nM,,Epacadostat,O=S(NCCNC1=NON=C1/C(NC2=CC(Br)=C(F)C=C2)=N/O)(N)=O,CCOCCOCCOCC=O,PEG,12,4,9,804.5870000000004,No,,5WN8,BBJ,33163345,2a,No,,Reviewed,P14902,No,No,No,No,24,247.94
808,O=C(CCC1N(C(C2=C3C=CC=C2NC(COCCOCCOCCOCCOCCNCCNC4=NON=C4/C(NC5=CC(Br)=C(C=C5)F)=N/O)=O)=O)C3=O)NC1=O,Inactive,No,HeLa,1.3435000000000064,Cytotoxicity IC50 (CC50): 35.38uM,Yangwode Jing,,,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,Cereblon,12 nM,,other,17,6,72 nM,,Epacadostat,O=S(NCCNC1=NON=C1/C(NC2=CC(Br)=C(F)C=C2)=N/O)(N)=O,CCOCCOCCOCCOCCOCC=O,PEG,18,6,15,892.6930000000003,No,,5WN8,BBJ,33163345,2b,No,,Reviewed,P14902,No,No,No,No,24,266.4
809,O=C(CCC1N(C(C2=C3C=CC=C2NC(COCCOCCOCCOCCOCCOCCOCCNCCNC4=NON=C4/C(NC5=CC(Br)=C(C=C5)F)=N/O)=O)=O)C3=O)NC1=O,Active,Yes,HeLa,1.376700000000008,Cytotoxicity IC50 (CC50): 37.43uM,Yangwode Jing,2.84 uM,93 %,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,Cereblon,12 nM,,other,19,6,72 nM,,Epacadostat,O=S(NCCNC1=NON=C1/C(NC2=CC(Br)=C(F)C=C2)=N/O)(N)=O,CCOCCOCCOCCOCCOCCOCCOCC=O,PEG,24,8,21,980.7990000000002,No,,5WN8,BBJ,33163345,2c,No,,Reviewed,P14902,Yes,Yes,No,Yes,24,284.85999999999996
810,O=C(CCC1N(C(C2=C3C=CC=C2NC(COCCOCCOCCOCCOCCOCCOCCOCCOCCNCCNC4=NON=C4/C(NC5=CC(Br)=C(C=C5)F)=N/O)=O)=O)C3=O)NC1=O,Inactive,No,HeLa,1.4099000000000113,Cytotoxicity IC50 (CC50): >40uM,Yangwode Jing,,,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,Cereblon,12 nM,,other,21,6,72 nM,,Epacadostat,O=S(NCCNC1=NON=C1/C(NC2=CC(Br)=C(F)C=C2)=N/O)(N)=O,CCOCCOCCOCCOCCOCCOCCOCCOCCOCC=O,PEG,30,10,27,1068.905,No,,5WN8,BBJ,33163345,2d,No,,Reviewed,P14902,No,No,No,No,24,303.31999999999994
811,O=C1C2=C(C(N1C3CCC(NC3=O)=O)=O)C=CC=C2OCC(NCCCCCC(NC4=CC=C(C(NC(C=CC=C5)=C5N)=O)C=C4)=O)=O,Inactive,No,E14 mouse embryonic stem cells; Human colon cancer cell line HCT116,2.6163999999999987,,Yangwode Jing,,,O=C(CC1)NC(C1N2C(C(C=CC=C3)=C3C2=O)=O)=O,Cereblon,,,aliphatic_CC,9,5,0.53 uM,0.92 uM,CI-994,O=C(NC1=CC=CC=C1N)C2=CC=C(NC(C)=O)C=C2,CCCCNC(=O)CO,Alkane,9,3,4,654.6800000000004,No,,4LY1,20Y,32201871,1,No,,Reviewed,"O15379, Q13547, Q92769",No,No,No,No,24,206.1
812,O=C1C2=C(C(N1C3CCC(NC3=O)=O)=O)C=CC=C2OCC(NCCCCCCCCCCCC(NC4=CC=C(C(NC(C=CC=C5)=C5N)=O)C=C4)=O)=O,Active,No,E14 mouse embryonic stem cells; Human colon cancer cell line HCT116,4.957000000000002,,Yangwode Jing,~ 10 uM,,O=C(CC1)NC(C1N2C(C(C=CC=C3)=C3C2=O)=O)=O,Cereblon,,,aliphatic_CC,9,5,0.53 uM,8.6 uM,CI-994,O=C(NC1=CC=CC=C1N)C2=CC=C(NC(C)=O)C=C2,CCCCCCCCCCNC(=O)CO,Alkane,15,3,10,738.8420000000006,No,,4LY1,20Y,32201871,2,No,,Reviewed,"O15379, Q13547, Q92769",No,No,No,No,24,206.1
813,O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@H](C(C)(C)C)NC(CCCCC(NC4=CC=C(C(NC5=CC=CC=C5N)=O)C=C4)=O)=O)=O,Inactive,No,E14 mouse embryonic stem cells; Human colon cancer cell line HCT116,5.261020000000003,,Yangwode Jing,,,O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@H](C(C)(C)C)N)=O,VHL,,,aliphatic_CC,9,6,0.53 uM,0.70 uM,CI-994,O=C(NC1=CC=CC=C1N)C2=CC=C(NC(C)=O)C=C2,CCCC=O,Alkane,5,1,2,767.9530000000003,No,,4LY1,20Y,32201871,3,No,,Reviewed,"O15379, Q13547, Q92769",No,No,No,No,24,195.85
814,O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@H](C(C)(C)C)NC(CCCCCCCCCCC(NC4=CC=C(C(NC5=CC=CC=C5N)=O)C=C4)=O)=O)=O,Active,Yes,E14 mouse embryonic stem cells; Human colon cancer cell line HCT116,7.601620000000008,"For HDAC1/HDAC2/HDAC3, the Dmax of this PROTAC is: >85%, >76%, >63%, respectively.",Yangwode Jing,~ 1 uM,,O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@H](C(C)(C)C)N)=O,VHL,,,aliphatic_CC,9,6,0.53 uM,16.8 uM,CI-994,O=C(NC1=CC=CC=C1N)C2=CC=C(NC(C)=O)C=C2,CCCCCCCCCC=O,Alkane,11,1,8,852.115,No,,4LY1,20Y,32201871,4,No,,Reviewed,"O15379, Q13547, Q92769",Yes,No,No,No,24,195.85
815,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCCCCC4CCN(CCNC(C5=CC6=C(O5)C(C7=CC=CC=C7C6=O)=O)=O)CC4,Active,Yes,Pancreatic cancer cell lines BxPC-3; MIA PaCa-2,3.570500000000002,"XD2-149 was initially designed to degrade STAT3. However, experiments showed that XD2-149 down-regulate STAT3 level in a proteasome-independent manner. Proteomics data revealed that an E3 ligase, ZFP91, was the true substrate for this PROTAC. This paper reported a total of 22 PROTACs, which differed from each other in linker design and E3 binder choices (pomalidomide/thalidomide/lenalidomide). However, the authors didn't mention whether the remaining 21 molecules could degrade ZFP91 or not. It is also interesting that pomalidomide itself can induce the degradation of CRBN neo-substrates like ZFP91 (DC50: 0.42uM, 5-fold less potent than XD2-149), since pomalidomide can remodel CRBN surface for binding proteins like ZFP91 (Nat Med., 2019, doi: 10.1038/s41591-019-0668-z).",Yangwode Jing,~ 70 nM,> 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,~ 1 uM,other,10,3,,,Napabucasin,O=C(C1=C2C=C(C(C)=O)O1)C3=CC=CC=C3C2=O,CCCCCC1CCN(CCN)CC1,Other,14,2,6,693.7570000000003,No,,,,33506674,XD2-149,Yes,,Reviewed,Q96JP5,Yes,Yes,No,Yes,"16, 24",175.2
816,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCNC(CC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Inactive,No,KYSE520 esophageal cancer cell line,4.817920000000003,,Yangwode Jing,,,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CNC=O,Alkane,4,2,1,948.6169999999996,No,,5EHR,5OD,32437146,SHP2-D7,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
817,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCNC(CC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Inactive,No,KYSE520 esophageal cancer cell line,5.208020000000002,,Yangwode Jing,,,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCNC=O,Alkane,5,2,2,962.6439999999996,No,,5EHR,5OD,32437146,SHP2-D8,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
818,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCCNC(CC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Inactive,No,KYSE520 esophageal cancer cell line,5.598120000000003,,Yangwode Jing,,,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCNC=O,Alkane,6,2,3,976.6709999999995,No,,5EHR,5OD,32437146,SHP2-D9,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
819,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCCCNC(CC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Inactive,No,KYSE520 esophageal cancer cell line,5.988220000000004,,Yangwode Jing,,,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCNC=O,Alkane,7,2,4,990.6979999999995,No,,5EHR,5OD,32437146,SHP2-D10,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
820,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCCCCNC(CC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Inactive,No,KYSE520 esophageal cancer cell line,6.378320000000005,,Yangwode Jing,,,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCNC=O,Alkane,8,2,5,1004.7249999999995,No,,5EHR,5OD,32437146,SHP2-D11,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
821,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCCCCCNC(CC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Inactive,No,KYSE520 esophageal cancer cell line,6.768420000000005,Degradation rate: 20% (0.1uM compound) or 14% (1uM compound),Yangwode Jing,,,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCNC=O,Alkane,9,2,6,1018.7519999999994,No,,5EHR,5OD,32437146,SHP2-D12,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
822,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCCCCCCNC(CC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Active,No,KYSE520 esophageal cancer cell line,7.158520000000006,,Yangwode Jing,,80 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCNC=O,Alkane,10,2,7,1032.7789999999993,No,,5EHR,5OD,32437146,SHP2-D13,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
823,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCCCCCCCNC(CC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Active,No,KYSE520 esophageal cancer cell line,7.548620000000006,,Yangwode Jing,,> 95 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCCNC=O,Alkane,11,2,8,1046.8059999999991,No,,5EHR,5OD,32437146,SHP2-D14,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
824,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCCCCCCCCNC(CC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Active,No,KYSE520 esophageal cancer cell line,7.938720000000007,,Yangwode Jing,,> 95 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCCCNC=O,Alkane,12,2,9,1060.8329999999992,No,,5EHR,5OD,32437146,SHP2-D15,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
825,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCCCCCCCCCNC(CC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Active,No,KYSE520 esophageal cancer cell line,8.328820000000007,,Yangwode Jing,,> 95 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCCCCNC=O,Alkane,13,2,10,1074.859999999999,No,,5EHR,5OD,32437146,SHP2-D16,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
826,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCCCCCCCCNC(CCC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Active,No,KYSE520 esophageal cancer cell line,8.328820000000007,,Yangwode Jing,,> 95 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCCCNC(C)=O,Alkane,13,2,8,1074.859999999999,No,,5EHR,5OD,32437146,SHP2-D17,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
827,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCCCCCCCCCNC(CCC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Active,No,KYSE520 esophageal cancer cell line,8.718920000000006,,Yangwode Jing,,> 95 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCCCCNC(C)=O,Alkane,14,2,9,1088.886999999999,No,,5EHR,5OD,32437146,SHP2-D18,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
828,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(CCCCCCCCCCCNC(CCCC(NC4=CC=CC(SC5=NC=C(N=C5N)N6CCC(C)(CC6)N)=C4Cl)=O)=O)=O)=O,Active,No,KYSE520 esophageal cancer cell line,9.109020000000005,,Yangwode Jing,,> 95 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,14,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCCCCNC(=O)CC,Alkane,15,2,10,1102.913999999999,No,,5EHR,5OD,32437146,SHP2-D19,No,,Reviewed,Q06124,No,No,No,No,6,250.89000000000001
829,O=C([C@H]1N(C([C@H](NC(COCCOCCOCCNC(CCC(CCC(NC2=CC=CC(SC3=NC=C(N4CCC(CC4)(N)C)N=C3N)=C2Cl)=O)=O)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C,Active,No,KYSE520 esophageal cancer cell line; MV4;11 cell line,5.217020000000012,,Yangwode Jing,,> 95 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,18,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CC(=O)CCC(=O)NCCOCCOCCO,PEG,17,6,11,1136.8399999999992,No,,5EHR,5OD,32437146,SHP2-D20,No,,Reviewed,Q06124,No,No,No,No,6,295.6499999999999
830,O=C([C@H]1N(C([C@H](NC(CCOCCOCCOCCNC(CCC(CCC(NC2=CC=CC(SC3=NC=C(N4CCC(CC4)(N)C)N=C3N)=C2Cl)=O)=O)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C,Active,No,KYSE520 esophageal cancer cell line; MV4;11 cell line,5.607120000000012,Degradation rate for KYSE520 cell: 87% (1uM compound); Degradation rate for MV4;11 cell: 85% (0.1uM compound),Yangwode Jing,,,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,18,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,COCCOCCOCCNC(=O)CCC(C)=O,PEG,18,6,12,1150.8669999999993,No,,5EHR,5OD,32437146,SHP2-D21,No,,Reviewed,Q06124,No,No,No,No,6,295.6499999999999
831,O=C([C@H]1N(C([C@H](NC(CCOCCOCCOCCOCCNC(CCC(CCC(NC2=CC=CC(SC3=NC=C(N4CCC(CC4)(N)C)N=C3N)=C2Cl)=O)=O)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C,Active,No,KYSE520 esophageal cancer cell line; MV4;11 cell line,5.623720000000012,,Yangwode Jing,,> 95 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,19,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,COCCOCCOCCOCCNC(=O)CCC(C)=O,PEG,21,7,15,1194.9199999999992,No,,5EHR,5OD,32437146,SHP2-D22,No,,Reviewed,Q06124,No,No,No,No,6,304.88
832,O=C([C@H]1N(C([C@H](NC(CCCCCCCCCCN2CCN(CC2)CC(NC3=CC=CC(SC4=NC=C(N5CCC(CC5)(N)C)N=C4N)=C3Cl)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C,Active,No,KYSE520 esophageal cancer cell line; MV4;11 cell line,8.050020000000009,Dmax for KYSE520 cell: >95%; Degradation rate in MV4;11 cell: 47% (0.1uM compound),Yangwode Jing,,,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,other,15,6,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCCCN1CCNCC1,Other,15,2,8,1101.9299999999992,No,,5EHR,5OD,32437146,SHP2-D23,No,,Reviewed,Q06124,No,No,No,No,6,228.26999999999998
833,O=C([C@H]1N(C([C@H](NC(CCCCCCCCCCCN2CCN(CC2)CC(NC3=CC=CC(SC4=NC=C(N5CCC(CC5)(N)C)N=C4N)=C3Cl)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C,Active,No,KYSE520 esophageal cancer cell line; MV4;11 cell line,8.440120000000006,Dmax for KYSE520 cell: >95%; Degradation rate in MV4;11 cell: 6% (0.1uM compound),Yangwode Jing,,,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,other,15,6,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCCCCN1CCNCC1,Other,16,2,9,1115.9569999999992,No,,5EHR,5OD,32437146,SHP2-D24,No,,Reviewed,Q06124,No,No,No,No,6,228.26999999999998
834,O=C([C@H]1N(C([C@H](NC(CCCCCCCCCCCCCCC(NC2=CC=CC(SC3=NC=C(N4CCC(CC4)(N)C)N=C3N)=C2Cl)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C,Active,No,KYSE520 esophageal cancer cell line; MV4;11 cell line,10.382919999999995,Degradation rate in KYSE520 cell: 90% (1uM compound); Degradation rate in MV4;11 cell: 8% (0.1uM compound),Yangwode Jing,,,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,13,6,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCCCCCC,Alkane,12,0,9,1059.8889999999992,No,,5EHR,5OD,32437146,SHP2-D25,No,,Reviewed,Q06124,No,No,No,No,6,221.78999999999996
835,O=C([C@H]1N(C([C@H](NC(CCCCCCCCN2CCN(C(CCC(NC3=CC=CC(SC4=NC=C(N5CCC(CC5)(N)C)N=C4N)=C3Cl)=O)=O)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C,Active,Yes,KYSE520 esophageal cancer cell line; MV4;11 cell line,7.576620000000008,DC50 for KYSE520 cell: 6.0nM;DC50 for MV4;11 cell: 2.6nM; EC50 for KYSE520 cell: 0.66uM; EC50 for MV4;11 cell: 9.9nM;,Yangwode Jing,6.0 nM,100 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,0.66 uM,aliphatic_CC,15,6,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCN1CCN(C(C)=O)CC1,Other,16,3,6,1115.912999999999,No,,5EHR,5OD,32437146,SHP2-D26,No,,Reviewed,Q06124,No,Yes,No,Yes,"6, 12",245.33999999999997
836,O=C([C@H]1N(C([C@H](NC(CCCCCCCCCN2CCN(C(CCC(NC3=CC=CC(SC4=NC=C(N5CCC(CC5)(N)C)N=C4N)=C3Cl)=O)=O)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C,Active,No,KYSE520 esophageal cancer cell line; MV4;11 cell line,7.9667200000000085,,Yangwode Jing,,> 95 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,15,6,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCCCN1CCN(C(C)=O)CC1,Other,17,3,7,1129.939999999999,No,,5EHR,5OD,32437146,SHP2-D27,No,,Reviewed,Q06124,No,No,No,No,6,245.33999999999997
837,O=C([C@H]1N(C([C@H](NC(CCCCCCCN2CCN(C(CCC(NC3=CC=CC(SC4=NC=C(N5CCC(CC5)(N)C)N=C4N)=C3Cl)=O)=O)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C,Active,No,KYSE520 esophageal cancer cell line; MV4;11 cell line,7.186520000000008,Dmax for KYSE520 cell: >95%; Dmax for MV4;11 cell: >90%,Yangwode Jing,,> 95 %,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,15,6,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCCCCN1CCN(C(C)=O)CC1,Other,15,3,5,1101.885999999999,No,,5EHR,5OD,32437146,SHP2-D28,No,,Reviewed,Q06124,No,No,No,No,6,245.33999999999997
838,O=C([C@H]1N(C([C@H](NC(CCCCN2CCN(CCCCNC(CCC(NC3=CC=CC(SC4=NC=C(N5CCC(CC5)(N)C)N=C4N)=C3Cl)=O)=O)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C,Active,No,KYSE520 esophageal cancer cell line; MV4;11 cell line,6.386020000000012,Dmax for KYSE520 cell: >80%; Degradation rate for MV4;11 cell: 9% (0.1uM compound),Yangwode Jing,,,O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](C(C)(C)C)NC(C)=O)=O,VHL,,,aliphatic_CC,16,7,98.7 nM,,SHP2 inhibitor 5,ClC1=C(C=CC=C1NC(C)=O)SC2=NC=C(N=C2N)N3CCC(C)(CC3)N,CCCN1CCN(CCCCNC(C)=O)CC1,Other,17,4,7,1130.927999999999,No,,5EHR,5OD,32437146,SHP2-D29,No,,Reviewed,Q06124,No,No,No,No,6,257.36999999999995
839,ClC1=CC=C(C2=N[C@H](C3=NN=C(N3C4=C2C(C)=C(S4)C)C)CC(NCCOCCOCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@@H](O)C5)C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)C=C1,Active,No,"HeLa, HL60, MV4;11",5.580080000000005,"pEC50 for MV4;11 and HL60 cells: 6.75±0.03 and 5.84±0.06, respectively.
pDC50 for Brd4 short/Brd4 long/Brd3/Brd2: 7.0/7.0/6.5/6.2, respectively (24h, HeLa cells).
Dmax for Brd4 short/Brd4 long/Brd3/Brd2: 96%/97%/97%/93%, respectively (HeLa cells).",Yangwode Jing,< 0.1 uM,> 93 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,~ 1 uM,ester_to_amide,14,4,,,JQ1,ClC1=CC=C(C2=N[C@H](C3=NN=C(N3C4=C2C(C)=C(S4)C)C)CC(OC(C)(C)C)=O)C=C1,NCCOCCOCC=O,PEG,10,4,7,958.608,No,,3MXF,JQ1,28595007,MZ4,No,,Reviewed,"O60885, P25440, Q15059",No,No,No,No,"4, 24, 48",202.26
840,ClC1=CC=C(C2=N[C@H](C3=NN=C(N3C4=C2C(C)=C(S4)C)C)CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@@H](O)C5)C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)C=C1,Active,Yes,"HeLa, HL60, MV4;11",5.596680000000004,"pEC50 for MV4;11 and HL60 cells: 7.57±0.03 and 6.66±0.05, respectively. pDC50 for Brd4 short/Brd4 long/Brd3/Brd2: 8.1/8.6/7.0/7.4, respectively (24h, HeLa cells). Dmax for Brd4 short/Brd4 long/Brd3/Brd2: 98%/100%/100%/98%, respectively (HeLa cells).",Yangwode Jing,< 2.5 nM,> 98 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,~ 0.1 uM,ester_to_amide,15,4,,,JQ1,ClC1=CC=C(C2=N[C@H](C3=NN=C(N3C4=C2C(C)=C(S4)C)C)CC(OC(C)(C)C)=O)C=C1,NCCOCCOCCOCC=O,PEG,13,5,10,1002.661,No,,3MXF,JQ1,28595007,MZ1,No,,Reviewed,"O60885, P25440, Q15059",No,No,No,No,"4, 24, 48",211.48999999999995
841,ClC1=CC=C(C2=N[C@H](C3=NN=C(N3C4=C2C(C)=C(S4)C)C)CC(NCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@@H](O)C5)C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)C=C1,Active,No,"HeLa, HL60, MV4;11",5.613280000000005,"pEC50 for MV4;11 and HL60 cells: 6.91±0.04 and 5.90±0.05, respectively. pDC50 for Brd4 short/Brd4 long/Brd3/Brd2: 8.4/8.0/6.5/6.7, respectively (24h, HeLa cells). Dmax for Brd4 short/Brd4 long/Brd3/Brd2: 99%/100%/99%/97%, respectively (HeLa cells).",Yangwode Jing,< 4 nM,> 97 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,~ 0.4 uM,ester_to_amide,16,4,,,JQ1,ClC1=CC=C(C2=N[C@H](C3=NN=C(N3C4=C2C(C)=C(S4)C)C)CC(OC(C)(C)C)=O)C=C1,NCCOCCOCCOCCOCC=O,PEG,16,6,13,1046.714,No,,3MXF,JQ1,28595007,MZ2,No,,Reviewed,"O60885, P25440, Q15059",No,No,No,No,"4, 24, 48",220.71999999999997
842,CC1=NN=C2N1C3=C(C(C4=CC=C(C=C4)Cl)=N[C@H]2CC(NC5=CC=C(C=C5)OCCOCCOCCOCCNC6=C(C7=CC=C6)C(N(C7=O)C8CCC(NC8=O)=O)=O)=O)C(C)=C(C)S3,Active,No,"HeLa, HL60, MV4;11",5.770260000000005,"pEC50 for MV4;11 and HL60 cells: 7.77±0.06 and 7.46±0.03, respectively. pDC50 for Brd4 short/Brd4 long/Brd3/Brd2: 9.2/9.0/9.1/8.2, respectively (24h, HeLa cells). Dmax for Brd4 short/Brd4 long/Brd3/Brd2: 97%/100%/98%/83%, respectively (HeLa cells).",Yangwode Jing,< 1 nM,> 83 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,~ 32 nM,ester_to_amide,15,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,CCOCCOCCOCCOc1ccc(N)cc1,PEG,19,5,11,923.4489999999998,No,,3MXF,JQ1,28595007,ARV-825,No,,Reviewed,"O60885, P25440, Q15059",No,No,No,No,"4, 24, 48",204.67
843,O=C(NCCOCCOCC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@@H](O)C1)C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O)C4=CC=C(C5=CC6=C(N(C(C)=O)[C@@H](C)C[C@H]6NC7=CC=C(Cl)C=C7)C=C5)C=C4,Active,No,"HeLa, HL60, MV4;11",7.309320000000011,"pEC50 for MV4;11 and HL60 cells: 6.24±0.05 and 6.17±0.03, respectively. pDC50 for Brd4 short/Brd4 long/Brd3/Brd2: 6.9/6.7/6.8/NA, respectively (24h, HeLa cells). Dmax for Brd4 short/Brd4 long/Brd3/Brd2: 94%/78%/74%/37%, respectively (HeLa cells).",Yangwode Jing,~ 0.1 uM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,~ 1 uM,carboxilic_acid_to_amide,11,5,~ 30 nM,,I-BET726,O=C(O)C1=CC=C(C2=CC3=C(N(C(C)=O)[C@@H](C)C[C@H]3NC4=CC=C(Cl)C=C4)C=C2)C=C1,NCCOCCOCC=O,PEG,10,4,7,992.64,No,,4BJX,73B,28595007,MZP-61,No,,Reviewed,"O60885, Q15059",No,No,No,No,"4, 24, 48",191.53
844,O=C(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@@H](O)C1)C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O)C4=CC=C(C5=CC6=C(N(C(C)=O)[C@@H](C)C[C@H]6NC7=CC=C(Cl)C=C7)C=C5)C=C4,Active,No,"HeLa, HL60, MV4;11",7.325920000000011,"pEC50 for MV4;11 and HL60 cells: 7.31±0.03 and 6.57±0.02, respectively. pDC50 for Brd4 short/Brd4 long/Brd3/Brd2: 8.1/7.6/7.3/NA, respectively (24h, HeLa cells). Dmax for Brd4 short/Brd4 long/Brd3/Brd2: 98%/95%/91%/43%, respectively (HeLa cells).",Yangwode Jing,~ 7.9 nM,> 90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,~ 0.1 uM,carboxilic_acid_to_amide,12,5,~ 30 nM,,I-BET726,O=C(O)C1=CC=C(C2=CC3=C(N(C(C)=O)[C@@H](C)C[C@H]3NC4=CC=C(Cl)C=C4)C=C2)C=C1,NCCOCCOCCOCC=O,PEG,13,5,10,1036.693,No,,4BJX,73B,28595007,MZP-54,No,,Reviewed,"O60885, Q15059",No,No,No,No,"4, 24, 48",200.76
845,O=C(NCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@@H](O)C1)C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O)C4=CC=C(C5=CC6=C(N(C(C)=O)[C@@H](C)C[C@H]6NC7=CC=C(Cl)C=C7)C=C5)C=C4,Active,No,"HeLa, HL60, MV4;11",7.342520000000013,"pEC50 for MV4;11 and HL60 cells: 7.08±0.05 and 6.37±0.03, respectively. pDC50 for Brd4 short/Brd4 long/Brd3/Brd2: 8.1/7.5/7.7/NA, respectively (24h, HeLa cells). Dmax for Brd4 short/Brd4 long/Brd3/Brd2: 95%/93%/92%/26%, respectively (HeLa cells).",Yangwode Jing,~ 7.9 nM,> 90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,~ 0.25 uM,carboxilic_acid_to_amide,13,5,,,I-BET726,O=C(O)C1=CC=C(C2=CC3=C(N(C(C)=O)[C@@H](C)C[C@H]3NC4=CC=C(Cl)C=C4)C=C2)C=C1,NCCOCCOCCOCCOCC=O,PEG,16,6,13,1080.7459999999999,No,,4BJX,73B,28595007,MZP-55,No,,Reviewed,"O60885, Q15059",No,No,No,No,"4, 24, 48",209.99
846,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H]3N(C([C@H](C(C)(C)C)NC(COCCOCCOCCOCC(N[C@H](C(C)(C)C)C(N4[C@H](C[C@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O)=O)C[C@H](O)C3,Active,No,"HeLa, HEK293, U2OS",3.5348400000000106,,Yangwode Jing,< 1 uM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_amide,16,6,,,Vh032,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H]3N(C([C@H](C(C)(C)C)N)=O)C[C@H](O)C3,O=CCOCCOCCOCCOCC=O,PEG,16,6,13,1091.364,No,,5LLI,6Z3,29018234,CM09,Yes,,Reviewed,P40337,Yes,No,No,No,"4, 10, 24, 48",260.18
847,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H]3N(C([C@H](C(C)(C)C)NC(COCCOCCOCCOCCOCC(N[C@H](C(C)(C)C)C(N4[C@H](C[C@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O)=O)C[C@H](O)C3,Active,No,"HeLa, HEK293, U2OS",3.551440000000012,,Yangwode Jing,< 0.1 uM,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_amide,17,6,,,Vh032,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H]3N(C([C@H](C(C)(C)C)N)=O)C[C@H](O)C3,O=CCOCCOCCOCCOCCOCC=O,PEG,19,7,16,1135.417,No,,5LLI,6Z3,29018234,CM10,Yes,,Reviewed,P40337,Yes,No,No,No,"4, 10, 24, 48",269.41
848,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H]3N(C([C@H](C(C)(C)C)NC(COCCOCCOCCOCCOCCOCC(N[C@H](C(C)(C)C)C(N4[C@H](C[C@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O)=O)C[C@H](O)C3,Active,Yes,"HeLa, HEK293, U2OS",3.568040000000013,ITC/SEC/AlphaLISA assays were carried out for CM09/10/11 to confirm the formation of ternary complex in vitro.,Yangwode Jing,< 100 nM,100 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_amide,18,6,,,Vh032,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H]3N(C([C@H](C(C)(C)C)N)=O)C[C@H](O)C3,O=CCOCCOCCOCCOCCOCCOCC=O,PEG,22,8,19,1179.47,No,,5LLI,6Z3,29018234,CM11,Yes,,Reviewed,P40337,Yes,Yes,No,Yes,"4, 10, 24, 48",278.64
849,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1OCCOCCOCCOCCOCCOC3=C(CNC([C@H]4N(C([C@H](C(C)(C)C)NC(C)=O)=O)C[C@H](O)C4)=O)C=CC(C5=C(C)N=CS5)=C3)[C@@H]6N(C([C@@H](C(C)(C)C)NC(C)=O)=O)C[C@@H](O)C6,Inactive,No,HeLa,4.332240000000012,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,"['amine_to_amide', 'aryl_O']",18,6,,,Vh032,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H]3N(C([C@H](C(C)(C)C)N)=O)C[C@H](O)C3,OCCOCCOCCOCCOCCO,PEG,16,6,13,1179.47,No,,5LLI,6Z3,29018234,CMP106,No,,Reviewed,P40337,No,No,No,No,10,278.64000000000004
850,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@@H]3N(C([C@@H](C(C)(C)C)NC(COCCOCCOCCOCCOCCOC4=C(CNC([C@H]5N(C([C@H](C(C)(C)C)NC(C)=O)=O)C[C@H](O)C5)=O)C=CC(C6=C(C)N=CS6)=C4)=O)=O)C[C@@H](O)C3,Inactive,No,HeLa,3.9501400000000126,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,"['amine_to_amide', 'aryl_O']",18,6,,,Vh032,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H]3N(C([C@H](C(C)(C)C)N)=O)C[C@H](O)C3,O=CCOCCOCCOCCOCCOCCO,PEG,19,7,16,1179.47,No,,5LLI,6Z3,29018234,CMP112,No,,Reviewed,P40337,No,No,No,No,10,278.64
