Automated medicinal chemistry.

With the advent of high throughput technologies in biological screening in the 1980s, providing sufficient numbers of small molecules for screening became a bottleneck in the drug discovery process. Combinatorial chemistry was the first attempt by chemists to address this issue. However, since its first applications, combinatorial chemistry has evolved rapidly into diverse fields. This review will focus on the evolution and the current status of what we refer to today as automated medicinal chemistry.