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GPCR Screening & Profiling with Functional Assays

Creative Biogene provides the best GPCR functional assay services. As a well-known expert in this field, our talented scientists with abundant experience and innovative techniques are confident in offering the highest quality services for your GPCR assays with the most competitive price.

Creative Biogene offers cell based assays covering multiple second messenger readouts, including GTPγS binding assays, cAMP assay, IP3/IP1 and Ca2+ assays, reporter assay, etc. In addition, we also offer receptor internalization assay, β-arrestin recruitment assay, label-free whole cell assay, and so on. The abundant experience in above assays enables us better understand compound activity and provide professional services. Our GPCR functional assays can evaluate the downstream effects of compounds against a broad range of GPCR targets. By combining with binding assays, Creative Biogene’s functional assays can provide a full profile of a compound's in vitro pharmacology.

It is important to understand compound on and off target activity, if we are evaluating a GPCR therapeutic's potential efficacy and liabilities. GPCRs can transmit signal through a variety of cascades, and a drug will activate, inhibit, or regulate one or more of these pathways.

Ligand-binding assays are useful to identify new compounds that target GPCRs. Further analysis of the biological responses after compound binding will help complete the whole picture concerning the overall characteristics of the compound. Upon ligand binding, GPCRs change their conformation and activate coupled G proteins, which subsequently promote second messenger production via downstream effectors. By GPCR functional assays, we can detect the activity of target GPCR, and may provide additional information on functional selectivity of candidate compounds.

Fig.1 The principle mechanisms involved in different G-protein signaling pathways (Peter, et al. 2005)Fig.1 The principle mechanisms involved in different G-protein signaling pathways (Peter, et al. 2005)

Creative Biogene has a wide range of GPCR functional assay services, which including but not limited to the following assays:

  1. GTPγS binding assay
  2. cAMP assay
  3. IP3/IP1 assay
  4. Ca2+ assay
  5. Reporter assay
  6. Receptor internalization assay
  7. β-arrestin recruitment assay
  8. Label-free whole cell assay

Advantages of functional assay services in Creative Biogene:

  1. Multiple assays formats to choose
  2. Providing G-protein independent functional assay, including internalization assay, β-arrestin recruitment assay, and label-free whole cell assay,
  3. Single concentration or dose response screening for EC50 and IC50 determination
  4. Covering more than 100 GPCR targets
  5. Quick turnaround time

Creative Biogene can offer you GPCR compounds functional assays with high-quality and efficiently. We are dedicated to profiling the compounds against GPCR targets with the greatest chance to succeed. Our experienced scientists along with our broad portfolio make it easier to meet the demands of different researchers. Together, our collection of functional assays, combined with our binding studies, can provide an orthogonal method to verify the in vitro pharmacology of your compounds. With years’ of experience in GPCR compounds functional assay, Creative Biogene has capability and confidence in tailoring the best-fit assay to meet your specific needs and facilitate your project in time.

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

1.Peter, J. G. and Frank, P. J., (2005) ‘G-protein-coupled receptor screening technologies’. Drug Discovery Today: Technologies, 2(2), 163-170

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