DNA-PK inhibitor III [Ligand Id: 5960] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1317546
  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
  • protein kinase, DNA-activated, catalytic subunit in Mouse [GtoPdb: 2800] [UniProtKB: P97313]
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  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase catalytic subunit in Mouse [ChEMBL: CHEMBL2176779] [GtoPdb: 2800] [UniProtKB: P97313]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
ChEMBL Inhibition of DNA-PK purified from HeLa nuclear extracts assessed as EPPLSQEAFADLWKKR peptide substrate phosphorylation B 6.92 pIC50 120 nM IC50 J Med Chem (2015) 58: 41-71 [PMID:25387153]
protein kinase, DNA-activated, catalytic subunit in Mouse [GtoPdb: 2800] [UniProtKB: P97313]
GtoPdb Inhibition of PRKDC in C57BL6 mouse endothelial cells - 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2012) 22: 5352-9 [PMID:22835870]
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase catalytic subunit in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176779] [GtoPdb: 2800] [UniProtKB: P97313]
GtoPdb Inhibition of PRKDC in C57BL6 mouse endothelial cells - 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2012) 22: 5352-9 [PMID:22835870]
ChEMBL Inhibition of DNA-PK in C57BL6 mouse endothelial cells B 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2012) 22: 5352-5359 [PMID:22835870]

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]