Cdk2 inhibitor IV [Ligand Id: 5949] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1802728
  • aurora kinase A in Human [GtoPdb: 1936] [UniProtKB: O14965]
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  • aurora kinase B in Human [GtoPdb: 1937] [UniProtKB: Q96GD4]
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  • cyclin dependent kinase 1 in Human [GtoPdb: 1961] [UniProtKB: P06493]
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  • cyclin dependent kinase 2 in Human [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 4 in Human [GtoPdb: 1976] [UniProtKB: P11802]
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  • cyclin dependent kinase 5 in Human [GtoPdb: 1977] [UniProtKB: Q00535]
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  • cyclin dependent kinase 7 in Human [GtoPdb: 1979] [UniProtKB: P50613]
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  • eukaryotic translation initiation factor 2 alpha kinase 2 in Human [GtoPdb: 2016] [UniProtKB: P19525]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
aurora kinase A in Human [GtoPdb: 1936] [UniProtKB: O14965]
GtoPdb - - 7.17 pIC50 67 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
aurora kinase B in Human [GtoPdb: 1937] [UniProtKB: Q96GD4]
GtoPdb - - 7.46 pIC50 35 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 1 in Human [GtoPdb: 1961] [UniProtKB: P06493]
GtoPdb CDK1/cyclin B complex used in assay - 5.18 pIC50 6600 nM IC50 Mol Cancer Ther (2005) 4: 1328-37 [PMID:16170024]
cyclin dependent kinase 2 in Human [GtoPdb: 1973] [UniProtKB: P24941]
GtoPdb CDK2/cyclin A complex used in assay - 6.39 pIC50 410 nM IC50 Mol Cancer Ther (2005) 4: 1328-37 [PMID:16170024]
GtoPdb - - 6.4 pIC50 400 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 4 in Human [GtoPdb: 1976] [UniProtKB: P11802]
GtoPdb CDK4/cyclin D complex used in assay - 5.26 pIC50 5500 nM IC50 Mol Cancer Ther (2005) 4: 1328-37 [PMID:16170024]
cyclin dependent kinase 5 in Human [GtoPdb: 1977] [UniProtKB: Q00535]
GtoPdb CDK5/p25 complex used in assay - 4.82 pIC50 15000 nM IC50 Mol Cancer Ther (2005) 4: 1328-37 [PMID:16170024]
cyclin dependent kinase 7 in Human [GtoPdb: 1979] [UniProtKB: P50613]
GtoPdb CDK7/cyclin H complex used in assay - 5.41 pIC50 3900 nM IC50 Mol Cancer Ther (2005) 4: 1328-37 [PMID:16170024]
eukaryotic translation initiation factor 2 alpha kinase 2 in Human [GtoPdb: 2016] [UniProtKB: P19525]
GtoPdb - - 5.7 pIC50 2000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4108-14 [PMID:21632247]

ChEMBL data shown on this page come from version 36:

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]