lovingscience/chembl-v37-raw-activities huggingface dataset:
Compound (SMILES): O=C1C[C@@H](COc2nc(-c3ccc(C(F)(F)F)cc3)cc3ncccc23)CN1
InChIKey: VQFWVFLJYSXTBW-GFCCVEGCSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 34.7 nM (pChEMBL 7.460000038146973)
Descriptors: MW 387.36, ALogP 3.83, HBA 4, HBD 1, PSA 64.11, QED 0.74
Compound (SMILES): Cc1cc(-c2cc3ncccc3c(OC[C@H]3CNC(=O)C3)n2)no1
InChIKey: DIWUONCXNMQZFG-LLVKDONJSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 207.8 nM (pChEMBL 6.679999828338623)
Descriptors: MW 324.34, ALogP 2.11, HBA 6, HBD 1, PSA 90.14, QED 0.79
Compound (SMILES): COc1c(F)cc(-c2cc3ncccc3c(OC[C@H]3CNC(=O)C3)n2)cc1F
InChIKey: GWIAFYCLLASSNP-LLVKDONJSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 22.3 nM (pChEMBL 7.650000095367432)
Descriptors: MW 385.37, ALogP 3.1, HBA 5, HBD 1, PSA 73.34, QED 0.73
Compound (SMILES): COc1c(F)cc(-c2cc3ncccc3c(O[C@H](C)[C@H]3CNC(=O)C3)n2)cc1F
InChIKey: YELDWGRYCRSCOM-DGCLKSJQSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 0.7 nM (pChEMBL 9.149999618530273)
Descriptors: MW 399.4, ALogP 3.49, HBA 5, HBD 1, PSA 73.34, QED 0.71
Compound (SMILES): Cc1ccc(OC2CCOCC2)c(C(F)(F)F)c1
InChIKey: NCEOTVRVWOKJHI-UHFFFAOYSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 10.1 nM (pChEMBL 8)
Descriptors: MW 260.25, ALogP 3.57, HBA 2, HBD 0, PSA 18.46, QED 0.81
Compound (SMILES): COc1ccc(-c2cc3ncccc3c(OC[C@H]3CNC(=O)C3)n2)cc1Cl
InChIKey: NIORITCVKCMJBR-GFCCVEGCSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 7.2 nM (pChEMBL 8.140000343322754)
Descriptors: MW 383.84, ALogP 3.47, HBA 5, HBD 1, PSA 73.34, QED 0.73
Compound (SMILES): COc1cc(-c2cc3ncccc3c(OC[C@H]3CNC(=O)C3)n2)ccc1Cl
InChIKey: MMDOXFZLVNQHNH-GFCCVEGCSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 14.5 nM (pChEMBL 7.840000152587891)
Descriptors: MW 383.84, ALogP 3.47, HBA 5, HBD 1, PSA 73.34, QED 0.73
Compound (SMILES): COc1cc(C)cc(OC)c1OCCN1CCOCC1
InChIKey: BOMZQLOCWLHCAV-UHFFFAOYSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 13.6 nM (pChEMBL 7.869999885559082)
Descriptors: MW 281.35, ALogP 1.72, HBA 5, HBD 0, PSA 40.16, QED 0.79
Compound (SMILES): COc1cc(-c2cc3ncccc3c(O[C@H](C)[C@H]3CNC(=O)C3)n2)cc(OC)c1OCCN1CCOCC1
InChIKey: ZAXXYXWMMRHEGZ-UYAOXDASSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 0.8 nM (pChEMBL 9.100000381469727)
Descriptors: MW 522.6, ALogP 2.93, HBA 9, HBD 1, PSA 104.27, QED 0.43
Compound (SMILES): CC[C@@H](Oc1nc(-c2cc(OC)c(OCCN3CCOCC3)c(OC)c2)cc2ncccc12)[C@H]1CNC(=O)C1
InChIKey: AVGXUNVNNIZQOV-HYBUGGRVSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 0.7 nM (pChEMBL 9.149999618530273)
Descriptors: MW 536.63, ALogP 3.32, HBA 9, HBD 1, PSA 104.27, QED 0.4
Compound (SMILES): COc1cc(-c2cc3ncccc3c(O[C@H](C)[C@H]3CNC(=O)C3)n2)cc2c1OCO2