851,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1OCCOCCOCCOCCOCCOC3=C(CNC([C@H]4N(C([C@H](C(C)(C)C)NC(C5(C#N)CC5)=O)=O)C[C@H](O)C4)=O)C=CC(C6=C(C)N=CS6)=C3)[C@@H]7N(C([C@@H](C(C)(C)C)NC(C8(C#N)CC8)=O)=O)C[C@@H](O)C7,Inactive,No,HeLa,4.900000000000013,,Yangwode Jing,,,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@@H]3N(C([C@@H](C(C)(C)C)NC(C4(C#N)CC4)=O)=O)C[C@@H](O)C3,VHL,,,aryl_O,20,6,,,Vh298,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@@H]3N(C([C@@H](C(C)(C)C)NC(C4(C#N)CC4)=O)=O)C[C@@H](O)C3,OCCOCCOCCOCCOCCO,PEG,16,6,13,1281.5659999999998,No,,5LLI,6Z3,29018234,CMP108,No,,Reviewed,P40337,No,No,No,No,10,326.21999999999997
852,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@@H]3N(C([C@@H](C(C)(C)C)NC(COCCOCCOCCOCCOCCOC4=C(CNC([C@H]5N(C([C@H](C(C)(C)C)NC(C6(C#N)CC6)=O)=O)C[C@H](O)C5)=O)C=CC(C7=C(C)N=CS7)=C4)=O)=O)C[C@@H](O)C3,Inactive,No,HeLa,4.2340200000000126,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,19,6,,,Vh298,O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@@H]3N(C([C@@H](C(C)(C)C)NC(C4(C#N)CC4)=O)=O)C[C@@H](O)C3,OCCOCCOCCOCCOCCO,PEG,16,6,13,1230.5179999999998,No,,5LLI,6Z3,29018234,CMP113,No,,Reviewed,P40337,No,No,No,No,10,302.43
853,O=C(C1=CC=C2C(N=C(NC3=CC=CC(Cl)=C3)C4=C2C=NC=C4)=C1)OCCC5=CN(N=N5)CC(NC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O,Active,No,"MDA-MB-231, A549, A549/DDP, HUVEC",4.210900000000003,"EC50 of PROTAC1: 22.56±1.89uM/25.75±0.91uM/79.51±3.10uM/29.92±1.81uM for MDA-MB-231, A549, A549/DDP, HUVEC cells, respectively (MTT assay, 72h).",Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_ester,13,3,,,CX-4945,O=C(C1=CC=C2C(N=C(NC3=CC=CC(Cl)=C3)C4=C2C=NC=C4)=C1)O,CCc1cn(CC=O)nn1,Other,10,4,3,758.1510000000001,No,,3PE1 6HMB,3NG,30245235,1,No,,Reviewed,P68400,No,No,No,No,"24, 72",207.46999999999997
854,O=C(C1=CC=C2C(N=C(NC3=CC=CC(Cl)=C3)C4=C2C=NC=C4)=C1)OCCCC5=CN(N=N5)CC(NC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O,Active,Yes,"MDA-MB-231, A549, A549/DDP, HUVEC",4.601000000000004,"EC50 of PROTAC2: 17.36±1.43uM/31.19±2.95uM/57.55±4.20uM/34.39±2.99uM for MDA-MB-231, A549, A549/DDP, HUVEC cells, respectively (MTT assay, 72h).",Yangwode Jing,,> 80 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_ester,13,3,,,CX-4945,O=C(C1=CC=C2C(N=C(NC3=CC=CC(Cl)=C3)C4=C2C=NC=C4)=C1)O,CCCc1cn(CC=O)nn1,Other,11,4,4,772.1780000000001,No,,3PE1 6HMB,3NG,30245235,2,No,,Reviewed,P68400,No,No,No,Yes,"24, 72",207.46999999999997
855,O=C(C1=CC=C2C(N=C(NC3=CC=CC(Cl)=C3)C4=C2C=NC=C4)=C1)OCCCCCC5=CN(N=N5)CC(NC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O,Active,No,"MDA-MB-231, A549, A549/DDP, HUVEC",5.381200000000006,"EC50 of PROTAC3: 21.32±1.85uM/29.77±0.84uM/30.68±2.45uM/33.92±2.84uM for MDA-MB-231, A549, A549/DDP, HUVEC cells, respectively (MTT assay, 72h).",Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_ester,13,3,,,CX-4945,O=C(C1=CC=C2C(N=C(NC3=CC=CC(Cl)=C3)C4=C2C=NC=C4)=C1)O,CCCCCc1cn(CC=O)nn1,Other,13,4,6,800.2320000000001,No,,3PE1 6HMB,3NG,30245235,3,No,,Reviewed,P68400,No,No,No,No,"24, 72",207.46999999999997
856,O=C(C1=CC=C2C(N=C(NC3=CC=CC(Cl)=C3)C4=C2C=NC=C4)=C1)OCCOCC5=CN(N=N5)CC(NC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O,Active,No,"MDA-MB-231, A549, A549/DDP, HUVEC",4.185000000000004,"EC50 of PROTAC4: 31.67±2.97uM/36.46±0.52uM/>200uM/37.13±2.52uM for MDA-MB-231, A549, A549/DDP, HUVEC cells, respectively (MTT assay, 72h).",Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_ester,14,3,,,CX-4945,O=C(C1=CC=C2C(N=C(NC3=CC=CC(Cl)=C3)C4=C2C=NC=C4)=C1)O,CCOCc1cn(CC=O)nn1,Other,12,5,5,788.177,No,,3PE1 6HMB,3NG,30245235,4,No,,Reviewed,P68400,No,No,No,No,"24, 72",216.7
857,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Inactive,No,HeLa,0.90672000000001,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,15,6,1.2 uM,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)COCCOCCOCC=O,PEG,16,6,11,933.054,No,,4CI3,Y70,30826187,7a,No,,Reviewed,Q96SW2,No,No,No,No,4,264.0
858,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Inactive,No,HeLa,0.9399200000000099,7b can degrade VHL at higher concentration. See Target UniprotID P40337 for details.,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,17,6,1.2 uM,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)COCCOCCOCCOCCOCC=O,PEG,22,8,17,1021.1599999999999,Yes,,4CI3,Y70,30826187,7b,No,,Reviewed,Q96SW2,No,No,No,No,4,282.46
859,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCCCCOCCOCCCCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Active,Yes,"HeLa, HEK293",3.2639200000000104,Reported DC50 and Dmax above are in HeLa cells. DC50 for HEK293 cells: 230nM; Dmax for HEK293 cells: 98%. 14a can degrade VHL at higher concentration. See Target UniprotID P40337 for details.,Yangwode Jing,200 nM,88 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,16,6,1.2 uM,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)COCCCCCOCCOCCCCCOCC=O,non-PEG polyether,25,7,20,1061.2689999999996,Yes,,4CI3,Y70,30826187,14a,No,,Reviewed,Q96SW2,No,No,No,No,4,273.22999999999996
860,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCCCCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Active,No,HeLa,2.450520000000008,14b can degrade VHL at higher concentration. See Target UniprotID P40337 for details.,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,14,6,1.2 uM,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)COCCCCCCOCC=O,non-PEG polyether,17,5,12,945.109,Yes,,4CI3,Y70,30826187,14b,No,,Reviewed,Q96SW2,No,No,No,No,4,254.76999999999998
861,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Inactive,No,HeLa,0.9565200000000094,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,18,6,1.2 uM,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)COCCOCCOCCOCCOCCOCC=O,PEG,25,9,20,1065.2129999999997,No,,4CI3,Y70,30826187,14c,No,,Reviewed,Q96SW2,No,No,No,No,4,291.68999999999994
862,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOCCOCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Inactive,No,HeLa,1.0063200000000043,14d can degrade VHL at higher concentration. See Target UniprotID P40337 for details.,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,21,6,1.2 uM,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)COCCOCCOCCOCCOCCOCCOCCOCCOCC=O,PEG,34,12,29,1197.3719999999994,Yes,,4CI3,Y70,30826187,14d,No,,Reviewed,Q96SW2,No,No,No,No,4,319.37999999999994
863,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Inactive,No,HeLa,0.9233200000000112,14e can degrade VHL at higher concentration. See Target UniprotID P40337 for details.,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,16,6,1.2 uM,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)COCCOCCOCCOCC=O,PEG,19,7,14,977.107,Yes,,4CI3,Y70,30826187,14e,No,,Reviewed,Q96SW2,No,No,No,No,4,273.22999999999996
864,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOC4=CC(C5=C(C)N=CS5)=CC=C4CNC([C@H]6N(C([C@@H](NC(C7(F)CC7)=O)C(C)(C)C)=O)C[C@H](O)C6)=O)=O,Active,No,HeLa,1.7876200000000084,,Yangwode Jing,,,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,VHL,,,amine_to_methylamine,16,6,,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)COCCOCCOCC,PEG,15,5,10,1021.1349999999999,No,,4CI3,Y70,30826187,18a,No,,Reviewed,Q96SW2,No,No,No,No,4,273.23
865,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOCCOCCOC4=CC(C5=C(C)N=CS5)=CC=C4CNC([C@H]6N(C([C@@H](NC(C7(F)CC7)=O)C(C)(C)C)=O)C[C@H](O)C6)=O)=O,Active,No,HeLa,1.8208200000000119,,Yangwode Jing,,,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,VHL,,,amine_to_methylamine,18,6,,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)COCCOCCOCCOCCOCC,PEG,21,7,16,1109.241,No,,4CI3,Y70,30826187,18b,No,,Reviewed,Q96SW2,No,No,No,No,4,291.69
866,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(CCCCOC4=CC(C5=C(N=CS5)C)=CC=C4CNC([C@@H]6C[C@H](CN6C([C@H](C(C)(C)C)NC(C7(CC7)F)=O)=O)O)=O)=O,Inactive,No,HeLa,2.9081200000000025,18c can degrade VHL at higher concentration. See Target UniprotID P40337 for details.,Yangwode Jing,,,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,VHL,,,amine_to_methylamine,13,6,,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCCCC(=O)NCC,Alkane,9,2,4,931.0569999999998,Yes,,4CI3,Y70,30826187,18c,No,,Reviewed,Q96SW2,No,No,No,No,4,245.54
867,O=C(NCCNC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O)COCCOCCOCCSC(C)([C@@H](C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)NC(C7(CC7)F)=O)C,Active,No,HeLa,1.874520000000009,,Yangwode Jing,,,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,VHL,,,amine_to_methylamine,16,6,,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)COCCOCCOCCS,PEG,16,5,11,1023.1759999999998,No,,4CI3,Y70,30826187,22a,No,,Reviewed,Q96SW2,No,No,No,No,4,263.99999999999994
868,O=C(NCCNC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O)COCCOCCOCCOCCOCCSC(C)([C@@H](C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)NC(C7(CC7)F)=O)C,Active,No,HeLa,1.9077200000000116,,Yangwode Jing,,,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,VHL,,,amine_to_methylamine,18,6,,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)COCCOCCOCCOCCOCCS,PEG,22,7,17,1111.282,No,,4CI3,Y70,30826187,22b,No,,Reviewed,Q96SW2,No,No,No,No,4,282.4599999999999
869,O=C(NCCNC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O)CCCCSC(C)([C@@H](C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)NC(C7(CC7)F)=O)C,Inactive,No,HeLa,2.995020000000004,22c can degrade VHL at higher concentration. See Target UniprotID P40337 for details.,Yangwode Jing,,,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,VHL,,,amine_to_methylamine,13,6,,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCNC(=O)CCCCS,Other,10,2,5,933.0980000000001,Yes,,4CI3,Y70,30826187,22c,No,,Reviewed,Q96SW2,No,No,No,No,4,236.30999999999995
870,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Inactive,No,HeLa,0.90672000000001,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,15,6,,,Vh032,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,CCNC(=O)COCCOCCOCC=O,PEG,16,6,11,933.054,No,,6GFZ,EXE,30826187,7a,No,,Reviewed,P40337,No,No,No,No,4,264.0
871,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Active,No,HeLa,0.9399200000000099,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,17,6,,,Vh032,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,CCNC(=O)COCCOCCOCCOCCOCC=O,PEG,22,8,17,1021.1599999999999,No,,6GFZ,EXE,30826187,7b,No,,Reviewed,P40337,No,No,No,No,4,282.46
872,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCCCCOCCOCCCCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Active,No,HeLa,3.2639200000000104,14a can degrade Cereblon at lower concentration. See Target UniprotID Q96SW2 for details.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,16,6,,,Vh032,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,CCNC(=O)COCCCCCOCCOCCCCCOCC=O,non-PEG polyether,25,7,20,1061.2689999999996,Yes,,6GFZ,EXE,30826187,14a,No,,Reviewed,P40337,No,No,No,No,4,273.22999999999996
873,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCCCCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Active,No,HeLa,2.450520000000008,14b can degrade Cereblon at lower concentration. See Target UniprotID Q96SW2 for details.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,14,6,,,Vh032,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,CCNC(=O)COCCCCCCOCC=O,non-PEG polyether,17,5,12,945.109,Yes,,6GFZ,EXE,30826187,14b,No,,Reviewed,P40337,No,No,No,No,4,254.76999999999998
874,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Inactive,No,HeLa,0.9565200000000094,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,18,6,,,Vh032,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,CCNC(=O)COCCOCCOCCOCCOCCOCC=O,PEG,25,9,20,1065.2129999999997,No,,6GFZ,EXE,30826187,14c,No,,Reviewed,P40337,No,No,No,No,4,291.68999999999994
875,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOCCOCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Active,No,HeLa,1.0063200000000043,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,21,6,,,Vh032,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,CCNC(=O)COCCOCCOCCOCCOCCOCCOCCOCCOCC=O,PEG,34,12,29,1197.3719999999994,No,,6GFZ,EXE,30826187,14d,No,,Reviewed,P40337,No,No,No,No,4,319.37999999999994
876,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O,Active,No,HeLa,0.9233200000000112,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,16,6,,,Vh032,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,CCNC(=O)COCCOCCOCCOCC=O,PEG,19,7,14,977.107,No,,6GFZ,EXE,30826187,14e,No,,Reviewed,P40337,No,No,No,No,4,273.22999999999996
877,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOC4=CC(C5=C(C)N=CS5)=CC=C4CNC([C@H]6N(C([C@@H](NC(C7(F)CC7)=O)C(C)(C)C)=O)C[C@H](O)C6)=O)=O,Inactive,No,HeLa,1.7876200000000084,18a can degrade Cereblon at lower concentration. See Target UniprotID Q96SW2 for details.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,6,,,Vh101,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,CCNC(=O)COCCOCCOCC,PEG,15,5,10,1021.1349999999999,Yes,,5LLI,6Z3,30826187,18a,No,,Reviewed,P40337,No,No,No,No,4,273.23
878,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(COCCOCCOCCOCCOCCOC4=CC(C5=C(C)N=CS5)=CC=C4CNC([C@H]6N(C([C@@H](NC(C7(F)CC7)=O)C(C)(C)C)=O)C[C@H](O)C6)=O)=O,Inactive,No,HeLa,1.8208200000000119,18b can degrade Cereblon at lower concentration. See Target UniprotID Q96SW2 for details.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,6,,,Vh101,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,CCNC(=O)COCCOCCOCCOCCOCC,PEG,21,7,16,1109.241,Yes,,5LLI,6Z3,30826187,18b,No,,Reviewed,P40337,No,No,No,No,4,291.69
879,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCCNC(CCCCOC4=CC(C5=C(N=CS5)C)=CC=C4CNC([C@@H]6C[C@H](CN6C([C@H](C(C)(C)C)NC(C7(CC7)F)=O)=O)O)=O)=O,Active,No,HeLa,2.9081200000000025,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,6,,,Vh101,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,CCCCC(=O)NCC,Alkane,9,2,4,931.0569999999998,No,,5LLI,6Z3,30826187,18c,No,,Reviewed,P40337,No,No,No,No,4,245.54
880,O=C(NCCNC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O)COCCOCCOCCSC(C)([C@@H](C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)NC(C7(CC7)F)=O)C,Inactive,No,HeLa,1.874520000000009,22a can degrade Cereblon at lower concentration. See Target UniprotID Q96SW2 for details.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,6,,,Vh101,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,CCNC(=O)COCCOCCOCCS,PEG,16,5,11,1023.1759999999998,Yes,,5LLI,6Z3,30826187,22a,No,,Reviewed,P40337,No,No,No,No,4,263.99999999999994
881,O=C(NCCNC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O)COCCOCCOCCOCCOCCSC(C)([C@@H](C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)NC(C7(CC7)F)=O)C,Inactive,No,HeLa,1.9077200000000116,22b can degrade Cereblon at lower concentration. See Target UniprotID Q96SW2 for details.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,6,,,Vh101,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,CCNC(=O)COCCOCCOCCOCCOCCS,PEG,22,7,17,1111.282,Yes,,5LLI,6Z3,30826187,22b,No,,Reviewed,P40337,No,No,No,No,4,282.4599999999999
882,O=C(NCCNC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O)CCCCSC(C)([C@@H](C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)NC(C7(CC7)F)=O)C,Active,No,HeLa,2.995020000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,6,,,Vh101,O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3O,CCNC(=O)CCCCS,Other,10,2,5,933.0980000000001,No,,5LLI,6Z3,30826187,22c,No,,Reviewed,P40337,No,No,No,No,4,236.30999999999995
883,ClCC(N(CC1=CC=CC=C1)C2=CC=C(OC3=CC=C(OCCCCNC(C[C@@H](C4=NN=C(N4C5=C6C(C)=C(S5)C)C)N=C6C(C=C7)=CC=C7Cl)=O)C=C3)C=C2)=O,Active,Yes,"231MFP breast cancer cells, HeLa",9.729359999999998,,Yangwode Jing,,> 50 %,ClCC(N(CC1=CC=CC=C1)C2=CC=C(OC3=CC=C(OC)C=C3)C=C2)=O,RNF4,,,ester_to_amide,9,1,,0.54 uM,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,CCCN,Alkane,4,1,1,821.8310000000002,"Yes, MT2A, ZC2HC1A, ZNF367, and ENSA were also down-regulated",,3MXF 3ONI,JQ1,31059647,CCW 28-3,Yes,,Reviewed,O60885,No,Yes,No,Yes,3,110.94
884,O=C(N1C2C(NC(CC2)=O)=O)C(C=CC=C3NCCOCCOCCNC4=CC=CC(C(N5C6C(NC(CC6)=O)=O)=O)=C4C5=O)=C3C1=O,Active,Yes,MM1S,0.04620000000000385,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,12,4,,,Pomalidomide,NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O,CCOCCOCC,PEG,8,2,5,660.6400000000002,No,,4CI3,Y70,31157769,8,No,,Reviewed,Q96SW2,Yes,Yes,No,Yes,"3, 24, 48, 96",209.61999999999998
885,ClC1=CC=C(C2=N[C@H](C3=NN=C(N3C4=C2C(C)=C(S4)C)C)CC(NCCCNC(C5=CC=C(C(OC=C6)=C6[C@@H]7C[C@@]([H])(O[C@]([C@@]8([H])C9[C@]%10(C)C(C=C[C@@]9(C)C(O8)=O)=O)([C@]%11(C)[C@@H]%10CC(OC)=O)[H])C%11=C7C)C=C5)=O)=O)C=C1,Active,Yes,231MFP,8.849460000000004,IC50: 0.24±0.12 uM,"Yangwode Jing, Nir London",,,CC1=C2[C@](O[C@]([C@@]3([H])C4[C@]5(C)C(C=C[C@@]4(C)C(O3)=O)=O)([C@]2(C)[C@@H]5CC(OC)=O)[H])(C[C@H]1C6=COC=C6)[H],RNF114,,,ester_to_amide,14,2,,0.24 uM,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCCNC(=O)c1ccccc1,Other,13,3,4,1025.625,No,,3MXF,JQ1,31209351,XH2,Yes,,Reviewed,O60885,No,Yes,No,Yes,12,193.30999999999997
886,O=C(NCCNC(COC1=C(OC)C=C(/N=N/C2=CC=CC3=C2CN([C@@H](CC4)C(NC4=O)=O)C3=O)C=C1OC)=O)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5,Active,No,RS4;11,5.694660000000005,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,15,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,COc1cc(N)cc(OC)c1OCC(=O)NCCN,Other,19,7,7,907.4099999999996,No,,3MXF,JQ1,32128406,PHOTAC-I-1,No,,Reviewed,O60885,No,No,No,No,4,220.15999999999997
887,O=C(NCCCNC(COC1=C(OC)C=C(/N=N/C2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)C=C1OC)=O)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5,Active,No,RS4;11,6.0847600000000055,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,15,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,COc1cc(N)cc(OC)c1OCC(=O)NCCCN,Other,20,7,8,921.4369999999997,No,,3MXF,JQ1,32128406,PHOTAC-I-2,No,,Reviewed,O60885,No,No,No,No,4,220.15999999999997
888,O=C(NCCCCNC(COC1=C(OC)C=C(/N=N/C2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)C=C1OC)=O)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5,Active,Yes,RS4;11,6.474860000000007,"Light-activated PROTAC. The cis form is active. Tested Cullin-RING inhibitors (MLN4924), which proved that PROTAC is UPS-dependent.",Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,88.5 nM,ester_to_amide,15,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,COc1cc(N)cc(OC)c1OCC(=O)NCCCCN,Other,21,7,9,935.4639999999997,No,,3MXF,JQ1,32128406,PHOTAC-I-3,No,,Reviewed,O60885,Yes,No,No,No,4,220.15999999999997
889,O=C(NCCCCCNC(COC1=C(OC)C=C(/N=N/C2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)C=C1OC)=O)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5,Active,No,RS4;11,6.864960000000008,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,15,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,COc1cc(N)cc(OC)c1OCC(=O)NCCCCCN,Other,22,7,10,949.4909999999996,No,,3MXF,JQ1,32128406,PHOTAC-I-4,No,,Reviewed,O60885,No,No,No,No,4,220.15999999999997
890,O=C(NCCCCCCNC(COC1=C(OC)C=C(/N=N/C2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)C=C1OC)=O)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5,Active,No,RS4;11,7.255060000000009,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,15,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,COc1cc(N)cc(OC)c1OCC(=O)NCCCCCCN,Other,23,7,11,963.5179999999997,No,,3MXF,JQ1,32128406,PHOTAC-I-5,No,,Reviewed,O60885,No,No,No,No,4,220.15999999999997
891,O=C(NCCNC(COC1=CC=C(/N=N/C2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)C=C1)=O)C[C@@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5,Active,No,RS4;11,5.677460000000005,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,13,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCNC(=O)COc1ccc(N)cc1,Other,15,5,5,847.3579999999998,No,,3MXF,JQ1,32128406,PHOTAC-I-6,No,,Reviewed,O60885,No,No,No,No,4,201.7
892,O=C(NCCCCNC(COC1=CC=C(/N=N/C2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)C=C1)=O)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5,Active,No,RS4;11,6.457660000000007,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,13,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCCCNC(=O)COc1ccc(N)cc1,Other,17,5,7,875.4119999999997,No,,3MXF,JQ1,32128406,PHOTAC-I-7,No,,Reviewed,O60885,No,No,No,No,4,201.7
893,O=C(NCCCCCCNC(COC1=CC=C(/N=N/C2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)C=C1)=O)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5,Active,No,RS4;11,7.237860000000008,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,13,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCCCCCNC(=O)COc1ccc(N)cc1,Other,19,5,9,903.4659999999998,No,,3MXF,JQ1,32128406,PHOTAC-I-8,No,,Reviewed,O60885,No,No,No,No,4,201.7
894,O=C(NCCNC(COC1=C(OC)C=C(/N=N/C2=CC3=C(C(N(C(CC4)C(NC4=O)=O)C3=O)=O)C=C2)C=C1OC)=O)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5,Active,No,RS4;11,5.334860000000004,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,16,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,COc1cc(N)cc(OC)c1OCC(=O)NCCN,Other,19,7,7,921.3929999999997,No,,3MXF,JQ1,32128406,PHOTAC-I-9,No,,Reviewed,O60885,No,No,No,No,4,237.22999999999996
895,O=C(NC1=CC=C(/N=N/C2=CC=C(NC(COC3=CC=CC(C(N4C(CC5)C(NC5=O)=O)=O)=C3C4=O)=O)C=C2)C=C1)C[C@H]6C7=NN=C(C)N7C8=C(C(C)=C(C)S8)C(C9=CC=C(Cl)C=C9)=N6,Active,No,RS4;11,7.662460000000007,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,14,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,Nc1ccc(/N=N/c2ccc(NC(=O)CO)cc2)cc1,Other,20,6,4,909.3849999999998,No,,3MXF,JQ1,32128406,PHOTAC-I-10,No,,Reviewed,O60885,No,No,No,No,4,218.76999999999998
896,O=C(NCC1=CC=C(/N=N/C2=CC=C(NC(COC3=CC=CC(C(N4C(CC5)C(NC5=O)=O)=O)=C3C4=O)=O)C=C2)C=C1)C[C@H]6C7=NN=C(C)N7C8=C(C(C)=C(C)S8)C(C9=CC=C(Cl)C=C9)=N6,Active,No,RS4;11,7.340160000000007,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,14,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCc1ccc(/N=N/c2ccc(NC(=O)CO)cc2)cc1,Other,21,6,5,923.4119999999997,No,,3MXF,JQ1,32128406,PHOTAC-I-11,No,,Reviewed,O60885,No,No,No,No,4,218.76999999999998
897,O=C(NCCC1=CC=C(/N=N/C2=CC=C(NC(COC3=CC=CC(C(N4C(CC5)C(NC5=O)=O)=O)=C3C4=O)=O)C=C2)C=C1)C[C@H]6C7=NN=C(C)N7C8=C(C(C)=C(C)S8)C(C9=CC=C(Cl)C=C9)=N6,Active,No,RS4;11,7.3826600000000075,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,14,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,NCCc1ccc(/N=N/c2ccc(NC(=O)CO)cc2)cc1,Other,22,6,6,937.4389999999997,No,,3MXF,JQ1,32128406,PHOTAC-I-12,No,,Reviewed,O60885,No,No,No,No,4,218.76999999999998
898,O=C(NC1=CC=C2/N=N\C3=CC=C(NC(COC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=O)C=C3CCC2=C1)C[C@H]7C8=NN=C(C)N8C9=C(C(C)=C(C)S9)C(C%10=CC=C(Cl)C=C%10)=N7,Active,No,RS4;11,7.761060000000008,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,ester_to_amide,14,3,,,JQ1,Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)OC(C)(C)C)c1nnc(C)n1-2,Nc1c-c2c(-cc1)/N=N\c1ccc(NC(=O)CO)cc1CC2,Other,22,6,2,935.4229999999995,No,,3MXF,JQ1,32128406,PHOTAC-I-13,No,,Reviewed,O60885,No,No,No,No,4,218.76999999999998
899,O=C([C@H]1N(C(C(C(C)(C)CC)=O)=O)CCCC1)O[C@@H](C2=CC=CC(OCC(NC3=CC=C(/N=N/C4=CC=C(NC(COC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)C=C4)C=C3)=O)=C2)CCC8=CC=C(OC)C(OC)=C8,Active,No,RS4;11,8.158900000000006,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_ether,16,3,,,SLF,CCC(C)(C)C(=O)C(=O)N1CCCC[C@H]1C(=O)OC(CCc1ccc(OC)c(OC)c1)c1cccc(N)c1,O=C(CO)Nc1ccc(/N=N/c2ccc(NC(=O)CO)cc2)cc1,Other,24,8,6,1092.1719999999993,No,,,,32128406,PHOTAC-II-6,No,,Reviewed,P62942,No,No,No,No,4,267.07
900,O=C(NCCCNC(COC1=C(OC)C=C(/N=N/C2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)C=C1OC)=O)COc5cc([C@@H](CCc6cc(OC)c(OC)cc6)OC([C@@H]7CCCCN7C(C(C(C)(C)CC)=O)=O)=O)ccc5,Active,No,RS4;11,6.581200000000007,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_ether,17,3,,,SLF,CCC(C)(C)C(=O)C(=O)N1CCCC[C@H]1C(=O)OC(CCc1ccc(OC)c(OC)c1)c1cccc(N)c1,COc1cc(N)cc(OC)c1OCC(=O)NCCCNC(=O)CO,Other,24,9,10,1104.2239999999995,No,,,,32128406,PHOTAC-II-1,No,,Reviewed,P62942,No,No,No,No,4,268.4599999999999
