Hit-to-Lead

Charles River conducts hit-to-lead projects in an efficient cycle of rational design, synthesis and biological evaluation. Typically, multiple hit series are evaluated in parallel, with a view to establishing the scope for further optimization. One or two series are then selected for progression into lead optimization studies.

We will work closely with you to define the compound profile required, prioritizing compounds for detailed evaluation and interpreting results from a customized screening cascade including primary target and cellular activity together with ADME/PK assessment and target engagement biomarker assay development. Our medicinal chemists have an impressive track record of delivering high-quality lead series to our clients within agreed timelines across a broad range of target classes and therapeutic areas.

Hit-to-Lead Activities

  • Design and synthesis of new analogues for rapid SAR determination
  • Increasing compound potency and selectivity
  • Improvement of drug-like properties
  • Applying CADD to generate binding hypotheses and to investigate SAR
  • Early assessment of ADME properties
  • Evaluation of target engagement biomarker assays
  • Ranking of hits or hit series for lead optimization

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