MK-8776 [Ligand Id: 7943] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1643208
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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396]
ChEMBL Inhibition of recombinant CDK2/Cyclin A expressed in insect Sf9 cells assessed as inhibition of [33P]-ATP incorporation into biotinylated histone H1 after 1 hr by liquid scintillation counting B 6.8 pIC50 160 nM IC50 Bioorg Med Chem Lett (2011) 21: 471-474 [PMID:21094607]
GtoPdb CDK2/cyclin A complex in assay - 6.8 pIC50 160 nM IC50 Bioorg Med Chem Lett (2011) 21: 471-4 [PMID:21094607]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
GtoPdb - - 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2011) 21: 471-4 [PMID:21094607]
ChEMBL Inhibition of histidine-tagged recombinant CHK1 expressed in baculovirus expression system after 2 hrs by scintillation proximity assay B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2011) 21: 471-474 [PMID:21094607]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]