901,O=C(NCCCCNC(COC1=C(OC)C=C(/N=N/C2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)C=C1OC)=O)COc5cc([C@@H](CCc6cc(OC)c(OC)cc6)OC([C@@H]7CCCCN7C(C(C(C)(C)CC)=O)=O)=O)ccc5,Inactive,No,RS4;11,6.971300000000007,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_ether,17,3,,,SLF,CCC(C)(C)C(=O)C(=O)N1CCCC[C@H]1C(=O)OC(CCc1ccc(OC)c(OC)c1)c1cccc(N)c1,COc1cc(N)cc(OC)c1OCC(=O)NCCCCNC(=O)CO,Other,25,9,11,1118.2509999999995,No,,,,32128406,PHOTAC-II-2,No,,Reviewed,P62942,No,No,No,No,4,268.4599999999999
902,O=C(NCCCCCNC(COC1=C(OC)C=C(/N=N/C2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)C=C1OC)=O)COc5cc([C@@H](CCc6cc(OC)c(OC)cc6)OC([C@@H]7CCCCN7C(C(C(C)(C)CC)=O)=O)=O)ccc5,Inactive,No,RS4;11,7.361400000000008,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_ether,17,3,,,SLF,CCC(C)(C)C(=O)C(=O)N1CCCC[C@H]1C(=O)OC(CCc1ccc(OC)c(OC)c1)c1cccc(N)c1,COc1cc(N)cc(OC)c1OCC(=O)NCCCCCNC(=O)CO,Other,26,9,12,1132.2779999999996,No,,,,32128406,PHOTAC-II-3,No,,Reviewed,P62942,No,No,No,No,4,268.4599999999999
903,O=C(NCCCCCCNC(COC1=C(OC)C=C(/N=N/C2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)C=C1OC)=O)COc5cc([C@@H](CCc6cc(OC)c(OC)cc6)OC([C@@H]7CCCCN7C(C(C(C)(C)CC)=O)=O)=O)ccc5,Inactive,No,RS4;11,7.751500000000008,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_ether,17,3,,,SLF,CCC(C)(C)C(=O)C(=O)N1CCCC[C@H]1C(=O)OC(CCc1ccc(OC)c(OC)c1)c1cccc(N)c1,COc1cc(N)cc(OC)c1OCC(=O)NCCCCCCNC(=O)CO,Other,27,9,13,1146.3049999999994,No,,,,32128406,PHOTAC-II-4,No,,Reviewed,P62942,No,No,No,No,4,268.4599999999999
904,O=C([C@H]1N(C(C(C(C)(C)CC)=O)=O)CCCC1)O[C@@H](C2=CC=CC(OCC(NCCNC(COC3=CC=C(/N=N\C4=CC=CC5=C4CN(C(CC6)C(NC6=O)=O)C5=O)C=C3)=O)=O)=C2)CCC7=CC=C(OC)C(OC)=C7,Active,No,RS4;11,6.173900000000006,Light-activated PROTAC. The cis form is active.,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_ether,15,3,,,SLF,CCC(C)(C)C(=O)C(=O)N1CCCC[C@H]1C(=O)OC(CCc1ccc(OC)c(OC)c1)c1cccc(N)c1,Nc1ccc(OCC(=O)NCCNC(=O)CO)cc1,Other,19,7,7,1030.1449999999995,No,,,,32128406,PHOTAC-II-5,No,,Reviewed,P62942,No,No,No,No,4,249.99999999999997
905,O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCOC4=CC=C(/N=N/C5=CC=C(C(NC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)=O)C=C5)C=C4)CC3)=C2)S1)NC9=C(C)C=CC=C9Cl,Active,No,K562,7.828940000000008,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,4,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,O=Cc1ccc(/N=N/c2ccccc2)cc1,Other,16,3,3,953.4859999999998,No,,2GQG,1N1,32153174,Azo-PROTAC-2C,No,,Reviewed,P00519,No,No,No,No,24,215.80999999999997
906,O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCCOC4=CC=C(/N=N/C5=CC=C(C(NC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)=O)C=C5)C=C4)CC3)=C2)S1)NC9=C(C)C=CC=C9Cl,Active,No,K562,8.219040000000007,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,hydroxyl_to_carbon,15,4,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,COc1ccc(/N=N/c2ccc(C=O)cc2)cc1,Other,18,4,4,967.5129999999997,No,,2GQG,1N1,32153174,Azo-PROTAC-3C,No,,Reviewed,P00519,No,No,No,No,24,215.80999999999997
907,O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCCCOC4=CC=C(/N=N/C5=CC=C(C(NC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)=O)C=C5)C=C4)CC3)=C2)S1)NC9=C(C)C=CC=C9Cl,Active,Yes,"K562, A549, HCT116, MCF-7, HEK293T",8.609140000000005,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,28 nM,hydroxyl_to_carbon,15,4,,68 nM,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCOc1ccc(/N=N/c2ccc(C=O)cc2)cc1,Other,19,4,5,981.5399999999997,No,,2GQG,1N1,32153174,Azo-PROTAC-4C,No,,Reviewed,P00519,Yes,Yes,No,No,24,215.80999999999997
908,O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCCCCOC4=CC=C(/N=N/C5=CC=C(C(NC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)=O)C=C5)C=C4)CC3)=C2)S1)NC9=C(C)C=CC=C9Cl,Inactive,No,K562,8.999240000000004,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,hydroxyl_to_carbon,15,4,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCOc1ccc(/N=N/c2ccc(C=O)cc2)cc1,Other,20,4,6,995.5669999999998,No,,2GQG,1N1,32153174,Azo-PROTAC-5C,No,,Reviewed,P00519,No,No,No,No,24,215.80999999999997
909,O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCCCCCOC4=CC=C(/N=N/C5=CC=C(C(NC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)=O)C=C5)C=C4)CC3)=C2)S1)NC9=C(C)C=CC=C9Cl,Inactive,No,K562,9.38934,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,hydroxyl_to_carbon,15,4,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCCCOc1ccc(/N=N/c2ccc(C=O)cc2)cc1,Other,21,4,7,1009.5939999999998,No,,2GQG,1N1,32153174,Azo-PROTAC-6C,No,,Reviewed,P00519,No,No,No,No,24,215.80999999999997
910,O=C(N/N=C/C1=CC=C(OCCOCCOCCN2N=NC(CNC3=CC=CC4=C3C(N(C4=O)C5CCC(NC5=O)=O)=O)=C2)C=C1)CCCCCCC(NO)=O,Active,No,MM1S,1.6997000000000053,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,5,,,AB3,O=C(N/N=C/C1=CC=C(OC)C=C1)CCCCCCC(NO)=O,COCCOCCn1cc(C)nn1,Other,13,5,6,775.8199999999998,No,,5WGL,AH4,32292566,1,No,,Reviewed,Q9UBN7,No,No,No,No,6,244.76999999999998
911,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3NCC4=CN(N=N4)CCCCCOC5=CC=C(NC(N(CCCC)CC6=CC=C(C(NO)=O)C=C6)=O)C=C5,Active,No,MM1S,4.493900000000003,,Yangwode Jing,2.2 nM,86 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,12,5,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,Cc1cn(CCCCCO)nn1,Other,12,4,5,779.855,Yes,,5G0I 5G0J,N4R,32292566,2,No,,Reviewed,Q9UBN7,No,No,No,No,"0.5, 1, 2, 4, 6",217.19
912,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCC2=CN(CCOC3=CC=C(NC(N(CCCC)CC4=CC=C(C(NO)=O)C=C4)=O)C=C3)N=N2)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5,Active,No,MM1S,6.2641200000000055,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCO)nn1,Other,14,5,7,965.191,No,,5G0I 5G0J,N4R,32292566,3a,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999995
913,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCC2=CN(CCCOC3=CC=C(NC(N(CCCC)CC4=CC=C(C(NO)=O)C=C4)=O)C=C3)N=N2)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5,Active,No,MM1S,6.654220000000007,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCCO)nn1,Other,15,5,8,979.2180000000001,No,,5G0I 5G0J,N4R,32292566,3b,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999995
914,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCC2=CN(CCCCOC3=CC=C(NC(N(CCCC)CC4=CC=C(C(NO)=O)C=C4)=O)C=C3)N=N2)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5,Active,No,MM1S,7.044320000000007,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCCCO)nn1,Other,16,5,9,993.2450000000001,No,,5G0I 5G0J,N4R,32292566,3c,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999995
915,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCC2=CN(CCCCCOC3=CC=C(NC(N(CCCC)CC4=CC=C(C(NO)=O)C=C4)=O)C=C3)N=N2)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5,Active,No,MM1S,7.434420000000007,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCCCCO)nn1,Other,17,5,10,1007.2720000000002,No,,5G0I 5G0J,N4R,32292566,3d,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999995
916,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCC2=CN(CCCCCCOC3=CC=C(NC(N(CCCC)CC4=CC=C(C(NO)=O)C=C4)=O)C=C3)N=N2)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5,Active,No,MM1S,7.824520000000008,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCCCCCO)nn1,Other,18,5,11,1021.2990000000001,No,,5G0I 5G0J,N4R,32292566,3e,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999995
917,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCC2=CN(CCCCCCCOC3=CC=C(NC(N(CCCC)CC4=CC=C(C(NO)=O)C=C4)=O)C=C3)N=N2)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5,Active,No,MM1S,8.214620000000007,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCCCCCCO)nn1,Other,19,5,12,1035.326,No,,5G0I 5G0J,N4R,32292566,3f,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999995
918,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCC2=CN(CCCCCCCCOC3=CC=C(NC(N(CCCC)CC4=CC=C(C(NO)=O)C=C4)=O)C=C3)N=N2)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5,Active,No,MM1S,8.604720000000006,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCCCCCCCO)nn1,Other,20,5,13,1049.353,No,,5G0I 5G0J,N4R,32292566,3g,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999995
919,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCC2=CN(CCCCCCCCCOC3=CC=C(NC(N(CCCC)CC4=CC=C(C(NO)=O)C=C4)=O)C=C3)N=N2)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5,Active,No,MM1S,8.994820000000002,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCCCCCCCCO)nn1,Other,21,5,14,1063.3799999999999,No,,5G0I 5G0J,N4R,32292566,3h,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999995
920,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCC2=CN(CCCCCCCCCCOC3=CC=C(NC(N(CCCC)CC4=CC=C(C(NO)=O)C=C4)=O)C=C3)N=N2)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5,Active,No,MM1S,9.384920000000003,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCCCCCCCCCO)nn1,Other,22,5,15,1077.4069999999997,No,,5G0I 5G0J,N4R,32292566,3i,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999995
921,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCC2=CN(CCCCCCCCCCCOC3=CC=C(NC(N(CCCC)CC4=CC=C(C(NO)=O)C=C4)=O)C=C3)N=N2)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5,Active,Yes,MM1S; Mouse 4935 cells,9.77502,,Yangwode Jing,7.1 nM,90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCCCCCCCCCCO)nn1,Other,23,5,16,1091.434,No,,5G0I 5G0J,N4R,32292566,3j,No,,Reviewed,Q9UBN7,No,Yes,No,Yes,"0.5, 1, 2, 4, 6",233.23999999999995
922,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCC2=CN(CCCCCCCCCCCCOC3=CC=C(NC(N(CCCC)CC4=CC=C(C(NO)=O)C=C4)=O)C=C3)N=N2)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5,Active,No,MM1S,10.165119999999996,,Yangwode Jing,11 nM,89 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCCCCCCCCCCCO)nn1,Other,24,5,17,1105.4609999999998,No,,5G0I 5G0J,N4R,32292566,3k,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999995
923,O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](NC(CCC4=CN(N=N4)CCCOC5=CC=C(C=C5)NC(N(CC6=CC=C(C=C6)C(NO)=O)CCCC)=O)=O)C(C)(C)C)=O,Inactive,No,MM1S,5.874020000000003,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCc1cn(CCCO)nn1,Other,13,5,6,951.1639999999999,No,,5G0I 5G0J,N4R,32292566,WH174,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999998
924,O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](NC(CCCC4=CN(N=N4)CCCOC5=CC=C(C=C5)NC(N(CC6=CC=C(C=C6)C(NO)=O)CCCC)=O)=O)C(C)(C)C)=O,Inactive,No,MM1S,6.264120000000005,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,13,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCc1cn(CCCO)nn1,Other,14,5,7,965.1909999999998,No,,5G0I 5G0J,N4R,32292566,WH167,No,,Reviewed,Q9UBN7,No,No,No,No,6,233.23999999999998
925,O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](NC(CCCCC4=CN(CCOCCOC5=CC=C(C=C5)NC(N(CC6=CC=C(C=C6)C(NO)=O)CCCC)=O)N=N4)=O)C(C)(C)C)=O,Inactive,No,MM1S,6.280720000000004,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,14,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCOCCO)nn1,Other,17,6,10,1009.2439999999997,No,,5G0I 5G0J,N4R,32292566,WH221,No,,Reviewed,Q9UBN7,No,No,No,No,6,242.46999999999997
926,O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](NC(CCCCC4=CN(CCOCCOCCOC5=CC=C(C=C5)NC(N(CC6=CC=C(C=C6)C(NO)=O)CCCC)=O)N=N4)=O)C(C)(C)C)=O,Inactive,No,MM1S,6.297320000000005,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aryl_O,15,6,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,O=CCCCCc1cn(CCOCCOCCO)nn1,Other,20,7,13,1053.2969999999996,No,,5G0I 5G0J,N4R,32292566,WH212,No,,Reviewed,Q9UBN7,No,No,No,No,6,251.7
927,COC1=C(C=C(C(N(CCN(CCOCCOCC(NC2=CC=CC3=C2CN(C3=O)C4CCC(NC4=O)=O)=O)C)C)=C1)NC(C=C)=O)NC5=NC=CC(C6=CN(C7=C6C=CC=C7)C)=N5,Active,No,PC9; HCC827; H1975,4.3129000000000035,"EC50: 1.425±0.052uM, 1.874±0.098uM, 1.388±0.556uM for PC9/HCC827/H1975 cells, respectively.",Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,1.425 uM,aliphatic_CC,14,4,,,Osimertinib,COC1=C(C=C(C(N(CCN(C)C)C)=C1)NC(C=C)=O)NC2=NC=CC(C3=CN(C4=C3C=CC=C4)C)=N2,COCCOCC=O,PEG,8,3,5,872.9839999999998,,,3IKA,0UN,32317208,16a,No,,Reviewed,P00533,No,No,No,No,"6, 24",201.58999999999997
928,COC1=C(C=C(C(N(CCN(CCOCCOCCOCC(NC2=CC=CC3=C2CN(C3=O)C4CCC(NC4=O)=O)=O)C)C)=C1)NC(C=C)=O)NC5=NC=CC(C6=CN(C7=C6C=CC=C7)C)=N5,Active,No,PC9; HCC827; H1975,4.329500000000005,"EC50: 1.117±0.105uM, 1.611±0.139uM, 1.698±0.614uM for PC9/HCC827/H1975 cells, respectively.",Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,1.117 uM,aliphatic_CC,15,4,,,Osimertinib,COC1=C(C=C(C(N(CCN(C)C)C)=C1)NC(C=C)=O)NC2=NC=CC(C3=CN(C4=C3C=CC=C4)C)=N2,COCCOCCOCC=O,PEG,11,4,8,917.0369999999999,No,,3IKA,0UN,32317208,16b,No,,Reviewed,P00533,No,No,No,No,"6, 24",210.82
929,COC1=C(C=C(C(N(CCN(CCOCCOCCOCCOCC(NC2=CC=CC3=C2CN(C3=O)C4CCC(NC4=O)=O)=O)C)C)=C1)NC(C=C)=O)NC5=NC=CC(C6=CN(C7=C6C=CC=C7)C)=N5,Active,Yes,PC9; HCC827; H1975,4.346100000000006,"EC50: 0.413±0.087uM, 1.344±0.112uM, 0.657±0.008uM for PC9/HCC827/H1975 cells, respectively.",Yangwode Jing,0.161 uM,68 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,0.413 uM,aliphatic_CC,16,4,,,Osimertinib,COC1=C(C=C(C(N(CCN(C)C)C)=C1)NC(C=C)=O)NC2=NC=CC(C3=CN(C4=C3C=CC=C4)C)=N2,COCCOCCOCCOCC=O,PEG,14,5,11,961.0899999999997,No,,3IKA,0UN,32317208,16c,No,,Reviewed,P00533,No,No,No,Yes,"1, 3, 6, 12, 24, 48",220.04999999999995
930,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3OCC(NCCOCCOCCOCCNC(C4=CC=C(C5=CC=C(F)C(C)=C5)C(N6CCC(C7=C(C)N=CN7)CC6)=C4)=O)=O,Active,No,"T47D, BT474, MDAMB231, MCF7, HS578T, LS180, HCT116, HCT15, DLD1, SW480, LOVO, SW620, HEL, KCL22, THP1, K562, ML2, NOMO1, MONOMAC6, MOLM13, LAMA84, SHI1, MV411, KU812, KG1, KBM7, HL60, BV173, HUH7, NCIH460, A549, NCIH2228, PC9, NCIH446, HELA, T98G, MCF10A, HAP1, DU145, PC3, LNCaP, A375, LOXIMVI",3.592640000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,12,4,,,carboxy-w9A,FC1=CC=C(C2=CC=C(C(O)=O)C=C2N3CCC(C4=C(C)N=CN4)CC3)C=C1C,NCCOCCOCCOCCNC(=O)CO,PEG,17,7,12,881.959,"Possible, since d9A-2 was reported.",,,,32386596,d9A-1,No,,Reviewed,P19634,No,No,No,No,8,210.59
931,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3OCC(NCCOCCOCCOCCOCCNC(C4=CC=C(C5=CC=C(F)C(C)=C5)C(N6CCC(C7=C(C)N=CN7)CC6)=C4)=O)=O,Active,Yes,"T47D, BT474, MDAMB231, MCF7, HS578T, LS180, HCT116, HCT15, DLD1, SW480, LOVO, SW620, HEL, KCL22, THP1, K562, ML2, NOMO1, MONOMAC6, MOLM13, LAMA84, SHI1, MV411, KU812, KG1, KBM7, HL60, BV173, HUH7, NCIH460, A549, NCIH2228, PC9, NCIH446, HELA, T98G, MCF10A, HAP1, DU145, PC3, LNCaP, A375, LOXIMVI",3.609240000000006,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,< 0.1 uM,carboxilic_acid_to_amide,13,4,,,carboxy-w9A,FC1=CC=C(C2=CC=C(C(O)=O)C=C2N3CCC(C4=C(C)N=CN4)CC3)C=C1C,NCCOCCOCCOCCOCCNC(=O)CO,PEG,20,8,15,926.0119999999998,"Yes, could also degrade SLC9A2, SLC9A4, SLC9A7, SLC9B1",,,,32386596,d9A-2,No,,Reviewed,P19634,No,No,No,Yes,"8, 72",219.82000000000002
932,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3OCC(NCCOCCCOCCCOCCNC(C4=CC=C(C5=CC=C(F)C(C)=C5)C(N6CCC(C7=C(C)N=CN7)CC6)=C4)=O)=O,Active,No,"T47D, BT474, MDAMB231, MCF7, HS578T, LS180, HCT116, HCT15, DLD1, SW480, LOVO, SW620, HEL, KCL22, THP1, K562, ML2, NOMO1, MONOMAC6, MOLM13, LAMA84, SHI1, MV411, KU812, KG1, KBM7, HL60, BV173, HUH7, NCIH460, A549, NCIH2228, PC9, NCIH446, HELA, T98G, MCF10A, HAP1, DU145, PC3, LNCaP, A375, LOXIMVI",4.3728400000000045,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,12,4,,,carboxy-w9A,FC1=CC=C(C2=CC=C(C(O)=O)C=C2N3CCC(C4=C(C)N=CN4)CC3)C=C1C,NCCOCCCOCCCOCCNC(=O)CO,non-PEG polyether,19,7,14,910.0129999999999,"Possible, since d9A-2 was reported",,,,32386596,d9A-3,No,,Reviewed,P19634,No,No,No,No,8,210.59
933,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3OCC(NCCOCCOCCNC(C4=CC=C(C5=CC=C(F)C(C)=C5)C(N6CCC(C7=C(C)N=CN7)CC6)=C4)=O)=O,Inactive,No,"T47D, BT474, MDAMB231, MCF7, HS578T, LS180, HCT116, HCT15, DLD1, SW480, LOVO, SW620, HEL, KCL22, THP1, K562, ML2, NOMO1, MONOMAC6, MOLM13, LAMA84, SHI1, MV411, KU812, KG1, KBM7, HL60, BV173, HUH7, NCIH460, A549, NCIH2228, PC9, NCIH446, HELA, T98G, MCF10A, HAP1, DU145, PC3, LNCaP, A375, LOXIMVI",3.5760400000000034,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,11,4,,,carboxy-w9A,FC1=CC=C(C2=CC=C(C(O)=O)C=C2N3CCC(C4=C(C)N=CN4)CC3)C=C1C,NCCOCCOCCNC(=O)CO,PEG,14,6,9,837.906,Possible,,,,32386596,d9A-4,No,,Reviewed,P19634,No,No,No,No,8,201.35999999999999
934,O=C(N(C1=O)C2CCC(NC2=O)=O)C3=C1C=CC=C3OCC(NCCCCCCNC(C4=CC=C(C5=CC=C(F)C(C)=C5)C(N6CCC(C7=C(C)N=CN7)CC6)=C4)=O)=O,Inactive,No,"T47D, BT474, MDAMB231, MCF7, HS578T, LS180, HCT116, HCT15, DLD1, SW480, LOVO, SW620, HEL, KCL22, THP1, K562, ML2, NOMO1, MONOMAC6, MOLM13, LAMA84, SHI1, MV411, KU812, KG1, KBM7, HL60, BV173, HUH7, NCIH460, A549, NCIH2228, PC9, NCIH446, HELA, T98G, MCF10A, HAP1, DU145, PC3, LNCaP, A375, LOXIMVI",5.103240000000005,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,9,4,,,carboxy-w9A,FC1=CC=C(C2=CC=C(C(O)=O)C=C2N3CCC(C4=C(C)N=CN4)CC3)C=C1C,NCCCCCCNC(=O)CO,Alkane,12,4,7,805.9079999999999,Possible,,,,32386596,d9A-5,No,,Reviewed,P19634,No,No,No,No,8,182.9
935,O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCOCCOCCNC(CCN2[C@H](COC3=NC(N4C[C@H](CC#N)N(C(C(F)=C)=O)CC4)=C5C(CN(C6=C7C(Cl)=CC=CC7=CC=C6)CC5)=N3)CCC2)=O)=O)=O)C[C@H](O)C1)NCC8=CC=C(C9=C(C)N=CS9)C=C8,Inactive,No,NCI-H2030,6.273800000000012,,Yangwode Jing,,~ 30 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,17,4,~ 0.10 uM,,MRTX849,N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C(CN(C4=C5C(Cl)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1,CC(=O)NCCOCCOCCC=O,PEG,14,5,9,1233.9099999999996,No,,6UT0,M1X,32875077,LC-1,No,,Reviewed,P01116,No,No,No,No,"24, 72",248.01999999999998
936,O=C([C@H]1N(C([C@@H](NC(CCOCCCN2[C@H](COC3=NC(N4C[C@H](CC#N)N(C(C(F)=C)=O)CC4)=C5C(CN(C6=C7C(Cl)=CC=CC7=CC=C6)CC5)=N3)CCC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC8=CC=C(C9=C(C)N=CS9)C=C8,Active,Yes,5W1573; NCI-H2030; NCI-H358; HCT116; MIA-PaCa-2,7.14100000000001,"EC50/DC50/Dmax reported above were obtained using NCI-H2030 cells. DC50: 0.25~0.76uM; Dmax: ~75%-90%, specific value depends on the cell line.",Yangwode Jing,0.59 uM,~ 80 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,3.8 uM,aliphatic_CC,15,3,~ 0.10 uM,,MRTX849,N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C(CN(C4=C5C(Cl)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1,CCOCCC=O,Other,7,2,4,1132.8049999999994,No,,6UT0,M1X,32875077,LC-2,No,,Reviewed,P01116,Yes,No,No,Yes,"24, 72",209.69
937,O=C([C@H]1N(C([C@@H](NC(CCNC(CCN2[C@H](COC3=NC(N4C[C@H](CC#N)N(C(C(F)=C)=O)CC4)=C5C(CN(C6=C7C(Cl)=CC=CC7=CC=C6)CC5)=N3)CCC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC8=CC=C(C9=C(C)N=CS9)C=C8,Active,No,NCI-H2030,6.24060000000001,,Yangwode Jing,6.4 uM,~ 85 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,4,~ 0.10 uM,,MRTX849,N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C(CN(C4=C5C(Cl)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1,CC(=O)NCCC=O,Other,8,3,3,1145.8039999999994,No,,6UT0,M1X,32875077,LC-3,No,,Reviewed,P01116,No,No,No,No,"24, 72",229.55999999999995
938,O=C([C@H]1N(C([C@@H](NC(CCOCCCCN2[C@H](COC3=NC(N4C[C@H](CC#N)N(C(C(F)=C)=O)CC4)=C5C(CN(C6=C7C(Cl)=CC=CC7=CC=C6)CC5)=N3)CCC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC8=CC=C(C9=C(C)N=CS9)C=C8,Active,No,SW1573,7.53110000000001,,Yangwode Jing,0.88 uM,~ 90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,15,3,~ 0.10 uM,,MRTX849,N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C(CN(C4=C5C(Cl)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1,CCCOCCC=O,Other,8,2,5,1146.8319999999994,No,,6UT0,M1X,32875077,LC-4,No,,Reviewed,P01116,No,No,No,No,"24, 72",209.69
939,O=C([C@H]1N(C([C@@H](NC(CCOCCOCCN2[C@H](COC3=NC(N4C[C@H](CC#N)N(C(C(F)=C)=O)CC4)=C5C(CN(C6=C7C(Cl)=CC=CC7=CC=C6)CC5)=N3)CCC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC8=CC=C(C9=C(C)N=CS9)C=C8,Active,No,SW1573,6.767500000000011,,Yangwode Jing,> 10 uM,~ 50 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,3,~ 0.10 uM,,MRTX849,N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C(CN(C4=C5C(Cl)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1,COCCOCCC=O,PEG,9,3,6,1162.8309999999992,No,,6UT0,M1X,32875077,LC-5,No,,Reviewed,P01116,No,No,No,No,"24, 72",218.91999999999996
940,O=C([C@H]1N(C([C@@H](NC(CCOCCNC(CCN2[C@H](COC3=NC(N4C[C@H](CC#N)N(C(C(F)=C)=O)CC4)=C5C(CN(C6=C7C(Cl)=CC=CC7=CC=C6)CC5)=N3)CCC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC8=CC=C(C9=C(C)N=CS9)C=C8,Inactive,No,NCI-H2030,6.25720000000001,,Yangwode Jing,,~ 35 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,aliphatic_CC,16,4,~ 0.10 uM,,MRTX849,N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C(CN(C4=C5C(Cl)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1,CC(=O)NCCOCCC=O,Other,11,4,6,1189.8569999999993,No,,6UT0,M1X,32875077,LC-6,No,,Reviewed,P01116,No,No,No,No,"24, 72",238.78999999999996
941,O=C(NCCOCCOCCNC1=CC=C(C=C1)C2=NC3=CC=C(C)C=C3S2)[C@H](CC(C)C)NC([C@@H](O)[C@@H](CC4=CC=CC=C4)N)=O,Active,Yes,Fibroblasts from patients; HeLa,4.294820000000002,,Yangwode Jing,,,CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O,Iap,,,aliphatic_CC,9,5,,,BTA,CC1=CC=C2C(SC(C3=CC=C(NC)C=C3)=N2)=C1,COCCOCCN,PEG,8,3,5,661.8690000000001,No,,,,28703441,1,No,,Reviewed,P42858,Yes,No,No,Yes,"24, 48",147.83
942,O=C(NCCOCCOCCOC1=CC(SC(/N=N/C2=CC=C(N(C)C)C=C2)=N3)=C3C=C1)[C@H](CC(C)C)NC([C@@H](O)[C@@H](CC4=CC=CC=C4)N)=O,Active,No,Fibroblasts from patients; HeLa,4.767700000000003,,Yangwode Jing,,,CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O,Iap,,,aliphatic_CC,12,4,,,PDB,CN(C)C1=CC=C(/N=N/C2=NC3=C(S2)C=C(OC)C=C3)C=C1,COCCOCCN,PEG,8,3,5,719.9090000000001,No,,,,28703441,2,No,,Reviewed,P42858,No,No,No,No,"24, 48",172.99
943,O=C([C@H]1N(C[C@@H](C1)O)C([C@@H](NC(CCCC(N2CCC(C3=C(C)C=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5S(=O)(C(C)C)=O)=N4)C(OC(C)C)=C3)CC2)=O)=O)C(C)(C)C)=O)NCC6=CC=C(C=C6)C7=C(N=CS7)C,Active,Yes,SU-DHL-1; H3122,9.012240000000004,"EC50: 0.058uM/0.18uM/>10uM for SU-DHL-1/H3122/A549 cells, respectively.",Yangwode Jing,,> 90 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,0.058 uM,amine_to_amide,14,5,7 nM,0.11 uM,LDK378,O=S(C1=CC=CC=C1NC2=NC(NC3=CC(C)=C(C4CCNCC4)C=C3OC(C)C)=NC=C2Cl)(C(C)C)=O,O=CCCCC=O,Alkane,7,2,4,1084.8069999999996,No,,4MKC,4MK,30274779,TD-004,No,,Reviewed,Q9UM73,No,No,No,Yes,16,225.14999999999998
944,O=C([C@@H]1N(C([C@H](NC(CCCCCC(N2CCC(C3=CC(OC(C)C)=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5S(=O)(C(C)C)=O)=N4)C=C3C)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC6=CC=C(C7=C(C)N=CS7)C=C6,Active,No,SU-DHL-1,9.792439999999997,,Yangwode Jing,,> 95 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_amide,14,5,7 nM,0.14 uM,LDK378,O=S(C1=CC=CC=C1NC2=NC(NC3=CC(C)=C(C4CCNCC4)C=C3OC(C)C)=NC=C2Cl)(C(C)C)=O,O=CCCCCCC=O,Alkane,9,2,6,1112.8609999999996,No,,4MKC,4MK,30274779,TD-016,No,,Reviewed,Q9UM73,No,No,No,No,16,225.14999999999998
945,O=C([C@@H]1N(C([C@H](NC(CCCCN2CCC(C3=CC(OC(C)C)=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5S(=O)(C(C)C)=O)=N4)C=C3C)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC6=CC=C(C7=C(C)N=CS7)C=C6,Active,No,SU-DHL-1,9.485640000000004,,Yangwode Jing,,> 50 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,14,5,7 nM,0.032 uM,LDK378,O=S(C1=CC=CC=C1NC2=NC(NC3=CC(C)=C(C4CCNCC4)C=C3OC(C)C)=NC=C2Cl)(C(C)C)=O,CCCCC=O,Alkane,6,1,3,1070.8239999999994,No,,4MKC,4MK,30274779,TD-009,No,,Reviewed,Q9UM73,No,No,No,No,16,208.07999999999998
946,O=C([C@H]1N(C([C@@H](NC(COCCN2CCC(C3=CC(OC(C)C)=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5S(=O)(C(C)C)=O)=N4)C=C3C)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC6=CC=C(C7=C(C)N=CS7)C=C6,Active,No,SU-DHL-1,8.331940000000008,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,15,5,7 nM,0.089 uM,LDK378,O=S(C1=CC=CC=C1NC2=NC(NC3=CC(C)=C(C4CCNCC4)C=C3OC(C)C)=NC=C2Cl)(C(C)C)=O,CCOCC=O,Other,6,2,3,1072.7959999999994,No,,4MKC,4MK,30274779,TD-013,No,,Reviewed,Q9UM73,No,No,No,No,16,217.30999999999995
947,O=C([C@@H]1N(C([C@H](NC(COCCCN2CCC(C3=CC(OC(C)C)=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5S(=O)(C(C)C)=O)=N4)C=C3C)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC6=CC=C(C7=C(C)N=CS7)C=C6,Active,No,SU-DHL-1,8.722040000000005,,Yangwode Jing,,> 50 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,15,5,7 nM,0.02 uM,LDK378,O=S(C1=CC=CC=C1NC2=NC(NC3=CC(C)=C(C4CCNCC4)C=C3OC(C)C)=NC=C2Cl)(C(C)C)=O,CCCOCC=O,Other,7,2,4,1086.8229999999994,No,,4MKC,4MK,30274779,TD-020,No,,Reviewed,Q9UM73,No,No,No,No,16,217.30999999999995
