ABSTRACT
Drug discovery is a very complex and highly multidisciplinary process that requires constant reevaluation of best practices in order to improve the rather low success rate of the overall discovery workow. Every decade or so a revolutionary new principle is introduced that slowly begins to transform key steps of the well-established drug development process, which includes target identication and validation, lead identication, lead optimization, and preclinical and clinical development. These true game-changers that have signicantly enhanced the arsenal of tools available to biologists and medicinal chemists include computer-aided drug discovery, parallel and combinatorial chemistry, biologics, high-throughput screening (HTS), and in the early twenty-rst century fragment-based drug discovery (FBDD).
