N-desmethyl Enzalutamide 是 Enzalutamide 的活性代谢物，其主要和次要药效学作用与 Enzalutamide 本身相似，浓度与 Enzalutamide 在血浆中的浓度相当。

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.

ACP-105 is a potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone.

Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s = 25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50 = 1 μM).

Monobutyl phtalate is a metabolite of di(n-butyl)phthalate. It affects the expressions of EMT-related proteins and enhances the migration and invasion of MLTC-1 cells.

Hydroxyflutamide is a derivative of the synthetic steroid ethisterone, that suppresses the production of gonadotrophins, and has some weak androgenic effects.

ARV-110是一种首创的雄激素受体（AR）降解PROTAC，专为治疗转移性去势抵抗前列腺癌而设计。ARV-110展现了在应对难治性前列腺癌方面的显著潜力。

3,3'-Diindolylmethane is an AR structurally similar androgen receptor antagonist.

ARCC-4 是一种基于 PROTAC 技术的纳摩尔雄激素受体 (AR) 降解剂，D50 值为 5 nM。ARCC-4 是一种基于恩杂鲁胺的 von Hippel-Lindau (VHL) 招募的 AR PROTAC，能够有效降解与抗雄激素研究相关的 AR 突变体。

ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.

ARN-509 can compeitively and selectively inhibit androgen receptor with IC50 value of 16 nM.

Cortexolone 17 alpha-propionate is a topical and peripherally selective androgen antagonist, which is used in treatment of acne and androgenic alopecia.