Uptake of new technology in lead optimization for drug discovery

The arrival of combinatorial chemistry in pharmaceutical lead optimization has usually been greeted with reservation by chemists at the bench - it isn't what medicinal chemists have trained for years to do. The apparent mindless application of automated synthesis seems to have the potential to convert the demand for skilled chemists to one of machine operators. At Glare Wellcome, this initial concern has been converted to a widespread embrace of newer technologies and techniques in the ever-increasing race for new drugs. The author describes how this process has evolved over the past five years, and how the experiences, both successful and otherwise, provide both a salutary lesson and a useful reference for the changes that are undoubtedly yet to come.