CP466722 [Ligand Id: 9359] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2143829
  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
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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 (unknown origin) using p53-based peptide substrate preincubated for 5 min prior to ATP addition B 6.06 pIC50 879 nM IC50 J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
ChEMBL Inhibition of human recombinant PI3Kalpha using PIP2/ATP as substrate incubated for 20 mins followed by substrate addition by Kinase Glo reagent based luminescence assay B 5.83 pIC50 1490 nM IC50 J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
ChEMBL Inhibition of human recombinant PI3Kbeta using PIP2/ATP as substrate incubated for 20 mins followed by substrate addition by Kinase Glo reagent based luminescence assay B 5.26 pIC50 5440 nM IC50 J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
ChEMBL Inhibition of human recombinant PI3Kgamma using PIP2/ATP as substrate incubated for 20 mins followed by substrate addition by Kinase Glo reagent based luminescence assay B 6 pIC50 >1000 nM IC50 J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
ChEMBL Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based fluorescence plate reader analysis B 5.47 pIC50 3420 nM IC50 J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
ChEMBL Inhibition of ATM kinase in human MCF7 cells after 1 hr by immunofluorescence assay B 6.4 pIC50 400 nM IC50 J. Med. Chem. (2016) 59: 559-577 [PMID:26632965]
ChEMBL Inhibition of ATM (unknown origin) using p53 as substrate incubated for 30 mins followed by substrate addition measured after 2 hrs in presence of ATP by HTRF method B 7.68 pIC50 21 nM IC50 J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
ChEMBL Inhibition of flag-tagged ATM (unknown origin) using p53 as substrate by ELISA B 7.7 pIC50 20 nM IC50 J. Med. Chem. (2016) 59: 559-577 [PMID:26632965]
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 HT-29 cells assessed as reduction in Chk1 phosphorylation at Ser-345 residue after 60 mins in presence of 4-nitroquinoline-1-oxide by Hoechst 33258 staining based plate reader analysis B 4.52 pIC50 >30000 nM IC50 J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
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 C-terminal FLAG-tagged recombinant mTOR (1362 to 2549 residues) (unknown origin) using Biotin-Ahx-Lys-Lys-Ala-Asn-Gln-Val-Phe-Leu-Gly-Phe-Thr-Tyr-Val-Ala-Pro-Ser-Val-Leu-Glu-Ser-Val-Lys-Glu-NH2 as substrate after 90 mins by AlphaScreen assay B 5.34 pIC50 4590 nM IC50 J Med Chem (2016) 59: 6281-6292 [PMID:27259031]

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]