948,O=C([C@@H]1N(C([C@@H](C(C)(C)C)NC(COCCOCCOCCN2CCC(C3=CC(OC(C)C)=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5S(=O)(C(C)C)=O)=N4)C=C3C)CC2)=O)=O)C[C@H](O)C1)NCC6=CC=C(C7=C(C)N=CS7)C=C6,Active,No,SU-DHL-1; H3122,8.36514000000001,,Yangwode Jing,,> 50 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,amine_to_methylamine,17,5,7 nM,0.016 uM,LDK378,O=S(C1=CC=CC=C1NC2=NC(NC3=CC(C)=C(C4CCNCC4)C=C3OC(C)C)=NC=C2Cl)(C(C)C)=O,CCOCCOCCOCC=O,PEG,12,4,9,1160.9019999999996,No,,4MKC,4MK,30274779,TD-002,No,,Reviewed,Q9UM73,No,No,No,No,16,235.76999999999998
949,O=C(NO)C1=CC=C(CN(CCCCC2=CN(CCOCCOCCNC3=CC=CC(C(N4C(CC5)C(NC5=O)=O)=O)=C3C4=O)N=N2)C(NC6=CC=CC=C6)=O)C=C1,Active,Yes,IgEMM; hTERT-RPE1; HeLa; Jurkat; RPMI8226; MM.1S,3.000600000000004,,Yangwode Jing,3.8 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,1.21 uM,aliphatic_CC,13,5,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,CCOCCOCCn1ccnn1,PEG,13,5,7,795.8540000000003,No,,5G0J 5G0I,N4R,30603959,NP8,No,,Reviewed,Q9UBN7,Yes,Yes,No,Yes,"2, 4, 6, 8, 24",226.42
950,O=C(NO)C1=CC=C(CN(CCCCC2=CN(CCOCCNC3=CC=CC(C(N4C(CC5)C(NC5=O)=O)=O)=C3C4=O)N=N2)C(NC6=CC=CC=C6)=O)C=C1,Active,No,HeLa,2.9840000000000027,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,12,5,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,CCOCCn1ccnn1,PEG,10,4,4,751.8010000000002,No,,5G0J 5G0I,N4R,30603959,NP6,No,,Reviewed,Q9UBN7,No,No,No,No,24,217.18999999999997
951,O=C(NO)C1=CC=C(CN(CCCCC2=CN(CCOCCOCCOCCNC3=CC=CC(C(N4C(CC5)C(NC5=O)=O)=O)=C3C4=O)N=N2)C(NC6=CC=CC=C6)=O)C=C1,Active,No,HeLa,3.017200000000006,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,14,5,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,CCOCCOCCOCCn1ccnn1,PEG,16,6,10,839.907,No,,5G0J 5G0I,N4R,30603959,NP9,No,,Reviewed,Q9UBN7,No,No,No,No,24,235.64999999999995
952,O=C(NO)C1=CC=C(CN(CCCCC2=CN(CCOCCOCCOCCOCCNC3=CC=CC(C(N4C(CC5)C(NC5=O)=O)=O)=C3C4=O)N=N2)C(NC6=CC=CC=C6)=O)C=C1,Active,No,HeLa,3.0338000000000074,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,5,,,Nexturastat A (Next-A),O=C(N(CCCC)CC1=CC=C(C(NO)=O)C=C1)NC2=CC=CC=C2,CCOCCOCCOCCOCCn1ccnn1,PEG,19,7,13,883.96,No,,5G0J 5G0I,N4R,30603959,NP10,No,,Reviewed,Q9UBN7,No,No,No,No,24,244.87999999999997
953,O=C(NCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CN4CCN(C5=CC=C(NC6=NC=C(C(C)=C(C(C)=O)C(N7C8CCCC8)=O)C7=N6)N=C5)CC4,Active,No,Jurkat,2.324320000000003,,Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,16,4,,,Palbociclib,CC(C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O)=O,CC(=O)NCCOCCN,PEG,10,4,5,847.9339999999996,No,,5L2I,LQQ,30802347,BSJ-03-006,No,,Reviewed,"P11802, Q00534",No,No,No,No,4,230.15999999999997
954,O=C(NCCOCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CN4CCN(C5=CC=C(NC6=NC=C(C(C)=C(C(C)=O)C(N7C8CCCC8)=O)C7=N6)N=C5)CC4,Active,No,Jurkat,2.340920000000004,,Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,17,4,,,Palbociclib,CC(C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O)=O,CC(=O)NCCOCCOCCN,PEG,13,5,8,891.9869999999995,No,,5L2I,LQQ,30802347,BSJ-03-007,No,,Reviewed,"P11802, Q00534",No,No,No,No,4,239.39
955,O=C(NCCCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CN4CCN(C5=CC=C(NC6=NC=C(C(C)=C(C(C)=O)C(N7C8CCCC8)=O)C7=N6)N=C5)CC4,Active,No,Jurkat,3.868120000000003,"IC50: 77nM/27.6nM for CDK4/CDK6, respectively.",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,15,4,,77 nM,Palbociclib,CC(C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O)=O,CC(=O)NCCCCCCN,Alkane,11,3,6,859.9889999999996,No,,5L2I,LQQ,30802347,BSJ-03-008,No,,Reviewed,"P11802, Q00534",No,No,No,No,4,220.92999999999995
956,O=C(NCCOCCOCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CN4CCN(C5=CC=C(NC6=NC=C(C(C)=C(C(C)=O)C(N7C8CCCC8)=O)C7=N6)N=C5)CC4,Active,No,Jurkat,2.3575200000000054,"IC50: 137nM/39nM for CDK4/CDK6, respectively; Show selective degradation of CDK6 (therefore active for CDK6 and inactive for CDK4).",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,18,4,,39 nM,Palbociclib,CC(C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O)=O,CC(=O)NCCOCCOCCOCCN,PEG,16,6,11,936.0399999999993,"Yes, can also degrade IKZF1/3",,5L2I,LQQ,30802347,YKL-06-102,No,,Reviewed,Q00534,No,No,No,No,4,248.61999999999995
957,O=C(NCCOCCOCCOCCOCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CN4CCN(C5=CC=C(NC6=NC=C(C(C)=C(C(C)=O)C(N7C8CCCC8)=O)C7=N6)N=C5)CC4,Active,No,Jurkat,2.390720000000008,,Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,20,4,,,Palbociclib,CC(C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O)=O,CC(=O)NCCOCCOCCOCCOCCOCCN,PEG,22,8,17,1024.145999999999,No,,5L2I,LQQ,30802347,BSJ-03-009,No,,Reviewed,"P11802, Q00534",No,No,No,No,4,267.08
958,O=C(NCCOCCOCCOCCN1CCN(C2=CC=C(NC3=NC=C(C(C)=C(C(C)=O)C(N4C5CCCC5)=O)C4=N3)N=C2)CC1)COC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Active,No,Jurkat,2.3244200000000053,"IC50: 106nM/37.7nM for CDK4/CDK6, respectively. Show selectivity on CDK6 (therefore inactive for CDK4 and active for CDK6).",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,18,3,,37.7 nM,Palbociclib,CC(C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O)=O,CCOCCOCCOCCNC(=O)CO,PEG,16,6,11,937.0239999999994,No,,5L2I,LQQ,30802347,BSJ-03-123,Yes,,Reviewed,Q00534,No,No,No,No,4,245.82
959,O=C(NCCCCCCCCN1CCN(C2=CC=C(NC3=NC=C(C(C)=C(C(C)=O)C(N4C5CCCC5)=O)C4=N3)N=C2)CC1)COC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Active,No,Jurkat,4.615220000000004,,Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,15,3,,,Palbociclib,CC(C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O)=O,CCCCCCCCNC(=O)CO,Alkane,13,3,8,889.0269999999997,No,,5L2I,LQQ,30802347,BSJ-03-124,No,,Reviewed,"P11802, Q00534",No,No,No,No,4,218.12999999999997
960,O=C(NCCCCN1CCN(C2=CC=C(NC3=NC=C(C(C)=C(C(C)=O)C(N4C5CCCC5)=O)C4=N3)N=C2)CC1)COC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Active,Yes,Jurkat; Molt4; Granta-519; Mino; Jeko; Rec1; Maver,3.054820000000001,"IC50: 25.7nM/7.57nM for CDK4/CDK6, respectively. BSJ-02-162 is capable of degrading both CDK4 and CDK6.",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,15,3,,25.7 nM,Palbociclib,CC(C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O)=O,CCCCNC(=O)CO,Alkane,9,3,4,832.919,"Yes, can also degrade IKZF1/3",,5L2I,LQQ,30802347,BSJ-02-162,Yes,,Reviewed,"P11802, Q00534",No,No,No,No,"4, 24, 72, 96",218.12999999999997
961,O=C(NCCCN1CCN(C2=CC=C(NC3=NC=C(C(C)=C(C(C)=O)C(N4C5CCCC5)=O)C4=N3)N=C2)CC1)COC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Active,No,Jurkat,2.664720000000001,,Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,15,3,,,Palbociclib,CC(C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O)=O,CCCNC(=O)CO,Alkane,8,3,3,818.8919999999999,No,,5L2I,LQQ,30802347,BSJ-03-135,No,,Reviewed,"P11802, Q00534",No,No,No,No,4,218.12999999999997
962,O=C(NCCN1CCN(C2=CC=C(NC3=NC=C(C(C)=C(C(C)=O)C(N4C5CCCC5)=O)C4=N3)N=C2)CC1)COC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Active,No,Jurkat,2.2746200000000005,"IC50: 69.6nM/34.6nM for CDK4/CDK6, respectively.",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,15,3,,69.6 nM,Palbociclib,CC(C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O)=O,CCNC(=O)CO,Alkane,7,3,2,804.865,No,,5L2I,LQQ,30802347,BSJ-03-189,No,,Reviewed,"P11802, Q00534",No,No,No,No,4,218.12999999999997
963,O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3N4CCN(C5=CC=C(NC6=NC=C(C(C)=C(C(C)=O)C(N7C8CCCC8)=O)C7=N6)N=C5)CC4)=O,Active,No,Jurkat,3.284020000000001,IC50: 130nM/45.1nM for CDK4/CDK6 respectively.,Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,13,2,,130 nM,Palbociclib,CC(C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O)=O,None,Other,0,0,0,703.7599999999999,No,,5L2I,LQQ,30802347,BSJ-04-060,No,,Reviewed,"P11802, Q00534",No,No,No,No,4,179.79999999999995
964,O=C(C1=CC2=CN=C(NC3=NC=C(N4CCN(CCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)CC4)C=C3)N=C2N1C8CCCC8)N(C)C,Active,No,Jurkat,3.0553000000000026,"IC50: 175nM/142nM for CDK4/CDK6, respectively.",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,15,3,,175 nM,Ribociclib,O=C(C1=CC2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5)N(C)C,CCOCCOCCN,PEG,9,3,6,821.9399999999997,No,,5L2T,6ZZ,30802347,BSJ-01-151,No,,Reviewed,"P11802, Q00534",No,No,No,No,4,196.45999999999998
965,O=C(C1=CC2=CN=C(N([H])C3=NC=C(N4CCN(CCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)CC4)C=C3)N=C2N1C8CCCC8)N(C)C,Active,No,Jurkat,3.8023000000000025,"IC50: 79.7nM/65.5nM for CDK4/CDK6, respectively.",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,13,3,,79.7 nM,Ribociclib,O=C(C1=CC2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5)N(C)C,CCCCN,Alkane,5,1,2,761.8879999999996,No,,5L2T,6ZZ,30802347,BSJ-01-152,No,,Reviewed,"P11802, Q00534",No,No,No,No,4,178.0
966,O=C(C1=CC2=CN=C(NC3=NC=C(N4CCN(CCCCNC(CNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)CC4)C=C3)N=C2N1C8CCCC8)N(C)C,Active,No,Jurkat,2.9185000000000034,"IC50: 70.8nM/52.2nM for CDK4/CDK6, respectively; Show selective degradation of CDK4 (therefore active for CDK4 and inactive for CDK6).",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,14,4,,70.8 nM,Ribociclib,O=C(C1=CC2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5)N(C)C,CCCCNC(=O)CN,Other,9,3,4,818.9399999999997,"Yes, can also degrade IKZF1/3",,5L2T,6ZZ,30802347,BSJ-01-187,No,,Reviewed,P11802,No,No,No,No,4,207.09999999999997
967,O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCCCN4CCN(CC5=CC=C(NC6=NC=C(F)C(C7=CC(F)=C8C(N(C(C)C)C(C)=N8)=C7)=N6)N=C5)CC4)=O,Active,No,Jurkat,5.210520000000005,"IC50: 8.26nM/13.1nM for CDK4/CDK6, respectively.",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,13,3,,8.26 nM,Abemaciclib,CCN(CC1)CCN1CC(C=C2)=CN=C2NC3=NC=C(C(C4=CC(F)=C(N=C5C)C(N5C(C)C)=C4)=N3)F,CCN,Alkane,3,1,0,805.8909999999998,"Yes, can also degrade CDK9",,5L2S,6ZV,30802347,BSJ-01-158,No,,Reviewed,Q00534,No,No,No,No,4,170.57999999999998
968,O=C(NCCCCN1CCN(CC2=CC=C(NC3=NC=C(F)C(C4=CC(F)=C5C(N(C(C)C)C(C)=N5)=C4)=N3)N=C2)CC1)CNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Active,No,Jurkat,4.326720000000003,"IC50: 8.61nM/12.5nM for CDK4/CDK6, respectively.",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,aliphatic_CC,14,4,,8.61 nM,Abemaciclib,CCN(CC1)CCN1CC(C=C2)=CN=C2NC3=NC=C(C(C4=CC(F)=C(N=C5C)C(N5C(C)C)=C4)=N3)F,CCNC(=O)CN,Alkane,7,3,2,862.9429999999996,"Yes, can also degrade CDK9",,5L2S,6ZV,30802347,BSJ-01-184,No,,Reviewed,Q00534,No,No,No,No,4,199.67999999999998
969,O=C(NCCCCN1CCN(C2=CC=C(NC3=NC=C(C(C)=C(C(C)=O)C(N4C5CCCC5)=O)C4=N3)N=C2)CC1)COC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Active,Yes,Jurkat; Molt4; Granta-519; Mino; Jeko; Rec1; Maver,3.054820000000001,"IC50: 26.9nM/10.4nM for CDK4/CDK6, respectively. Can degrade both CDK4 and CDK6.",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,15,3,,26.9 nM,Palbociclib,CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O,CCCCNC(=O)CO,Alkane,9,3,4,832.919,No,,5L2I,LQQ,30802347,BSJ-03-204,Yes,,Reviewed,Q00534,No,No,No,No,"4, 24, 72, 96",218.12999999999997
970,O=C(C1=CN(CCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,Yes,Mice primary Sertoli cells and primary Germ cells,3.0322000000000013,"This is an article that use a previously reported PROTAC (PMID: 33062164) as chemical biology tool to investigate the non-enzymatic FAK function in mice. Therefore, the relevant data were not given in this article.","Yangwode Jing, Ronen Gabizon",~ 1 nM,~ 100 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,5,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,cn(CCOCCOCC)nn,PEG,12,5,7,949.93,No,,5TOB,YAM,32451721,FC-11,No,33062164,Reviewed,"Q05397, Q14289",No,No,No,No,8,273.96
971,O=C(NCC1=CN(CCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)C5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=NC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,2.0883,,Yangwode Jing,,> 70 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,18,5,,,VS6063,CNC(C(C=C1)=CC=C1NC2=NC(NCC3=C(N(C)S(C)(=O)=O)N=CC=N3)=C(C(F)(F)F)C=N2)=O,CCOCCn1ccnn1,PEG,10,4,4,920.8919999999999,No,,5TOB,7KD,33062164,FC-1,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,277.61999999999995
972,O=C(NCC1=CN(CCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)C5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=NC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,2.104900000000002,,Yangwode Jing,,> 60 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,19,5,,,VS6063,CNC(C(C=C1)=CC=C1NC2=NC(NCC3=C(N(C)S(C)(=O)=O)N=CC=N3)=C(C(F)(F)F)C=N2)=O,CCOCCOCCn1ccnn1,PEG,13,5,7,964.9449999999998,No,,5TOB,7KD,33062164,FC-2,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,286.84999999999997
973,O=C(NCC1=CN(CCOCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)C5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=NC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Inactive,No,PA1,2.121500000000005,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,20,5,,,VS6063,CNC(C(C=C1)=CC=C1NC2=NC(NCC3=C(N(C)S(C)(=O)=O)N=CC=N3)=C(C(F)(F)F)C=N2)=O,CCOCCOCCOCCn1ccnn1,PEG,16,6,10,1008.9979999999997,No,,5TOB,7KD,33062164,FC-3,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,296.08
974,O=C(C1=CN(CCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=NC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,2.4106000000000005,,Yangwode Jing,,> 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,5,,,VS6063,CNC(C(C=C1)=CC=C1NC2=NC(NCC3=C(N(C)S(C)(=O)=O)N=CC=N3)=C(C(F)(F)F)C=N2)=O,CCOCCn1cc(C(N)=O)nn1,PEG,13,6,5,906.865,No,,5TOB,7KD,33062164,FC-7,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,277.61999999999995
975,O=C(C1=CN(CCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=NC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,2.427200000000002,,Yangwode Jing,,> 95 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,19,5,,,VS6063,CNC(C(C=C1)=CC=C1NC2=NC(NCC3=C(N(C)S(C)(=O)=O)N=CC=N3)=C(C(F)(F)F)C=N2)=O,CCOCCOCCn1cc(C(N)=O)nn1,PEG,16,7,8,950.9179999999999,No,,5TOB,7KD,33062164,FC-8,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,286.84999999999997
976,O=C(C1=CN(CCOCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=NC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,2.443800000000003,,Yangwode Jing,,> 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,20,5,,,VS6063,CNC(C(C=C1)=CC=C1NC2=NC(NCC3=C(N(C)S(C)(=O)=O)N=CC=N3)=C(C(F)(F)F)C=N2)=O,CCOCCOCCOCCn1cc(C(N)=O)nn1,PEG,19,8,11,994.9709999999998,No,,5TOB,7KD,33062164,FC-9,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,296.0799999999999
977,O=C(NCC1=CN(CCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)C5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,2.6933,,Yangwode Jing,,> 80 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,5,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,CCOCCn1ccnn1,PEG,10,4,4,919.904,No,,5TOB,YAM,33062164,FC-4,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,264.72999999999996
978,O=C(NCC1=CN(CCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)C5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,2.709900000000001,,Yangwode Jing,,> 65 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,5,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,CCOCCOCCn1ccnn1,PEG,13,5,7,963.9569999999999,No,,5TOB,YAM,33062164,FC-5,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,273.96
979,O=C(NCC1=CN(CCOCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)C5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Inactive,No,PA1,2.726500000000005,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,19,5,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,CCOCCOCCOCCn1ccnn1,PEG,16,6,10,1008.0099999999998,No,,5TOB,YAM,33062164,FC-6,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,283.19
980,O=C(C1=CN(CCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,3.015600000000001,,Yangwode Jing,,> 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,5,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,cn(CCOCC)nn,PEG,9,4,4,905.8770000000001,No,,5TOB,YAM,33062164,FC-10,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,264.72999999999996
981,O=C(C1=CN(CCOCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,3.0488000000000026,,Yangwode Jing,,> 94 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,19,5,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,cn(CCOCCOCCOCC)nn,PEG,15,6,10,993.9829999999998,No,,5TOB,YAM,33062164,FC-12,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,283.18999999999994
982,O=C(C1=CN(CCOCCOCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,3.065400000000005,,Yangwode Jing,,> 80 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,20,5,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,cn(CCOCCOCCOCCOCC)nn,PEG,18,7,13,1038.0359999999998,No,,5TOB,YAM,33062164,FC-13,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,292.41999999999996
983,O=C(C1=CN(CCCCCCCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,5.339600000000003,,Yangwode Jing,,> 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,5,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,cn(CCCCCCCC)nn,Alkane,12,3,7,945.986,No,,5TOB,YAM,33062164,FC-14,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,255.49999999999994
984,O=C(C1=CN(CCOCCOCC#CC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,2.971800000000001,,Yangwode Jing,,> 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,4,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,C#CCOCCOCCn(-c)nn,PEG,13,5,7,944.91,No,,5TOB,YAM,33062164,FC-15,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,261.92999999999995
985,O=C(C1=CN(CCCCCOCC#CC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,4.1255000000000015,,Yangwode Jing,,> 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,4,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,C#CCOCCCCCn(-c)nn,Other,13,4,7,942.938,No,,5TOB,YAM,33062164,FC-16,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,252.7
986,O=C(C1=CN(CCCCCCCC#CC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,5.279200000000003,,Yangwode Jing,,> 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,4,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,C#CCCCCCCCn(-c)nn,Alkane,13,3,7,940.9659999999999,No,,5TOB,YAM,33062164,FC-17,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,243.46999999999997
987,O=C(C1=CN(CCOCCOCCCC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,3.552900000000003,,Yangwode Jing,,> 95 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,4,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,cn(CCOCCOCCC)nn,PEG,13,5,8,948.942,No,,5TOB,YAM,33062164,FC-18,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,261.92999999999995
988,O=C(C1=CN(CCCCCOCCCC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,4.706600000000002,,Yangwode Jing,,> 90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,4,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,cn(CCCCCOCCC)nn,Other,13,4,8,946.9699999999999,No,,5TOB,YAM,33062164,FC-19,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,252.7
989,O=C(C1=CN(CCCCCCCCCC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC=C(C(F)(F)F)C(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=N6)C=C5,Active,No,PA1,5.860300000000004,,Yangwode Jing,,> 85 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,4,,,PF562271,CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O,cn(CCCCCCCCC)nn,Alkane,13,3,8,944.9979999999999,No,,5TOB,YAM,33062164,FC-20,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,243.46999999999997
990,O=C(C1=CN(CCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=NC=C6C(F)(F)F)C=C5,Inactive,No,PA1,3.015600000000001,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,5,,,PF562271 analogue,O=S(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC(CC(N4)=O)=C4C=C3)=C(C(F)(F)F)C=N2)(C)=O,cn(CCOCC)nn,PEG,9,4,4,905.8770000000001,No,,5TOB,YAM,33062164,FC-21,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,264.72999999999996
991,O=C(C1=CN(CCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=NC=C6C(F)(F)F)C=C5,Inactive,No,PA1,3.0322000000000013,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,5,,,PF562271 analogue,O=S(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC(CC(N4)=O)=C4C=C3)=C(C(F)(F)F)C=N2)(C)=O,cn(CCOCCOCC)nn,PEG,12,5,7,949.93,No,,5TOB,YAM,33062164,FC-22,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,273.96
992,O=C(C1=CN(CCOCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)NC5=CC=C(NC6=NC(NCC7=CC=CN=C7N(C)S(=O)(C)=O)=NC=C6C(F)(F)F)C=C5,Inactive,No,PA1,3.0488000000000044,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,19,5,,,PF562271 analogue,O=S(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC(CC(N4)=O)=C4C=C3)=C(C(F)(F)F)C=N2)(C)=O,cn(CCOCCOCCOCC)nn,PEG,15,6,10,993.9829999999998,No,,5TOB,YAM,33062164,FC-23,No,,Reviewed,"Q05397, Q14289",No,No,No,No,8,283.18999999999994
993,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CC=C(N5CCN(CCOCCOCCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)CC5)N=C4)C=C2)C3=O)C9=CC=CC=C9,Active,Yes,Ba/F3; H1975,4.2260000000000035,EC50: 0.096uM for L858R/T790M mutant EGFR Ba/F3 cells; >10uM for wildtype EGFR Ba/F3 cells,Yangwode Jing,,> 70 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,4.9 uM,0.096 uM,amine_to_methylamine,15,3,1.1 nM,,JBJ-07-149,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CN=C(N5CCNCC5)C=C4)C=C2)C3=O)C6=CC=CC=C6,CCOCCOCCOCC,PEG,11,3,8,942.0680000000001,No,,,,32510788,DDC-01-163,No,,Reviewed,P00533,Yes,Yes,No,No,"0, 4, 6, 8, 24, 48, 72",204.94
994,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CC=C(N5CCN(CCOCCOCCOCCOC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)CC5)N=C4)C=C2)C3=O)C9=CC=CC=C9,Active,No,Ba/F3,4.192900000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,4.9 uM,2.07 uM,amine_to_methylamine,15,2,1.1 nM,,JBJ-07-149,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CN=C(N5CCNCC5)C=C4)C=C2)C3=O)C6=CC=CC=C6,CCOCCOCCOCCO,PEG,12,4,9,943.0520000000001,No,,,,32510788,11o,No,,Reviewed,P00533,No,No,No,No,72,202.14
995,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CC=C(N5CCN(CCOCCOCCOCCNC6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)CC5)N=C4)C=C2)C3=O)C9=CC=CC=C9,Inactive,No,Ba/F3,4.226000000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,4.9 uM,,amine_to_methylamine,15,3,1.1 nM,,JBJ-07-149,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CN=C(N5CCNCC5)C=C4)C=C2)C3=O)C6=CC=CC=C6,CCOCCOCCOCC,PEG,11,3,8,942.0680000000001,No,,,,32510788,11n,No,,Reviewed,P00533,No,No,No,No,72,204.94
996,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CC=C(N5CCN(CCOCCOCCNC6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)CC5)N=C4)C=C2)C3=O)C9=CC=CC=C9,Inactive,No,Ba/F3,4.209400000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,4.9 uM,,amine_to_methylamine,14,3,1.1 nM,,JBJ-07-149,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CN=C(N5CCNCC5)C=C4)C=C2)C3=O)C6=CC=CC=C6,CCOCCOCC,PEG,8,2,5,898.0150000000001,No,,,,32510788,11m,No,,Reviewed,P00533,No,No,No,No,72,195.70999999999998
997,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CC=C(N5CCN(CCOCCOCCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)CC5)C=C4)C=C2)C3=O)C9=CC(F)=CC=C9O,Active,No,Ba/F3,4.675700000000004,Targeting EGFR L858R/T790M mutant,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,0.477 uM,amine_to_methylamine,15,4,,19 nM,JBJ-04-125-02,O=C(NC1=NC=CS1)C(C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(N6CCNCC6)C=C5)C=C3)C4=O,CCOCCOCCOCC,PEG,11,3,8,975.0690000000002,No,,,,32510788,JBJ-07-038,No,,Reviewed,P00533,Yes,No,No,No,"6, 24, 48, 72",212.27999999999997
998,O=C(NC1=NC=CS1)C(C2=CC(F)=CC=C2F)N(CC3=C4C=C(C5=CC=C(N6CCN(CCOCCOCCOCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O)CC6)C=C5)C=C3)C4=O,Active,No,Ba/F3,5.109200000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,0.153 uM,amine_to_methylamine,14,3,,390 nM,JBJ-04-125-02 analogue,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CC=C(N5CCNCC5)C=C4)C=C2)C3=O)C6=CC(F)=CC=C6F,CCOCCOCCOCC,PEG,11,3,8,977.0599999999997,No,,,,32510788,JBJ-07-200,No,,Reviewed,P00533,Yes,No,No,No,"6, 24, 48, 72",192.04999999999998
999,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCN(CC(NCCOCCOCCOCCNC(COC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O)=O)CC5)NC9=NC=CS9,Inactive,No,Ba/F3,3.0303000000000084,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,amine_to_methylamine,16,4,,,JBJ-07-149 analogue,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)NC6=NC=CS6,CC(=O)NCCOCCOCCOCCNC(=O)CO,PEG,20,8,13,1056.1679999999994,No,,,,32510788,11a,No,,Reviewed,P00533,No,No,No,No,72,247.45
