GPCR Hit Identification

GPCR Hit Identification

For Research Use Only. Not For Clinical Use.

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

Introduction of Hit Identification

G protein-coupled receptors (GPCRs), which play a vital role in health and a variety of pathophysiological conditions, remain one of the most important therapeutic target class. They are estimated to account for 30-40% of marketed drugs. Nearly one quarter of the best-selling drugs in the United States are related to GPCRs. This makes GPCR drug discovery continue to represent a major focus in pharmaceutical research.

Hit identification is the process of identifying compounds that can interact with validated targets. It is the first committed and most critical step for successful drug discovery. Different strategies have been developed to identify high-quality hits. These strategies aim to maximize the number of initial hits, and can accelerate the drug discovery progress with lower attrition rates.

Figure 1. GPCR ligand identification through affinity MS screening. (Qin S, et al., 2018)Figure 1. GPCR ligand identification through affinity MS screening. (Qin S, et al., 2018)

Our Featured Services

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

Virtual Screening

Computational techniques are used in virtual screening to screen large libraries of small molecules to identify new hits with desired properties. We provide highly optimized and efficient workflow for virtual screening to help overcome potential challenges.

Fragment-Based Screening

Fragment-based screening (FBS), which concerns the screening of low-molecular weight compounds to identify new hits, has been widely used as a viable alternative to high-throughput screening. We have extensive capabilities in FBS to offer access to expertise in hit identification.

DNA Encoded Libraries

DNA encoded library (DEL) is a bridge connecting the fields of molecular biology, combinational chemistry, high throughput sequencing and informatics. It has become a widely accepted method for hit identification. We have established an advanced and efficient DEL screening platform to accelerate GPCR drug discovery.

Affinity Mass Spectrometry Screening

Affinity mass spectrometry is a qualitative analysis approach for the identification of compounds that bind to the target. We provide a high-throughput affinity mass spectrometry screening platform for hit identification in a highly efficient manner.

High-Throughput and High Content Screening

High-throughput screening (HTS) is a rapid and efficient technique for screening compounds from a huge number of candidates. High content screening (HCS) is a multi-parametric analysis method using high-throughput live cell imaging. We provide HTS and HCS techniques to meet different requirements.

Artificial Intelligence

Artificial intelligence (AI) can be applied for hit identification. Compared with traditional screening approaches, AI is a more efficient and cost-effective tool. We have established state-of-the-art AI platform to open more possibilities for drug discovery.

Creative Biolabs provides our customers with customized hit identification services to deliver high-quality and validated hit compounds for their drug discovery projects. Our experienced scientific team can offer tailored one-stop solutions in a 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. Qin S, et al. High-throughput identification of G protein-coupled receptor modulators through affinity mass spectrometry screening. Chemical science, 2018, 9(12): 3192-3199.
  2. Cvijic M E, et al. GPCR profiling: from hits to leads and from genotype to phenotype. Drug Discovery Today: Technologies, 2015, 18: 30-37.