InChIKey: IOHBEJVDQBRYNR-TZMCWYRMSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 0.7 nM (pChEMBL 9.149999618530273)
Descriptors: MW 407.43, ALogP 2.94, HBA 7, HBD 1, PSA 91.8, QED 0.7
Compound (SMILES): C[C@@H](Oc1nc(-c2ccc(=O)[nH]c2)cc2ncccc12)[C@H]1CNC(=O)C1
InChIKey: VJBFWUGBAQMLEW-DGCLKSJQSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 1 nM (pChEMBL 9)
Descriptors: MW 350.38, ALogP 1.89, HBA 5, HBD 2, PSA 96.97, QED 0.75
Compound (SMILES): CN1CCOc2cc(-c3cc4ncccc4c(OCC4CNC(=O)C4)n3)cnc21
InChIKey: UOECNKIDCIICKR-UHFFFAOYSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 17.2 nM (pChEMBL 7.760000228881836)
Descriptors: MW 391.43, ALogP 2.04, HBA 7, HBD 1, PSA 89.47, QED 0.73
Compound (SMILES): COc1cc(-c2cc3ncccc3c(NCc3n[nH]c(=O)o3)n2)cc(OC)c1OC
InChIKey: VKJBGUINZIZFKU-UHFFFAOYSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 5 nM (pChEMBL 8.300000190734863)
Descriptors: MW 409.4, ALogP 2.61, HBA 9, HBD 2, PSA 124.39, QED 0.47
Compound (SMILES): COc1cc(-c2cc3ncccc3c(NCc3n[nH]c(=O)[nH]3)n2)cc(OC)c1OC
InChIKey: SKNDEWTYWANGHH-UHFFFAOYSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 10.3 nM (pChEMBL 7.989999771118164)
Descriptors: MW 408.42, ALogP 2.35, HBA 8, HBD 3, PSA 127.04, QED 0.43
Compound (SMILES): COc1cc(-c2cc3ncccc3c(OC([C@H]3CNC(=O)C3)C(F)(F)F)n2)cc(OC)c1OC
InChIKey: FNZLSTSCXAVIBG-ILRUXTBWSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 4.1 nM (pChEMBL 8.390000343322754)
Descriptors: MW 477.44, ALogP 3.77, HBA 7, HBD 1, PSA 91.8, QED 0.55
Compound (SMILES): COc1cc(-c2cc3ncccc3c(OC[C@H]3CNC(=O)O3)n2)cc(OC)c1OC
InChIKey: NNQPVWOBOWFMFM-CYBMUJFWSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 1.2 nM (pChEMBL 8.920000076293945)
Descriptors: MW 411.41, ALogP 2.81, HBA 8, HBD 1, PSA 101.03, QED 0.63
Compound (SMILES): COc1cc(-c2cc3ncccc3c(OCC3CC(=O)NO3)n2)cc(OC)c1OC
InChIKey: HCNHJMCOTOMFJM-UHFFFAOYSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 67.1 nM (pChEMBL 7.170000076293945)
Descriptors: MW 411.41, ALogP 2.52, HBA 8, HBD 1, PSA 101.03, QED 0.63
Compound (SMILES): COc1cc(-c2cc3ncccc3c(NC[C@H]3CNC(=O)O3)n2)cc(OC)c1OC
InChIKey: KSODRXGOIPVAPA-ZDUSSCGKSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 3332.8 nM (pChEMBL 5.480000019073486)
Descriptors: MW 410.43, ALogP 2.84, HBA 8, HBD 2, PSA 103.83, QED 0.61
Compound (SMILES): COc1cc(-c2cc3ncccc3c(NCc3cc(=O)[nH]o3)n2)cc(OC)c1OC
InChIKey: ZIZNWDUBHFPLPV-UHFFFAOYSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 105.2 nM (pChEMBL 6.980000019073486)
Descriptors: MW 408.41, ALogP 3.22, HBA 8, HBD 2, PSA 111.5, QED 0.48
Compound (SMILES): COc1cc(-c2cc3ncccc3c(OC(C)C3CC(=O)NO3)n2)cc(OC)c1OC
InChIKey: KUQRPNPVOPROCG-UHFFFAOYSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 17.3 nM (pChEMBL 7.760000228881836)
Descriptors: MW 425.44, ALogP 2.91, HBA 8, HBD 1, PSA 101.03, QED 0.62
