GPCR Screening Assays

G protein-coupled receptors (GPCRs) superfamily is comprised of an estimate of 600-1,000 members and is the largest known class of molecular targets with proven therapeutic value. Over 40% of the approximately 500 pharmaceuticals on the market are GPCRs targeted. GPCR signaling is a extremely complex system based on three major elements: a GPCR with the ability to couple with a heterotrimeric GTP binding protein (G-protein), a GTP-transferase active G-protein and a second messenger generating enzyme. Currently, the main trends in GPCR drug discovery involve not only the search for common ligands such as agonists or antagonists, but also inverse agonists and allosteric modulators.

GPCR Screening Assays

From our over 10 years of expertise in the bio-pharmaceutical field, Creative BioMart provides hundreds of functional and radioligand binding GPCR assays that can be applied for high throughput screening, molecular pharmacology and profiling projects. Creative BioMart's GPCR screening service provides the most comprehensive cell-based assays along with the fastest turnaround time in the industry for rapid efficacy, potency, and selectivity determination. Our highly flexible service allows you to choose the ideal screening assay to meet your project needs in hit identification, selectivity profiling, lead optimization, as well as offers you a cost-effective screening approach to help narrow down your research to individual GPCRs.

Service Highlights and Benefits

  • Over 10 years of experience
  • Enriched active assay platform
  • Proven and trusted technology
  • Highly sensitive and quantitative assay
  • Flexibility in panel size
  • Rapid turnaround time
  • Competitive pricing
  • Proven track record
  • Precise and reproducible result
  • Applicable to established stable cell lines

GPCR drug screening is essentially based on testing available molecule libraries. Such libraries can contain thousands of different compounds derived either by natural sampling, random synthesis or both, which are tested for their ability to bind to or interfere with the function of a GPCR molecule. Given the large number of molecules in those libraries, the use of high-throughput screening technologies that enable rapid testing through miniaturization and parallelization is indispensable. Creative BioMart offers a comprehensive selection of binding and functional GPCR assays to meet the GPCR drug discovery research needs of both chemists and biologists.

Summary of GPCR Screening Assays

Assay classification Commonly used assays Pros
Receptor binding assays Radioligand binding assay High-throughput; less interference; agonist & antagonist in one assay
Other tagged-ligand binding Non-radioactive; high-throughput; agonist and antagonist in one assay
G-protein dependent assays GTPγS binding Functional cell-free assay; discrimination between full or partial agonists, neutral antagonists, inverse agonists, allosteric regulators
CRE/MRE reporter assay Homogenous assay; high-throughput; large signal to background window
cAMP assay High-throughput; very sensitive
Ca2+ High-throughput; functional assay for live cells; obtain agonist, antagonist and allosteric modulator in one assay
IP1/3 High-throughput; functional assay for live cells; good for slow binding ligands

G-protein independent assays

Receptor trafficking Image based, high-content; functional assay for live cells; generic method for all GPCRs
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 assay Label-free functional assay in live cells; summation of all cellular events
Receptor dimerization assay GPCR heterodimers are considered new pharmacological targets


  1. Ru Zhang and Xin Xie. Tools for GPCR drug discovery. Acta Pharmacol Sin. 2012 Mar; 33(3): 372-384. doi: 10.1038/aps.2011.173

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