GPCR Target Validation

GPCR Target Validation

For Research Use Only. Not For Clinical Use.

Creative Biolabs provides professional services and innovative technologies for GPCR target validation to help accelerate the drug development pipeline.

Introduction of GPCR Target Validation

Target validation is a key step in the early stage of drug development. It refers to the process involved the application of a range of techniques to prove that the regulation of identified targets has the expected effect on biological activity and the engagement of these targets has potential therapeutic effects. The failure of drug development is usually attributed to inadequate pre-clinical target validation. Early in-depth target validation can increase the understanding of the relationship between targets and diseases, thus increasing the possibility of clinical success.

G protein-coupled receptors (GPCRs), which play an important role in physiology and pathology, represent the most important therapeutic targets. They constitute the largest family of protein targets most frequently targeted by approved drugs. Genome mining has led to the identification of a large number of novel GPCRs. However, these drugs exhibit their activity at <10% of all known GPCRs. Target validation is essential to link many novel GPCRs with diseases, thus facilitating drug development.

Figure 1. Trends in the indications of approved GPCR-targeted drugs and agents in clinical trials. (Hauser A S, et al., 2017)Figure 1. Trends in the indications of approved GPCR-targeted drugs and agents in clinical trials. (Hauser A S, et al., 2017)

Our Featured Services

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

In Silico Target Validation

We provide computer simulation of biological systems for in silico target validation of GPCRs, especially orphan GPCRs. By expanding the number of parameters and avoiding experiments with less information, our services can facilitate the transition of valuable drug targets to clinical drugs.

Biological Target Validation

We provide many levels of biological experiments to gather evidence of targets involved in diseases.

  • Genetic manipulation

    —­­ Antisense technology and RNA interference are commonly used to identify the physiological role of the targets.

  • Expression profiling

    ­­—­­ Expression profiling of GPCRs can be used to identify the tissues and cell types in which the receptor is expressed and to determine whether the expression pattern is altered in diseases.

  • Reverse pharmacology

    ­­—­­ Reverse pharmacology is also known as target-based drug discovery. Orphan GPCRs can be used as “baits” to identify their ligands.

  • Chemical Genomics

    ­­— Chemical genomics can be used to discover specific molecular targets and pathways modulated by particular chemical molecules. It is an approach to find targets for known drugs.

Creative Biolabs provides customized GPCR target validation 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. Hauser A S, et al. Trends in GPCR drug discovery: new agents, targets and indications. Nature reviews Drug discovery, 2017, 16(12): 829.
  2. Wise A, et al. Target validation of G-protein coupled receptors. Drug discovery today, 2002, 7(4): 235-246.
  3. Thomsen W, et al. Orphan GPCR target validation. Current opinion in molecular therapeutics, 2004, 6(6): 640-656.