KU-55933 [Ligand Id: 5928] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL222102 (KU-55933)
  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • ATM serine/threonine kinase/Serine-protein kinase ATM in Human [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
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  • ATR serine/threonine kinase/Serine-protein kinase ATR in Human [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
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  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
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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 DNAPK after 2 hrs by radiometric phosphate incorporation assay B 5.6 pIC50 2500 nM IC50 J. Med. Chem. (2011) 54: 2320-2330 [PMID:21413798]
ChEMBL Inhibition of DNA-PK in HeLa cell nuclear extracts B 5.74 pIC50 1800 nM IC50 J. Med. Chem. (2007) 50: 1958-1972 [PMID:17371003]
ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
ChEMBL Inhibition of ATM B 8.66 pKi 2.2 nM Ki Chem. Biol. (2005) 12: 621-637 [PMID:15975507]
GtoPdb - - 8.66 pKi 2.2 nM Ki Cancer Res. (2004) 64: 9152-9 [PMID:15604286]
ChEMBL Inhibition of ATM kinase in human MCF7 cells after 1 hr by immunofluorescence assay B 6.52 pIC50 300 nM IC50 J. Med. Chem. (2016) 59: 559-577 [PMID:26632965]
ChEMBL Inhibition of ATM in human U2OS cells assessed as inhibition of p53 phosphorylation at Ser15 residue B 6.6 pIC50 250 nM IC50 J. Med. Chem. (2016) 59: 559-577 [PMID:26632965]
ChEMBL Inhibition of ATM isolated from human HeLa cell extract using glutathione S-transferase-p53N66 as substrate by ELISA B 7.85 pIC50 14 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 5352-5359 [PMID:22835870]
ChEMBL Inhibition of ATM kinase B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2007) 50: 1958-1972 [PMID:17371003]
ChEMBL Inhibition of full length recombinant ATM after 24 hrs by radiometric phosphate incorporation assay B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2011) 54: 2320-2330 [PMID:21413798]
ChEMBL Inhibition of human ATM using p53 as substrate preincubated for 10 mins by ELISA B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2016) 59: 559-577 [PMID:26632965]
GtoPdb - - 7.89 pIC50 13 nM IC50 Cancer Res. (2004) 64: 9152-9 [PMID:15604286]
ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
ChEMBL Inhibition of full length recombinant ATR after 24 hrs by radiometric phosphate incorporation assay B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2011) 54: 2320-2330 [PMID:21413798]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
ChEMBL Inhibition of mTOR by radiometric phosphate incorporation assay B 5.03 pIC50 9300 nM IC50 J. Med. Chem. (2011) 54: 2320-2330 [PMID:21413798]

ChEMBL data shown on this page come from version 27:

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