title: High-throughput screening assays for the identification of chemical probes.
abstract: High-throughput screening (HTS) assays enable the testing of large numbers of chemical substances for activity in diverse areas of biology. The biological responses measured in HTS assays span isolated biochemical systems containing purified receptors or enzymes to signal transduction pathways and complex networks functioning in cellular environments. This Review addresses factors that need to be considered when implementing assays for HTS and is aimed particularly at investigators new to this field. We discuss assay design strategies, the major detection technologies and examples of HTS assays for common target classes, cellular pathways and simple cellular phenotypes. We conclude with special considerations for configuring sensitive, robust, informative and economically feasible HTS assays.
authors.affiliation: US National Institutes of Health Chemical Genomics Center, National Institutes of Health, 9800 Medical Center Drive, Bethesda, Maryland 20892-3370, USA. jinglese@mail.nih.gov
authors.forename: James
authors.initials: J
authors.lastname: Inglese
authors.forename: Ronald L
authors.initials: RL
authors.lastname: Johnson
authors.forename: Anton
authors.initials: A
authors.lastname: Simeonov
authors.forename: Menghang
authors.initials: M
authors.lastname: Xia
authors.forename: Wei
authors.initials: W
authors.lastname: Zheng
authors.forename: Christopher P
authors.initials: CP
authors.lastname: Austin
authors.forename: Douglas S
authors.initials: DS
authors.lastname: Auld
mesh_terms: D000818:Animals; D002384:Catalysis; D002626:Chemistry, Pharmaceutical / Q000295:instrumentation / Q000379:methods*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000295:instrumentation* / Q000379:methods*; D004798:Enzymes / Q000737:chemistry; D006801:Humans; D007477:Ions; D007700:Kinetics; D008954:Models, Biological; D008956:Models, Chemical; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism; D015398:Signal Transduction; D013678:Technology, Pharmaceutical / Q000295:instrumentation / Q000379:methods*; D014158:Transcription, Genetic
chemical_list: D004798:Enzymes; D007477:Ions; D043562:Receptors, G-Protein-Coupled