1000,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCN(CC(NCCCCNC(COC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O)=O)CC5)NC9=NC=CS9,Inactive,No,Ba/F3,3.7607000000000026,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,amine_to_methylamine,13,4,,,JBJ-07-149 analogue,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)NC6=NC=CS6,CC(=O)NCCCCNC(=O)CO,Other,13,5,6,952.0629999999999,No,,,,32510788,11b,No,,Reviewed,P00533,No,No,No,No,72,219.76
1001,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCN(CCCCCCNC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)CC5)NC9=NC=CS9,Inactive,No,Ba/F3,6.341600000000006,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,amine_to_methylamine,11,3,,,JBJ-07-149 analogue,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)NC6=NC=CS6,CCCCCC,Alkane,6,0,3,865.0289999999999,No,,,,32510788,11c,No,,Reviewed,P00533,No,No,No,No,72,164.36
1002,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCN(CCCCCCCCNC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)CC5)NC9=NC=CS9,Inactive,No,Ba/F3,7.1218000000000075,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,amine_to_methylamine,11,3,,,JBJ-07-149 analogue,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)NC6=NC=CS6,CCCCCCCC,Alkane,8,0,5,893.083,No,,,,32510788,11d,No,,Reviewed,P00533,No,No,No,No,72,164.36
1003,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCN(C(CCOCCNC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O)CC5)NC9=NC=CS9,Inactive,No,Ba/F3,4.714500000000003,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,amine_to_amide,12,3,,,JBJ-07-149 analogue,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)NC6=NC=CS6,CCOCCC=O,Other,7,2,4,880.9839999999999,No,,,,32510788,11e,No,,Reviewed,P00533,No,No,No,No,72,190.65999999999997
1004,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCN(C(CCOCCOCCNC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O)CC5)NC9=NC=CS9,Inactive,No,Ba/F3,4.731100000000003,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,amine_to_amide,13,3,,,JBJ-07-149 analogue,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)NC6=NC=CS6,CCOCCOCCC=O,PEG,10,3,7,925.0369999999999,No,,,,32510788,11f,No,,Reviewed,P00533,No,No,No,No,72,199.89
1005,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCN(C(CCOCCOCCOCCNC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O)CC5)NC9=NC=CS9,Active,No,Ba/F3,4.747700000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,0.126 uM,amine_to_amide,14,3,,,JBJ-07-149 analogue,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)NC6=NC=CS6,CCOCCOCCOCCC=O,PEG,13,4,10,969.0899999999998,No,,,,32510788,11g,No,,Reviewed,P00533,No,No,No,No,72,209.12
1006,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCN(C(CCOCCOCCOCCOCCNC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O)CC5)NC9=NC=CS9,Inactive,No,Ba/F3,4.764300000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,amine_to_amide,15,3,,,JBJ-07-149 analogue,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)NC6=NC=CS6,CCOCCOCCOCCOCCC=O,PEG,16,5,13,1013.1429999999997,No,,,,32510788,11h,No,,Reviewed,P00533,No,No,No,No,72,218.34999999999997
1007,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCN(C(CCOCCOCCOCCOCCOCCNC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O)CC5)NC9=NC=CS9,Inactive,No,Ba/F3,4.780900000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,amine_to_amide,16,3,,,JBJ-07-149 analogue,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)NC6=NC=CS6,CCOCCOCCOCCOCCOCCC=O,PEG,19,6,16,1057.1959999999997,No,,,,32510788,11i,No,,Reviewed,P00533,No,No,No,No,72,227.57999999999998
1008,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCN(CCOCCOCCNC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)CC5)NC9=NC=CS9,Inactive,No,Ba/F3,4.814400000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,amine_to_methylamine,13,3,,,JBJ-07-149 analogue,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)NC6=NC=CS6,CCOCCOCC,PEG,8,2,5,897.0269999999999,No,,,,32510788,11j,No,,Reviewed,P00533,No,No,No,No,72,182.82
1009,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCN(CCOCCOCCOCCNC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)CC5)NC9=NC=CS9,Active,No,Ba/F3,4.831000000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,0.161 uM,amine_to_methylamine,14,3,,,JBJ-07-149 analogue,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CC=C(C=C4)N5CCNCC5)NC6=NC=CS6,CCOCCOCCOCC,PEG,11,3,8,941.0799999999997,No,,,,32510788,11k,No,,Reviewed,P00533,No,No,No,No,72,192.05
1010,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CN=C(C=C4)N5CCN(CCOCCOCCC(N[C@@H](C(C)(C)C)C(N(C[C@@H](C6)O)[C@@H]6C(N[C@@H](C)C7=CC=C(C=C7)C8=C(N=CS8)C)=O)=O)=O)CC5)NC9=NC=CS9,Inactive,No,Ba/F3,6.888220000000008,,Yangwode Jing,,,O=C([C@H]1N(C[C@@H](C1)O)C([C@H](C(C)(C)C)N)=O)N[C@@H](C)C2=CC=C(C=C2)C3=C(N=CS3)C,VHL,4.9 uM,> 10 uM,amine_to_methylamine,15,4,1.1 nM,,JBJ-07-149,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CN=C(N5CCNCC5)C=C4)C=C2)C3=O)C6=CC=CC=C6,CCOCCOCCC=O,PEG,10,3,7,1097.378,No,,,,32510788,11p,No,,Reviewed,P00533,No,No,No,No,72,211.76
1011,O=C(C(C1=CC=CC=C1)N(C2=O)CC3=C2C=C(C=C3)C4=CN=C(C=C4)N5CCN(CCOCCOCCOCCC(N[C@@H](C(C)(C)C)C(N(C[C@@H](C6)O)[C@@H]6C(N[C@@H](C)C7=CC=C(C=C7)C8=C(N=CS8)C)=O)=O)=O)CC5)NC9=NC=CS9,Inactive,No,Ba/F3,6.904820000000008,,Yangwode Jing,,,O=C([C@H]1N(C[C@@H](C1)O)C([C@H](C(C)(C)C)N)=O)N[C@@H](C)C2=CC=C(C=C2)C3=C(N=CS3)C,VHL,4.9 uM,> 10 uM,amine_to_methylamine,16,4,1.1 nM,,JBJ-07-149,O=C(NC1=NC=CS1)C(N(CC2=C3C=C(C4=CN=C(N5CCNCC5)C=C4)C=C2)C3=O)C6=CC=CC=C6,CCOCCOCCOCCC=O,PEG,13,4,10,1141.431,No,,,,32510788,11q,No,,Reviewed,P00533,No,No,No,No,72,220.99
1012,O=C(C1=CC2=CN=C(NC3=NC=C(N4CCN(CCCCNC(COC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)CC4)C=C3)N=C2N1C8CCCC8)N(C)C,Active,No,Jurkat,2.8854000000000024,"IC50: 50.6nM/30nM for CDK4/CDK6, respectively; Show selective degradation of CDK4 (therefore active for CDK4 and inactive for CDK6).",Yangwode Jing,,,O=C1CCC(N2C(=O)c3ccccc3C2=O)C(=O)N1,Cereblon,,,amine_to_methylamine,14,3,,50.6 nM,Ribociclib,O=C(C1=CC2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5)N(C)C,CCCCNC(=O)CO,Other,9,3,4,819.9239999999998,No,,5L2T,6ZZ,30802347,BSJ-04-132,Yes,,Reviewed,P11802,No,No,No,No,4,204.3
1013,O=C(O)/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)/C(CCC1(C)C)=N/OCC(NCCOCCOCCOC([C@@H](NC([C@@H](O)[C@H](N)CC2=CC=CC=C2)=O)CC(C)C)=O)=O,Active,No,"HT1080, IMR-32, MCF-7",4.739500000000006,,"Yangwode Jing, Ronen Gabizon",~ 100 nM,> 90 %,N[C@@H]([C@@H](C(N[C@H](C(OC)=O)CC(C)C)=O)O)CC1=CC=CC=C1,cIAP1,,,other,11,5,,,ATRA,CC(/C=C/C=C(/C=C/C1=C(CCCC(C)1C)C)C)=C\C(O)=O,COCCOCCNC(=O)CON,PEG,13,6,8,809.0140000000002,"Yes, can degrade both CRABP2 and cIAP1",,3CBS,R12,21515062,Ester-type SNIPER,No,,Reviewed,P29373,No,No,No,No,"0.25, 0.5, 1, 2, 6, 24, 48, 72",208.1
1014,O=C(O)/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)/C(CCC1(C)C)=N/OCC(NCCOCCOCCNC([C@@H](NC([C@@H](O)[C@H](N)CC2=CC=CC=C2)=O)CC(C)C)=O)=O,Active,Yes,"HT1080, IMR-32, MCF-7",4.312500000000007,,"Yangwode Jing, Ronen Gabizon",~ 100 nM,> 90 %,N[C@@H]([C@@H](C(N[C@H](C(NC)=O)CC(C)C)=O)O)CC1=CC=CC=C1,cIAP1,,,other,10,6,,,ATRA,CC(/C=C/C=C(/C=C/C1=C(CCCC(C)1C)C)C)=C\C(O)=O,COCCOCCNC(=O)CON,PEG,13,6,8,808.0300000000002,No,,3CBS,R12,21515062,Amide-type SNIPER,No,,Reviewed,P29373,No,Yes,No,Yes,"0.25, 0.5, 1, 2, 6, 24, 48, 72",210.9
1015,O=C(O)/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)/C(CCC1(C)C)=N/OCC(NCCOCCOCCNC([C@@H](NC(CCCC2=CC=CC=C2)=O)CC(C)C)=O)=O,Inactive,No,HT1080,6.404500000000007,,Yangwode Jing,,,O=C(CCCC1=CC=CC=C1)N[C@H](C(NC)=O)CC(C)C,cIAP1,,,other,8,4,,,ATRA,CC(/C=C/C=C(/C=C/C1=C(CCCC(C)1C)C)C)=C\C(O)=O,COCCOCCNC(=O)CON,PEG,13,6,8,777.0160000000001,No,,3CBS,R12,21515062,Compound 8,No,,Reviewed,P29373,No,No,No,No,6,164.65
1016,O=C(O)C1=CC=C(/C=C/C(C2=CC(C(C)(C)C)=CC(C(C)(C)C)=C2)=O)C=C1OCCCNC(COCCOCCOCCNC([C@@H](NC([C@@H](O)[C@H](N)CC3=CC=CC=C3)=O)CC(C)C)=O)=O,Active,Yes,HT1080,5.388800000000007,The PDB ligand ID is for Am80,"Yangwode Jing, Ronen Gabizon",~ 10 uM,~ 90 %,N[C@@H]([C@@H](C(N[C@H](C(NC)=O)CC(C)C)=O)O)CC1=CC=CC=C1,cIAP1,,,aryl_O,11,6,,,Ch55,CC(C)(C1=CC(C(/C=C/C(C=C2)=CC=C2C(O)=O)=O)=CC(C(C)(C)C)=C1)C,COCCOCCOCC(=O)NCCCO,PEG,16,6,11,917.1539999999999,No,,3KMR,EQN,22014751,9,No,,Reviewed,P10276,Yes,Yes,No,Yes,"6, 24",224.84
1017,CC(C)C[C@H](NC([C@@H](O)[C@H](N)CC1=CC=CC=C1)=O)C(NCCOCCOCCNC(CO/N=C2CC[C@@]3([H])[C@]4([H])CCC5=CC(O)=CC=C5[C@@]4([H])CC[C@]\23C)=O)=O,Active,No,MCF-7,3.3483000000000063,,Yangwode Jing,,,N[C@@H]([C@@H](C(N[C@H](C(NC)=O)CC(C)C)=O)O)CC1=CC=CC=C1,cIAP1,,,other,10,6,,,Estrone,OC(C=C1)=CC(CC[C@@]2([H])[C@]3([H])CC4)=C1[C@@]2([H])CC[C@]3(C)C4=O,COCCOCCNC(=O)CON,PEG,13,6,8,763.9770000000001,No,,,,22014751,11,No,,Reviewed,P03372,Yes,No,No,No,24,193.82999999999998
1018,O=C(O[C@H]1CC[C@@]2([H])[C@]3([H])CC[C@@]4([H])CC(CC[C@]4(C)[C@@]3([H])CC[C@]12C)=O)COCCOCCOCCNC([C@H](CC(C)C)NC([C@@H](O)[C@H](N)CC5=CC=CC=C5)=O)=O,Active,No,MCF-7,4.1378000000000075,,Yangwode Jing,,,N[C@@H]([C@@H](C(N[C@H](C(NC)=O)CC(C)C)=O)O)CC1=CC=CC=C1,cIAP1,,,other,10,4,,,DHT,O[C@H]1CC[C@@]2([H])[C@]3([H])CC[C@@]4([H])CC(CC[C@]4(C)[C@@]3([H])CC[C@]12C)=O,COCCOCCOCC=O,PEG,11,4,8,770.0210000000003,No,,1T5Z,DHT,22014751,13,No,,Reviewed,P10275,No,No,No,No,24,175.51000000000002
1019,CN(C(CCNC(CCNC([C@H](CC(C)C)NC([C@@H](O)[C@@H](CC1=CC=CC=C1)N)=O)=O)=O)=O)CCOC(C=C2)=CC=C2/C(C(C=C3)=CC=C3O)=C(CC)\C4=CC=CC=C4,Active,No,MCF-7,5.072900000000009,,Yangwode Jing,,,CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O,Iap,,,"['amine_to_amide', 'aliphatic_CC']",8,6,,,Endoxifen,OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1,CCNC(=O)CCN,Alkane,8,3,3,806.0170000000002,No,,3ERT,OHT,22277276,5,No,,Reviewed,P03372,No,No,No,Yes,6,183.31999999999996
1020,CN(C(CCCCNC(CCNC([C@H](CC(C)C)NC([C@@H](O)[C@@H](CC1=CC=CC=C1)N)=O)=O)=O)=O)CCOC(C=C2)=CC=C2/C(C(C=C3)=CC=C3O)=C(CC)\C4=CC=CC=C4,Active,No,MCF-7,5.853100000000011,,Yangwode Jing,,,CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O,Iap,,,"['amine_to_amide', 'aliphatic_CC']",8,6,,,Endoxifen,OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1,CCCCNC(=O)CCN,Alkane,10,3,5,834.071,No,,3ERT,OHT,22277276,6,No,,Reviewed,P03372,No,No,No,Yes,6,183.31999999999996
1021,CN(C(CCCCCCNC(CCNC([C@H](CC(C)C)NC([C@@H](O)[C@@H](CC1=CC=CC=C1)N)=O)=O)=O)=O)CCOC(C=C2)=CC=C2/C(C(C=C3)=CC=C3O)=C(CC)\C4=CC=CC=C4,Active,No,MCF-7,6.633300000000012,,Yangwode Jing,,,CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O,Iap,,,"['amine_to_amide', 'aliphatic_CC']",8,6,,,Endoxifen,OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1,CCCCCCNC(=O)CCN,Alkane,12,3,7,862.1249999999999,No,,3ERT,OHT,22277276,7,No,,Reviewed,P03372,No,No,No,Yes,6,183.31999999999996
1022,O=C([C@@H](NC([C@H]1N(CCC1)C([C@@H](NC([C@@H](NC)C)=O)C2CCCCC2)=O)=O)C(C3=CC=CC=C3)C4=CC=CC=C4)NCCOCCOCCNC(CO/N=C5CCC(C)(C)C(/C=C/C(C)=C/C=C/C(C)=C/C(O)=O)=C\5C)=O,Active,Yes,"HT1080, IMR-32",6.831600000000013,,"Yangwode Jing, Ronen Gabizon",~ 1 uM,,O=C([C@@H](NC([C@H]1N(CCC1)C([C@@H](NC([C@@H](NC)C)=O)C2CCCCC2)=O)=O)C(C3=CC=CC=C3)C4=CC=CC=C4)OC,cIAP1,,,other,11,6,,,ATRA,CC(/C=C/C=C(/C=C/C1=C(CCCC(C)1C)C)C)=C\C(O)=O,NCCOCCOCCNC(=O)CON,PEG,15,7,10,1062.3629999999994,No,,3CBS,R12,22658364,6,No,,Reviewed,"P29373, Q13490",No,No,No,Yes,"6, 24, 48, 72",226.08999999999995
1023,CC(C[C@H](C(NCCCCCCC(NCC1=CC=C(C(NC2=CC(NC3=NC=CC(C4=CN=CC=C4)=N3)=C(C=C2)C)=O)C=C1)=O)=O)NC([C@@H]([C@H](Cc5ccccc5)N)O)=O)C,Inactive,No,K562,5.987620000000005,BCR-ABL degredation,Yangwode Jing,,,CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O,Iap,,,other,10,7,,,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCCCN,Alkane,6,1,3,828.0310000000002,No,,2HYY,STI,27666635,SNIPER(ABL)-1,No,,Reviewed,P00519,No,No,No,No,"8, 24",213.35
1024,CC(C[C@H](C(NCCCCCCCC(NCC1=CC=C(C(NC2=CC(NC3=NC=CC(C4=CN=CC=C4)=N3)=C(C=C2)C)=O)C=C1)=O)=O)NC([C@@H]([C@H](Cc5ccccc5)N)O)=O)C,Active,Yes,K562,6.377720000000005,BCR-ABL degredation,"Yangwode Jing, Ronen Gabizon",~ 30 uM,,CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O,Iap,,,other,10,7,,,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCCCCN,Alkane,7,1,4,842.0580000000001,No,,2HYY,STI,27666635,SNIPER(ABL)-2,No,,Reviewed,P00519,No,No,No,No,"8, 24",213.35
1025,CC(C[C@H](C(NCCCCCCCCC(NCC1=CC=C(C(NC2=CC(NC3=NC=CC(C4=CN=CC=C4)=N3)=C(C=C2)C)=O)C=C1)=O)=O)NC([C@@H]([C@H](Cc5ccccc5)N)O)=O)C,Active,No,K562,6.767820000000007,BCR-ABL degredation,"Yangwode Jing, Ronen Gabizon",~ 30 uM,,CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O,Iap,,,other,10,7,,,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCCCCCN,Alkane,8,1,5,856.085,No,,2HYY,STI,27666635,SNIPER(ABL)-3,No,,Reviewed,P00519,No,No,No,No,"8, 24",213.35
1027,O=C(C(N1)=CC(C(C2=CC(NS(=O)(CC)=O)=CC=C2OC3=CC=C(F)C=C3F)=CN4C)=C1C4=O)NCC5=CN(CCOCC(NC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)=O)N=N5,Active,Yes,"BxPC3, DLD-1, HCT-116, MDA-MB-231, A549, PC-9",3.3035000000000014,"Above EC50 was obtained in BxPC3 cells. EC50 for DLD-1/HCT-116/MDA-MB-231/A549/PC-9 cells: 4.09uM/6.47uM/>10uM/2.42uM/>10uM, respectively.",Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,1.216 uM,0.165 uM,aryl_C,14,5,2.5 nM,2.7 nM,ABBV-075,CCS(=O)(NC1=CC=C(C(C2=CN(C(C3=C2C=CN3)=O)C)=C1)OC4=CC=C(C=C4F)F)=O,O=CCOCCn1cc(CNC=O)nn1,PEG,15,7,8,926.9159999999994,No,,5UVX,,32361153,32a,No,,Reviewed,O60885,No,No,No,No,"1, 2, 3, 4, 8, 24, 48",257.80999999999995
1028,O=C(C(N1)=CC(C(C2=CC(NS(=O)(CC)=O)=CC=C2OC3=CC=C(F)C=C3F)=CN4C)=C1C4=O)NCC5=CN(CCOCCOCC(NC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)=O)N=N5,Active,No,"BxPC3, DLD-1, HCT-116, MDA-MB-231, A549, PC-9",3.320100000000002,"Above EC50 was obtained in BxPC3 cells. EC50 for DLD-1/HCT-116/MDA-MB-231/A549/PC-9 cells: 5.96uM/2.22uM/>10uM/0.39uM/>10uM, respectively.",Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,1.216 uM,0.245 uM,aryl_C,15,5,2.5 nM,3.4 nM,ABBV-075,CCS(=O)(NC1=CC=C(C(C2=CN(C(C3=C2C=CN3)=O)C)=C1)OC4=CC=C(C=C4F)F)=O,O=CCOCCOCCn1cc(CNC=O)nn1,PEG,18,8,11,970.9689999999993,No,,5UVX,,32361153,32b,No,,Reviewed,O60885,No,No,No,No,"24, 48",267.03999999999996
1029,O=C(C(N1)=CC(C(C2=CC(NS(=O)(CC)=O)=CC=C2OC3=CC=C(F)C=C3F)=CN4C)=C1C4=O)NCC5=CN(CCOCCOCCOCC(NC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)=O)N=N5,Active,No,"BxPC3, DLD-1, HCT-116, MDA-MB-231, A549, PC-9",3.3367000000000013,"Above EC50 was obtained in BxPC3 cells. EC50 for DLD-1/HCT-116/MDA-MB-231/A549/PC-9 cells: 2.04uM/4.39uM/>10uM/0.30uM/>10uM, respectively.",Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,1.216 uM,4.138 uM,aryl_C,16,5,2.5 nM,3.7 nM,ABBV-075,CCS(=O)(NC1=CC=C(C(C2=CN(C(C3=C2C=CN3)=O)C)=C1)OC4=CC=C(C=C4F)F)=O,O=CCOCCOCCOCCn1cc(CNC=O)nn1,PEG,21,9,14,1015.0219999999991,No,,5UVX,,32361153,32c,No,,Reviewed,O60885,No,No,No,No,24,276.2699999999999
1030,O=C(C(N1)=CC(C(C2=CC(NS(=O)(CC)=O)=CC=C2OC3=CC=C(F)C=C3F)=CN4C)=C1C4=O)NCC5=CN(CCOCCOCCOCCOCC(NC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)=O)N=N5,Inactive,No,"BxPC3, DLD-1, HCT-116, MDA-MB-231, A549, PC-9",3.3533000000000017,"Above EC50 was obtained in BxPC3 cells. EC50 for DLD-1/HCT-116/MDA-MB-231/A549/PC-9 cells: >10uM/>10uM/>10uM/2.14uM/>10uM, respectively.",Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,1.216 uM,> 10 uM,aryl_C,17,5,2.5 nM,12.0 nM,ABBV-075,CCS(=O)(NC1=CC=C(C(C2=CN(C(C3=C2C=CN3)=O)C)=C1)OC4=CC=C(C=C4F)F)=O,O=CCOCCOCCOCCOCCn1cc(CNC=O)nn1,PEG,24,10,17,1059.0749999999991,No,,5UVX,,32361153,32d,No,,Reviewed,O60885,No,No,No,No,24,285.49999999999994
1031,O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=CC=NC5=CC(OCCCOCCCOCCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O)=C(OC)C=C45)C(F)=C3,Active,Yes,MDA-MB-231,8.494620000000006,,Yangwode Jing,210 nM,91 %,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,14,5,,,foretinib,COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1O,CCCOCCCOCCC=O,PEG,12,3,9,1106.2589999999996,Yes. This PROTAC can also degrade other 35 kinases including c-Met,,,,29129718,1,Yes,,Reviewed,Q16539,Yes,No,No,Yes,24,228.86999999999995
1032,O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=CC=NC5=CC(OCCCOCCCOCCC(NCCOC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)=C(OC)C=C45)C(F)=C3,Active,Yes,MDA-MB-231,5.850000000000005,,Yangwode Jing,27 nM,91 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,4,,,foretinib,COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1O,CCCOCCCOCCC(=O)NCCO,PEG,16,5,11,992.9859999999998,Yes. This PROTAC can also degrade other 61 proteins including c-Met,,,,29129718,2,Yes,,Reviewed,O15264,Yes,No,No,Yes,24,239.11999999999998
1033,O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCCCN4CCN(C5=NC(N6C(C(F)F)=NC7=CC=CC=C67)=NC(N8CCOCC8)=N5)CC4,Inactive,No,,2.7070000000000007,Compound A was not subjected to any cell experiment,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,14,2,16 nM,2847 nM,ZSTK474,FC(C1=NC2=CC=CC=C2N1C3=NC(N4CCOCC4)=NC(N5CCOCC5)=N3)F,NCCCCCC=O,Alkane,8,2,5,785.8129999999998,No,,2WXL,ZS4,29625382,A,No,,Reviewed,P42336,No,No,No,No,,188.08999999999997
1034,O=C(NCCCC(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)=O)CCC(N4CCN(C5=NC(N6C(C(F)F)=NC7=CC=CC=C67)=NC(N8CCOCC8)=N5)CC4)=O,Active,No,HepG2,1.3498000000000014,,"Yangwode Jing, Ronen Gabizon",> 10 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,15,3,16 nM,18 nM,ZSTK474,FC(C1=NC2=CC=CC=C2N1C3=NC(N4CCOCC4)=NC(N5CCOCC5)=N3)F,NC(=O)CCC(=O)NCCCC=O,Other,13,5,7,856.8479999999997,No,,2WXL,ZS4,29625382,B,No,,Reviewed,P42336,No,No,No,No,"6, 12, 24",234.26
1035,O=C(NCCCCCC(N1CCN(C2=NC(N3C(C(F)F)=NC4=CC=CC=C34)=NC(N5CCOCC5)=N2)CC1)=O)CCC(NCCCC(NC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)=O,Inactive,No,HepG2,2.026400000000006,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,16,4,16 nM,38 nM,ZSTK474,FC(C1=NC2=CC=CC=C2N1C3=NC(N4CCOCC4)=NC(N5CCOCC5)=N3)F,NC(=O)CCCCCNC(=O)CCC(=O)NCCCC=O,Other,21,7,13,970.0079999999994,No,,2WXL,ZS4,29625382,C,No,,Reviewed,P42336,No,No,No,No,6,263.36
1036,O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCCCNC(CCC(N4CCN(C5=NC(N6C(C(F)F)=NC7=CC=CC=C67)=NC(N8CCOCC8)=N5)CC4)=O)=O,Active,Yes,HepG2,2.130000000000001,,"Yangwode Jing, Ronen Gabizon",> 10 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,15,3,16 nM,24 nM,ZSTK474,FC(C1=NC2=CC=CC=C2N1C3=NC(N4CCOCC4)=NC(N5CCOCC5)=N3)F,NC(=O)CCC(=O)NCCCCCC=O,Other,15,5,9,884.9019999999998,No,,2WXL,ZS4,29625382,D,No,,Reviewed,P42336,No,No,No,No,"6, 12, 24",234.26
1037,O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCN4N=NC(CN5CCN(C6=NC(N7C(C(F)F)=NC8=CC=CC=C78)=NC(N9CCOCC9)=N6)CC5)=C4,Active,No,HepG2,1.7185000000000001,,"Yangwode Jing, Ronen Gabizon",> 10 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,17,2,16 nM,90 nM,ZSTK474,FC(C1=NC2=CC=CC=C2N1C3=NC(N4CCOCC4)=NC(N5CCOCC5)=N3)F,NCc1cn(CCCC=O)nn1,Other,12,5,5,838.8369999999998,No,,2WXL,ZS4,29625382,E,No,,Reviewed,P42336,No,No,No,No,"6, 12, 24",218.8
1038,O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCCCN4N=NC(CN5CCN(C6=NC(N7C(C(F)F)=NC8=CC=CC=C78)=NC(N9CCOCC9)=N6)CC5)=C4,Active,No,HepG2,2.4987000000000004,,"Yangwode Jing, Ronen Gabizon",> 10 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,morpholine_to_piperazine,17,2,16 nM,86 nM,ZSTK474,FC(C1=NC2=CC=CC=C2N1C3=NC(N4CCOCC4)=NC(N5CCOCC5)=N3)F,NCc1cn(CCCCCC=O)nn1,Other,14,5,7,866.8909999999997,No,,2WXL,ZS4,29625382,F,No,,Reviewed,P42336,No,No,No,No,"6, 12, 24",218.8
1041,O=P([O-])(NCCCCCC(NC1=CC=CC2=C1CN(C(CC3)C(NC3=O)=O)C2=O)=O)OC[C@@H]4O[C@H](N5C=NC6=C5N=C(N)NC6=O)[C@@H](O)[C@H]4O,Inactive,No,MDA-MB-231; K562,-1.6442999999999948,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,7,,,GMP,O=P([O-])OC[C@@H]1O[C@H](N2C=NC3=C2N=C(N)NC3=O)[C@@H](O)[C@H]1O,NCCCCCC=O,Alkane,8,2,5,716.6250000000002,No,,1EJ1,M7G,30735900,4,No,,Reviewed,P06730,No,No,No,No,"24, 72",296.25
1042,O[C@H]1[C@@H](O[C@@H]([C@H]1O)N2C3=C(C(NC(N)=N3)=O)[N+](CC4=CC=CC=C4)=C2)COP(O)(NCCCCCC(N[C@H](CCC=C56)C6CN([C@@H](CC7)C(NC7=O)=O)C5=O)=O)=O,Inactive,No,MDA-MB-231; K562,-1.0025999999999893,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,8,,,Bn7GMP,O[C@H]1[C@@H](O[C@@H]([C@H]1O)N2C3=C(C(NC(N)=N3)=O)[N+](CC4=CC=CC=C4)=C2)COP(O)=O,NCCCCCC=O,Alkane,8,2,5,812.7979999999999,No,,1EJ1,M7G,30735900,5a,No,,Reviewed,P06730,No,No,No,No,"24, 72",284.40999999999997
1043,O[C@H]1[C@@H](O[C@@H]([C@H]1O)N2C3=C(C(NC(N)=N3)=O)[N+](CC4=CC=C(F)C=C4)=C2)COP(O)(NCCCCCC(N[C@H](CCC=C56)C6CN([C@@H](CC7)C(NC7=O)=O)C5=O)=O)=O,Inactive,No,MDA-MB-231; K562,-0.8634999999999904,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,13,8,,,4F-Bn7GMP,O[C@H]1[C@@H](O[C@@H]([C@H]1O)N2C3=C(C(NC(N)=N3)=O)[N+](CC4=CC=C(F)C=C4)=C2)COP(O)=O,NCCCCCC=O,Alkane,8,2,5,830.7879999999998,No,,1EJ1,M7G,30735900,5b,No,,Reviewed,P06730,No,No,No,No,"24, 72",284.40999999999997
1044,O=C1NC(N)=NC2=C1[N+](CC3=CC=C(F)C=C3)=CN2[C@@H]4O[C@H](COS(=O)(NC(CCC(NCCCCCC(NC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)=O)=O)=O)=O)[C@@H](O)[C@H]4O,Inactive,No,MDA-MB-231; K562,-1.3649999999999913,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,8,,,Sulfamate-containing 4F-Bn7GMP,O[C@H]1[C@@H](O[C@@H]([C@H]1O)N2C3=C(C(NC(N)=N3)=O)[N+](CC4=CC=C(F)C=C4)=C2)COS(=O)(O)=O,NC(=O)CCC(=O)NCCCCCC=O,Other,15,5,9,925.9300000000001,No,,1EJ1,M7G,30735900,13b,No,,Reviewed,P06730,No,No,No,No,"24, 72",327.42
1045,O=C1NC(N)=NC2=C1[N+](CC3=CC=CC=C3)=CN2[C@@H]4O[C@H](COS(=O)(NC(CCC(NCCCCCC(NC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)=O)=O)=O)=O)[C@@H](O)[C@H]4O,Inactive,No,MDA-MB-231; K562,-1.504099999999991,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,8,,,Sulfamate-containing Bn7GMP,O[C@H]1[C@@H](O[C@@H]([C@H]1O)N2C3=C(C(NC(N)=N3)=O)[N+](CC4=CC=CC=C4)=C2)COS(=O)(O)=O,NC(=O)CCC(=O)NCCCCCC=O,Other,15,5,9,907.9400000000003,No,,1EJ1,M7G,30735900,13a,No,,Reviewed,P06730,No,No,No,No,"24, 72",327.42
1046,O=C1NC(N)=NC2=C1N=CN2[C@@H]3O[C@H](COS(=O)(NC(CCC(NCCCCCC(NC4=CC=CC5=C4CN(C(CC6)C(NC6=O)=O)C5=O)=O)=O)=O)=O)[C@@H](O)[C@H]3O,Inactive,No,MDA-MB-231; K562,-2.444899999999991,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,17,8,,,Sulfamate-containing GMP,O[C@H]1[C@@H](O[C@@H]([C@H]1O)N2C3=C(C(NC(N)=N3)=O)N=C2)COS(=O)(O)=O,NC(=O)CCC(=O)NCCCCCC=O,Other,15,5,9,816.8070000000004,No,,1EJ1,M7G,30735900,12,No,,Reviewed,P06730,No,No,No,No,"24, 72",336.43
1047,O=C1NC(N)=NC2=C1[N+](CC3=CC=C(F)C=C3)=CN2[C@H]4O[C@@H](COP(OP(NCCCCCC(NC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)=O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,Inactive,No,MDA-MB-231; K562,0.18460000000000198,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,9,,,4F-Bn7GDP,O=C1NC(N)=NC2=C1[N+](CC3=CC=C(F)C=C3)=CN2[C@H]4O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,NCCCCCC=O,Alkane,8,2,5,906.7350000000004,No,,1EJ1,M7G,30735900,23b,No,,Reviewed,P06730,No,No,No,No,"24, 72",330.94
1048,O=C1NC(N)=NC2=C1[N+](CC3=CC=CC=C3)=CN2[C@H]4O[C@@H](COP(OP(NCCCCCC(NC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)=O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,Inactive,No,MDA-MB-231; K562,0.04550000000000204,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,9,,,Bn7GDP,O=C1NC(N)=NC2=C1[N+](CC3=CC=CC=C3)=CN2[C@H]4O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,NCCCCCC=O,Alkane,8,2,5,888.7450000000003,No,,1EJ1,M7G,30735900,23a,No,,Reviewed,P06730,No,No,No,No,"24, 72",330.94
1049,O=C1NC(N)=NC2=C1N=CN2[C@H]3O[C@@H](COP(OP(NCCCCCC(NC4=CC=CC5=C4CN(C(CC6)C(NC6=O)=O)C5=O)=O)(O)=O)(O)=O)[C@H](O)[C@@H]3O,Inactive,No,MDA-MB-231; K562,-0.8952999999999975,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,9,,,GDP,O=C1NC(N)=NC2=C1N=CN2[C@H]3O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]3O,NCCCCCC=O,Alkane,8,2,5,797.6120000000005,,,1EJ1,M7G,30735900,20,No,,Reviewed,P06730,No,No,No,No,"24, 72",339.95000000000005
1050,O=C(NC1=CC=CC2=C1CN(C(CC3)C(NC3=O)=O)C2=O)CCOCCOCCOCCNP(OP(OC[C@@H]4O[C@H](N5C=NC6=C5N=C(N)NC6=O)[C@@H](O)[C@H]4O)(O)=O)(O)=O,Inactive,No,MDA-MB-231; K562,-2.0157999999999943,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,19,9,,,GDP,O=C1NC(N)=NC2=C1N=CN2[C@H]3O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]3O,NCCOCCOCCOCCC=O,PEG,14,5,11,887.6900000000004,No,,1EJ1,M7G,30735900,21,No,,Reviewed,P06730,No,No,No,No,"24, 72",367.64000000000004
