Current Topics in Medicinal Chemistry

Allen B. Reitz
Fox Chase Chemical Diversity Center, Inc.
Doylestown, PA
USA

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Facts, Figures and Trends in Lead Generation

Author(s): Rebecca Deprez-Poulain and Benoit Deprez

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

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

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.

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Article Details

VOLUME: 4
ISSUE: 6
Page: [569 - 580]
Pages: 12
DOI: 10.2174/1568026043451168