GPCR Ligand Identification

GPCR Ligand Identification

For Research Use Only. Not For Clinical Use.

Creative Biolabs provides professional services and innovative technologies for ligand identification to help accelerate GPCR drug discovery.

Introduction of GPCR Ligand Identification

G protein-coupled receptors (GPCRs), the major regulators of intercellular interactions, are involved in virtually every biological process. They can be activated by a variety of endogenous and synthetic ligands. GPCRs comprise the largest family of transmembrane receptors and represent the most leading family of druggable targets. Although many GPCRs have become targets of approved drugs, they are only a small part of the potentially druggable GPCRs.

Current drug development is still focused on those GPCRs that are widely validated as potential therapeutic targets. However, with the further elucidation of the regulatory mechanisms of diverse ligands on GPCR functions, these in-depth understanding of ligands have enabled the discovery of novel ligands, especially for orphan and understudied GPCRs that might be useful as therapeutic targets. Novel approaches and strategies have been developed to identify novel ligands that can selectively modulate the activity of GPCR targets with high efficacy.

Figure 1. Classical and Emerging Approaches of Peptide Drug Discovery to Identify Novel G Protein- Coupled Receptor (GPCR) Ligands. (Muratspahić E, et al., 2019)Figure 1. Classical and Emerging Approaches of Peptide Drug Discovery to Identify Novel G Protein-Coupled Receptor (GPCR) Ligands. (Muratspahić E, et al., 2019)

Our Featured Services

We are proud to offer the most robust and reliable services for the identification of GPCR ligands. Browse our featured services below or use our online inquiry form to get more information.

Sensor-Based Ligand Screening

Sensor-based ligand screening refers to immobilization of purified GPCRs on SPR surfaces before fragment library screening. It can be used for detergent-solubilized or affinity-purified receptors. We provide sensor-based ligand screening for GPCRs to handle on targets, especially signaling complexes.

Structure-Based Virtual Ligand Screening

Structure-based virtual ligand screening has been established as a powerful tool which can be used as complement to expensive experimental HTS experiments. We provide professional and efficient structure-based virtual screening for GPCR ligands to contribute to the drug discovery process.

Affinity Mass Spectrometry-Based Ligand Screening

Affinity mass spectrometry can be used to identify putative ligands based on qualitative analysis of compounds that bind to the target. We provide a high-throughput and quantitative affinity mass spectrometry-based ligand screening strategy for highly efficient identification of GPCR ligands.

Quantum Dot-Labeled Cell-Based Screening

Quantum dots are semiconductor nanocrystals with unique optical properties. We provide quantum dot-labeled cell-based screening services as a powerful tool for rapidly identifying GPCR ligands. This strategy can isolate ligands with high affinity and specificity against a variety of GPCRs at high-throughput and low cost.

GPCR Deorphanizatiton

There are many GPCR gene encode receptors whose endogenous ligands and biological roles have not yet been identified. They are called orphan GPCRs and regarded as emerging drug targets. We provide both the reverse and the forward pharmacology strategies to identify novel receptor-ligand pairs.

Creative Biolabs provides customized GPCR ligand identification services to fully meet the requirements of our customers. Our experienced scientific team can offer tailored one-stop solutions in a high-quality, timely and cost-effective manner to help you achieve your goals.

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


  1. Muratspahić E, et al. Nature-derived peptides: a growing niche for GPCR ligand discovery. Trends in pharmacological sciences, 2019.
  2. Wacker D, et al. How ligands illuminate GPCR molecular pharmacology. Cell, 2017, 170(3): 414-427.