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. Author manuscript; available in PMC: 2021 Aug 12.
Published in final edited form as: J Med Chem. 2020 Oct 23;63(21):12642–12665. doi: 10.1021/acs.jmedchem.0c00943

Figure 2.

Figure 2.

Antagonism of F876L-mutant AR transactivation. AR with phenylalanine 876 mutated to leucine (F876L), GRE-LUC, and CMV-renilla LUC were transfected in COS cells. Cells were treated 24 h after transfection with 0.1 nM R1881 (agonist) and a dose response of antagonists. Luciferase assay was performed 48 h after transfection. The effect of each compound was conducted in antagonistic mode (in the presence of 0.1 nM R1881). IC50 values were calculated and are provided in the figure.