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 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]
