title: Target (In)Validation: A Critical, Sometimes Unheralded, Role of Modern Medicinal Chemistry.
abstract: Small molecule drug discovery commonly ventures into previously unknown and unexplored target space. For such programs, an important role of medicinal chemistry is to generate molecules that enable the most reliable conclusions from a preclinical target validation/invalidation study. Multiple facets of chemistry that provide the most rigorous results for such an experiment are highlighted.
authors.affiliation: AbbVie, Inc. , 1 North Waukegan Road, North Chicago, Illinois 60064, United States.
authors.forename: Ramzi F
authors.initials: RF
authors.lastname: Sweis
keywords: Target validation; biomarkers; inactive controls; proof-of-concept; target invalidation