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As the name suggests, the hit to lead (H2L) stage of drug discovery aims to discover compounds of interest (leads) from a series of compounds (hits) that demonstrate promising therapeutic effects. The hit to lead process, also known as lead generation, typically occurs following target validation, assay development, and high-throughput screening studies.

This process first confirms that a true structure-activity relationship (SAR) exists within a number of hit series for the biological target. In addition, an early evaluation of in vitro ADMET properties is performed to help select the most promising leads for optimization.

H2L, which explores the chemical and biological properties of hits to eliminate dead-end structures and provides improvements to the remaining hit series so that development time and costs are saved, is now a key process for drug discovery organizations. Acting as a bridge between HTS and lead optimization, H2L presents an important opportunity to fail compounds early, before a large number of resources have been spent on their development.

At Creative Bioarray, we pay particular attention to the overall qualification of hits. To this end, hits are resynthesized, purified and characterized by multiple assays that are relevant to the target parameters/properties. Together with SAR analyses, profiling results enable a clear prioritization and selection of the most promising leads for optimization.

Our Capabilities

Whether your therapeutic goal focuses on the development of small molecules, peptides or other biologics, our team's award-winning chemistry experience ensures your initial hits will see a significant improvement in their properties to meet the necessary criteria to enter the lead optimization phase. Our capabilities include:

  • Hit series ranking and clustering
  • In silico profiling of compounds
  • Orthogonal testing to determine the suitability of promising hit series
  • Computer-assisted drug design tools to test chemical modifications and evaluate scaffold-hopping methods
  • Advanced chemical synthesis for hit expansion
  • Multi-dimensional optimization of drug-like properties
  • Drug feasibility assessment based on SAR and DMPK
  • Preliminary improvement of ADME properties
  • Biophysical testing and structural characterization

With a strategy designed specifically for your project, and a dedicated team working around the clock to ensure that extremely promising compounds are produced during the hit-to-lead phase, your drug discovery program advances smoothly, delivering striking compounds and superior confidence in the overall success of your project.


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