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ChEMBL ligand: CHEMBL267431 (Asoprisnil, Asoprisnilo, 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 |
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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 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]