Medicinal chemistry has become the most time-consuming step in the dru
g discovery process, and new discovery technologies are likely to incr
ease the burden on lead optimization and refinement. Although medicina
l chemists are able to optimize hits/leads very quickly and successful
ly with regard to potency, improving the kinetic, metabolic and toxico
logical properties of a compound remains a difficult challenge. The au
thor examines the role of the medicinal chemist in this increasingly c
omplex and changing environment.