Abstract

Future success for most pharmaceutical companies will depend on innovation leading to the discovery of new drugs that provide clear medical benefit to patients when compared to current therapies. There are three key steps in the discovery process; discovery of relevant biological targets, generation of ‘lead’ compounds and the optimization of leads to give potent, efficacious and safe drugs. There are, increasingly, many ‘biological’ approaches to treatment, such as gene therapy or antisense therapy. This article is focused solely on key aspects of lead generation for compounds of low molecular weight 1 . Part 1 focuses on aspects of biological target identification. Part 2, to be published in the February issue of Drug Discovery Today , will address lead generation, with special emphasis on the measurement of diversity within and between compound libraries.

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