In present-day drug discovery, bioactive molecules with a sought-after physiological effect are identified by screening large libraries of drug candidates for a quantifiable effect on a biological target. Because of the large number of candidate molecules involved, screening assays with high compound throughput have been developed that yield high-quality results in a short time. Backed by leading authorities, this is a professional guide to successful compound screening in pharmaceutical research and chemical biology, including the chemoinformatic tools needed for correct data evaluation. Chapter authors from leading pharmaceutical companies as well as from Harvard University discuss such factors as chemical genetics, binding, cell-based and biochemical assays, the efficient use of compound libraries and data mining using cell-based assay results. For both academics and professionals in the pharmaceutical and biotech industries working on small molecule screening.