title: Target engagement in lead generation.
abstract: The pharmaceutical industry is currently facing multiple challenges, in particular the low number of new drug approvals in spite of the high level of R&D investment. In order to improve target selection and assess properly the clinical hypothesis, it is important to start building an integrated drug discovery approach during Lead Generation. This should include special emphasis on evaluating target engagement in the target tissue and linking preclinical to clinical readouts. In this review, we would like to illustrate several strategies and technologies for assessing target engagement and the value of its application to medicinal chemistry efforts.
authors: Discovery Chemistry Research and Technologies, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
authors: Timothy B
authors: TB
authors: Durham
authors: Discovery Chemistry Research and Technologies, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
authors: Maria-Jesus
authors: MJ
authors: Blanco
mesh_terms: D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods*; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D008163:Luminescent Measurements / Q000379:methods; D061848:Optical Imaging / Q000379:methods; D004364:Pharmaceutical Preparations / Q000737:chemistry / Q000378:metabolism; D010599:Pharmacokinetics; D049268:Positron-Emission Tomography / Q000379:methods
chemical_list: D004364:Pharmaceutical Preparations
keywords: Bioluminescent imaging (BLI); Biomarker; Cellular thermal shift assay (CETSA); Lead Generation; Positron emission tomography (PET); Receptor occupancy (RO); Target engagement