A review of high-throughput screening approaches for drug discovery

proach to drug discovery that has gained widespread popularity over the last three or four years. HTS is the process of assaying a larg e number of potential effectors of biological activity against targets (a biological event). The methods of HTS are applied to the screening of combinatorial chemistry, genomics, protein, and peptide libraries. The goal of HTS is to accelerate drug discovery by screening large libraries often composed of hundreds of thousands of compounds (drug candidates) at a rate that may exceed 20,000 compounds per week. This paper will focus on assay adaptations, robotic equipment, and implementation strategies that allow HTS programs to be successful. Ultrahighthroughput screening (UHTS) issues (testing of 100,000 compounds/day) will also be discussed.