1051,O=C(NC1=CC=CC2=C1CN(C(CC3)C(NC3=O)=O)C2=O)CCOCCOCCOCCOCCOCCOCCOCCNP(OP(OC[C@@H]4O[C@H](N5C=NC6=C5N=C(N)NC6=O)[C@@H](O)[C@H]4O)(O)=O)(O)=O,Inactive,No,MDA-MB-231; K562,-1.94939999999999,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,23,9,,,GDP,O=C1NC(N)=NC2=C1N=CN2[C@H]3O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]3O,NCCOCCOCCOCCOCCOCCOCCOCCC=O,PEG,26,9,23,1063.9020000000003,No,,1EJ1,M7G,30735900,22,No,,Reviewed,P06730,No,No,No,No,"24, 72",404.56
1052,O=C1NC(N)=NC2=C1[N+](CC3=CC=CC=C3)=CN2[C@H]4O[C@@H](COP(OP(NCCOCCOCCOCCC(NC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)=O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,Inactive,No,MDA-MB-231; K562,-1.074999999999994,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,9,,,Bn7GDP,O=C1NC(N)=NC2=C1[N+](CC3=CC=CC=C3)=CN2[C@H]4O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,NCCOCCOCCOCCC=O,PEG,14,5,11,978.8230000000001,No,,1EJ1,M7G,30735900,24a,No,,Reviewed,P06730,No,No,No,No,"24, 72",358.63
1053,O=C1NC(N)=NC2=C1[N+](CC3=CC=CC=C3)=CN2[C@@H]4O[C@H](COP(OP(NCCOCCOCCOCCOCCOCCOCCOCCC(NC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)=O)(O)=O)(O)=O)[C@@H](O)[C@H]4O,Inactive,No,MDA-MB-231; K562,-1.0085999999999882,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,22,9,,,Bn7GDP,O=C1NC(N)=NC2=C1[N+](CC3=CC=CC=C3)=CN2[C@H]4O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,NCCOCCOCCOCCOCCOCCOCCOCCC=O,PEG,26,9,23,1155.0349999999996,No,,1EJ1,M7G,30735900,25a,No,,Reviewed,P06730,No,No,No,No,"24, 72",395.55
1054,O=C1NC(N)=NC2=C1[N+](CC3=CC=C(F)C=C3)=CN2[C@H]4O[C@@H](COP(OP(NCCOCCOCCOCCC(NC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)=O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,Inactive,No,MDA-MB-231; K562,-0.9358999999999942,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,9,,,4F-Bn7GDP,O=C1NC(N)=NC2=C1[N+](CC3=CC=C(F)C=C3)=CN2[C@H]4O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,NCCOCCOCCOCCC=O,PEG,14,5,11,996.813,No,,1EJ1,M7G,30735900,24b,No,,Reviewed,P06730,No,No,No,No,"24, 72",358.63
1055,O=C1NC(N)=NC2=C1[N+](CC3=CC=C(F)C=C3)=CN2[C@@H]4O[C@H](COP(OP(NCCOCCOCCOCCOCCOCCOCCOCCC(NC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)=O)(O)=O)(O)=O)[C@@H](O)[C@H]4O,Inactive,No,MDA-MB-231; K562,-0.8694999999999893,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,22,9,,,4F-Bn7GDP,O=C1NC(N)=NC2=C1[N+](CC3=CC=C(F)C=C3)=CN2[C@H]4O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,NCCOCCOCCOCCOCCOCCOCCOCCC=O,PEG,26,9,23,1173.0249999999994,No,,1EJ1,M7G,30735900,25b,No,,Reviewed,P06730,No,No,No,No,"24, 72",395.55
1056,O=C1NC(N)=NC2=C1[N+](CC3=CC=C(F)C=C3)=CN2[C@H]4O[C@@H](COP(OP(NCCCCCC(N[C@@H](C(C)(C)C)C(N5C(C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)C[C@H](O)C5)=O)=O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,Inactive,No,MDA-MB-231; K562,2.0259200000000033,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,17,10,,,4F-Bn7GDP,O=C1NC(N)=NC2=C1[N+](CC3=CC=C(F)C=C3)=CN2[C@H]4O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,NCCCCCC=O,Alkane,8,2,5,1078.0440000000003,No,,1EJ1,M7G,30735900,30b,No,,Reviewed,P06730,No,No,No,No,"24, 72",346.99
1057,O=C1NC(N)=NC2=C1[N+](CC3=CC=CC=C3)=CN2[C@H]4O[C@@H](COP(OP(NCCCCCC(N[C@@H](C(C)(C)C)C(N5C(C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)C[C@H](O)C5)=O)=O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,Inactive,No,MDA-MB-231; K562,1.8868200000000033,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,17,10,,,Bn7GDP,O=C1NC(N)=NC2=C1[N+](CC3=CC=CC=C3)=CN2[C@H]4O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]4O,NCCCCCC=O,Alkane,8,2,5,1060.054,No,,1EJ1,M7G,30735900,30a,No,,Reviewed,P06730,No,No,No,No,"24, 72",346.99
1058,O=C1NC(N)=NC2=C1N=CN2[C@H]3O[C@@H](COP(OP(NCCCCCC(N[C@@H](C(C)(C)C)C(N4C(C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@H](O)C4)=O)=O)(O)=O)(O)=O)[C@H](O)[C@@H]3O,Inactive,No,MDA-MB-231; K562,0.9460200000000021,,Yangwode Jing,,,Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1,VHL,,,other,18,10,,,GDP,O=C1NC(N)=NC2=C1N=CN2[C@H]3O[C@@H](COP(OP(O)(O)=O)(O)=O)[C@H](O)[C@@H]3O,NCCCCCC=O,Alkane,8,2,5,968.9210000000004,No,,1EJ1,M7G,30735900,29,No,,Reviewed,P06730,No,No,No,No,"24, 72",356.0
1059,O=C(C(N(CC1=C2C=CC=C1C#CCN3CCN(C(N4C(C5=CC=C(Cl)C=C5)C(C6=CC=C(Cl)C=C6)N=C4C7=CC=C(C(C)(C)C)C=C7OCC)=O)CC3)C2=O)CC8)NC8=O,Active,Yes,RS4;11,7.784700000000009,,"Yangwode Jing, Ronen Gabizon",~ 100 nM,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,7.2 nM,amine_to_methylamine,7,1,,,RG7112 analogue,O=C(N1CCNCC1)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CC,Other,3,0,0,859.8549999999994,No,,4IPF,1F0,31128449,20,No,,Reviewed,Q00987,No,No,No,No,6,114.85999999999999
1060,O=C(C(N(CC1=C2C=CC=C1C#CCCN3CCN(C(N4C(C5=CC=C(Cl)C=C5)C(C6=CC=C(Cl)C=C6)N=C4C7=CC=C(C(C)(C)C)C=C7OCC)=O)CC3)C2=O)CC8)NC8=O,Inactive,No,RS4;11,8.17480000000001,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,7,1,,,RG7112 analogue,O=C(N1CCNCC1)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CCC,Other,4,0,0,873.8819999999994,No,,4IPF,1F0,31128449,21,No,,Reviewed,Q00987,No,No,No,No,6,114.85999999999999
1061,O=C(C(N(CC1=C2C=CC=C1C#CCCCN3CCN(C(N4C(C5=CC=C(Cl)C=C5)C(C6=CC=C(Cl)C=C6)N=C4C7=CC=C(C(C)(C)C)C=C7OCC)=O)CC3)C2=O)CC8)NC8=O,Inactive,No,RS4;11,8.564900000000009,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,7,1,,,RG7112 analogue,O=C(N1CCNCC1)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CCCC,Other,5,0,1,887.9089999999994,No,,4IPF,1F0,31128449,22,No,,Reviewed,Q00987,No,No,No,No,6,114.85999999999999
1062,O=C(NCC(N1CCN(C(N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC)=O)CC1)=O)CCC#CC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O,Inactive,No,RS4;11,7.20770000000001,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,8,2,,,RG7112 analogue,O=C(N1CCNCC1)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CCCC(=O)NCC=O,Other,10,3,4,958.9439999999994,No,,4IPF,1F0,31128449,14,No,,Reviewed,Q00987,No,No,No,No,6,161.03
1063,O=C(NCC(N1CCN(C(N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC)=O)CC1)=O)CCCC#CC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O,Active,No,RS4;11,7.597800000000011,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,8,2,,,RG7112 analogue,O=C(N1CCNCC1)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CCCCC(=O)NCC=O,Other,11,3,5,972.9709999999993,No,,4IPF,1F0,31128449,15,No,,Reviewed,Q00987,No,No,No,No,6,161.03
1064,O=C(NCC(N1CCN(C(N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC)=O)CC1)=O)CCCCC#CC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O,Inactive,No,RS4;11,7.987900000000011,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,8,2,,,RG7112 analogue,O=C(N1CCNCC1)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CCCCCC(=O)NCC=O,Other,12,3,6,986.9979999999993,No,,4IPF,1F0,31128449,16,No,,Reviewed,Q00987,No,No,No,No,6,161.03
1065,O=C(C(N(CC1=C2C=CC=C1C#CCCC(N3CCN(C(N4C(C5=CC=C(Cl)C=C5)C(C6=CC=C(Cl)C=C6)N=C4C7=CC=C(C(C)(C)C)C=C7OCC)=O)CC3)=O)C2=O)CC8)NC8=O,Active,No,RS4;11,8.09150000000001,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,7,1,,,RG7112 analogue,O=C(N1CCNCC1)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CCCC=O,Other,6,1,2,901.8919999999995,No,,4IPF,1F0,31128449,7,No,,Reviewed,Q00987,No,No,No,No,6,131.92999999999998
1066,O=C(C(N(CC1=C2C=CC=C1C#CCCCC(N3CCN(C(N4C(C5=CC=C(Cl)C=C5)C(C6=CC=C(Cl)C=C6)N=C4C7=CC=C(C(C)(C)C)C=C7OCC)=O)CC3)=O)C2=O)CC8)NC8=O,Inactive,No,RS4;11,8.481600000000007,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,7,1,,,RG7112 analogue,O=C(N1CCNCC1)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CCCCC=O,Other,7,1,3,915.9189999999995,No,,4IPF,1F0,31128449,8,No,,Reviewed,Q00987,No,No,No,No,6,131.92999999999998
1067,O=C(C(N(CC1=C2C=CC=C1C#CCCCCC(N3CCN(C(N4C(C5=CC=C(Cl)C=C5)C(C6=CC=C(Cl)C=C6)N=C4C7=CC=C(C(C)(C)C)C=C7OCC)=O)CC3)=O)C2=O)CC8)NC8=O,Inactive,No,RS4;11,8.871700000000006,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,7,1,,,RG7112 analogue,O=C(N1CCNCC1)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CCCCCC=O,Other,8,1,4,929.9459999999996,No,,4IPF,1F0,31128449,9,No,,Reviewed,Q00987,No,No,No,No,6,131.92999999999998
1068,O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3N4CCN(C(N5C(C6=CC=C(Cl)C=C6)C(C7=CC=C(Cl)C=C7)N=C5C8=CC=C(C(C)(C)C)C=C8OCC)=O)CC4)=O,Inactive,No,RS4;11,7.57780000000001,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,8,1,,,RG7112 analogue,O=C(N1CCNCC1)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,None,Other,0,0,0,835.7889999999998,No,,4IPF,1F0,31128449,25,No,,Reviewed,Q00987,No,No,No,No,6,131.92999999999998
1069,O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCC(N4CCN(C(N5C(C6=CC=C(Cl)C=C6)C(C7=CC=C(Cl)C=C7)N=C5C8=CC=C(C(C)(C)C)C=C8OCC)=O)CC4)=O)=O,Inactive,No,RS4;11,7.01190000000001,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_amide,9,2,,,RG7112 analogue,O=C(N1CCNCC1)N2C(C3=CC=C(Cl)C=C3)C(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,CC=O,Other,3,1,0,892.8409999999998,No,,4IPF,1F0,31128449,26,No,,Reviewed,Q00987,No,No,No,No,6,161.02999999999997
1070,O=C(C(N(CC1=C2C=CC=C1C#CCN3CCN(C(N4[C@H](C5=CC=C(Cl)C=C5)[C@H](C6=CC=C(Cl)C=C6)N=C4C7=CC=C(C(C)(C)C)C=C7OCC)=O)CC3)C2=O)CC8)NC8=O,Active,Yes,RS4;11,7.784700000000009,,Yangwode Jing,23 nM,90 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,3.2 nM,amine_to_methylamine,7,1,,,"(4S,5R)-RG7112 analogue",O=C(N1CCNCC1)N2[C@H](C3=CC=C(Cl)C=C3)[C@H](C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CC,Other,3,0,0,859.8549999999994,No,,4IPF,1F0,31128449,32,No,,Reviewed,Q00987,No,Yes,No,Yes,6,114.85999999999999
1071,O=C(C(N(CC1=C2C=CC=C1C#CCCN3CCN(C(N4[C@H](C5=CC=C(Cl)C=C5)[C@H](C6=CC=C(Cl)C=C6)N=C4C7=CC=C(C(C)(C)C)C=C7OCC)=O)CC3)C2=O)CC8)NC8=O,Inactive,No,RS4;11,8.17480000000001,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,7,1,,,"(4S,5R)-RG7112 analogue",O=C(N1CCNCC1)N2[C@H](C3=CC=C(Cl)C=C3)[C@H](C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CCC,Other,4,0,0,873.8819999999994,No,,4IPF,1F0,31128449,33,No,,Reviewed,Q00987,No,No,No,No,6,114.85999999999999
1072,O=C(C(N(CC1=C2C=CC=C1C#CCCCN3CCN(C(N4[C@H](C5=CC=C(Cl)C=C5)[C@H](C6=CC=C(Cl)C=C6)N=C4C7=CC=C(C(C)(C)C)C=C7OCC)=O)CC3)C2=O)CC8)NC8=O,Inactive,No,RS4;11,8.564900000000009,,Yangwode Jing,,,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,amine_to_methylamine,7,1,,,"(4S,5R)-RG7112 analogue",O=C(N1CCNCC1)N2[C@H](C3=CC=C(Cl)C=C3)[C@H](C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC,C#CCCC,Other,5,0,1,887.9089999999994,No,,4IPF,1F0,31128449,34,No,,Reviewed,Q00987,No,No,No,No,6,114.85999999999999
1073,O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCCN4CCN(C5=CC=C(NC6=NC=C7C(N(C8=NC(C(C)(O)C)=CC=C8)N(CC=C)C7=O)=N6)C=C5)CC4)=O,Active,Yes,MOLT4; BT549; HCC1806; COV362; Kuramochi; OVCAR8,3.159600000000002,IC50 for AZD1175: 1.52±0.17 nM; IC50 for ZNL-02-096: 3.58±0.36 nM,"Yangwode Jing, Ronen Gabizon",~ 10 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,800 nM,390 nM,aliphatic_CC,15,4,1.52 nM,3.58 nM,AZD1775,O=C1N(CC=C)N(C2=NC(C(C)(O)C)=CC=C2)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=NC=C31,CC,Alkane,2,0,0,799.8929999999999,No,,5V5Y,8X7,31735695,ZNL-02-096,Yes,,Reviewed,P30291,Yes,Yes,No,Yes,"0.25, 0.5, 1, 2, 3, 4, 5, 24, 48",199.92000000000002
1074,O=C(NCCCN1CCN(C2=CC=C(NC3=NC=C4C(N(C5=NC(C(C)(O)C)=CC=C5)N(CC=C)C4=O)=N3)C=C2)CC1)CCOCCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Active,No,MOLT4,2.699100000000005,IC50: 7.28±0.67 nM,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,800 nM,,aliphatic_CC,18,5,1.52 nM,7.28 nM,AZD1775,O=C1N(CC=C)N(C2=NC(C(C)(O)C)=CC=C2)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=NC=C31,CCNC(=O)CCOCCOCC,PEG,13,4,8,959.0779999999995,No,,5V5Y,8X7,31735695,ZNL-02-012,No,,Reviewed,P30291,No,No,No,No,5,247.47999999999996
1075,O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCOCCOCCN4CCN(C5=CC=C(NC6=NC=C7C(N(C8=NC(C(C)(O)C)=CC=C8)N(CC=C)C7=O)=N6)C=C5)CC4)=O,Active,No,MOLT4,2.8193000000000037,IC50: 3.18±0.52 nM,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,800 nM,,aliphatic_CC,18,4,1.52 nM,3.18 nM,AZD1775,O=C1N(CC=C)N(C2=NC(C(C)(O)C)=CC=C2)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=NC=C31,CCOCCOCCOC,PEG,10,3,7,918.0249999999999,No,,5V5Y,8X7,31735695,ZNL-02-047,No,,Reviewed,P30291,No,No,No,No,5,227.61
1076,O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCCCCCN4CCN(C5=CC=C(NC6=NC=C7C(N(C8=NC(C(C)(O)C)=CC=C8)N(CC=C)C7=O)=N6)C=C5)CC4)=O,Active,No,MOLT4,4.329900000000002,IC50: 4.46±0.95 nM,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,800 nM,,aliphatic_CC,15,4,1.52 nM,4.46 nM,AZD1775,O=C1N(CC=C)N(C2=NC(C(C)(O)C)=CC=C2)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=NC=C31,CCCCC,Alkane,5,0,2,841.9739999999998,No,,5V5Y,8X7,31735695,ZNL-02-040,No,,Reviewed,P30291,No,No,No,No,5,199.92000000000002
1077,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCOCCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,Yes,SRD15; Huh7,6.496400000000007,,Yangwode Jing,0.1 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,18,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCOCCn1cc(CCCO)nn1,PEG,23,8,16,1159.2789999999993,No,,1HWK,117,32321253,P22A,Yes,,Reviewed,P04035,Yes,Yes,No,Yes,"4, 5, 16",284.22999999999996
1078,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,6.446600000000005,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,15,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCn1cc(CCCO)nn1,PEG,14,5,7,1027.1199999999997,No,,1HWK,117,32321253,P13A,No,,Reviewed,P04035,No,No,No,No,16,256.53999999999996
1079,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCC4=CN(CCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,6.836700000000007,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,15,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCn1cc(CCCCO)nn1,PEG,15,5,8,1041.1469999999995,No,,1HWK,117,32321253,P14A,No,,Reviewed,P04035,No,No,No,No,16,256.53999999999996
1080,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCCC4=CN(CCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,7.226800000000007,,Yangwode Jing,3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,15,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCn1cc(CCCCCO)nn1,PEG,16,5,9,1055.1739999999995,No,,1HWK,117,32321253,P15A,No,,Reviewed,P04035,No,No,No,No,16,256.53999999999996
1081,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,6.463200000000006,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,16,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCn1cc(CCCO)nn1,PEG,17,6,10,1071.1729999999995,No,,1HWK,117,32321253,P16A,No,,Reviewed,P04035,No,No,No,No,16,265.77
1082,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCC4=CN(CCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,6.853300000000006,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,16,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCn1cc(CCCCO)nn1,PEG,18,6,11,1085.1999999999994,No,,1HWK,117,32321253,P17A,No,,Reviewed,P04035,No,No,No,No,16,265.77
1083,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCCC4=CN(CCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,7.2434000000000065,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,16,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCn1cc(CCCCCO)nn1,PEG,19,6,12,1099.2269999999994,No,,1HWK,117,32321253,P18A,No,,Reviewed,P04035,No,No,No,No,16,265.77
1084,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,6.479800000000007,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,17,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCn1cc(CCCO)nn1,PEG,20,7,13,1115.2259999999994,No,,1HWK,117,32321253,P19A,No,,Reviewed,P04035,No,No,No,No,16,274.99999999999994
1085,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCC4=CN(CCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,6.8699000000000074,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,17,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCn1cc(CCCCO)nn1,PEG,21,7,14,1129.2529999999992,No,,1HWK,117,32321253,P20A,No,,Reviewed,P04035,No,No,No,No,16,274.99999999999994
1086,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCCC4=CN(CCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,7.260000000000007,,Yangwode Jing,1.8 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,17,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCn1cc(CCCCCO)nn1,PEG,22,7,15,1143.2799999999993,No,,1HWK,117,32321253,P21A,No,,Reviewed,P04035,No,No,No,No,16,274.99999999999994
1087,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCC4=CN(CCOCCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,6.886500000000008,,Yangwode Jing,0.4 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,18,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCOCCn1cc(CCCCO)nn1,PEG,24,8,17,1173.3059999999991,No,,1HWK,117,32321253,P23A,No,,Reviewed,P04035,No,No,No,No,16,284.22999999999996
1088,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCCC4=CN(CCOCCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,7.276600000000008,,Yangwode Jing,0.5 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,18,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCOCCn1cc(CCCCCO)nn1,PEG,25,8,18,1187.3329999999994,No,,1HWK,117,32321253,P24A,No,,Reviewed,P04035,No,No,No,No,16,284.22999999999996
1089,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCOCCOCCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,6.513000000000006,,Yangwode Jing,0.2 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,19,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCOCCOCCn1cc(CCCO)nn1,PEG,26,9,19,1203.3319999999992,No,,1HWK,117,32321253,P25A,No,,Reviewed,P04035,No,No,No,No,16,293.4599999999999
1090,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCCC4=CN(CCOCCOCCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,7.293200000000008,,Yangwode Jing,0.6 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,19,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCOCCOCCn1cc(CCCCCO)nn1,PEG,28,9,21,1231.3859999999993,No,,1HWK,117,32321253,P27A,No,,Reviewed,P04035,No,No,No,No,16,293.4599999999999
1091,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCC4=CN(CCCCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,7.947900000000008,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,14,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCCCCCn1cc(CO)nn1,Alkane,14,4,7,1025.1479999999997,No,,1HWK,117,32321253,P13A1,No,,Reviewed,P04035,No,No,No,No,16,247.30999999999997
1092,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,7.990400000000008,,Yangwode Jing,0.4 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,14,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCCCCn1cc(CCCO)nn1,Alkane,15,4,8,1039.1749999999995,No,,1HWK,117,32321253,P14A1,No,,Reviewed,P04035,No,No,No,No,16,247.30999999999997
1093,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,8.380500000000005,,Yangwode Jing,0.2 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,14,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCCCCCn1cc(CCCO)nn1,Alkane,16,4,9,1053.2019999999995,No,,1HWK,117,32321253,P15A1,No,,Reviewed,P04035,No,No,No,No,16,247.30999999999997
1094,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCC4=CN(CCCCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,8.770600000000004,,Yangwode Jing,0.3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,14,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCCCCCn1cc(CCCCO)nn1,Alkane,17,4,10,1067.2289999999994,No,,1HWK,117,32321253,P16A1,No,,Reviewed,P04035,No,No,No,No,16,247.30999999999997
1095,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCCC4=CN(CCCCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,9.160700000000002,,Yangwode Jing,0.4 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,14,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCCCCCn1cc(CCCCCO)nn1,Alkane,18,4,11,1081.2559999999992,No,,1HWK,117,32321253,P17A1,No,,Reviewed,P04035,No,No,No,No,16,247.30999999999997
1096,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCCCC4=CN(CCCCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,9.5508,,Yangwode Jing,0.3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,14,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCCCCCn1cc(CCCCCCO)nn1,Alkane,19,4,12,1095.2829999999992,No,,1HWK,117,32321253,P18A1,No,,Reviewed,P04035,No,No,No,No,16,247.30999999999997
1097,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCCCCC4=CN(CCCCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,9.940900000000001,,Yangwode Jing,0.5 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,14,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCCCCCn1cc(CCCCCCCO)nn1,Alkane,20,4,13,1109.3099999999993,No,,1HWK,117,32321253,P19A1,No,,Reviewed,P04035,No,No,No,No,16,247.30999999999997
1098,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCOCCOCCOCCNC5=CC6=C(C(N(C(CC7)C(NC7=O)=O)C6=O)=O)C=C5)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,6.479800000000007,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,17,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCn1cc(CCCO)nn1,PEG,20,7,13,1115.2259999999994,No,,1HWK,117,32321253,P19AM,No,,Reviewed,P04035,No,No,No,No,16,274.99999999999994
1099,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCC4=CN(CCOCCOCCOCCNC5=CC6=C(C(N(C(CC7)C(NC7=O)=O)C6=O)=O)C=C5)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,6.8699000000000074,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,17,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCn1cc(CCCCO)nn1,PEG,21,7,14,1129.2529999999992,No,,1HWK,117,32321253,P20AM,No,,Reviewed,P04035,No,No,No,No,16,274.99999999999994
1100,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCCC4=CN(CCOCCOCCOCCNC5=CC6=C(C(N(C(CC7)C(NC7=O)=O)C6=O)=O)C=C5)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,7.260000000000008,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,17,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCn1cc(CCCCCO)nn1,PEG,22,7,15,1143.2799999999993,No,,1HWK,117,32321253,P21AM,No,,Reviewed,P04035,No,No,No,No,16,274.99999999999994
1101,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCOCCOCCOCCOCCNC5=CC6=C(C(N(C(CC7)C(NC7=O)=O)C6=O)=O)C=C5)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,6.496400000000007,,Yangwode Jing,0.3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,18,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCOCCn1cc(CCCO)nn1,PEG,23,8,16,1159.2789999999993,No,,1HWK,117,32321253,P22AM,No,,Reviewed,P04035,No,No,No,No,16,284.22999999999996
1102,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCC4=CN(CCOCCOCCOCCOCCNC5=CC6=C(C(N(C(CC7)C(NC7=O)=O)C6=O)=O)C=C5)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,6.886500000000008,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,18,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCOCCn1cc(CCCCO)nn1,PEG,24,8,17,1173.3059999999991,No,,1HWK,117,32321253,P23AM,No,,Reviewed,P04035,No,No,No,No,16,284.22999999999996
1103,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCCCC4=CN(CCOCCOCCOCCOCCNC5=CC6=C(C(N(C(CC7)C(NC7=O)=O)C6=O)=O)C=C5)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,7.276600000000008,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,18,6,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCOCCOCCOCCOCCn1cc(CCCCCO)nn1,PEG,25,8,18,1187.3329999999994,No,,1HWK,117,32321253,P24AM,No,,Reviewed,P04035,No,No,No,No,16,284.22999999999996
