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Enabling Innovative Drug Discovery with Advanced Technologies

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  2. Hit-to-Lead Optimization

Hit-to-Lead Optimization

Hit-to-lead stage of drug discovery is to refine each hit series to try to produce more potent and selective compounds which possess PK properties adequate to examine their efficacy in any in vivo models that are available. Typically, the work consists of intensive SAR investigations around each core compound structure, with measurements being made to establish the magnitude of activity and selectivity of each compound.


HitGen has a series of capabilities supporting compound design and SAR. HitGen provide services in hit expansion by DEL, strcutre-based design, parallel synthesis, biochemical assays, biophysical assays, cellular assays, permeability and solubility study, ADME and DMPK.

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