NU-7026 [Ligand Id: 5959] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL104468 (LY-293646)
  • 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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  • phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p85-alpha subunit in Human [ChEMBL: CHEMBL2506] [GtoPdb: 2503] [UniProtKB: P27986]
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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 DNA-PK B 6.52 pIC50 300 nM IC50 Bioorg. Med. Chem. (2011) 19: 3983-3994 [PMID:21664823]
ChEMBL Inhibition of DNA dependent protein kinase isolated from HeLa cells B 6.64 pIC50 230 nM IC50 J. Med. Chem. (2005) 48: 569-585 [PMID:15658870]
ChEMBL Inhibitory activity against DNA-dependent protein kinase (DNA-PK) B 6.64 pIC50 230 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6083-6087 [PMID:15546735]
ChEMBL Inhibitory activity against DNA-dependent protein kinase receptor B 6.64 pIC50 230 nM IC50 J. Med. Chem. (2005) 48: 7829-7846 [PMID:16302822]
ChEMBL Inhibition of DNA-PK B 6.64 pIC50 230 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of DNAPK after 2 hrs by radiometric phosphate incorporation assay B 6.64 pIC50 230 nM IC50 J. Med. Chem. (2011) 54: 2320-2330 [PMID:21413798]
ChEMBL In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells. B 6.64 pIC50 230 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 3083-3086 [PMID:12941339]
ChEMBL Inhibition of DNA-PK purified from human HeLa nuclear extracts B 6.64 pIC50 230 nM IC50 J. Med. Chem. (2015) 58: 41-71 [PMID:25387153]
GtoPdb - - 6.64 pIC50 230 nM IC50 Bioorg Med Chem Lett (2003) 13: 3083-6 [PMID:12941339]
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 Phosphatidylinositol 3-kinase B 4.89 pIC50 13000 nM IC50 J. Med. Chem. (2005) 48: 569-585 [PMID:15658870]
ChEMBL Inhibition of Phosphatidylinositol 3-kinase p110 alpha subunit B 4.89 pIC50 13000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6083-6087 [PMID:15546735]
ChEMBL Inhibition of PI3K p110alpha (unknown origin) B 4.89 pIC50 13000 nM IC50 J. Med. Chem. (2015) 58: 41-71 [PMID:25387153]
phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p85-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2506] [GtoPdb: 2503] [UniProtKB: P27986]
ChEMBL Inhibition of PI3K B 4.89 pIC50 13000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
ChEMBL Inhibition of ATM kinase using rabbit polyclonal antisera; No inhibition observed at 100 uM B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2005) 48: 569-585 [PMID:15658870]
ChEMBL Inhibition of Mutated in ataxia telangiectasia protein ATM kinase B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6083-6087 [PMID:15546735]
ChEMBL Inhibition of ATM B 4 pIC50 >100000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of full length recombinant ATM after 24 hrs by radiometric phosphate incorporation assay B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2011) 54: 2320-2330 [PMID:21413798]
ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
ChEMBL Inhibition of ATR kinase using rabbit polyclonal antisera; No inhibition observed at 100 uM B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2005) 48: 569-585 [PMID:15658870]
ChEMBL Inhibition of Ataxia telangiectasia related protein ATR kinase B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6083-6087 [PMID:15546735]
ChEMBL Inhibition of ATR B 4 pIC50 >100000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
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 protein isolated from HeLa cells B 5.19 pIC50 6400 nM IC50 J. Med. Chem. (2005) 48: 569-585 [PMID:15658870]
ChEMBL Inhibition of Mammalian target of Rapamycin mTOR B 5.19 pIC50 6400 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 6083-6087 [PMID:15546735]
ChEMBL Inhibition of mTOR by radiometric phosphate incorporation assay B 5.19 pIC50 6400 nM IC50 J. Med. Chem. (2011) 54: 2320-2330 [PMID:21413798]

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]