drospirenone [Ligand Id: 2874] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1509 (Angeliq, Drospirenone, NSC-760103, Slynd, ZK 30595, ZK-30595)
  • 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 Assay: The test was carried out as in 1, with the following modifications: cytosol from androgen receptor-expressing insect cells (Hi5) was used, and the reference substance was 3H-testosterone.The results of the binding tests and the ratio of the competition factors CF(PR) and CR(MR) are shown in Table 1, which for comparison also shows receptor binding values of drospirenone as reference substance A. B 6.2 pIC50 630 nM IC50 US-8987239-B2. 19-nor-steroid derivatives with a 15α,16α-methylene group and a saturated 17,17-spirolactone ring, use thereof, and medicaments containing said derivatives (2015)
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL Binding Assay: Using cytosol from progesterone receptor-expressing insect cells (Hi5), competitive binding to the progesterone receptor was determined from the ability to displace 3H-progesterone as reference substance from the receptor. If a compound has an affinity corresponding to progesterone, this corresponds to a competition factor (CF) of 1. CF values greater than 1 are characterized by a lower affinity for the progesterone receptor, and CF values of less than 1 are characterized by higher affinity. B 7.36 pIC50 43.3 nM IC50 US-8987239-B2. 19-nor-steroid derivatives with a 15α,16α-methylene group and a saturated 17,17-spirolactone ring, use thereof, and medicaments containing said derivatives (2015)

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]