High‐Throughput Screening for Lead Discovery

Abstract High‐throughput screening is now an integral part of the early drug discovery process. This high capacity technology addresses the need to screen large numbers of biological targets against large numbers of compounds to find starting points for medicinal chemistry programs. Over the last decade, technological innovation, integrated automation, and novel biological reagents have been combined to create high‐throughput screening systems. This technology connects disease targets of interest with large arrays of test compounds to enable the discovery of potential new drug candidates. The process of bioassay design, screen construction, hit identification, and compound profiling is the basic backbone of the lead discovery process. It is underpinned by a set of large scale, novel technologies that provide a seamless, highly efficient discovery process.