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 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]