Target Classes
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G-Protein Coupled Receptors (GPCRs)

The optimum functioning of living cells, and consequently the health of the entire organism, depends on how cells respond to the multitude of physical and chemical stimuli that continually bombard them. The majority of chemical stimuli are comprised of hormones and neurotransmitters that bind to specific cell surface receptor proteins.

The G-protein-coupled receptor (GPCR) superfamily is comprised of 600 to 1,000 members, and is the largest known class of molecular targets with proven therapeutic value. As a target class, GPCRs comprise more than 40 percent of drug screening programs and account for more than 50 percent of today's commercially available pharmaceuticals.

Some key challenges facing researchers include understanding novel modes of regulation of GPCRs in an effort to identify novel targets. Researchers are investigating this critical target class from all angles: GPCR structure/function, including analysis of the functional significance of single nucleotide polymorphisms; RNA-editing and alternate mRNA splicing; signaling via G proteins and downstream messenger systems; interaction of receptors with accessory proteins; novel allosteric binding sites; and others.

Molecular Devices offers high-throughput screening systems for GPCR assays as well as other analytical systems for follow-on studies of these two target classes, confirmatory screens, cardiac safety, and hERG testing. Learn more about our products to support GPCR-based drug discovery by clicking on the appropriate link below.


CellKey® Label-Free Cellular Analysis System

FLIPR® Tetra High-Throughput Cellular Screening System

FLIPR® Calcium Flux Assays

LiveWare® Assay

ImageXpress® High-Content Screening Systems

Transfluor® Assay Kit