The goal of the lead optimisation process is to identify compounds suitable for testing in a clinical setting. In order to achieve this the medicinal chemist needs to optimise all the parameters described in the Hits-to-Leads section as well as taking into account information for dosing the compound to rats or mice. Where necessary the molecular features will be modified to optimise potency against the enzyme target, cellular and toxicity assays as well as those that govern good oral absorption, slow metabolic clearance in vivo and display activity in an animal model of the disease. This labour intensive process requires the skill of Medicinal Chemists to hone the physicochemical and biological properties of the active molecules to the level required for a clinical candidate.
