ABSTRACT
Prior to the 1980s, the discovery of a marketable bioactive molecule relied upon a company’s ability to structurally modify known active molecules to yield a candidate with an improved activity profile. The discovery of structural features that were accountable for new activity modes was most often serendipitous and rarely through deductive analysis. For the most part, companies relied upon the chemist’s skills in synthesis and the pharmacologist’s observational abilities to find the developmental candidate or “lead” that would yield a “new and improved” therapeutic or agrochemical entity. These activities required legions of chemists and development scientists, and tedious and expensive time lines to the clinic and market. New targets and approaches were needed and sought.
