ABSTRACT

Today, the most common method of drug discovery is a process that starts by identifying a small-molecule starting point (a hit) and then optimizes its biological, physical, and pharmaceutical properties to generate a lead, and eventually a drug candidate, through an iterative process of design, synthesis, and testing. For the sake of consistency and clarity, a hit is defined as a small molecule of confirmed structure and purity that exhibits biological activity at some defined threshold in a particular biological test.