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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1643208
There should be some charts here, you may need to enable JavaScript!
  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
There should be some charts here, you may need to enable JavaScript!
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]