Selective non-steroidal androgen receptor (AR) antagonist (IC50
values are 26 nM and 90 nM in AR binding assays and cellular assays respectively). Displays low affinity for progesterone receptor (IC50
> 10 μ
M). Active in vivo
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Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.
Li et al.