CHIR-98014 [Ligand Id: 8016] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3185148
  • casein kinase 1 epsilon/Casein kinase I epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
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  • cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
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  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
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  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL Inhibition of human CK1epsilon using biotin peptide substrate after 1 hr by scintillation counting method B 5.3 pIC50 >5000 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
ChEMBL Inhibition of human CDC2 using biotin histone H1 peptide substrate after 1 hr by scintillation counting method B 5.4 pIC50 4000 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibition of human bFGF receptor tyrosine kinase using KDRY1175 [B91616] biotin-GGGGQDGKDYIVLPI-NH2 peptide substrate after 1 hr by scintillation counting method B 6 pIC50 >1000 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
ChEMBL Inhibition of human GSK3alpha using biotin-CREB peptide substrate after 1 hr by scintillation counting method B 8.15 pIC50 7 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
GtoPdb - - 9.19 pIC50 0.65 nM IC50 Diabetes (2003) 52: 588-95 [PMID:12606497]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of human GSK3beta using biotin-CREB peptide substrate after 1 hr by scintillation counting method B 9.22 pIC50 0.6 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
GtoPdb - - 9.24 pIC50 0.58 nM IC50 Diabetes (2003) 52: 588-95 [PMID:12606497]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Inhibition of human IGF1 receptor tyrosine kinase using biotin-GGGGKKKSPGEYVNIEFG-amide peptide substrate after 1 hr by scintillation counting method B 5.7 pIC50 >2000 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of human insulin receptor tyrosine kinase after 1 hr by scintillation counting method B 5.7 pIC50 >2000 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Inhibition of human ERK2 using myelin basic protein substrate after 1 hr by scintillation counting method B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of human AKT1/PKB using phospho-AKT peptide substrate after 1 hr by scintillation counting method B 5.3 pIC50 >5000 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL Inhibition of human CHK1 using biotin-CDC25 peptide substrate after 1 hr by scintillation counting method B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL Inhibition of human Tie2 using biotin-GGGGAPDLYKDFLT peptide substrate after 1 hr by scintillation counting method B 5.3 pIC50 >5000 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
ChEMBL Inhibition of human FLT1 using KDRY1175 [B91616] biotin-GGGGQDGKDYIVLPI-NH2 peptide substrate after 1 hr by scintillation counting method B 5.3 pIC50 >5000 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of human KDR using KDRY1175 [B91616] biotin-GGGGQDGKDYIVLPI-NH2 peptide substrate after 1 hr by scintillation counting method B 5.7 pIC50 >2000 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]