NU-7441 [Ligand Id: 8010] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL188678 (NU-7432) |
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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 catalytic subunit 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 human HeLa cell nuclear extract purified DNA-PK using p53 peptide as substrate by ELISA | B | 7.85 | pIC50 | 14 | nM | IC50 | Cancer Res (2006) 66: 5354-5362 [PMID:16707462] |
| 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] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 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/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 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/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 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/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 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 checkpoint kinase/Serine/threonine-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] |
| Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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] |
ChEMBL data shown on this page come from version 36:
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]
