GPCR Lead Generation and Optimization
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)
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.
- Hit characterization services to fully identify active components.
Our services include but not limited to active fraction characterization, single active(s) purification, small/large scale synthesis of pure actives, SAR/SLR profiling, and biophysical characterization.
- In silico profiling to generate new hit series with improved properties.
Our computer science/informatics experts can provide professional in silico tools, such as computer-aided drug design, structure-based techniques and ADMET prediction tools, to help accelerate drug discovery process.
- Toxicogenomics for early assessment of lead chemical series due to potential toxicity.
Our services based on toxicogenomic assays can help improve the evaluation of drug safety and toxicity in drug discovery process, and characterize leads for toxicity liabilities as early as possible to ensure later success.
- Crystallographic approaches for structure-based lead optimization.
Our experienced expertise in structural biology can provide high quality and reliable crystallography services with a short turnaround time. Our services can help enhanced potency of lead compounds to the drug targets.
- DMPK and ADME studies to assess the safety and efficacy of lead compounds.
Our scientific team with extensive experience in DMPK and ADME studies can help make the right decision on whether the lead compound can be selected as a drug candidate in the early stage of drug discovery.
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.
- Bleicher K H, et al. Hit and lead generation: beyond high-throughput screening. Nature reviews Drug discovery, 2003, 2(5): 369-378.
- Cvijic M E, et al. GPCR profiling: from hits to leads and from genotype to phenotype. Drug Discovery Today: Technologies, 2015, 18: 30-37.