Lead Optimization

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Lead Optimization

[/vc_column_text][dt_gap height=”10″][vc_column_text]Making the right compounds.  Compound synthesis is typically the most costly part of preclinical discovery efforts.  Despite this, many groups persist in focusing on “numbers of compounds” rather than “quality of compounds”.  This results in the wasted effort of making compounds that should have been predicted as not being viable drugs.

Using synthesis resources effectively.  We thoroughly evaluate each issue to be addressed in view every synthetic target. We employ computational methods to influence and rank the design of synthetic targets in these ways:

  • Predicting target activity
  • Predicting physical properties such as solubility, and lipophilicity
  • Understanding transporter substrate and/or efflux susceptibility
  • Predicting metabolic risks
  • Predicting off-target activities such as hERG and phospholipidosis
[/vc_column_text][/vc_column][vc_column width=”1/2″][dt_gap height=”10″][vc_column_text]Identifying a clinical candidate comes from finding the compound(s) that best balance all relevant activity and risk factors.  Our multi-disciplinary team has a demonstrated track record of optimizing against multiple parameters including these:

  • Target potency
  • Selectivity
  • Permeability and efflux
  • Exposure and free fraction at the site of action, and susceptibility to transporters
  • Maintaining excellent physical properties
  • Metabolic rate, disposition, and knowledge of reactive metabolites