1104,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCOCC#CC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,6.746000000000007,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,C#CCOCCn1cc(CCCO)nn1,Other,15,5,7,1008.1169999999997,No,,1HWK,117,32321253,L13A,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1105,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCOCC#CC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,7.136100000000007,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,C#CCOCCCn1cc(CCCO)nn1,Other,16,5,8,1022.1439999999997,No,,1HWK,117,32321253,L14A,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1106,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCCOCC#CC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,7.526200000000008,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,C#CCOCCCCn1cc(CCCO)nn1,Other,17,5,9,1036.1709999999996,No,,1HWK,117,32321253,L15A,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1107,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCCCOCC#CC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,7.9163000000000086,,Yangwode Jing,0.3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,C#CCOCCCCCn1cc(CCCO)nn1,Other,18,5,10,1050.1979999999994,No,,1HWK,117,32321253,L16A,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1108,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCCCCOCC#CC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,8.306400000000007,,Yangwode Jing,0.2 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,C#CCOCCCCCCn1cc(CCCO)nn1,Other,19,5,11,1064.2249999999995,No,,1HWK,117,32321253,L17A,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1109,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCCCCCOCC#CC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,8.696500000000006,,Yangwode Jing,0.7 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,C#CCOCCCCCCCn1cc(CCCO)nn1,Other,20,5,12,1078.2519999999993,No,,1HWK,117,32321253,L18A,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1110,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCOCCCC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,7.327100000000008,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCOCCn1cc(CCCO)nn1,Other,15,5,8,1012.1489999999997,No,,1HWK,117,32321253,L13AR,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1111,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCOCCCC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,7.717200000000009,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCOCCCn1cc(CCCO)nn1,Other,16,5,9,1026.1759999999995,No,,1HWK,117,32321253,L14AR,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1112,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCCOCCCC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Inactive,No,SRD15,8.10730000000001,,Yangwode Jing,> 3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCOCCCCn1cc(CCCO)nn1,Other,17,5,10,1040.2029999999995,No,,1HWK,117,32321253,L15AR,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1113,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCCCOCCCC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,8.497400000000006,,Yangwode Jing,2.3 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCOCCCCCn1cc(CCCO)nn1,Other,18,5,11,1054.2299999999993,No,,1HWK,117,32321253,L16AR,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1114,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCCCCOCCCC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,8.887500000000003,,Yangwode Jing,0.5 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCOCCCCCCn1cc(CCCO)nn1,Other,19,5,12,1068.2569999999994,No,,1HWK,117,32321253,L17AR,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1115,O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC(OCCCC4=CN(CCCCCCCOCCCC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)N=N4)=C3)C(C(NC8=CC=CC=C8)=O)=C1C(C)C,Active,No,SRD15,9.277600000000001,,Yangwode Jing,0.6 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aryl_O,13,5,,,Atorvastatin,O=C(C[C@@H](C[C@@H](CCN1C(C2=CC=C(F)C=C2)=C(C(C(NC3=CC=CC=C3)=O)=C1C(C)C)C4=CC=CC=C4)O)O)O,CCCOCCCCCCCn1cc(CCCO)nn1,Other,20,5,13,1082.2839999999992,No,,1HWK,117,32321253,L18AR,No,,Reviewed,P04035,No,No,No,No,16,227.43999999999997
1116,O=C(NS(=O)(C1=CC=C(N[C@H](CCN2CCN(C(CCCN3N=NC(COCCOCCOC4=CC=CC(C(C5=CSC([C@H]6N(C([C@@H](C7CCCCC7)NC([C@@H](NC)C)=O)=O)CCC6)=N5)=O)=C4)=C3)=O)CC2)CSC8=CC=CC=C8)C(S(=O)(C(F)(F)F)=O)=C1)=O)C9=CC=C(N%10CCN(CC%11=C(C%12=CC=C(Cl)C=C%12)CCC(C)(C)C%11)CC%10)C=C9,Active,No,MyLa1929,12.353299999999988,,Yangwode Jing,,,C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O,Iap,,157 nM,morpholine_to_piperazine,23,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCCn1cc(COCCOCCO)nn1,PEG,19,8,11,1709.5579999999998,No,,6QGH,1XJ,32388279,3a,No,,Reviewed,Q07817,No,No,No,No,72,289.24
1117,O=C(NS(=O)(C1=CC=C(N[C@H](CCN2CCN(C(CCCN3N=NC(COCCOCCOCCOC4=CC=CC(C(C5=CSC([C@H]6N(C([C@@H](C7CCCCC7)NC([C@@H](NC)C)=O)=O)CCC6)=N5)=O)=C4)=C3)=O)CC2)CSC8=CC=CC=C8)C(S(=O)(C(F)(F)F)=O)=C1)=O)C9=CC=C(N%10CCN(CC%11=C(C%12=CC=C(Cl)C=C%12)CCC(C)(C)C%11)CC%10)C=C9,Active,No,MyLa1929,12.369899999999989,,Yangwode Jing,,,C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O,Iap,,147 nM,morpholine_to_piperazine,24,4,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCCn1cc(COCCOCCOCCO)nn1,PEG,22,9,14,1753.6109999999999,No,,4QNQ,1XJ,32388279,3b,No,,Reviewed,Q07817,No,No,No,No,72,298.47
1119,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(COCCOCCOC8=CC=CC(C(C9=CSC([C@H]%10N(CCC%10)C([C@H](NC([C@H](C)NC)=O)C%11CCCCC%11)=O)=N9)=O)=C8)=O)=O,Active,No,MyLa1929,11.78139999999999,,Ronen Gabizon,,,C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O,Iap,,143 nM,morpholine_to_piperazine,20,4,,, ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)COCCOCCO,PEG,11,5,7,1600.4260000000002,,,4QNQ,1XJ,32388279,4a,No,,Reviewed,Q07817,No,No,No,No,72,258.53
1120,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(COCCOCCOCCOCCOC8=CC=CC(C(C9=CSC([C@H]%10N(CCC%10)C([C@H](NC([C@H](C)NC)=O)C%11CCCCC%11)=O)=N9)=O)=C8)=O)=O,Active,No,MyLa1929,11.81459999999999,,Ronen Gabizon,,,C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O,Iap,,75 nM,morpholine_to_piperazine,22,4,,, ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)COCCOCCOCCOCCO,PEG,17,7,13,1688.5320000000004,,,4QNQ,1XJ,32388279,4b,No,,Reviewed,Q07817,No,No,No,No,72,276.98999999999995
1121,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCOC8=CC=CC(C(C9=CSC([C@H]%10N(CCC%10)C([C@H](NC([C@H](C)NC)=O)C%11CCCCC%11)=O)=N9)=O)=C8)=O)=O,Active,No,MyLa1929,12.528399999999987,,Ronen Gabizon,,,C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O,Iap,,997 nM,morpholine_to_piperazine,18,4,,, ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCCO,Alkane,7,3,3,1540.3739999999998,,,4QNQ,1XJ,32388279,5a,No,,Reviewed,Q07817,No,No,No,No,72,240.06999999999994
1122,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCCOC8=CC=CC(C(C9=CSC([C@H]%10N(CCC%10)C([C@H](NC([C@H](C)NC)=O)C%11CCCCC%11)=O)=N9)=O)=C8)=O)=O,Active,No,MyLa1929,12.918499999999986,,Ronen Gabizon,,,C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O,Iap,,1959 nM,morpholine_to_piperazine,18,4,,, ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCCCO,Alkane,8,3,4,1554.4009999999998,,,4QNQ,1XJ,32388279,5b,No,,Reviewed,Q07817,No,No,No,No,72,240.06999999999994
1123,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCCCOC8=CC=CC(C(C9=CSC([C@H]%10N(CCC%10)C([C@H](NC([C@H](C)NC)=O)C%11CCCCC%11)=O)=N9)=O)=C8)=O)=O,Inactive,No,MyLa1929,13.308599999999982,,Ronen Gabizon,,,C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O,Iap,,,morpholine_to_piperazine,18,4,,, ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCCCCO,Alkane,9,3,5,1568.4279999999999,,,4QNQ,1XJ,32388279,5c,No,,Reviewed,Q07817,No,No,No,No,72,240.06999999999994
1124,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCCCCOC8=CC=CC(C(C9=CSC([C@H]%10N(CCC%10)C([C@H](NC([C@H](C)NC)=O)C%11CCCCC%11)=O)=N9)=O)=C8)=O)=O,Inactive,No,MyLa1929,13.698699999999981,,Ronen Gabizon,,,C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O,Iap,,,morpholine_to_piperazine,18,4,,, ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,NC(=O)CCCCCCO,Alkane,10,3,6,1582.455,,,4QNQ,1XJ,32388279,5d,No,,Reviewed,Q07817,No,No,No,No,72,240.06999999999994
1125,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCN8N=NC(COCCOCCOC9=CC=C%10C(CCC[C@H]%10NC([C@H]%11C(C)(C)C[C@@]([H])(OCC[C@H]%12NC([C@@H](C)NC)=O)N%11C%12=O)=O)=C9)=C8)=O)=O,Active,No,MyLa1929,10.289100000000001,,Ronen Gabizon,,,O=C([C@H]1C(C)(C)C[C@@]([H])(OCC[C@H]2NC([C@@H](C)NC)=O)N1C2=O)N[C@@H]3CCCC4=CC(O)=CC=C43,Iap,,153 nM,morpholine_to_piperazine,22,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCc1cn(CCCC(N)=O)nn1,non-PEG polyether,18,7,10,1683.495,,,4QNQ,1XJ,32388279,6a,No,,Reviewed,Q07817,No,No,No,No,72,297.60999999999996
1126,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCN8N=NC(COCCOCCOCCOC9=CC=C%10C(CCC[C@H]%10NC([C@H]%11C(C)(C)C[C@@]([H])(OCC[C@H]%12NC([C@@H](C)NC)=O)N%11C%12=O)=O)=C9)=C8)=O)=O,Active,No,MyLa1929,10.305700000000002,,Ronen Gabizon,,,O=C([C@H]1C(C)(C)C[C@@]([H])(OCC[C@H]2NC([C@@H](C)NC)=O)N1C2=O)N[C@@H]3CCCC4=CC(O)=CC=C43,Iap,,119 nM,morpholine_to_piperazine,23,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCCOCc1cn(CCCC(N)=O)nn1,non-PEG polyether,21,8,13,1727.548,,,4QNQ,1XJ,32388279,6b,No,,Reviewed,Q07817,No,No,No,No,72,306.8399999999999
1127,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(COCCOCCOC8=CC=C9C(CCC[C@H]9NC([C@H]%10C(C)(C)C[C@@]([H])(OCC[C@H]%11NC([C@@H](C)NC)=O)N%10C%11=O)=O)=C8)=O)=O,Active,No,MyLa1929,9.717200000000004,,Ronen Gabizon,,,O=C([C@H]1C(C)(C)C[C@@]([H])(OCC[C@H]2NC([C@@H](C)NC)=O)N1C2=O)N[C@@H]3CCCC4=CC(O)=CC=C43,Iap,,100 nM,morpholine_to_piperazine,19,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCOCCOCC(N)=O,PEG,10,4,6,1574.3629999999998,,,4QNQ,1XJ,32388279,7a,No,,Reviewed,Q07817,No,No,No,No,72,266.9
1128,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(COCCOCCOCCOCCCOC8=CC=C9C(CCC[C@H]9NC([C@H]%10C(C)(C)C[C@@]([H])(OCC[C@H]%11NC([C@@H](C)NC)=O)N%10C%11=O)=O)=C8)=O)=O,Active,No,MyLa1929,10.140500000000005,,Ronen Gabizon,,,O=C([C@H]1C(C)(C)C[C@@]([H])(OCC[C@H]2NC([C@@H](C)NC)=O)N1C2=O)N[C@@H]3CCCC4=CC(O)=CC=C43,Iap,,70 nM,morpholine_to_piperazine,21,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCOCCOCCOCCOCC(N)=O,PEG,17,6,13,1676.496,,,4QNQ,1XJ,32388279,7b,No,,Reviewed,Q07817,No,No,No,No,72,285.35999999999996
1129,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCOC8=CC=C9C(CCC[C@H]9NC([C@H]%10C(C)(C)C[C@@]([H])(OCC[C@H]%11NC([C@@H](C)NC)=O)N%10C%11=O)=O)=C8)=O)=O,Active,No,MyLa1929,10.464199999999998,,Ronen Gabizon,,,O=C([C@H]1C(C)(C)C[C@@]([H])(OCC[C@H]2NC([C@@H](C)NC)=O)N1C2=O)N[C@@H]3CCCC4=CC(O)=CC=C43,Iap,,62 nM,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCC(N)=O,Alkane,6,2,2,1514.3109999999995,,,4QNQ,1XJ,32388279,8a,No,,Reviewed,Q07817,No,No,No,No,72,248.43999999999997
1130,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCCOC8=CC=C9C(CCC[C@H]9NC([C@H]%10C(C)(C)C[C@@]([H])(OCC[C@H]%11NC([C@@H](C)NC)=O)N%10C%11=O)=O)=C8)=O)=O,Active,No,MyLa1929,10.854299999999995,,Ronen Gabizon,,,O=C([C@H]1C(C)(C)C[C@@]([H])(OCC[C@H]2NC([C@@H](C)NC)=O)N1C2=O)N[C@@H]3CCCC4=CC(O)=CC=C43,Iap,,76 nM,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCC(N)=O,Alkane,7,2,3,1528.3379999999995,,,4QNQ,1XJ,32388279,8b,No,,Reviewed,Q07817,No,No,No,No,72,248.43999999999997
1131,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCCCOC8=CC=C9C(CCC[C@H]9NC([C@H]%10C(C)(C)C[C@@]([H])(OCC[C@H]%11NC([C@@H](C)NC)=O)N%10C%11=O)=O)=C8)=O)=O,Active,No,MyLa1929,11.244399999999994,,Ronen Gabizon,,,O=C([C@H]1C(C)(C)C[C@@]([H])(OCC[C@H]2NC([C@@H](C)NC)=O)N1C2=O)N[C@@H]3CCCC4=CC(O)=CC=C43,Iap,,127 nM,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCC(N)=O,Alkane,8,2,4,1542.3649999999996,,,4QNQ,1XJ,32388279,8c,No,,Reviewed,Q07817,No,No,No,No,72,248.43999999999997
1132,O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3=C(CCC(C)(C3)C)C4=CC=C(C=C4)Cl)NS(=O)(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCCCCOC8=CC=C9C(CCC[C@H]9NC([C@H]%10C(C)(C)C[C@@]([H])(OCC[C@H]%11NC([C@@H](C)NC)=O)N%10C%11=O)=O)=C8)=O)=O,Active,No,MyLa1929,11.634499999999992,,Ronen Gabizon,,,O=C([C@H]1C(C)(C)C[C@@]([H])(OCC[C@H]2NC([C@@H](C)NC)=O)N1C2=O)N[C@@H]3CCCC4=CC(O)=CC=C43,Iap,,274 nM,morpholine_to_piperazine,17,5,,,ABT-263,CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCN(c3ccc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)cc3)CC2)C1,CCCCCCC(N)=O,Alkane,9,2,5,1556.3919999999996,,,4QNQ,1XJ,32388279,8d,No,,Reviewed,Q07817,No,No,No,No,72,248.43999999999997
1133,O=C(NCCCCCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCN4N=C(C)C5=C(C)N(C6=CC=C(C)C=C6)N=C5C4=O,Active,Yes,"SW480, HCT116",4.257760000000003,,Yangwode Jing,3.6 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,56 uM,8 uM,other,11,3,,,PDEδ inhibitor 2,O=C(N)CCCN1N=C(C)C2=C(C)N(C3=CC=C(C)C=C3)N=C2C1=O,CCCCCCCC,Alkane,8,0,5,722.8470000000001,No,,5E80,5KP,32603594,17f,No,,Reviewed,O43924,No,Yes,No,Yes,"1, 2, 4, 8, 24",177.39
1134,O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C4=CC=C(CN5CCN(C(CCCC6=CN(CCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O)N=N6)=O)CC5)C=C4,Inactive,No,K562,4.614820000000002,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,4,,,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCc1cn(CC)nn1,Other,10,3,3,916.0159999999997,No,,2HYY,STI,32657579,P10Im,No,,Reviewed,P00519,No,No,No,No,32,229.63999999999993
1135,O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C4=CC=C(CN5CCN(C(CCCC6=CN(CCOCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O)N=N6)=O)CC5)C=C4,Inactive,No,K562,4.631420000000002,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,16,4,,,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCc1cn(CCOCC)nn1,Other,13,4,6,960.0689999999996,No,,2HYY,STI,32657579,P13Im,No,,Reviewed,P00519,No,No,No,No,32,238.86999999999995
1136,O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C4=CC=C(CN5CCN(C(CCCC6=CN(CCOCCOCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O)N=N6)=O)CC5)C=C4,Inactive,No,K562,4.648020000000003,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,17,4,,,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCc1cn(CCOCCOCC)nn1,PEG,16,5,9,1004.1219999999995,No,,2HYY,STI,32657579,P16Im,No,,Reviewed,P00519,No,No,No,No,32,248.0999999999999
1137,O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C4=CC=C(CN5CCN(C(CCCC6=CN(CCOCCOCCOCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O)N=N6)=O)CC5)C=C4,Inactive,No,K562,4.664620000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,18,4,,,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCc1cn(CCOCCOCCOCC)nn1,PEG,19,6,12,1048.1749999999995,No,,2HYY,STI,32657579,P19Im,No,,Reviewed,P00519,No,No,No,No,32,257.3299999999999
1138,O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C4=CC=C(CN5CCN(C(CCCC6=CN(CCOCCOCCOCCOCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O)N=N6)=O)CC5)C=C4,Inactive,No,K562,4.681220000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,19,4,,,imatinib,Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1,CCCc1cn(CCOCCOCCOCCOCC)nn1,PEG,22,7,15,1092.2279999999994,No,,2HYY,STI,32657579,P20Im,No,,Reviewed,P00519,No,No,No,No,32,266.55999999999995
1139,O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(C(CCCC4=CN(CCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=O)CC3)=C2)S1)NC8=C(C)C=CC=C8Cl,Active,No,K562,3.9755400000000023,,Yangwode Jing,~ 56 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,hydroxyl_to_carbon,16,4,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCc1cn(CC)nn1,Other,9,3,2,880.392,No,,2GQG,1N1,32657579,P10D,No,,Reviewed,P00519,No,No,No,No,32,229.63999999999996
1140,O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(C(CCCC4=CN(CCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=O)CC3)=C2)S1)NC8=C(C)C=CC=C8Cl,Active,No,K562,3.992140000000002,,Yangwode Jing,~ 56 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,hydroxyl_to_carbon,17,4,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCOCCn1cc(CC)nn1,Other,12,4,5,924.4449999999998,No,,2GQG,1N1,32657579,P13D,No,,Reviewed,P00519,No,No,No,No,32,238.86999999999998
1141,O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(C(CCCC4=CN(CCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=O)CC3)=C2)S1)NC8=C(C)C=CC=C8Cl,Active,No,K562,4.008740000000004,,Yangwode Jing,~ 20 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,hydroxyl_to_carbon,18,4,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCOCCOCCn1cc(CC)nn1,PEG,15,5,8,968.4979999999998,No,,2GQG,1N1,32657579,P16D,No,,Reviewed,P00519,No,No,No,No,32,248.1
1142,O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(C(CCCC4=CN(CCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=O)CC3)=C2)S1)NC8=C(C)C=CC=C8Cl,Active,No,K562,4.025340000000007,,Yangwode Jing,~ 56 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,hydroxyl_to_carbon,19,4,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCOCCOCCOCCn1cc(CC)nn1,PEG,18,6,11,1012.5509999999999,No,,2GQG,1N1,32657579,P19D,No,,Reviewed,P00519,No,No,No,No,32,257.3299999999999
1143,O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(C(CCCC4=CN(CCOCCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=O)CC3)=C2)S1)NC8=C(C)C=CC=C8Cl,Active,No,K562,4.041940000000007,,Yangwode Jing,~ 10 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,9.2 nM,hydroxyl_to_carbon,20,4,,,Dasatinib,Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1,CCOCCOCCOCCOCCn1cc(CC)nn1,PEG,21,7,14,1056.6039999999998,No,,2GQG,1N1,32657579,P22D,No,,Reviewed,P00519,No,No,No,No,32,266.55999999999995
1144,O=C(NC1=CC=C(OC(F)(Cl)F)C=C1)C2=CN=C(N3C[C@H](NC(CCCC4=CN(CCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=O)CC3)C(C8=NNC=C8)=C2,Active,No,K562,3.714500000000001,,Yangwode Jing,> 625 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,14,5,,,Asciminib,O=C(C1=CC(C2=NNC=C2)=C(N3C[C@H](O)CC3)N=C1)NC4=CC=C(OC(F)(Cl)F)C=C4,CCn1cc(CCCC(N)=O)nn1,Other,13,5,5,885.2889999999998,No,,5MO4,AY7,32657579,P10As,No,,Reviewed,P00519,No,No,No,No,32,238.52999999999994
1145,O=C(NC1=CC=C(OC(F)(Cl)F)C=C1)C2=CN=C(N3C[C@H](NC(CCCC4=CN(CCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=O)CC3)C(C8=NNC=C8)=C2,Active,No,K562,3.7311000000000014,,Yangwode Jing,~ 400 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,15,5,,,Asciminib,O=C(C1=CC(C2=NNC=C2)=C(N3C[C@H](O)CC3)N=C1)NC4=CC=C(OC(F)(Cl)F)C=C4,CCOCCn1cc(CCCC(N)=O)nn1,Other,16,6,8,929.3419999999998,No,,5MO4,AY7,32657579,P13As,No,,Reviewed,P00519,No,No,No,No,32,247.7599999999999
1146,O=C(NC1=CC=C(OC(F)(Cl)F)C=C1)C2=CN=C(N3C[C@H](NC(CCCC4=CN(CCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=O)CC3)C(C8=NNC=C8)=C2,Active,No,K562,3.747700000000002,,Yangwode Jing,~ 300 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,16,5,,,Asciminib,O=C(C1=CC(C2=NNC=C2)=C(N3C[C@H](O)CC3)N=C1)NC4=CC=C(OC(F)(Cl)F)C=C4,CCOCCOCCn1cc(CCCC(N)=O)nn1,PEG,19,7,11,973.3949999999996,No,,5MO4,AY7,32657579,P16As,No,,Reviewed,P00519,No,No,No,No,32,256.98999999999995
1147,O=C(NC1=CC=C(OC(F)(Cl)F)C=C1)C2=CN=C(N3C[C@H](NC(CCCC4=CN(CCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=O)CC3)C(C8=NNC=C8)=C2,Active,No,K562,3.764300000000002,,Yangwode Jing,~ 200 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,121 nM,other,17,5,,,Asciminib,O=C(C1=CC(C2=NNC=C2)=C(N3C[C@H](O)CC3)N=C1)NC4=CC=C(OC(F)(Cl)F)C=C4,CCOCCOCCOCCn1cc(CCCC(N)=O)nn1,PEG,22,8,14,1017.4479999999995,No,,5MO4,AY7,32657579,P19As,No,,Reviewed,P00519,No,No,No,No,32,266.21999999999997
1148,O=C(NC1=CC=C(OC(F)(Cl)F)C=C1)C2=CN=C(N3C[C@H](NC(CCCC4=CN(CCOCCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)=O)CC3)C(C8=NNC=C8)=C2,Active,No,K562,3.7809000000000026,,Yangwode Jing,~ 500 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,18,5,,,Asciminib,O=C(C1=CC(C2=NNC=C2)=C(N3C[C@H](O)CC3)N=C1)NC4=CC=C(OC(F)(Cl)F)C=C4,CCOCCOCCOCCOCCn1cc(CCCC(N)=O)nn1,PEG,25,9,17,1061.5009999999995,No,,5MO4,AY7,32657579,P22As,No,,Reviewed,P00519,No,No,No,No,32,275.44999999999993
1149,O=C(NC1=CC=C(CN2CCN(C(CCCC3=CN(CCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)N=N3)=O)CC2)C(C(F)(F)F)=C1)C7=CC=C(C)C(C#CC8=CN=C9C=CC=NN98)=C7,Active,No,K562,4.480520000000004,,Yangwode Jing,~ 625 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,14,3,,,Ponatinib,CN1CCN(CC1)CC2=CC=C(C=C2C(F)(F)F)NC(C3=CC(C#CC4=CN=C5C=CC=NN45)=C(C=C3)C)=O,CCCc1cn(CC)nn1,Other,10,3,3,954.9709999999997,No,,3IK3,0LI,32657579,P10P,No,,Reviewed,P00519,No,No,No,No,32,209.1299999999999
1150,O=C(NC1=CC=C(CN2CCN(C(CCCC3=CN(CCOCCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)N=N3)=O)CC2)C(C(F)(F)F)=C1)C7=CC=C(C)C(C#CC8=CN=C9C=CC=NN98)=C7,Active,No,K562,4.497120000000003,,Yangwode Jing,~ 70 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,3,,,Ponatinib,CN1CCN(CC1)CC2=CC=C(C=C2C(F)(F)F)NC(C3=CC(C#CC4=CN=C5C=CC=NN45)=C(C=C3)C)=O,CCCc1cn(CCOCC)nn1,Other,13,4,6,999.0239999999998,No,,3IK3,0LI,32657579,P13P,No,,Reviewed,P00519,No,No,No,No,32,218.35999999999993
1151,O=C(NC1=CC=C(CN2CCN(C(CCCC3=CN(CCOCCOCCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)N=N3)=O)CC2)C(C(F)(F)F)=C1)C7=CC=C(C)C(C#CC8=CN=C9C=CC=NN98)=C7,Active,No,K562,4.513720000000005,,Yangwode Jing,~ 70 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,16,3,,,Ponatinib,CN1CCN(CC1)CC2=CC=C(C=C2C(F)(F)F)NC(C3=CC(C#CC4=CN=C5C=CC=NN45)=C(C=C3)C)=O,CCCc1cn(CCOCCOCC)nn1,PEG,16,5,9,1043.0769999999998,No,,3IK3,0LI,32657579,P16P,No,,Reviewed,P00519,No,No,No,No,32,227.58999999999995
1152,O=C(NC1=CC=C(CN2CCN(C(CCCC3=CN(CCOCCOCCOCCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)N=N3)=O)CC2)C(C(F)(F)F)=C1)C7=CC=C(C)C(C#CC8=CN=C9C=CC=NN98)=C7,Active,No,K562,4.530320000000007,,Yangwode Jing,~ 20 nM,50 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,7.5 nM,aliphatic_CC,17,3,,,Ponatinib,CN1CCN(CC1)CC2=CC=C(C=C2C(F)(F)F)NC(C3=CC(C#CC4=CN=C5C=CC=NN45)=C(C=C3)C)=O,CCCc1cn(CCOCCOCCOCC)nn1,PEG,19,6,12,1087.1299999999999,No,,3IK3,0LI,32657579,P19P,No,,Reviewed,P00519,No,No,No,No,32,236.81999999999996
1153,O=C(NC1=CC=C(CN2CCN(C(CCCC3=CN(CCOCCOCCOCCOCCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)N=N3)=O)CC2)C(C(F)(F)F)=C1)C7=CC=C(C)C(C#CC8=CN=C9C=CC=NN98)=C7,Active,No,K562,4.54692000000001,,Yangwode Jing,~ 70 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,18,3,,,Ponatinib,CN1CCN(CC1)CC2=CC=C(C=C2C(F)(F)F)NC(C3=CC(C#CC4=CN=C5C=CC=NN45)=C(C=C3)C)=O,CCCc1cn(CCOCCOCCOCCOCC)nn1,PEG,22,7,15,1131.183,No,,3IK3,0LI,32657579,P22P,No,,Reviewed,P00519,No,No,No,No,32,246.04999999999993
1154,O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCOCCOCCOCCN4N=NC(CCCC(N5CCN(C6=NC(C)=NC(NC7=NC=C(/C=C/C8=CC=CC(C)=C8)S7)=C6)CC5)=O)=C4)=O,Active,Yes,"K562, BaF3",4.306640000000008,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,0.45 uM,6.1 uM,other,19,3,,,Dasatinib analogue,O=C(N1CCN(C2=NC(C)=NC(NC3=NC=C(/C=C/C4=CC=CC(C)=C4)S3)=C2)CC1)CCCC#C,cn(CCOCCOCCOCCOCC)nn,PEG,18,7,13,1005.1719999999996,No,,2GQG,1N1,32657579,P22D1,No,,Reviewed,P00519,No,No,No,No,48,237.45999999999998
1155,O=C(NCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)C4=CC=C(C)C(N5C(C)=CC(OCC6=CC=C(F)C=C6F)=C(Br)C5=O)=C4,Inactive,No,"BBL358, T47D",5.097340000000005,"Dmax in BBL358/T47D: 8% and 0, respectively.",Yangwode Jing,,8 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,9,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCC,Alkane,3,0,0,790.6180000000003,No,,3HLL,I45,32634680,NR-1a,No,,Reviewed,Q16539,No,No,No,No,24,155.90999999999997
1156,O=C(C1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1)NCCCCNC(C4=CC=C(C)C(N5C(C)=CC(OCC6=CC=C(F)C=C6F)=C(Br)C5=O)=C4)=O,Active,No,"BBL358, T47D",4.415240000000003,"Dmax in BBL358/T47D: 40%±27% and 0, respectively.",Yangwode Jing,,40 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,9,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCC,Alkane,3,0,0,818.6280000000003,No,,3HLL,I45,32634680,NR-2a,No,,Reviewed,Q16539,No,No,No,No,24,172.98
1157,O=C(NCCOCCOCCOCCOCCOCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)C4=CC=C(C)C(N5C(C)=CC(OCC6=CC=C(F)C=C6F)=C(Br)C5=O)=C4,Active,No,"BBL358, T47D",4.416740000000008,,Yangwode Jing,,60 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCOCCOCCOCCOCCOCCOC,PEG,19,6,16,1026.882,No,,3HLL,I45,32634680,NR-1c,No,,Reviewed,Q16539,No,No,No,No,24,211.29
1158,O=C(NCCOCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)C4=CC=C(C)C(N5C(C)=CC(OCC6=CC=C(F)C=C6F)=C(Br)C5=O)=C4,Active,No,"BBL358, T47D",4.350340000000004,,Yangwode Jing,,60 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,11,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCOCCOC,PEG,7,2,4,850.6700000000002,No,,3HLL,I45,32634680,NR-1b,No,,Reviewed,Q16539,No,No,No,No,24,174.36999999999998
1159,O=C(C1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1)NCCOCCOCCNC(C4=CC=C(C)C(N5C(C)=CC(OCC6=CC=C(F)C=C6F)=C(Br)C5=O)=C4)=O,Active,No,"BBL358, T47D",3.6682400000000035,,Yangwode Jing,,55 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,11,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCOCCOC,PEG,7,2,4,878.6800000000002,No,,3HLL,I45,32634680,NR-2b,No,,Reviewed,Q16539,No,No,No,No,24,191.44
