AZD2906 [Ligand Id: 11780] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3937635 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
| ChEMBL | Binding affinity to AR (unknown origin) by FP assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243] |
| Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
| ChEMBL | Binding affinity to ERalpha (unknown origin) by FP assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243] |
| Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] | ||||||||
| ChEMBL | Binding affinity to ERbeta (unknown origin) by FP assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243] |
| Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
| ChEMBL | Transrepression of GR in human whole blood assessed as inhibition of LPS-induced TNF-alpha release preincubated for 45 mins followed by LPS addition after 18 hrs by AlphaLISA method | B | 7.34 | pIC50 | 46 | nM | IC50 | J Med Chem (2018) 61: 1785-1799 [PMID:29424542] |
| ChEMBL | Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assay | B | 8.2 | pIC50 | 6.3 | nM | IC50 | J Med Chem (2018) 61: 1785-1799 [PMID:29424542] |
| ChEMBL | Binding affinity to GR (unknown origin) by FP assay | B | 8.55 | pIC50 | 2.8 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243] |
| ChEMBL | Agonist activity at glucocorticoid receptor in human ChaGoK1 cells assessed as inhibition of AP1-mediated transcriptional activity by measuring reduction in PMA-stimulated TRE-LacZ activity after 24 hrs in presence of MUG by fluorometric assay | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243] |
| ChEMBL | Transrepression activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of PMA-stimulated gene expression incubated for 24 hrs by beta-galactosidase reporter gene assay | B | 9.62 | pIC50 | 0.24 | nM | IC50 | J Med Chem (2018) 61: 1785-1799 [PMID:29424542] |
| ChEMBL | Transactivation activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells incubated for 24 hrs by beta-galactosidase reporter gene assay | B | 8.89 | pEC50 | 1.3 | nM | EC50 | J Med Chem (2018) 61: 1785-1799 [PMID:29424542] |
| GtoPdb | Measuring hGR-mediated transactivation in ChaGoK1 cells | - | 8.89 | pEC50 | 1.3 | nM | EC50 | J Med Chem (2018) 61: 1785-1799 [PMID:29424542] |
| Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| ChEMBL | Displacement of 3H-aldosterone from MR (unknown origin) ligand binding domain by SPA assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243] |
| Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
| ChEMBL | Binding affinity to PR (unknown origin) by FP assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243] |
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]
