KU-60019 [Ligand Id: 8041] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2140173
  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
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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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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 isolated from human HeLa cells assessed as reduction in p53 Ser15 phosphorylation by HTRF assay B 7.11 pIC50 77 nM IC50 J Med Chem (2019) 62: 2988-3008 [PMID:30840447]
phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
ChEMBL Binding affinity to human Vps34 expressed in mammalian expression system B 8.77 pKd 1.7 nM Kd J Med Chem (2019) 62: 2988-3008 [PMID:30840447]
ChEMBL Inhibition of recombinant full-length human VPS34 incubated for 60 mins by ADP-Glo kinase assay B 7.77 pIC50 17 nM IC50 J Med Chem (2019) 62: 2988-3008 [PMID:30840447]
ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
ChEMBL Inhibition of ATM in human MCF7 cells assessed as reduction in etoposide-stimulated KAP1 phosphorylation incubated for 1 hr by ICW assay B 6.59 pIC50 260 nM IC50 J Med Chem (2019) 62: 2988-3008 [PMID:30840447]
ChEMBL Inhibition of recombinant full-length human FLAG-tagged ATM assessed as reduction in p53 S15 phosphorylation incubated for 30 mins by ELISA B 7.7 pIC50 20 nM IC50 J Med Chem (2019) 62: 2988-3008 [PMID:30840447]
GtoPdb - - 8.2 pIC50 6.3 nM IC50 Mol Cancer Ther (2009) 8: 2894-902 [PMID:19808981]
ChEMBL Inhibition of ATM kinase in human glioma cells B 8.22 pIC50 6 nM IC50 J. Med. Chem. (2015) 58: 41-71 [PMID:25387153]
ChEMBL Inhibition of ATM (unknown origin) by biochemical assay B 8.22 pIC50 6 nM IC50 J Med Chem (2019) 62: 2988-3008 [PMID:30840447]
ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
ChEMBL Inhibition of ATR in human HeLa cells incubated for 4 hrs B 4.68 pIC50 21000 nM IC50 J Med Chem (2019) 62: 2988-3008 [PMID:30840447]

ChEMBL data shown on this page come from version 28:

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]