onapristone [Ligand Id: 2882] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1908373 (Onapristone, ZK-299, ZK299, Zk-98299, Zk98299, ZK-98299) |
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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 for human Androgen receptor | B | 7 | pKi | >100 | nM | Ki | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Cross-reactivity as binding to human androgen receptor (hAR) | F | 6.57 | pIC50 | 269 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 415-418 [PMID:10743938] |
| ChEMBL | Inhibitory activity against human Androgen receptor | B | 6.57 | pIC50 | 269 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Inhibition of antagonist activity towards Androgen receptor | F | 6.57 | pIC50 | 269 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
| ChEMBL | Binding affinity was determined for human glucocorticoid receptor(hGR). | B | 7.38 | pKi | 41.8 | nM | Ki | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Cross-reactivity as binding to human glucocorticoid receptor (hGR) | F | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 415-418 [PMID:10743938] |
| ChEMBL | Inhibitory activity against human glucocorticoid receptor (hGR) | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Inhibition of antagonist activity towards glucocorticoid receptor | F | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| GtoPdb | - | - | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2075-8 [PMID:12781198] |
| Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| ChEMBL | Cross-reactivity as binding to human mineralocorticoid receptor (hMR) | F | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 415-418 [PMID:10743938] |
| ChEMBL | Inhibitory activity against human mineralocorticoid receptor (hMR) | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Inhibition of antagonist activity towards mineralocorticoid receptor (hMR) | F | 6.33 | pIC50 | 470 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| GtoPdb | - | - | 6.33 | pIC50 | 470 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2075-8 [PMID:12781198] |
| Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
| GtoPdb | - | - | 7.74 | pKi | 18 | nM | Ki | J Med Chem (1996) 39: 1778-89 [PMID:8627601] |
| ChEMBL | Binding affinity against human progesterone receptor (hPR) in a competitive binding assay | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 415-418 [PMID:10743938] |
| ChEMBL | Binding affinity determined for human Progesterone receptor A isoform | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Binding affinity was determined against hPR-A (human progesterone receptor) using progesterone radioligand in competitive binding assay | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3365-3370 [PMID:9873735] |
| ChEMBL | Binding affinity at human progesterone receptor. | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| ChEMBL | Binding affinity against Baculovirus-Expressed hPR-A | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (1998) 41: 3461-3466 [PMID:9719599] |
| ChEMBL | Antagonist activity against human progesterone receptor (hPR) in T47D human breast cancer cell line | F | 8.48 | pIC50 | 3.3 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 415-418 [PMID:10743938] |
| ChEMBL | Inhibition of human progesterone receptor activation in T47D human breast cancer cell. | B | 8.48 | pIC50 | 3.3 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| ChEMBL | Antagonistic potency to the human progesterone receptor measured in the T-47D alkaline phosphatase assay | F | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Antagonist activity against human progesterone receptor (hPR) using cotransfection assay in CV-1 cells | F | 8.66 | pIC50 | 2.2 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 415-418 [PMID:10743938] |
| ChEMBL | In vitro antagonist activity against human progesterone receptor isoform B(hPR-B) in mammalian(CV-1) cells | F | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (1998) 41: 3461-3466 [PMID:9719599] |
| ChEMBL | Concentration required to give half-maximal inhibition against human Progesterone receptor B isoform in co-transfected CV-1 cell lines. | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Agonist activity was determined against hPR (human progesterone receptor) compared to that of progesterone (100%) | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 3365-3370 [PMID:9873735] |
| ChEMBL | Antagonistic activity at human progesterone receptor in CV-1 cells. | F | 8.66 | pEC50 | 2.2 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| ChEMBL | Antagonist activity against hPR (human progesterone receptor) compared to that of progesterone (100%) | F | 8.8 | pEC50 | 1.6 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 3365-3370 [PMID:9873735] |
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]
