Modern Lead Generation Strategies

Abstract

Lead generation (LG) plays a key role in defining the chemotype of a future candidate drug. Traditionally, lead generation has relied strongly on screening larger compound libraries such as high- or medium-throughput screening against a target of interest, followed by analysis of the singleton or cluster actives or hits, and followed by hit expansion and lead series development. In addition to the traditional compound screening, today the lead generation chemist has several powerful lead generation methods to choose from, for example, fragment-based lead generation (FBLG), rational lead design, competitive intelligence-based lead generation (CILG) and selective optimization of side activities (SOSA). The ultimate goal of every LG chemist is to deliver a choice of high quality lead series to the lead optimization colleagues in order to enable the successful delivery of a clinical candidate that can test a target hypothesis in a disease.