Cdk/Crk inhibitor [Ligand Id: 5943] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL258721 (RGB-286147)
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  • cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 6/CDK6/cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111448] [GtoPdb: 1978] [UniProtKB: P30281Q00534]
ChEMBL Inhibition of Cdk6/cyclin D3 B 6.55 pIC50 282 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
GtoPdb CDK6/cyclin D3 complex - 6.55 pIC50 282 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
cyclin dependent kinase 7/Cyclin-dependent kinase 7/ cyclin H in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111288] [GtoPdb: 1979] [UniProtKB: P50613P51946]
ChEMBL Inhibition of Cdk7/H/MAT1 B 7.15 pIC50 71 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
GtoPdb CDK7/cyclin H - 7.15 pIC50 71 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
ChEMBL Inhibition of Cdk9 B 8.05 pIC50 9 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
GtoPdb - - 6.12 pIC50 754 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
ChEMBL Inhibition of GSK3-beta B 6.12 pIC50 754 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]

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]