High throughput screening has become a necessary part of drug discovery for identifying lead molecules for specific disease targets. The pharmaceutical industry invests considerable effort and resources in screening compounds against G protein-coupled receptors (GPCRs) because they are considered sources of attractive therapeutic targets. Formats used for identifying modulators of GPCR function range from simple receptor-ligand-binding assays to high content screening platforms. Each format has its own advantages and disadvantages and the decision to utilize a specific screening methodology depends on the availability and costs of reagents and equipment as well as the expected properties of lead molecules. As the understanding of signal transduction and GPCR regulation increases, new assay formats that provide improved sensitivity, ease of use and increased throughput become available. Most of the screening technologies available to date rely on classic GPCR mechanisms such as ligand binding, GTP binding, cAMP formation, and cytosolic Ca2+ influx. The introduction of high content imaging technology makes it now possible to screen compounds and elucidate the detailed molecular mechanisms involved with GPCR trafficking.

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