G-protein-coupled receptors (GPCRs) represent the largest and most versatile family of cell surface receptors. The ubiquitous cell surface distribution and involvement of these proteins in virtually all biological processes accounts for the fact that the largest percentage of currently marketed therapeutic drugs target GPCRs. Work in our laboratory is focused on the development of biochemical and cell-based functional assays to monitor GPCR activity using both high throughput and high content technologies. In collaboration with other disciplines such as chemistry, DMPK and in vivo pharmacology we aim to identify and develop small molecule modulators of GPCRs for the therapeutic treatment of metabolic and CNS disorders.