GPCR Lead Generation and Optimization

GPCR Lead Generation and Optimization

For Research Use Only. Not For Clinical Use.

Creative Biolabs provides professional services and innovative technologies for lead generation and optimization to help accelerate GPCR drug discovery.

Introduction of Lead Generation and Optimization

Lead generation, also known as hit to lead (H2L), plays an important role in early drug discovery. It is a multi-dimensional and challenging process aimed at optimizing the properties of numerous hits and identifying lead compounds. In this process, the chemistry and biological properties of hits are fully explored to obtain active compounds that meet the threshold level of activity. The identified lead compounds must be proven to reach their targets and modulate their activity in vivo, while acting within acceptable safety margins.

After lead generation, lead compounds need to undergo a subsequent step of drug discovery called lead optimization. It is a critical process aimed at culminating in the identification of a preclinical candidate by improving effectiveness, diminishing toxicity or increasing absorption of the most promising compounds. The higher the quality of lead compounds, the higher the success rate of drug development.

Figure 1. Stage-by-stage quality assessment to reduce costly late-stage attrition. (Bleicher K H, et al., 2003)Figure 1. Stage-by-stage quality assessment to reduce costly late-stage attrition. (Bleicher K H, et al., 2003)

Our Featured Services

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

Creative Biolabs provides our customers with customized lead generation and optimization services to deliver high-quality and validated drug candidates 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. Bleicher K H, et al. Hit and lead generation: beyond high-throughput screening. Nature reviews Drug discovery, 2003, 2(5): 369-378.
  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.