High throughput screening (HTS) refers to the scientific method of rapid detection of thousands of biological samples or compounds by the manual operation or fully automated equipment. HTS assays have a variety of strategies, including the measurement of catalytic activity of enzymes and the identification of compounds, biomolecules, and phenotype of cells. The increase in various libraries and the miniaturization of high-sensitivity assays drive the parallel processing concept that is practiced in the 96-, 384- or 1,536-microwell plate formats.

HTS is widely used in drug discovery to quickly screen out candidates that specifically target selected enzymes or proteins from a large number of compounds. When used in combination with different types of libraries, the potential for HTS in drug discovery is enormous.