onapristone [Ligand Id: 2882] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1908373 (Onapristona, 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 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]
