Figure 2.

Competitive binding assay of the 58 compounds identified through VS

A. Relative AR binding affinity of the 58 compounds (10 µM) analyzed using PolarScreen™ AR Competitor Assay using DHT as control. The numbers at X axis represent the numerical codes of the identified compounds; e.g., 10 represents HBP1-10. The AR binding affinity of DHT was set as 100%. B. Four AR favorable compounds HBP1-3, HBP1-38, HBP1-51, and HBP1-58 were evaluated under various concentrations for their precise binding affinity with Enz as control. Standard errors were derived from at least triplicate assays. C. Structures of HBP1-3, HBP1-17, HBP1-38, HBP1-51, and HBP1-58, and four known AR ligands tested in this study. These include testosterone (endogenous androgen), EM-5744 (reported AR agonist), Bic (marketed AR antagonist), and Enz (marketed AR antagonist). DHT, dihydrotestosterone; Bic, bicalutamide; Enz, enzalutamide.