NU-7441 [Ligand Id: 8010] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL188678 (NU-7432, NU-7441)
  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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  • bromodomain testis associated/Bromodomain testis-specific protein in Human [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
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  • 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 delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
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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
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL Inhibition of N-terminal 6His-tagged human BRD4 bromodomain 1 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated histone H4 peptide (1 to 21 residues) containing KAc (K5/8/12/16Ac) as substrate by Alpha screen assay B 6 pIC50 1000 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
ChEMBL Inhibition of N-terminal 6His-tagged human BRDT bromodomain 1 (21 to 137 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated histone H4 peptide (1 to 21 residues) containing KAc (K5/8/12/16Ac) as substrate by Alpha screen assay B 5.46 pIC50 3500 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
ChEMBL Inhibitory activity against DNA-dependent protein kinase receptor B 9.19 pKi 0.65 nM Ki J Med Chem (2005) 48: 7829-7846 [PMID:16302822]
ChEMBL Inhibition of human DNA-PK using GST-tagged p53N66 as substrate after 1 hr by ELISA-based chemiluminiscence assay B 7.38 pIC50 42 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
ChEMBL Inhibition of DNA-PK (unknown origin) B 7.4 pIC50 40 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
ChEMBL Inhibition of DNA-PK autophosphorylation at Ser2056 residue in human CLL cells by Western blot method B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2012) 22: 5352-5359 [PMID:22835870]
ChEMBL Inhibition of DNA-PK B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2012) 57: 85-101 [PMID:23059543]
ChEMBL Inhibition of DNA-dependent protein kinase B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2010) 20: 3649-3653 [PMID:20472428]
ChEMBL Inhibition of DNA-PK B 7.55 pIC50 28 nM IC50 Bioorg Med Chem Lett (2011) 21: 966-970 [PMID:21216595]
ChEMBL Inhibitory activity against DNA-dependent protein kinase (DNA-PK) at 0.5 uM B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2004) 14: 6083-6087 [PMID:15546735]
ChEMBL Inhibitory activity against DNA-dependent protein kinase receptor B 7.7 pIC50 20 nM IC50 J Med Chem (2005) 48: 7829-7846 [PMID:16302822]
GtoPdb ELISA measuring the ability of DNA-PK (extracted from HeLa cells) to phosphorylate Ser15 of a p53 peptide - 7.85 pIC50 14 nM IC50 Bioorg Med Chem Lett (2004) 14: 6083-7 [PMID:15546735]
ChEMBL Inhibition of DNA-PK (unknown origin) B 7.85 pIC50 14 nM IC50 J Med Chem (2015) 58: 41-71 [PMID:25387153]
ChEMBL Inhibition of DNA-PK (unknown origin) B 7.85 pIC50 14 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
ChEMBL Inhibition of DNA-dependent protein kinase B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2008) 18: 4885-4890 [PMID:18678488]
ChEMBL Inhibitory activity against DNA-dependent protein kinase (DNA-PK) B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2004) 14: 6083-6087 [PMID:15546735]
ChEMBL Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells B 6.67 pEC50 212 nM EC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in cisapride treated CHO cells by Ion Works assay B 4.85 pIC50 14000 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
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 p110 alpha subunit B 5.3 pIC50 5000 nM IC50 Bioorg Med Chem Lett (2004) 14: 6083-6087 [PMID:15546735]
ChEMBL Inhibition of PI3Kalpha after 80 mins B 6.89 pIC50 130 nM IC50 Bioorg Med Chem Lett (2011) 21: 966-970 [PMID:21216595]
ChEMBL Inhibition of PI-3K alpha (unknown origin) B 6.89 pIC50 130 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
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 PI-3K beta (unknown origin) B 7.8 pIC50 16 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
ChEMBL Inhibition of PI-3K delta (unknown origin) B 7.52 pIC50 30 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
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 PI-3K gamma (unknown origin) B 6.66 pIC50 220 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
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 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
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 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
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 (unknown origin) B 5.62 pIC50 2400 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
ChEMBL Inhibition of Mammalian target of Rapamycin mTOR B 5.77 pIC50 1700 nM IC50 Bioorg Med Chem Lett (2004) 14: 6083-6087 [PMID:15546735]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]