GPCR Assays, G-Protein Coupled Receptor Assays

Abnormal function, expression, and regulation of G-protein-coupled receptors (GPCRs) have been implicated in many diseases and, as a result, GPCRs represent one of the largest receptor classes targeted by drug discovery programs. Historically, ligand-binding assays were used to identify compounds that target GPCRs.  While these assays measure a compound's affinity to a receptor, they cannot measure its activity, are not amenable to high throughput discovery, and some use radioactivity, which is difficult and expensive to use on a large scale.  Today, researchers use assays that monitor the accumulation of a second messenger, such as cAMP, calcium, or beta-arrestin, in response to GPCR activation, instead of the problematic ligand-binding assays.

Molecular Devices offers a portfolio of GPCR assay kits: FLIPR® Calcium Assay Kits, a suite of no wash, homogeneous calcium mobilization assay kits for measuring intracellular calcium levels; CatchPoint® Cyclic-AMP and Cyclic-GMP Assay Kits, which are ideal for screening agonists and antagonists of G_i/o-coupled and G_s-coupled families of GPCRs and other signaling pathways; Liveware® G-Protein Cells and Plasmids, a series of cells and expression vectors to study GPCRs that do not couple through intracellular calcium. Transfluor® Assay Technology monitors GPCR "desensitiation" through the beta-arrestin pathway.

To simplify assay development and deliver maximum performance, the GPCR assay kits have been optimized for use with Molecular Devices' FLIPR® Tetra, FlexStation® 3, SpectraMax®, and ImageXpress® Systems. CatchPoint Assay Kits can be read on any SpectraMax Fluorescence Microplate Reader and the Transfluor technollogy can be monitored on high content imaging systems. The kits are conveniently packaged in Bulk kits for high throughput screening applications and Explorer kits for lower throughput applications.

Please use the links below to learn more about how we can support the success of your GPCR screening efforts.