DOI: 10.7270/q2x067wt
title: BindingDB Entry 50038051: Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

description: Small molecule binding data for protein 5'-AMP-activated protein kinase subunit beta-1, AKT/p21CIP1, CDK7/Cyclin H/MNAT1, CaM kinase I alpha, CaM kinase IV, Casein Kinase II, Casein kinase I, Casein kinase I isoform alpha (CK1 Alpha), Casein kinase I isoform delta, Cyclin-Dependent Kinase 5 (CDK5), Cyclin-dependent kinase 1, Cyclin-dependent kinase 2, Cyclin-dependent kinase 6, Cyclin-dependent kinase 9, Death-associated protein kinase 3, Dual specificity protein kinase CLK2, Dual specificity protein kinase CLK4, Dual-specificity tyrosine-phosphorylation regulated kinase 1A, Dual-specificity tyrosine-phosphorylation regulated kinase 3, Ephrin receptor, Epidermal growth factor receptor, Epidermal growth factor receptor and ErbB2 (HER1 and HER2), Fibroblast growth factor receptor 1, Fibroblast growth factor receptor 3, Focal adhesion kinase 1/vascular endothelial growth factor receptor 3, Glycogen synthase kinase-3, Homeodomain-interacting protein kinase 2 (HIPK2), IKK epsilon/TBK1, Inhibitor of NF-kappa-B kinase (IKK), Insulin receptor, Insulin-like growth factor I receptor, Interleukin-1 receptor-associated kinase 1, Interleukin-1 receptor-associated kinase 4, JAK2/TYK2, JAK3/JAK1, LIM domain kinase 1, MAP kinase ERK2, MAP kinase signal-integrating kinase 2, MAP kinase-activated protein kinase 2, MAP kinase-activated protein kinase 3, MAP kinase-activated protein kinase 5, MAP/microtubule affinity-regulating kinase 2, Misshapen-like kinase 1, Mitogen-activated protein kinase 13 (MAPK13), Mitogen-activated protein kinase 2, Mitogen-activated protein kinase kinase kinase 9 (MLK1), Mixed lineage kinase 7, Muscle, skeletal receptor tyrosine protein kinase, NUAK family SNF1-like kinase 1, Neurotrophic tyrosine kinase receptor, Neurotrophic tyrosine kinase receptor type 2, PAK1, PDZ-binding kinase, Protein kinase C (PKC), Protein kinase C delta type, Protein kinase C, gamma, Protein kinase N2, Pyruvate dehydrogenase kinase isoenzyme 1 (PDK1), Receptor tyrosine-protein kinase erbB-4 (HER4), Rho-associated protein kinase, Ribosomal protein S6 kinase (P70S6K), Ribosomal protein S6 kinase alpha 3, Ribosomal protein S6 kinase alpha 4, Ribosomal protein S6 kinase alpha 5, SRC, Serine/threonine protein kinase NLK, Serine/threonine-protein kinase 31, Serine/threonine-protein kinase 33, Serine/threonine-protein kinase AKT, Serine/threonine-protein kinase CHK2, Serine/threonine-protein kinase Chk1, Serine/threonine-protein kinase D2 (PKD2), Serine/threonine-protein kinase D3, Serine/threonine-protein kinase DCLK2, Serine/threonine-protein kinase MRCK alpha, Serine/threonine-protein kinase Nek11, Serine/threonine-protein kinase Nek2, Serine/threonine-protein kinase Nek3, Serine/threonine-protein kinase Nek4, Serine/threonine-protein kinase PAK 4, Serine/threonine-protein kinase PIM, Serine/threonine-protein kinase PLK1, Serine/threonine-protein kinase PLK3, Serine/threonine-protein kinase PRKX, Serine/threonine-protein kinase SRPK1, Serine/threonine-protein kinase SRPK3, Serine/threonine-protein kinase Sgk1, Serine/threonine-protein kinase TAO1, Serine/threonine-protein kinase WNK2, Serine/threonine-protein kinase c-TAK1, Testis-specific serine/threonine-protein kinase 1, Testis-specific serine/threonine-protein kinase 2, Tyrosine-protein kinase ABL1, Tyrosine-protein kinase Blk, Tyrosine-protein kinase ITK/TSK, Tyrosine-protein kinase JAK2, Tyrosine-protein kinase Kit (Kit), Tyrosine-protein kinase receptor FLT3, VEGF-receptor 2 and tyrosine-protein kinase SRC, Vascular endothelial growth factor receptor, Vascular endothelial growth factor receptor 2, and p38 delta/gamma, Uniprot L7RSL3, O00141, O14757, O14920, O15111, O15146, O15264, O43293, O43781, O60285, O60674, O75116, O75582, O75676, O94806, O96013, O96017, P00519, P00533, P04626, P04629, P05129, P06213, P06239, P06241, P06493, P07948, P08069, P10721, P11309, P11362, P12931, P17948, P22607, P23443, P24941, P27448, P28482, P29317, P29597, P31749, P31751, P35916, P35968, P36888, P48729, P48730, P49137, P49760, P49840, P49841, P50613, P50750, P51451, P51617, P51812, P51817, P51955, P51956, P51957, P52333, P53350, P53667, P53778, P68400, P78368, P80192, Q00534, Q00535, Q05513, Q05655, Q08881, Q12851, Q13153, Q13464, Q13627, Q14012, Q15118, Q15303, Q16513, Q16566, Q16620, Q16644, Q5VT25, Q7KZI7, Q7L7X3, Q8IW41, Q8N4C8, Q8N568, Q8NG66, Q96KB5, Q96PF2, Q96SB4, Q9BXA7, Q9BXU1, Q9BYT3, Q9BZL6, Q9H2X6, Q9H4B4, Q9HAZ1, Q9HBH9, Q9NWZ3, Q9NYL2, Q9P1W9, Q9UBE8, Q9UHD2, Q9UPE1, Q9Y243, Q9Y3S1, and Q9Y478