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GPCR Screening & Profiling with Binding Assays

Creative Biogene is a leading company in the process of GPCR binding assay services. We have talented scientists with years of experience in GPCR binding assays. The experts in Creative Biogene would work closely with you to provide help in GPCR binding assays, including platform choosing, experiment designing and performing, and so on. As an experienced drug discovery company, our goal is effectively saving your cost and time during GPCR compounds binding assays by taking advantage of our expertise and innovative technology platforms.

Creative Biogene provides the capacity of performing HTS-compatible large scale binding assay screening for all the GPCRs with the most competitive price. We offer a wide range of platforms to perform compounds binding assays with GPCR target. Moreover, Creative Biogene has developed robust, reliable and stable methods to help you profile your lead compounds interaction with GPCR target.

Fig.1 The sketch of GPCR bindingFig.1 The sketch of GPCR binding

GPCR binding assay can be used to describe in great detail the interaction between GCPR and its ligands/compounds, for example, the intrinsic affinity of ligands/compounds to the GPCR, association/dissociation rates, and the density of receptor in tissues or cells (Bylund et al. 1993). GPCR binding assay is a cell-free method which theoretically suit for any GPCR screening without involving downstream signaling from the receptor. This type of assay can also obtain agonists and antagonists in one experiment. Furthermore, combined with functional assays, binding studies can provide a complete profile of a compound's in vitro pharmacology.

Creative Biogene offers radioligand binding assay and other tagged-ligand binding assay, including filtration assay, SPA, and TR-FRET based technology assays.

Radioligand binding is the standard method for detecting compound interaction with GPCRs, allowing for the simplest interpretation of assay results. The first radioligand binding assay was carried out in 1970 by Lefkowitz et al. using a radio-labeled hormone to determine the binding affinity for its receptor. Radioligand displacement assays can be applied for simple yes/no interaction determination or to calculate a compound's affinity for a receptor of your interest.

In scintillation proximity assay (SPA), which can be easily scaled down and automated for HTS applications, only the radio-labeled molecules binding to the GPCR immobilized on the surface of SPA beads can activate the scintillation beads, producing photons detectable with a scintillation counter. SPA thus allows binding reactions to be tested without washing or filtration steps.

Time-resolved fluorescence resonance energy transfer (FRET) has provided the means to label GPCRs expressed on the cell surface to replace utilization of radioactive ligands. The assay is performed in a “mix and measure” format, which can be used not only for ligand binding studies but also for receptor activity analysis and GPCR dimerization assessment.

Fig.2 Time-resolved FRET based assays (Candide et al. 2015)Fig.2 Time-resolved FRET based assays (Candide et al. 2015)

Advantages of binding assay services in Creative Biogene:

  1. Providing both radioligand assay and TR-FRET based platforms
  2. Covering more than 100 GPCR targets
  3. Single concentration or dose response for IC50 determinations
  4. Capability of membrane preparations produced in house
  5. Short turn-around time

Creative Biogene is dedicated to ensuring our services and compounds binding assays are at the highest level of quality. For the past 10 years, Creative Biogene has built several comprehensive technical platforms for detecting compounds interaction with GPCRs. We are confidence in accelerating the speed to profiling compounds affinity with your GPCR target.

If you have any special requirements in GPCR compounds binding 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. Bylund, D. B., Toews, M. L. (1993) ‘Radioligand binding methods: practical guide and tips’. Am J Physiol, 265, L421–9
  2. Candide, H., Jean-Fran?ois, M., Nadia, O., Abderazak, B., Elodie, D., Cécile, T., André, M., Brigitte, I., Didier, R., Eric, T., Marcel, H., Jean-Philippe, P., Dominique, B., Thierry, D. (2015) ‘Time-Resolved FRET Binding Assay to Investigate Hetero-Oligomer Binding Properties: Proof of Concept with Dopamine D1/D3 Heterodimer’. ACS Chem. Biol., 10, 466?474

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