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Biography

Benjamin PFauber is a medicinal chemist at Genentech in South San Francisco, California.He earned his BSc from Colorado State University and PhD from the University of Texas at Austin.Prior to joining Genentech, he was employed by AstraZeneca and Array BioPharma as a medicinal chemist working in the areas of inflammatory disease and oncology.

Abstract

Screening a nuclear receptor compound subset in a RORc biochemical binding assay revealed a benzylic tertiary sulfonamide hit. Using structure-based drug design principles, we created compounds with improved RORc biochemical inverse agonist activity and cellular potencies (<100 nm).These improved compounds also possessed appreciable selectivity for RORc over other nuclear receptors (>100-fold) and favorable physiochemical properties.