1160,O=C(NCCCCC1=CN(CCOCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",4.981340000000006,,Yangwode Jing,,78 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCc1cn(CCOCCOCCOCC)nn1,PEG,19,6,12,1017.8819999999997,No,,3HLL,I45,32634680,NR-3a,No,,Reviewed,Q16539,No,No,No,No,24,214.30999999999997
1161,O=C(NCCCCC1=CN(CCOCCOCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",4.997940000000009,,Yangwode Jing,,92 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,16,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCc1cn(CCOCCOCCOCCOCC)nn1,PEG,22,7,15,1061.935,No,,3HLL,I45,32634680,NR-3b,No,,Reviewed,Q16539,No,No,No,No,24,223.54
1162,O=C(NCCCCC1=CN(CCCC(NCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",4.861140000000009,,Yangwode Jing,,79 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,4,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCc1cn(CCCC(=O)NCCOCCOCC)nn1,PEG,22,7,13,1058.935,No,,3HLL,I45,32634680,NR-3c,No,,Reviewed,Q16539,No,No,No,No,24,234.17999999999998
1163,O=C(NCCCCC1=CN(CCCC(NCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(N(CC5=CC=CC=C5[N+]([O-])=O)C4=O)=O)=O)=C2C3=O)=O)N=N1)C6=CC=C(C)C(N7C(C)=CC(OCC8=CC=C(F)C=C8F)=C(Br)C7=O)=C6,Inactive,No,"BBL358, T47D",6.68194000000001,"Dmax in BBL358/T47D: 3%±3% and 20%±20%, respectively.",Yangwode Jing,,3 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,17,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCc1cn(CCCC(=O)NCCOCCOCC)nn1,PEG,22,7,13,1194.057,No,,3HLL,I45,32634680,NR-3d,No,,Reviewed,Q16539,No,No,No,No,24,268.53
1164,O=C(C1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1)NCCOCCOCCNC(CCCN4N=NC(CCCCNC(C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5)=O)=C4)=O,Active,No,"BBL358, T47D",4.179040000000007,"Dmax in BBL358/T47D: 0.5% and 76%, respectively.",Yangwode Jing,,76 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,4,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCc1cn(CCCC(=O)NCCOCCOCC)nn1,PEG,22,7,13,1086.9449999999997,No,,3HLL,I45,32634680,NR-4,No,,Reviewed,Q16539,No,No,No,No,24,251.25
1165,O=C(NCCCCC1=CN(CCCC(NCCCCCCC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",6.518940000000007,"Dmax in BBL358/T47D: 67%±17% and 47%±32%, respectively.",Yangwode Jing,,67 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,12,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCCCCNC(=O)CCCn1cc(CCC)nn1,Alkane,20,5,11,1011.9219999999999,No,,3HLL,I45,32634680,NR-5a,No,,Reviewed,Q16539,No,No,No,No,24,203.68999999999997
1166,O=C(NCCCCC1=CN(CCCC(NCCCCCC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",6.128840000000007,"Dmax in BBL358/T47D: 77%±3% and 82%±10%, respectively.",Yangwode Jing,,77 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,12,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCCCNC(=O)CCCn1cc(CCC)nn1,Alkane,19,5,10,997.8949999999999,No,,3HLL,I45,32634680,NR-5b,No,,Reviewed,Q16539,No,No,No,No,24,203.68999999999997
1167,O=C(NCCCCC1=CN(CCCC(NCCCCCCC2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,Yes,"BBL358, T47D",6.878740000000008,"Dmax in BBL358/T47D: 93%±5% and 87%±3%, respectively.",Yangwode Jing,,93 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,11,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCCCCNC(=O)CCCn1cc(CCC)nn1,Alkane,20,5,11,997.939,No,,3HLL,I45,32634680,NR-6a,No,,Reviewed,Q16539,No,No,No,No,24,186.61999999999998
1168,O=C(NCCCCC1=CN(CCCC(NCCCCCC2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",6.488640000000007,"Dmax in BBL358/T47D: 74%±3% and 16%±13%, respectively.",Yangwode Jing,,74 %,Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,11,3,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCCCNC(=O)CCCn1cc(CCC)nn1,Alkane,19,5,10,983.9119999999999,No,,3HLL,I45,32634680,NR-6b,No,,Reviewed,Q16539,No,No,No,No,24,186.61999999999998
1169,O=C(NCCC1=CN(CCCC(NCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Inactive,No,"BBL358, T47D",4.047740000000005,,Yangwode Jing,,0,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,4,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCNC(=O)CCCn1cc(C)nn1,Alkane,14,5,5,942.775,No,,3HLL,I45,32634680,NR-7a,No,,Reviewed,Q16539,No,No,No,No,24,215.71999999999994
1170,O=C(NCCC1=CN(CCCC(NCCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",4.437840000000004,,Yangwode Jing,,36 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,4,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCNC(=O)CCCn1cc(C)nn1,Alkane,15,5,6,956.8019999999999,No,,3HLL,I45,32634680,NR-7b,No,,Reviewed,Q16539,No,No,No,No,24,215.71999999999994
1171,O=C(NCCCC1=CN(CCCC(NCCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",4.827940000000005,,Yangwode Jing,,60 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,4,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCNC(=O)CCCn1cc(CC)nn1,Alkane,16,5,7,970.8289999999998,No,,3HLL,I45,32634680,NR-7c,No,,Reviewed,Q16539,No,No,No,No,24,215.71999999999994
1172,O=C(NCCC1=CN(CCCC(NCCCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",4.827940000000005,,Yangwode Jing,,40 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,4,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCCNC(=O)CCCn1cc(C)nn1,Alkane,16,5,7,970.8289999999998,No,,3HLL,I45,32634680,NR-7d,No,,Reviewed,Q16539,No,No,No,No,24,215.71999999999994
1173,O=C(NCCCCC1=CN(CCCC(NCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",4.827940000000005,,Yangwode Jing,,40 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,4,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCc1cn(CCCC(=O)NCC)nn1,Alkane,16,5,7,970.8289999999998,No,,3HLL,I45,32634680,NR-7e,No,,Reviewed,Q16539,No,No,No,No,24,215.71999999999994
1174,O=C(NCCCC1=CN(CCCC(NCCCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",5.218040000000006,,Yangwode Jing,,84 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,4,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCCNC(=O)CCCn1cc(CC)nn1,Alkane,17,5,8,984.8559999999998,No,,3HLL,I45,32634680,NR-7f,No,,Reviewed,Q16539,No,No,No,No,24,215.71999999999994
1175,O=C(NCCCCC1=CN(CCCC(NCCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,No,"BBL358, T47D",5.218040000000006,,Yangwode Jing,,74 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,4,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCNC(=O)CCCn1cc(CCC)nn1,Alkane,17,5,8,984.8559999999998,No,,3HLL,I45,32634680,NR-7g,No,,Reviewed,Q16539,No,No,No,No,24,215.71999999999994
1176,O=C(NCCCCC1=CN(CCCC(NCCCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)N=N1)C5=CC=C(C)C(N6C(C)=CC(OCC7=CC=C(F)C=C7F)=C(Br)C6=O)=C5,Active,Yes,"BBL358, T47D",5.608140000000005,"Dmax in BBL358/T47D: 84%±2% and 89%±2%, respectively.",Yangwode Jing,24 nM,84 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,4,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCCNC(=O)CCCn1cc(CCC)nn1,Alkane,18,5,9,998.8829999999998,No,,3HLL,I45,32634680,NR-7h,Yes,,Reviewed,Q16539,Yes,No,No,No,24,215.71999999999994
1177,O=C([O-])N(C(C)(C)C)C(CCN1N=NC(CCCCNC(C2=CC=C(C)C(N3C(C)=CC(OCC4=CC=C(F)C=C4F)=C(Br)C3=O)=C2)=O)=C1)C(NCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O,Active,No,"BBL358, T47D",5.030440000000004,,Yangwode Jing,,81 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,15,4,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCCNC(=O)C(CCn1cc(CCC)nn1)N(C(=O)[O-])C(C)(C)C,Other,26,8,10,1113.0069999999996,No,,3HLL,I45,32634680,NR-7i,No,,Reviewed,Q16539,No,No,No,No,24,259.09
1178,[NH3+]C(CCN1N=NC(CCCCNC(C2=CC=C(C)C(N3C(C)=CC(OCC4=CC=C(F)C=C4F)=C(Br)C3=O)=C2)=O)=C1)C(NCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O.[Cl-],Inactive,No,"BBL358, T47D",0.8325400000000056,,Yangwode Jing,,0,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,aliphatic_CC,13,5,,,PH-797804,O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1,CCCCNC(=O)C([NH3+])CCn1cc(CCC)nn1,Other,19,6,9,1050.3589999999997,No,,3HLL,I45,32634680,NR-7j,No,,Reviewed,Q16539,No,No,No,No,24,243.35999999999999
1179,O=C(NCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCN4N=C(C)C5=C(C)N(C6=CC=C(C)C=C6)N=C5C4=O,Inactive,No,"SW480, HCT116",2.3072599999999985,,Yangwode Jing,30 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,56 uM,81 uM,other,11,3,,,PDEδ inhibitor 2,O=C(N)CCCN1N=C(C)C2=C(C)N(C3=CC=C(C)C=C3)N=C2C1=O,CCC,Alkane,3,0,0,652.7120000000002,No,,5E80,5KP,32603594,17a,No,,Reviewed,O43924,No,No,No,No,24,177.39
1180,O=C(NCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCN4N=C(C)C5=C(C)N(C6=CC=C(C)C=C6)N=C5C4=O,Inactive,No,"SW480, HCT116",2.6973599999999998,,Yangwode Jing,25 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,56 uM,76 uM,other,11,3,,,PDEδ inhibitor 2,O=C(N)CCCN1N=C(C)C2=C(C)N(C3=CC=C(C)C=C3)N=C2C1=O,CCCC,Alkane,4,0,1,666.7390000000003,No,,5E80,5KP,32603594,17b,No,,Reviewed,O43924,No,No,No,No,24,177.39
1181,O=C(NCCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCN4N=C(C)C5=C(C)N(C6=CC=C(C)C=C6)N=C5C4=O,Inactive,No,"SW480, HCT116",3.087460000000001,,Yangwode Jing,22 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,56 uM,17 uM,other,11,3,,,PDEδ inhibitor 2,O=C(N)CCCN1N=C(C)C2=C(C)N(C3=CC=C(C)C=C3)N=C2C1=O,CCCCC,Alkane,5,0,2,680.7660000000002,No,,5E80,5KP,32603594,17c,No,,Reviewed,O43924,No,No,No,No,24,177.39
1182,O=C(NCCCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCN4N=C(C)C5=C(C)N(C6=CC=C(C)C=C6)N=C5C4=O,Active,No,"SW480, HCT116",3.4775600000000013,,Yangwode Jing,15 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,56 uM,15 uM,other,11,3,,,PDEδ inhibitor 2,O=C(N)CCCN1N=C(C)C2=C(C)N(C3=CC=C(C)C=C3)N=C2C1=O,CCCCCC,Alkane,6,0,3,694.7930000000002,No,,5E80,5KP,32603594,17d,No,,Reviewed,O43924,No,No,No,No,24,177.39
1183,O=C(NCCCCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCN4N=C(C)C5=C(C)N(C6=CC=C(C)C=C6)N=C5C4=O,Active,No,"SW480, HCT116",3.8676600000000025,,Yangwode Jing,14 nM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,56 uM,12 nM,other,11,3,,,PDEδ inhibitor 2,O=C(N)CCCN1N=C(C)C2=C(C)N(C3=CC=C(C)C=C3)N=C2C1=O,CCCCCCC,Alkane,7,0,4,708.8200000000002,No,,5E80,5KP,32603594,17e,No,,Reviewed,O43924,No,No,No,No,24,177.39
1184,O=C(NCCOCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCN4N=C(C)C5=C(C)N(C6=CC=C(C)C=C6)N=C5C4=O,Inactive,No,"SW480, HCT116",1.950360000000004,,Yangwode Jing,30 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,56 uM,58 uM,other,13,3,,,PDEδ inhibitor 2,O=C(N)CCCN1N=C(C)C2=C(C)N(C3=CC=C(C)C=C3)N=C2C1=O,CCOCCOCC,PEG,8,2,5,726.791,No,,5E80,5KP,32603594,17g,No,,Reviewed,O43924,No,No,No,No,24,195.84999999999997
1185,O=C(NCCCOCCOCCOCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCN4N=C(C)C5=C(C)N(C6=CC=C(C)C=C6)N=C5C4=O,Active,No,"SW480, HCT116",2.7471600000000054,,Yangwode Jing,10 uM,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,56 uM,26 uM,other,14,3,,,PDEδ inhibitor 2,O=C(N)CCCN1N=C(C)C2=C(C)N(C3=CC=C(C)C=C3)N=C2C1=O,CCCOCCOCCOCCC,PEG,13,3,10,798.8979999999996,No,,5E80,5KP,32603594,17h,No,,Reviewed,O43924,No,No,No,No,24,205.07999999999998
1186,O=C(NCCNC(C1N(CC2=CC=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C(Br)=C2)CCCC1)=O)CCCC(NC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O,Inactive,No,,5.800620000000006,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,9,4,,> 200 nM,BMS-8,O=C([C@@H]1N(CC2=CC=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C(Br)=C2)CCCC1)O,NCCNC(=O)CCCC=O,Other,11,4,6,905.8469999999994,No,,5J8O,6GZ,32388281,P1,No,,Reviewed,Q9NZQ7,No,No,No,No,,183.32
1187,O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCC(N4CCN(C(C5N(CC6=CC=C(OCC7=C(C)C(C8=CC=CC=C8)=CC=C7)C(Br)=C6)CCCC5)=O)CC4)=O,Inactive,No,,6.239020000000008,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,9,2,,> 200 nM,BMS-8,O=C([C@@H]1N(CC2=CC=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C(Br)=C2)CCCC1)O,O=CCCCC(=O)N1CCNCC1,Other,13,4,4,931.8849999999998,No,,5J8O,6GZ,32388281,P2,No,,Reviewed,Q9NZQ7,No,No,No,No,,165.73999999999998
1188,O=C(C1N(CC2=CC=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C(Br)=C2)CCCC1)NCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O,Inactive,No,,6.767720000000007,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,8,3,,197.4 nM,BMS-8,O=C([C@@H]1N(CC2=CC=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C(Br)=C2)CCCC1)O,CCCCN,Other,5,1,2,820.7849999999997,No,,5J8O,6GZ,32388281,P3,No,,Reviewed,Q9NZQ7,No,No,No,No,,137.14999999999998
1189,O=C(NCCNC(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)=O)CCCC(NC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O,Inactive,No,,7.142200000000008,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,11,4,,122.5 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,NCCNC(=O)CCCC=O,Other,11,4,6,992.5299999999994,No,,5J8O,6GZ,32388281,P4,No,,Reviewed,Q9NZQ7,No,No,No,No,,216.33999999999995
1190,O=C(NCCCCNC(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)=O)CCCC(NC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O,Inactive,No,,7.9224000000000085,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,11,4,,120.8 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,NCCCCNC(=O)CCCC=O,Other,13,4,8,1020.5839999999994,No,,5J8O,6GZ,32388281,P5,No,,Reviewed,Q9NZQ7,No,No,No,No,,216.33999999999995
1191,O=C(NCCCNC(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)=O)CCC(NC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O,Inactive,No,,7.142200000000008,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,11,4,,> 200 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,NCCCNC(=O)CCC=O,Other,11,4,6,992.5299999999995,No,,5J8O,6GZ,32388281,P6,No,,Reviewed,Q9NZQ7,No,No,No,No,,216.33999999999995
1192,O=C(NCCCCCNC(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)=O)CCCC(NC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O,Inactive,No,,8.312500000000009,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,11,4,,> 200 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,NCCCCCNC(=O)CCCC=O,Other,14,4,9,1034.6109999999992,,,5J8O,6GZ,32388281,P7,No,,Reviewed,Q9NZQ7,No,No,No,No,,216.33999999999995
1193,O=C(NCCNC(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)=O)CCCC(NC6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)=O,Inactive,No,,7.142200000000008,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,11,4,,101.9 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,NCCNC(=O)CCCC=O,Other,11,4,6,992.5299999999994,No,,5J8O,6GZ,32388281,P8,No,,Reviewed,Q9NZQ7,No,No,No,No,,216.33999999999995
1194,O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCC(N4CCN(C(C5N(CC6=CC(Cl)=C(OCC7=C(C)C(C8=CC=CC=C8)=CC=C7)C=C6OCC9=CC=CC(C#N)=C9)CCCC5)=O)CC4)=O,Active,No,A549; H1299; B16-F10; MDAMB231; Jurkat,7.580600000000011,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,carboxilic_acid_to_amide,11,2,,26.1 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,O=CCCCC(=O)N1CCNCC1,Other,13,4,4,1018.5679999999996,No,,5J8O,6GZ,32388281,P9,No,,Reviewed,Q9NZQ7,No,No,No,No,48,198.75999999999996
1195,O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCC(N4CCN(C(C5N(CC6=CC(Cl)=C(OCC7=C(C)C(C8=CC=CC=C8)=CC=C7)C=C6OCC9=CC=CC(C#N)=C9)CCCC5)=O)CC4)=O,Active,No,A549; H1299; B16-F10; MDAMB231; Jurkat,7.19050000000001,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,carboxilic_acid_to_amide,11,2,,44.5 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,O=CCCC(=O)N1CCNCC1,Other,12,4,3,1004.5409999999996,,,5J8O,6GZ,32388281,P10,No,,Reviewed,Q9NZQ7,No,No,No,No,48,198.75999999999996
1196,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)NCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Inactive,No,,7.329100000000008,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,10,3,,117.6 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,CCN,Alkane,3,1,0,879.4139999999994,No,,5J8O,6GZ,32388281,P11,No,,Reviewed,Q9NZQ7,No,No,No,No,,170.17
1197,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)NCCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Inactive,No,,7.71920000000001,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,10,3,,97.3 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,CCCN,Alkane,4,1,1,893.4409999999993,No,,5J8O,6GZ,32388281,P12,No,,Reviewed,Q9NZQ7,No,No,No,No,,170.17
1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)NCCCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Active,No,A549; H1299; B16-F10; MDAMB231; Jurkat,8.10930000000001,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,8.2 uM,carboxilic_acid_to_amide,10,3,,52.8 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,CCCCN,Alkane,5,1,2,907.4679999999993,No,,5J8O,6GZ,32388281,P13,No,,Reviewed,Q9NZQ7,No,No,No,No,48,170.17
1199,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)NCCCCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Inactive,No,,8.499400000000009,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,10,3,,170.9 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,CCCCCN,Alkane,6,1,3,921.4949999999992,No,,5J8O,6GZ,32388281,P14,No,,Reviewed,Q9NZQ7,No,No,No,No,,170.17
1200,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)NCCCCCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O,Inactive,No,,8.889500000000005,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,10,3,,> 200 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,CCCCCCN,Alkane,7,1,4,935.5219999999991,No,,5J8O,6GZ,32388281,P15,No,,Reviewed,Q9NZQ7,No,No,No,No,,170.17
1201,O=C(NCCNC(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)=O)CCC(NC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O,Inactive,No,,6.7521000000000075,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,11,4,,98.8 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,NCCNC(=O)CCC=O,Other,10,4,5,978.5029999999995,No,,5J8O,6GZ,32388281,P16,No,,Reviewed,Q9NZQ7,No,No,No,No,,216.33999999999995
1202,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)NCCNC(COCC(NC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)=O,Inactive,No,,5.988500000000005,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,12,4,,> 200 nM,BMS-1233,O=C(C1N(CC2=CC(Cl)=C(OCC3=C(C)C(C4=CC=CC=C4)=CC=C3)C=C2OCC5=CC=CC(C#N)=C5)CCCC1)O,NCCNC(=O)COCC=O,Other,11,5,6,994.5019999999993,No,,5J8O,6GZ,32388281,P17,No,,Reviewed,Q9NZQ7,No,No,No,No,,225.56999999999996
1203,O=C(NCCNC(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)=O)CCCC(NC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O)=O,Inactive,No,,6.913400000000007,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,13,4,,> 200 nM,BMS-1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)O,NCCNC(=O)CCCC=O,Other,11,4,6,1050.5659999999993,No,,5J8O,6GZ,32388281,P18,No,,Reviewed,Q9NZQ7,No,No,No,No,,234.79999999999998
1204,O=C(NCCNC(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)=O)CCCC(NC7=CC8=C(C(N(C(CC9)C(NC9=O)=O)C8=O)=O)C=C7)=O,Inactive,No,,6.913400000000007,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,13,4,,> 200 nM,BMS-1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)O,NCCNC(=O)CCCC=O,Other,11,4,6,1050.5659999999993,No,,5J8O,6GZ,32388281,P19,No,,Reviewed,Q9NZQ7,No,No,No,No,,234.79999999999998
1205,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)NCCNC(COCC(NC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O)=O)=O,Inactive,No,,5.759700000000004,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,14,4,,> 200 nM,BMS-1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)O,NCCNC(=O)COCC=O,Other,11,5,6,1052.5379999999993,No,,5J8O,6GZ,32388281,P20,No,,Reviewed,Q9NZQ7,No,No,No,No,,244.02999999999997
1206,O=C(NCCNC(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)=O)CCC(NC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O)=O,Inactive,No,,6.523300000000007,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,13,4,,> 200 nM,BMS-1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)O,NCCNC(=O)CCC=O,Other,10,4,5,1036.5389999999993,No,,5J8O,6GZ,32388281,P21,No,,Reviewed,Q9NZQ7,No,No,No,No,,234.79999999999998
1207,O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCC(N4CCN(C(C5N(CC6=CC(Cl)=C(OCC7=CC=CC(C8=CC=C9OCCOC9=C8)=C7C)C=C6OCC%10=CC=CC(C#N)=C%10)CCCC5)=O)CC4)=O,Active,Yes,A549; H1299; B16-F10; MDAMB231; Jurkat,7.3518000000000105,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,carboxilic_acid_to_amide,13,2,,39.2 nM,BMS-1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)O,O=CCCCC(=O)N1CCNCC1,Other,13,4,4,1076.6039999999996,No,,5J8O,6GZ,32388281,P22,No,,Reviewed,Q9NZQ7,No,No,No,No,48,217.21999999999994
1208,O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCC(N4CCN(C(C5N(CC6=CC(Cl)=C(OCC7=CC=CC(C8=CC=C9OCCOC9=C8)=C7C)C=C6OCC%10=CC=CC(C#N)=C%10)CCCC5)=O)CC4)=O,Active,No,A549; H1299; B16-F10; MDAMB231; Jurkat,6.96170000000001,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,9.2 uM,carboxilic_acid_to_amide,13,2,,25.2 nM,BMS-1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)O,O=CCCC(=O)N1CCNCC1,Other,12,4,3,1062.5769999999998,No,,5J8O,6GZ,32388281,P23,No,,Reviewed,Q9NZQ7,No,No,No,No,48,217.21999999999994
1209,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)NCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O,Inactive,No,,7.100300000000008,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,12,3,,143.7 nM,BMS-1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)O,CCN,Alkane,3,1,0,937.4499999999995,No,,5J8O,6GZ,32388281,P24,No,,Reviewed,Q9NZQ7,No,No,No,No,,188.63
1210,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)NCCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O,Inactive,No,,7.490400000000009,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,12,3,,135.2 nM,BMS-1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)O,CCCN,Alkane,4,1,1,951.4769999999994,No,,5J8O,6GZ,32388281,P25,No,,Reviewed,Q9NZQ7,No,No,No,No,,188.63
1211,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)NCCCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O,Active,No,A549; H1299; B16-F10; MDAMB231; Jurkat,7.880500000000009,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,> 10 uM,carboxilic_acid_to_amide,12,3,,102.7 nM,BMS-1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)O,CCCCN,Alkane,5,1,2,965.5039999999993,No,,5J8O,6GZ,32388281,P26,No,,Reviewed,Q9NZQ7,No,No,No,No,48,188.63
1212,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)NCCCCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O,Inactive,No,,8.270600000000009,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,12,3,,193.2 nM,BMS-1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)O,CCCCCN,Alkane,6,1,3,979.5309999999993,No,,5J8O,6GZ,32388281,P27,No,,Reviewed,Q9NZQ7,No,No,No,No,,188.63
1213,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)NCCCCCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O,Inactive,No,,8.660700000000007,,Yangwode Jing,,,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,carboxilic_acid_to_amide,12,3,,> 200 nM,BMS-1198,O=C(C1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)CCCC1)O,CCCCCCN,Alkane,7,1,4,993.5579999999992,No,,5J8O,6GZ,32388281,P28,No,,Reviewed,Q9NZQ7,No,No,No,No,,188.63
1214,O=C1N(C2CCC(NC2=O)=O)C(C3=C(NCCCCCCCC(NC(C=C4)=CC=C4N5CC6=CC=C(O)C=C6OC5=O)=O)C=CC=C31)=O,Active,Yes,A549,4.703600000000003,,Zhangping Xiao,200 nM,90 %,Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O,Cereblon,,,other,9,4,150 nM,108 nM,"3-(3,4-dimethoxyphenyl)-7-hydroxy-3,4-dihydro-2H-benzo[e][1,3]oxazin-2-one",OC1=CC=C(CN(C2=CC=C(OC)C(OC)=C2)C(O3)=O)C3=C1,CCCCCCCC(N)=O,Alkane,10,2,6,653.6920000000003,,,,,34018657,MD13,No,,Reviewed,P14174,Yes,Yes,No,Yes,12,174.45
1215,O=C(N[C@@H](C(C)(C)C)C(N1C[C@@H](C[C@H]1C(N[C@@H](C)C2=CC=C(C3=C(N=CS3)C)C=C2)=O)O)=O)CCCC/C=C/C[C@H]([C@H]([C@H]4C(N[C@H](C(N(CC(N([C@H](C(N[C@H](C(N([C@H](C(N[C@H](C(N[C@@H](C(N([C@H](C(N([C@H](C(N([C@H](C(N4C)=O)C(C)C)C)=O)CC(C)C)C)=O)CC(C)C)C)=O)C)=O)C)=O)CC(C)C)C)=O)C(C)C)=O)CC(C)C)C)=O)C)=O)CC)=O)O)C,Active,Yes,Huh7,6.611520000000009,Exhibits potent anti-HCV activity. The first demonstration of a PROTAC antiviral effect by degradation of a host protein (cyclophilin A).,David Selwood,30 nM,90 %,N[C@@H](C(C)(C)C)C(N1[C@H](C(N[C@@H](C)C2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O.Cl,VHL,188 nM,16 nM,aliphatic_CC,18,8,85 nM,183 nM,cyclosporine A,C/C=C/C[C@H]([C@H]([C@H]1C(N[C@H](C(N(CC(N([C@H](C(N[C@H](C(N([C@H](C(N[C@H](C(N[C@@H](C(N([C@H](C(N([C@H](C(N([C@H](C(N1C)=O)C(C)C)C)=O)CC(C)C)C)=O)CC(C)C)C)=O)C)=O)C)=O)CC(C)C)C)=O)C(C)C)=O)CC(C)C)C)=O)C)=O)CC)=O)O)C,CCCC=O,Alkane,5,1,2,1715.3109999999967,,,1m63,,32539931,JW4-10,No,,Reviewed,P62937,Yes,Yes,No,Yes,"4,8,16,24,48",390.43