The hit to lead phase is a critical phase of drug discovery programs. The first set of compounds, or hits, that demonstrate promising activity against a target of interest are further characterized. Through limited medicinal chemistry efforts, the aim is to turn these hits into leads: compounds that we believe can be optimized into drug candidates.

  • How do we select the most promising chemical matter from all hit series? 
  • How do we start optimizing a scaffold? 
  • How do we make sure the optimization is progressing as it should? 
  • When do we know when to stop working on a chemical series? 

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