GPCR Binding Assay

In the realm of drug discovery, G protein-coupled receptors (GPCRs) have emerged as a prominent target family due to their pivotal role in various physiological processes. With approximately 800-1000 members, GPCRs constitute one of the largest and most diverse receptor superfamilies, making them highly sought after in the development of therapeutics.

The general architecture of class A G protein-coupled receptors (GPCRs)The general architecture of class A G protein-coupled receptors (GPCRs) (de et al., 2015).

Why Analyse GPCR Binding?

GPCR binding is a key step in GPCR function and involves the interaction between the receptor and the ligand (which can be an agonist or antagonist). This interaction sets off a chain reaction of downstream signaling events, leading to the orchestration of a multitude of physiological processes.

In the realm of drug development, determining the affinity of ligands for GPCRs takes center stage. This affinity serves as a reflection of the strength of the binding interaction between the receptor and the ligand. Quantitative information regarding the binding affinity and kinetics is obtained through parameters like IC50, Ki, and Kd.

Schematic diagram shows a GPCR and possible ligand binding sitesSchematic diagram shows a GPCR and possible ligand binding sites (Zhang et al., 2013).

Creative Proteomics specializes in providing comprehensive GPCR binding analysis services to facilitate the identification of compounds with high binding potential to target GPCRs. Our state-of-the-art technologies, combined with our team's expertise, enable accurate and reliable assessments of ligand-receptor interactions.

By assessing the binding capabilities of compounds to specific GPCRs, researchers can gain valuable insights into the potential therapeutic applications of these compounds. This analysis provides a solid foundation for subsequent studies, aiding in the design and optimization of drugs that selectively target GPCRs.

Technology Platform for GPCR Binding at Creative Proteomics

Creative Proteomics utilizes a diverse range of cutting-edge technologies to perform GPCR binding analysis. Our comprehensive technology platform includes:

a) High-throughput screening (HTS):

High-throughput screening techniques allow rapid assessment of the binding affinity of compounds to target GPCRs. This approach allows efficient screening of large compound libraries, enabling faster identification of potential drug candidates.

b) Fluorescence-based assays:

The fluorescence resonance energy transfer (FRET) technique can be used to detect ligand-receptor interactions. By measuring the change in fluorescence intensity or energy transfer, we can accurately determine the binding affinity and kinetics of the compound.

c) Surface plasmon resonance (SPR):

SPR is a powerful label-free technique for real-time monitoring of molecular interactions, including ligand-receptor binding. At Creative Proteomics, we use SPR technology to measure the binding kinetics, affinity and specificity of compounds to GPCRs.

d) Biophysical techniques:

Biophysical techniques can help provide insight into the molecular interactions involved in GPCR binding, such as isothermal titration calorimetry (ITC) and nuclear magnetic resonance (NMR). These methods provide quantitative information on the binding thermodynamics and structural details of the ligand-receptor complexes, facilitating the optimization of drug candidates.

e) Computational methods:

In addition to experimental techniques, Creative Proteomics uses computational methods for GPCR binding analysis. Molecular docking and molecular dynamics simulations are used to predict the binding mode, energetics and stability of ligand-receptor complexes. These computational methods contribute to the rational design of novel compounds and optimization of their binding properties.

f) Custom Assay Development:

We offer custom assay development services to meet specific customer requirements. Our experienced scientists work closely with our clients to design and optimize assays to suit their target GPCR and compound properties. This flexibility allows us to adapt and customize our technology platform to the unique needs of each project.

In addition to binding analysis, Creative Proteomics also offers GPCR functional analysis experiments. These experiments involve assessing various functional aspects, such as calcium influx and second messengers (cAMP, IP-1), to analyze the activation and inhibitory effects of compounds on target GPCRs.

GP-first mechanism of GP activationGP-first mechanism of GP activation (Mafi et al., 2022).

Data Interpretation and Reporting

We understand that our clients need not only accurate data, but also meaningful interpretation to make informed decisions. At Creative Proteomics, we offer comprehensive data interpretation and reporting services. Detailed results analysis, visualization, and professional report writing ensure that our clients can easily understand and utilize the information obtained from GPCR binding analysis.

In addition, we are committed to maintaining the highest standards of data security and complying with industry regulations. Our strict data processing protocols and secure infrastructure ensure the confidentiality and privacy of our customers' data.


  1. de Munnik, Sabrina M., et al. "Modulation of cellular signaling by herpesvirus-encoded G protein-coupled receptors." Frontiers in pharmacology 6 (2015): 40.
  2. Zhang, Xin, and Ulrike S. Eggert. "Non-traditional roles of G protein-coupled receptors in basic cell biology." Molecular bioSystems 9.4 (2013): 586-595.
  3. Mafi, Amirhossein, Soo-Kyung Kim, and William A. Goddard III. "The mechanism for ligand activation of the GPCR–G protein complex." Proceedings of the National Academy of Sciences 119.18 (2022): e2110085119.
* This service is for RESEARCH USE ONLY, not intended for any clinical use.