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ChEMBL ligand: CHEMBL188678 (NU-7432, NU-7441) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]