GPCRs Binding Assays

GPCRs Binding Assays

For Research Use Only. Not For Clinical Use.

Creative Biolabs has professional platforms and years of experience in binding assays to assist our customers with GPCR research and drug development. We can help speed up your drug discovery by combining high-throughput screening techniques.

Importance of Binding Assays

G protein-coupled receptors (GPCRs) are the largest class of cell-surface receptors in eukaryotes. They play a critical role in an incredible array of physiological functions. GPCRs are valuable targets for drug discovery. At present, GPCR-targeted drugs account for almost 40% of existing drugs.

The binding of signaling molecules to GPCRs results in the activation of G proteins, which in turn triggers the production of second messengers. Binding is the first step for GPCRs to exert their functions. Binding assays can be used to determine the detailed interactions between receptors and their ligands, and also to identify compounds that are involved in the modulation of GPCR activity. It is an indispensable part in drug development. Further understanding of GPCRs will have a significant impact on modern medicine.

Receptor binding and G-protein-dependent assays.Figure 1. Receptor binding and G-protein-dependent assays. (Zhang R & Xie X, 2012)

Our Services

We offer our customers with a comprehensive selection of binding assays based on isotope labeling, non-isotope labeling or label-free methods to meet their different research needs.

Labelled Technologies in GPCR-Ligand Binding Assays

Assay Method Description Applicable Sample
Radioligand Binding Assay Radioligand binding assay is widely used to measure and characterize the affinity of compounds or ligands to a target GPCR. There are three types of assays: competitive, saturation and kinetic.
  • Cell membrane purified from tissue homogenates
  • Cells transfected with receptors
  • Newly isolated or cultured cells
Fluorescent Ligand Binding Assay Fluorescent-labelled ligand has the advantage of high sensitivity and less hazardous. Multiple colors can be applied for the detection of specific targets.
  • Living cells
  • Cellular membranes
Scintillation Proximity Assay SPA depends on the energy conversion of radioactive decay. It can be easily scaled down and automated for high-throughput screening applications.
  • Whole cells
  • Purified cellular membranes
Time-Resolved Fluorescence Resonance Energy Transfer Many of the newly developed binding assays are based on TR-FRET, which provides a nonradioactive and fast, assay format with high sensitivity. It can be easily adapted to high-throughput screening.
  • Living cells

Label-Free Technologies in GPCR-Ligand Binding Assays

Assay Method Description Applicable Sample
Biosensor Resonant waveguide gratings biosensor, surface plasmon resonance biosensor, and electrical biosensor can be used as label-free instruments for real-time monitoring of GPCR signaling.
  • Wide applicable range from molecules to whole cells.
Frontal affinity chromatography with MS detection FAC-MS can be used for binding studies and has the ability to rank ligands.
It is a convenient and efficient tool for screening new potential drug leads with the advantages of label-free operation and relatively high throughput ability.
  • Native cellular membranes.
  • Receptors entrapped on immobilized artificial membrane

Creative Biolabs provides our customers with customized binding assay services in a time- and cost-effective manner. Our experts will work closely with you to fully meet your requirements.

If you are interested in our services or have any specific needs, please feel free to contact us for more details.


  1. Zhang R & Xie X. Tools for GPCR drug discovery. Acta Pharmacologica Sinica, 2012, 33(3): 372-384.
  2. Thomsen W, et al. Functional assays for screening GPCR targets. Current opinion in biotechnology, 2005, 16(6): 655-665.