AZ20 [Ligand Id: 8477] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2325697 |
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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-mediated autophosphorylation at serine 2056 in human HT29 cells | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 2125-2138 [PMID:23394205] |
| ChEMBL | Inhibition of DNA-PK phosphorylation at Ser2056 residue in human HT-29 cells using ionizing radiation | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2018) 61: 9889-9907 [PMID:30346772] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG by whole-cell electrophysiology assay | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (2013) 56: 2125-2138 [PMID:23394205] |
| ChEMBL | Inhibition of human ERG by whole cell electrophysiology analysis | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (2018) 61: 9889-9907 [PMID:30346772] |
| 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 PI3Kalpha-mediated AKT phosphorylation at threonine 308 in human BT474 cells | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 2125-2138 [PMID:23394205] |
| ChEMBL | Inhibition of PI3Kalpha in human BT-474 cells assessed as decrease in AKT phosphorylation at T308 residue | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2018) 61: 9889-9907 [PMID:30346772] |
| ChEMBL | Inhibition of PI3Kalpha (unknown origin) | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (2013) 56: 2125-2138 [PMID:23394205] |
| ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315] | ||||||||
| ChEMBL | Inhibition of ATM-mediated autophosphorylation at serine 1981 in human HT29 cells | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 2125-2138 [PMID:23394205] |
| ChEMBL | Inhibition of ATM phosphorylation at Ser1981 residue in human HT-29 cells using ionizing radiation | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2018) 61: 9889-9907 [PMID:30346772] |
| ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535] | ||||||||
| ChEMBL | Inhibition of ATR in human HT29 cells after 60 mins by Hoechst 33258 staining-based assay | B | 7.21 | pIC50 | 61 | nM | IC50 | J Med Chem (2018) 61: 9889-9907 [PMID:30346772] |
| ChEMBL | Inhibition of ATR (unknown origin) | B | 7.21 | pIC50 | 61 | nM | IC50 | Bioorg Med Chem (2022) 56: 116614-116614 [PMID:35033884] |
| ChEMBL | Inhibition of ATR-mediated CHK1 phosphorylation at serine 345 in human HT29 cells after 1 hr in presence of 4-nitroquinoline 1-oxide | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2013) 56: 2125-2138 [PMID:23394205] |
| GtoPdb | Inhibition of ATR immunoprecipitated from HeLa cells. | - | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2013) 56: 2125-38 [PMID:23394205] |
| ChEMBL | Inhibition of ATR (unknown origin) using peptide as substrate preincubated for 10 mins followed by substrate addition by microplate reader analysis | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2023) 246: 114945-114945 [PMID:36462444] |
| ChEMBL | Inhibition of ATR in human HeLa cell nuclear extracts using glutathione S-transferase-p53N66 and ATP as substrate incubated for 10 mins prior to ATP addition measured after 1 hr by ELISA | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2013) 56: 2125-2138 [PMID:23394205] |
| ChEMBL | Inhibition of ATR in human HeLa cell nuclear extract using GST-fused p53N66 as substrate preincubated for 10 mins followed by ATP addition and measured after 1 hr by ELISA | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2018) 61: 9889-9907 [PMID:30346772] |
| ChEMBL | Inhibition of ATR (unknown origin) | B | 8.39 | pIC50 | 4.1 | nM | IC50 | Eur J Med Chem (2023) 255: 115370-115370 [PMID:37130473] |
| ChEMBL | Inhibition of 5'-TAMRA-labeled tracer 3',6'-bis(dimethylamino)-N-(4-{[2(1H-indol-4-yl)-6-(morpholin-4-yl)-pyrimidin-4-yl]amino}butyl)-3-oxo-3H-spiro[2-benzofuran-1,9'-xanthene]-5-carboxamide binding to recombinant human full-length N-terminal Flag-tagged ATR expressed in HEK293-6E cells co-expressing human full-length STREP-tagged ATRIP preincubated for 10 mins followed by tracer addition and measured after 30 mins by TR-FRET assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2020) 63: 7293-7325 [PMID:32502336] |
| 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-mediated AKT phosphorylation at serine 473 in human MDA-MB-468 cells | B | 5.62 | pIC50 | 2400 | nM | IC50 | J Med Chem (2013) 56: 2125-2138 [PMID:23394205] |
| ChEMBL | Inhibition of mTOR in human MDA-MB-468 cells assessed as decrease in AKT phosphorylation at S473 residue | B | 5.62 | pIC50 | 2400 | nM | IC50 | J Med Chem (2018) 61: 9889-9907 [PMID:30346772] |
| ChEMBL | Inhibition of mTOR in human MDA-MB-468 cells assessed as decrease in 70S6K S235/236 phosphorylation | B | 6.14 | pIC50 | 720 | nM | IC50 | J Med Chem (2018) 61: 9889-9907 [PMID:30346772] |
| ChEMBL | Inhibition of recombinant mTOR (unknown origin) | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2013) 56: 2125-2138 [PMID:23394205] |
| ChEMBL | Inhibition of mTOR (unknown origin) | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2018) 61: 9889-9907 [PMID:30346772] |
| ChEMBL | Inhibition of mTOR (unknown origin) using peptide as substrate preincubated for 10 mins followed by substrate addition by microplate reader analysis | B | 7.42 | pIC50 | 38 | nM | IC50 | Eur J Med Chem (2023) 246: 114945-114945 [PMID:36462444] |
| TATA-box binding protein associated factor 1/Transcription initiation factor TFIID subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3217390] [GtoPdb: 2231] [UniProtKB: P21675] | ||||||||
| ChEMBL | Binding affinity to human TAF1 BD 2 (1501 to 1635 residues) transfected in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetric analysis | B | 4.6 | pKd | >25000 | nM | Kd | J Med Chem (2022) 65: 4182-4200 [PMID:35191694] |
| ChEMBL | Binding affinity to human TAF1 tandem bromodomain (1373 to 1499 residues) transfected in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetric analysis | B | 4.6 | pKd | >25000 | nM | Kd | J Med Chem (2022) 65: 4182-4200 [PMID:35191694] |
| ChEMBL | Binding affinity to human TAF1 BD 2 (1501 to 1635 residues) transfected in Escherichia coli BL21 (DE3) by Alphascreen assay | B | 4.6 | pKd | >25000 | nM | Kd | J Med Chem (2022) 65: 4182-4200 [PMID:35191694] |
| ChEMBL | Binding affinity to human TAF1 BD 2 (1501 to 1635 residues) transfected in Escherichia coli BL21 (DE3) assessed as dissociation constant by q-PCR based bromoscan assay | B | 5.21 | pKd | 6167 | nM | Kd | J Med Chem (2022) 65: 4182-4200 [PMID:35191694] |
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]
