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GPCR Screening & Profiling Services

Brief Introduction

Creative Biogene is offering GPCR drug screening and profiling services. As a pioneer in this field, we can save your time and cost of the discovery programs by taking advantage of our expertise and innovative technology platforms.

Creative Biogene offers enriched active assay platforms in multiple direct functional readouts, including ligand binding, calcium flux, IP-3/1, cAMP, pERK, GTPγS, reporter assays and internalization assays. GPCR assays in Creative Biogene assist the evaluation of binding and downstream effects of small molecules against a wide variety of GPCR targets. Our GPCR screening assays include over one hundred targets and cover receptors from all major GPCR classes. Whether you're looking for hit identification, selectivity profiling or SAR optimization services, we have all the GPCR drug discovery solutions for you.

G protein-coupled receptors (GPCRs), or seven transmembrane receptors (7TMs), are the largest family of cell-surface molecules involved in signal transmission (Rebert 2007). GPCRs have drawn much attention for treating hypertension, neurological, pain and other disorders, as more than 40% of the clinically marketed drugs are targeting GPCRs. Different assay platforms are demanded to monitor ligand binding, GPCRs activation, change in second messengers and GPCRs internalization, which requires specialized methods and instrument for each pathway.

GPCR Screening & Profiling Services Fig.1 The structure sketch of GPCR protein

GPCRs are expressed throughout the body and modulate a wide array of essential physiological processes, including regulating the senses of vision, taste, and olfaction, as well as mediating cellular responses to hormones and neurotransmitters. GPCR signal transduction is accomplished by the binding of a receptor agonist to an exposed extracellular or intra-membrane site on the receptor, which induces a conformational change in the receptor protein. The assortment of known GPCR ligands is as expansive and diverse as the biological functions they regulate, including photons, ions, odorants, amino acids, peptides, nucleotides, lipids, and small organic molecules. Because of the range of biological processes and pathologies, the screening and profiling of GPCR is an important tool to select drug candidates in drug discovery industry (Jinifer et al. 2015).

GPCR Screening & Profiling Services Fig.2 Examples of GPCR screening approaches (Annette et al. 2007)

In terms of years’ professional experience in this field, Creative Biogene can provide you an effective screening approach with advanced screening platform, quick turnaround, and uncompromising quality results to identify the compounds with the greatest chance to succeed. Creative Biogene is a reliable partner that can work with you to accelerate the speed to achieve your research goals.

If you have any special requirements in GPCR compound screening, please feel free to contact us at or 1-631-626-9181. We are looking forward to working together with your attractive projects.


  1. Rebert T. (2007) ‘G-protein-coupled receptors and cancer’, Nature Reviews, 7, 79-94
  2. Jinifer AS and Lakshmi AD. (2015) ‘Advancements in therapeutically targeting orphan GPCRs’, Frontiers in Pharmacology, 6,100
  3. Annette G. (2007) ‘Modulating G-protein-coupled receptors: from traditional pharmacology to allosterics’, TRENDS in Pharmacological Sciences, 28(8), 431-437

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