GPCR Screening Services - Creative Bioarray

G-protein-coupled receptors (GPCRs) play an incredible role in a range of functions in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third and one-half of the marketed drugs act by binding to GPCRs.

GPCRs mediate many important physiological functions and are considered to be one of the most successful therapeutic targets for a broad spectrum of diseases. The design and application of high-throughput GPCR assays are critical for early drug discovery, which allow the cost-effective screening of large compound libraries to identify novel drug candidates. Early functional GPCR assays rely primarily on the measurement of G-protein-mediated 2nd messenger. Taking advantage of the continuously deepening understanding of GPCR signal transduction, many G-protein-independent pathways are used to detect the activity of GPCRs, and may provide additional information for the functional selectivity of candidate compounds. With the combination of automated imaging systems and label-free detection systems, such assays are now suitable for high-throughput screening (HTS).

Creative Bioarray offers a comprehensive selection of binding and functional GPCR assays to meet the GPCR drug discovery research needs of both chemists and biologists.

Assay classification	Commonly used assays	Pros
Receptor binding assays	Radioligand binding assay	High-throughput; less interference; agonist & antagonist in one assay
Receptor binding assays	Fluorescent ligand binding assay	Non-radioactive; high-throughput; agonist and antagonist in one assay
G-protein dependent assays	GTPγS binding assay	Functional cell-free assay; discrimination between full or partial agonists, neutral antagonists, inverse agonists, allosteric regulators
	Reporter assay	Homogenous assay; high-throughput; large signal to background window
	cAMP assay	High-throughput; very sensitive
	Ca²⁺ mobilization assay	High-throughput; functional assay for live cells; obtain agonist, antagonist and allosteric modulator in one assay
	IP3/IP1 assay	High-throughput; functional assay for live cells; good for slow binding ligands
G-protein independent assays	GPCR internalization assay	Image based, high-content; functional assay for live cells; generic method for all
	β-Arrestin recruitment assay	High-throughput; image or non-image based; functional assay for live cells; useful in biased signal detection; generic method for all GPCRs
	Label-free whole cell assay	Label-free functional assay in live cells; summation of all cellular events
Receptor dimerization assay		GPCR heterodimers are considered new pharmacological targets

Advantages of Creative Bioarray's GPCR Assay Services:

An ideal assay for GPCR ligand screening should be simple, nonradioactive, robust, homogenous, and easily adapted to a microtiter plate format (96-, 384-, or 1536-well) for automation. With more than 10 years of expertise in biopharmaceuticals, Creative Bioarray offers hundreds of functional and radioligand-binding GPCR assays for high-throughput screening, molecular pharmacology and molecular profiling.