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. Author manuscript; available in PMC: 2023 Sep 9.
Published in final edited form as: J Med Chem. 2023 Feb 24;66(5):3372–3392. doi: 10.1021/acs.jmedchem.2c01858

Figure 5.

Figure 5.

Class I~III antagonism of F876L mutant AR transactivation. (A) R1881. (B) Enzalutamide (2) and UT-155 (8). (C) Class I: carbazole and benzotriazole in B-ring). (D) Class II (benzimidazole and indazole in B-ring). (E) Class III (3-substituted indazoles in B-ring): AR with F876L (phenylalanine 876 mutated to leucine), GRE-LUC, and CMV-renilla LUC transfected in COS cells. Cells treated 24 h after transfection with 0.1 nM R1881 (agonist) and a dose response of antagonists. Luciferase assay performed 48 h after transfection. The effect of each compound conducted in antagonistic mode (in the presence of 0.1 nM R1881). IC50 values of the Class I~III calculated and provided in the figure.