title: GPCR assay automation for leveraging lead optimization.
abstract: The drug discovery process is dependent on the ability of screening efforts to identify and optimize lead compounds with therapeutic potential. Because G-protein-coupled receptors (GPCRs) account for the most "druggable" targets, the development of high-throughput, low-cost, and high-density GPCR assays to accommodate the increasing size of compound collections is significant. In this study, we report the application of an advanced LEADseeker robotic platform equipped with customized IT solutions for rapid data transfer to reduce assay cycles times for support of GPCR panel screening. The advantages of assay throughput, format, automation design, data management flow, and data reproducibility are discussed in terms of gains in productivity for lead optimization. The GPCR robotic platform demonstrates how automation technology can leverage traditional drug discovery processes by providing consistent and reliable data packages to expedite lead optimization efforts.
authors.affiliation: Department of Lead Evaluation, Bristol-Myers Squibb Company, Princeton, New Jersey 08543, USA. maryellen.cvijic@bms.com
authors.forename: Mary Ellen
authors.initials: ME
authors.lastname: Cvijic
authors.forename: Jing
authors.initials: J
authors.lastname: Chen
authors.forename: Steve
authors.initials: S
authors.lastname: Kubala
authors.forename: Joseph
authors.initials: J
authors.lastname: Nolfo
authors.forename: Garrett
authors.initials: G
authors.lastname: Kolodin
authors.forename: Litao
authors.initials: L
authors.lastname: Zhang
mesh_terms: D057205:Automation, Laboratory / Q000295:instrumentation / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D055808:Drug Discovery / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D057166:High-Throughput Screening Assays; D006801:Humans; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000037:antagonists & inhibitors*
chemical_list: D043562:Receptors, G-Protein-Coupled