lead optimisation

https://doi.org/10.1351/goldbook.14156
Process in which the drug-like properties of an initial lead or lead series are improved.
Note: Typically, biological activity will be enhanced, in vivo efficacy will be demonstrated, and compounds with a physicochemical, pharmacological, and toxicological profile consistent with progression to the clinic will be identified.
Source:
PAC, 2011, 83, 1129. (Glossary of terms used in biomolecular screening (IUPAC Recommendations 2011)) on page 1147 [Terms] [Paper]