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 34:

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]