Definitions for "Lead Optimization"
The synthetic modification of a biologically active compound, to fulfill stereo electronic, physicochemical, pharmacokinetic and toxicological clinical usefulness.
The process of creating the most advantageous lead drug compound, in terms of its biological activity, by refining its chemical and pharmacological properties.
The process of converting a putative lead compound ("hit") into a therapeutic drug with maximal activity and minimal side affects, typically using a combination of computer-based drug design, medicinal chemistry and pharmacology
Further research to determine if a bound lead is able to stimulate a target. This stimulation is usually in terms of changes in gene expression that is assayed using gene expression microarrays. Additional tests include toxicity to insure that the lead is not toxic or has other undesirable side effects.