The G protein-coupled receptors (GPCRs), known to be one of the largest superfamilies in the human genome, underpin a multitude of physiological processes and represent a significant target for bioactive and drug discovery programs. In G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols, experts in the field provide a range of classic and cutting-edge laboratory protocols developed for GPCR research, as well as several current review articles relevant to the area of high throughput GPCR screening, with discussion on GPCR structure and GPCR signalling. Written in the highly successful Methods in Molecular Biology™ series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and notes on troubleshooting and avoiding known pitfalls.