Compound (SMILES): COc1cc(-c2cc3ncccc3c(OCC3CNC(=O)C3)n2)cc(OC)c1OC
InChIKey: WDWSNLBHZHEKLL-UHFFFAOYSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 7.1 nM (pChEMBL 8.149999618530273)
Descriptors: MW 409.44, ALogP 2.84, HBA 7, HBD 1, PSA 91.8, QED 0.64
Compound (SMILES): COCC[C@@H](Oc1nc(-c2cc(OC)c(OC)c(OC)c2)cc2ncccc12)[C@H]1CNC(=O)C1
InChIKey: BMOIDQWKLFTNLC-OXQOHEQNSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 12.4 nM (pChEMBL 7.909999847412109)
Descriptors: MW 467.52, ALogP 3.24, HBA 8, HBD 1, PSA 101.03, QED 0.49
Compound (SMILES): COc1cc(-c2cc3ncccc3c(O[C@H](C)[C@H]3CNC(=O)C3)n2)cc(OC)c1OC
InChIKey: BRYUNLVJDCMANZ-UKRRQHHQSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 0.2 nM (pChEMBL 9.699999809265137)
Descriptors: MW 423.47, ALogP 3.23, HBA 7, HBD 1, PSA 91.8, QED 0.62
Compound (SMILES): COc1cc(-c2cc3ncccc3c(OC[C@H]3CNC(=O)[C@@H]3C)n2)cc(OC)c1OC
InChIKey: OIEJMJOKHPFVEW-UKRRQHHQSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 17.4 nM (pChEMBL 7.760000228881836)
Descriptors: MW 423.47, ALogP 3.08, HBA 7, HBD 1, PSA 91.8, QED 0.62
Compound (SMILES): COc1cc(-c2cc3c(ccc[n+]3[O-])c(O[C@H](C)[C@H]3CNC(=O)C3)n2)cc(OC)c1OC
InChIKey: QIQJFCADRQIFSY-UKRRQHHQSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 4.3 nM (pChEMBL 8.369999885559082)
Descriptors: MW 439.47, ALogP 2.46, HBA 7, HBD 1, PSA 105.85, QED 0.45
Compound (SMILES): COc1cc(-c2cc3ncccc3c(NC[C@H]3CC(=O)N[C@@H]3C)n2)cc(OC)c1OC
InChIKey: BKOLXFNOHXONLP-UKRRQHHQSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 251.5 nM (pChEMBL 6.599999904632568)
Descriptors: MW 422.49, ALogP 3.26, HBA 7, HBD 2, PSA 94.6, QED 0.6
Compound (SMILES): COc1cc(-c2cc3ncccc3c(N[C@H](C)[C@H]3CNC(=O)C3)n2)cc(OC)c1OC
InChIKey: SOIJWEWGKXPXPV-UKRRQHHQSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 13.3 nM (pChEMBL 7.880000114440918)
Descriptors: MW 422.49, ALogP 3.26, HBA 7, HBD 2, PSA 94.6, QED 0.6
Compound (SMILES): COc1cc(-c2cc3ncccc3c(NCc3ccc(=O)[nH]c3)n2)cc(OC)c1OC
InChIKey: TTXGFQVBNRYFBZ-UHFFFAOYSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 410.8 nM (pChEMBL 6.389999866485596)
Descriptors: MW 418.45, ALogP 3.62, HBA 7, HBD 2, PSA 98.36, QED 0.47
Compound (SMILES): CC[C@@H](Oc1nc(-c2cc(OC)c(OC)c(OC)c2)cc2ncccc12)[C@H]1CNC(=O)C1
InChIKey: KDBBHCQXKQMERW-DNVCBOLYSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 0.3 nM (pChEMBL 9.520000457763672)
Descriptors: MW 437.5, ALogP 3.62, HBA 7, HBD 1, PSA 91.8, QED 0.58
Compound (SMILES): COc1cc(-c2cc3ncccc3c(OC[C@H]3CNC(=O)C3(C)C)n2)cc(OC)c1OC
InChIKey: UFDCMNNLCZUOBP-OAHLLOKOSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 11.7 nM (pChEMBL 7.929999828338623)
Descriptors: MW 437.5, ALogP 3.47, HBA 7, HBD 1, PSA 91.8, QED 0.61
Compound (SMILES): CC[C@H]1NC(=O)C[C@@H]1CNc1nc(-c2cc(OC)c(OC)c(OC)c2)cc2ncccc12
