ABSTRACT

High-throughput screening (HTS) is a large-scale process that screens hundreds of thousands to millions of compounds in order to identify biologically active compounds as candidates for further validation and confirmation. HTS started and developed as an early discovery platform in the pharmaceutical industry in the late 1980s to mid-1990s. The goal of HTS is to generate chemical structures that will lead to drug discovery through testing chemicals for their biological activity against target molecules (An and Tolliday 2009). Devlin (1997) and Hüser et al. (2006) provide more details on HTS in drug discovery. Recently, advances in HTS technologies in drug discovery have been used in other research fields. For example, approaches developed for small-molecule screening have been applied to, and improved, identification and validation of specific gene functions in RNA interference (Zhang 2011).