title: Designing in vitro assays for drug discovery: a study with the human MAP3 kinase COT.
abstract: In drug discovery research, developing a validated and robust in vitro assay is crucial for high-throughput screening and subsequent hit characterization. There are many kinase assay technologies, so an assay developer has several decisions to make prior to undertaking experiments: which assay technology should be used? What are the advantages and disadvantages of a cascade assay compared with a direct assay format? Should the substrate be a peptide or a protein? When using a protein substrate, should it be physiologically relevant? In this perspective article, these questions will be addressed using examples from a study with the human mitogen-activated protein kinase kinase kinase COT.
authors.affiliation: Department of Molecular Pharmacology, Abbott Laboratories, 100 Research Drive, Worcester, MA 01605, USA +1 508 849 2971 ; +1 508 754 7784 ; yong.jia@abbott.com.
authors.forename: Yong
authors.initials: Y
authors.lastname: Jia
authors.forename: Christopher M
authors.initials: CM
authors.lastname: Quinn
authors.forename: Robert V
authors.initials: RV
authors.lastname: Talanian