Facts, Figures and Trends in Lead Generation

Authors: Deprez-Poulain, Rebecca¹; Deprez, Benoit¹

Source: Current Topics in Medicinal Chemistry, Volume 4, Number 6, February 2004 , pp. 569-580(12)

Publisher: Bentham Science Publishers

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Abstract:

The goal of this paper is to review the variety of approaches adopted to improve lead generation, and make the process easier for the chemist, faster and more likely to succeed in later phases of drug development. Our analysis shows that successful lead generation requires not only an accurate definition of the needs (to define the most relevant assay protocols and readouts), but most of all a good hit as a starting point. It also appears that teams where techniques are combined are more successful in that difficult game.

Keywords: hit-to-lead; optimisation; high throughput screening; parallel synthesis; library design; structure-property relationships; functional assay

Document Type: Review article

DOI: 10.2174/1568026043451168

Affiliations: 1: Faculte des Sciences Pharmaceutiques et Biologiques, 3, rue du Prof. Laguesse, 59000 Lille, France.

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