title: GPCR profiling: from hits to leads and from genotype to phenotype.
abstract: GPCRs remain one of the most important classes of drug targets and, therefore, GPCR assay development and high-throughput GPCR ligand profiling continue to be major efforts in drug discovery. This article focuses on GPCR platform strategies from hits to leads with miniaturized complex pharmacology approaches. Three main areas of GPCR profiling are discussed including pharmacologically relevant hit identification, the pharmacology dossier applied to parallel structure activity and structure liability relationships and high-throughput mechanism studies from genotype to phenotype.
authors.affiliation: Bristol-Myers Squibb, Hopewell, NJ 08534, United States. Electronic address: maryellen.cvijic@bms.com.
authors.forename: Mary Ellen
authors.initials: ME
authors.lastname: Cvijic
authors.affiliation: Bristol-Myers Squibb, Hopewell, NJ 08534, United States.
authors.forename: Chi Shing
authors.initials: CS
authors.lastname: Sum
authors.affiliation: Bristol-Myers Squibb, Hopewell, NJ 08534, United States.
authors.forename: Andrew
authors.initials: A
authors.lastname: Alt
authors.affiliation: Bristol-Myers Squibb, Hopewell, NJ 08534, United States.
authors.forename: Litao
authors.initials: L
authors.lastname: Zhang
mesh_terms: D000818:Animals; D001665:Binding Sites; D055808:Drug Discovery / Q000379:methods*; D005838:Genotype; D057166:High-Throughput Screening Assays / Q000379:methods*; D006801:Humans; D008024:Ligands; D011485:Protein Binding; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics* / Q000378:metabolism*; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D043562:Receptors, G-Protein-Coupled; D054852:Small Molecule Libraries