Synthesis, Structure−Activity Relationships, and Characterization of Novel Nonsteroidal and Selective Androgen Receptor Modulators Nathalie Schlienger Birgitte W. Lund Jan Pawlas Fabrizio Badalassi Fabio Bertozzi Rasmus Lewinsky Alma Fejzic Mikkel B. Thygesen Ali Tabatabaei Stefania Risso Bradley Luis R. Gardell Fabrice Piu Roger Olsson 10.1021/jm901149c.s001 https://acs.figshare.com/articles/journal_contribution/Synthesis_Structure_Activity_Relationships_and_Characterization_of_Novel_Nonsteroidal_and_Selective_Androgen_Receptor_Modulators/2810146 Herein we describe the discovery of ACP-105 (<b>1</b>), a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone. Compound <b>1</b> was developed from a series of compounds found in a HTS screen using the receptor selection and amplification technology (R-SAT). In vivo, <b>1</b> improved anabolic parameters in a 2-week chronic study in castrated male rats. In addition to compound <b>1</b>, a number of potent antiandrogens were discovered from the same series of compounds whereof one compound, <b>13</b>, had antagonist activity at the AR T877A mutant involved in prostate cancer. 2009-11-26 00:00:00 amplification technology series HTS screen Novel Nonsteroidal Selective Androgen Receptor ModulatorsHerein agonist activity AR T 877A receptor selection prostate cancer anabolic parameters antagonist activity androgen testosterone compound SARM Compound 1 androgen receptor modulator ACP