CHIR-98014 [Ligand Id: 8016] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3185148 |
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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] |
| LIM domain kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667] | ||||||||
| ChEMBL | Inhibition of recombinant LIMK1 (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 13705-13713 [PMID:36205722] |
| ChEMBL | Inhibition of PAK mediated recombinant LIMK1 phosphorylation (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 13705-13713 [PMID:36205722] |
| ChEMBL | Inhibition of recombinant LIMK1(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 13705-13713 [PMID:36205722] |
| LIM domain kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5932] [GtoPdb: 2055] [UniProtKB: P53671] | ||||||||
| ChEMBL | Inhibition of recombinant LIMK2 (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 13705-13713 [PMID:36205722] |
| ChEMBL | Inhibition of PAK mediated recombinant LIMK2 phosphorylation (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 13705-13713 [PMID:36205722] |
| ChEMBL | Inhibition of recombinant LIMK2(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 13705-13713 [PMID:36205722] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
