Lead generation

The identification of lead compounds containing an optimal scaffold through either direct selection from screening hits or scaffold hopping, is highly consequential to the success of lead optimization and is a main focus of the lead-generation.

The aim of lead generation process is to identify multiple diverse analogues that possess adequate potency, selectivity and favorable PK properties, to ensure a desirable level of drug exposure in targeted tissues. The key at the lead-generation stage is to identify an appropriate scaffold capable of providing sufficient numbers of high-quality analogs.