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Synonyms: AGN-193491 | BMS189532 | compound 2 [PMID: 24040487]
Compound class: Synthetic organic
Comment: BMS-189532 is a retinoic acid receptor-α (RAR-α) selective antagonist, that was designed for activity as a non-hormonal male contraceptive [1-2]. Antagonising RAR-α is predicted to disrupt spermatogenesis. Despite potent antagonism of RAR-α in vitro, the compound was ineffective in vivo by oral administration. A modified chemotype with the expected in vivo effect on sperm development is represented by YCT529.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Chung SS, Cuellar RA, Wang X, Reczek PR, Georg GI, Wolgemuth DJ. (2013)
Pharmacological activity of retinoic acid receptor alpha-selective antagonists in vitro and in vivo..
ACS Med Chem Lett, 4 (5): 446-450. [PMID:24040487]
2. Noman MAA, Kyzer JL, Chung SSW, Wolgemuth DJ, Georg GI. (2020)
Retinoic acid receptor antagonists for male contraception: current status†.
Biol Reprod, 103 (2): 390-399. [PMID:32671394]
3. Teng M, Duong TT, Johnson AT, Klein ES, Wang L, Khalifa B, Chandraratna RA. (1997)
Identification of highly potent retinoic acid receptor alpha-selective antagonists.
J Med Chem, 40 (16): 2445-51. [PMID:9258350]