onapristone [Ligand Id: 2882] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1908373 (Onapristone, ZK299, ZK-299, Zk98299, Zk-98299, ZK-98299)
  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
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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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]