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Review
. 2005 Dec;16(6):666-73.
doi: 10.1016/j.copbio.2005.10.007. Epub 2005 Oct 28.

Improving success rates for lead generation using affinity binding technologies

Gergely M Makara  1 , John Athanasopoulos
Affiliations
Review

Improving success rates for lead generation using affinity binding technologies

Gergely M Makara et al. Curr Opin Biotechnol. 2005 Dec.

Abstract

Affinity technologies have been applied at several stages of the drug discovery process, ranging from target identification and purification to the identification of preclinical candidates. The detection of ligand-macromolecule interactions in lead discovery is the best studied and most powerful of these techniques. Although affinity methods have been in widespread use for about a decade, only recently have many reports emerged on their utility. Primary affinity screens of large libraries of small molecules or fragments have begun to produce results for challenging targets. Furthermore, in secondary assays affinity methods are opening new avenues to tackle important medicinal chemistry tasks.

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Figures

Figure 1
Figure 1
Compounds derived from affinity screens of drug-like molecules. See text for details.
Figure 2
Figure 2
Compounds derived from fragment-based techniques. See text for details.
See this image and copyright information in PMC

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