title: Overview of high-throughput screening.
abstract: High-throughput screening (HTS) is a key process used in drug discovery to identify hits from compound libraries that may become leads for medicinal chemistry optimization. This updated overview discusses the utilization of compound libraries, compounds derived from combinatorial and parallel synthesis campaigns and natural product sources; creation of mother and daughter plates; and compound storage, handling, and bar coding in HTS. The unit also presents an overview of established and emerging assay technologies (i.e., time-resolved fluorescence, fluorescence polarization, fluorescence-correlation spectroscopy, functional whole cell assays, and high-content assays) and their integration in automation hardware and IT systems. This revised unit provides updated descriptions of state-of-the-art instrumentation and technologies in this rapidly changing environment. The section on assay methodologies now also covers enzyme complementation assays and methods for high-throughput screening of ion channel activities. Finally, a section on criteria for assay robustness is included discussing the Z'-factor, which is now a widely accepted criterion for evaluation and validation of high throughput screening assays.
authors.affiliation: Experimental Therapeutics Centre, Agency for Science, Technology, and Research (A*STAR), Singapore.
authors.forename: Michael
authors.initials: M
authors.lastname: Entzeroth
authors.forename: Horst
authors.initials: H
authors.lastname: Flotow
authors.forename: Peter
authors.initials: P
authors.lastname: Condron
mesh_terms: D001688:Biological Products / Q000737:chemistry; D055808:Drug Discovery / Q000379:methods*; D004356:Drug Storage; D057075:Enzyme Assays / Q000379:methods; D005434:Flow Cytometry; D017930:Genes, Reporter; D057166:High-Throughput Screening Assays / Q000295:instrumentation / Q000379:methods*; D006801:Humans; D007473:Ion Channels; D008490:Medical Informatics; D011786:Quality Control; D011868:Radioisotopes; D011955:Receptors, Drug / Q000032:analysis; D012371:Robotics
chemical_list: D001688:Biological Products; D007473:Ion Channels; D011868:Radioisotopes; D011955:Receptors, Drug