asoprisnil [Ligand Id: 2883] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL267431 (Asoprisnil, BAY86-5294, J-867, J867) |
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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 | Antagonist activity at androgen receptor by cellular reporter gene assay | F | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7119-7122 [PMID:23079530] |
| ChEMBL | Antagonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells in presence of 5-alpha-dihydrotestosterone by Gal4 hybrid assay | B | 8.21 | pIC50 | 6.1 | nM | IC50 | J Med Chem (2008) 51: 1861-1873 [PMID:18318463] |
| Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
| ChEMBL | Antagonist activity at estrogen receptor by cellular reporter gene assay | F | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7119-7122 [PMID:23079530] |
| ChEMBL | Antagonist activity at human ER ligand binding domain expressed in african green monkey COS7 cells in presence of 17-beta-estradiol by Gal4 hybrid assay | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (2008) 51: 1861-1873 [PMID:18318463] |
| Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
| ChEMBL | Antagonist activity at glucocorticoid receptor by cellular reporter gene assay | F | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7119-7122 [PMID:23079530] |
| ChEMBL | Antagonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells in presence of Dexamethasone by Gal4 hybrid assay | B | 7.07 | pIC50 | 85 | nM | IC50 | J Med Chem (2008) 51: 1861-1873 [PMID:18318463] |
| Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| ChEMBL | Antagonist activity at human MR ligand binding domain expressed in african green monkey COS7 cells in presence of aldosterone by Gal4 hybrid assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2008) 51: 1861-1873 [PMID:18318463] |
| ChEMBL | Antagonist activity at mineralocorticoid receptor by cellular reporter gene assay | F | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7119-7122 [PMID:23079530] |
| Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | Biochem Pharmacol (2011) 82: 1709-19 [PMID:21854761] |
| ChEMBL | Antagonist activity at progesterone receptor by cellular reporter gene assay | F | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7119-7122 [PMID:23079530] |
| ChEMBL | Antagonist activity against progesterone receptor in human T47D cells by alkaline phosphatase assay | F | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7119-7122 [PMID:23079530] |
| ChEMBL | Antagonist activity at human PRB expressed in CHO cells assessed as inhibition of Org 2058 induced-transactivation | F | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem (2008) 16: 2753-2763 [PMID:18243712] |
| ChEMBL | Agonist activity at human PRB expressed in CHO cells | F | 7 | pEC50 | >100 | nM | EC50 | Bioorg Med Chem (2008) 16: 2753-2763 [PMID:18243712] |
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]
