AZ20 [Ligand Id: 8477] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL2325697 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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-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 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 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] |
| 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 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]