InChIKey: JAUUFXCCRHLAQJ-NVXWUHKLSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 1525 nM (pChEMBL 5.820000171661377)
Descriptors: MW 436.51, ALogP 3.65, HBA 7, HBD 2, PSA 94.6, QED 0.56
Compound (SMILES): COc1cc(-c2cc3ncccc3c(OC[C@H]3CNC(=O)C3)n2)cc(OC)c1OC1CCOCC1
InChIKey: VMCYYSDFUKICIM-MRXNPFEDSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 16.1 nM (pChEMBL 7.789999961853027)
Descriptors: MW 479.53, ALogP 3.39, HBA 8, HBD 1, PSA 101.03, QED 0.52
Compound (SMILES): C[C@@H](Oc1nc(-c2ccc(N3CCOCC3)nc2)cc2ncccc12)[C@H]1CNC(=O)C1
InChIKey: CQHSODKUZPODHU-NVXWUHKLSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 0.1 nM (pChEMBL 10)
Descriptors: MW 419.49, ALogP 2.43, HBA 7, HBD 1, PSA 89.47, QED 0.68
Compound (SMILES): COc1ccc(-c2cc3ncccc3c(O[C@H](C)[C@H]3CNC(=O)C3)n2)cn1
InChIKey: HACNKVZFEWDXCA-TZMCWYRMSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 0.4 nM (pChEMBL 9.399999618530273)
Descriptors: MW 364.41, ALogP 2.6, HBA 6, HBD 1, PSA 86.23, QED 0.75
Compound (SMILES): COc1ccc(-c2cc3ncccc3c(OC[C@H]3CNC(=O)C3)n2)cc1OC
InChIKey: YSFVSZHFOYRRJX-CYBMUJFWSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 10.7 nM (pChEMBL 7.96999979019165)
Descriptors: MW 379.42, ALogP 2.83, HBA 6, HBD 1, PSA 82.57, QED 0.71
Compound (SMILES): COc1ccc(-c2cc3ncccc3c(OC[C@H]3CNC(=O)C3)n2)cc1F
InChIKey: UONXLDBCAGMDQX-GFCCVEGCSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 6.3 nM (pChEMBL 8.199999809265137)
Descriptors: MW 367.38, ALogP 2.96, HBA 5, HBD 1, PSA 73.34, QED 0.75
Compound (SMILES): COc1cc(-c2cc3ncccc3c(OC[C@H]3CNC(=O)C3)n2)ccc1F
InChIKey: AYFLFKHHVVQKAL-GFCCVEGCSA-N
Target: Tyrosine-protein kinase SYK (SINGLE PROTEIN), Homo sapiens
UniProt: P43405
Assay: Kinase Glo Luminescence Kinase Assay: Recombinant human Syk (amino acids 342-635) was expressed as a fusion protein with an N-terminal GST tag, affinity-purified and deep-frozen at a concentration of approx. 50 - 100 uM in test buffer (25 mM HEPES pH7.5; 25 mM MgCI2;5 mM MnCI2; 50 mM KCI; 0.2% BSA; 0.01 % CHAPS; 100 uM Na3V04; 0.5 mM DTT) and 10% glycerol at -80 C until use.The catalytic activity of the GST-Syk kinase fusion protein was determined using the Kinase Glo Luminescence Kinase test (Promega; V6712). In this homogeneous test the amount of ATP remaining after the kinase reaction is quantified by a luciferin-luciferase reaction using luminescence. The luminescence signal obtained correlates with the amount of ATP still present and thus correlates inversely with the activity of the protein kinase. Method:The test compounds were dissolved in 100 % DMSO at a concentration of 10 mM and diluted in DMSO to a concentration of 1 mM.
Measurement: IC50 = 14 nM (pChEMBL 7.849999904632568)
Descriptors: MW 367.38, ALogP 2.96, HBA 5, HBD 1, PSA 73.34, QED 0.75