Targeting the Binding Function 3 (BF3) Site of the Androgen Receptor Through Virtual Screening. 2. Development of 2-((2-phenoxyethyl) thio)-1H-benzimidazole Derivatives

Munuganti, R S, et al., 56(3), 1136-48, J Med Chem, 2013

The authors develop structure-activity relationships that allowed the design of small molecule inhibitors of the human androgen receptor (AR) binding function 3 (BF3). The Octet RED system was used to quantify interactions between the small molecules and the AR. Purified biotinylated AR LBD was loaded onto Super Streptavidin biosensors and BLI dose-response curves were generated.

Read More