Solutions Case Studies
Download DocumentApplying combinatorial chemistry to lead optimization
As functional genomics and structural bioinformatics reveal more and more information about molecular targets, research organizations have begun exploiting this information to create focused combinatorial libraries. The rationale is simple. Libraries designed to meet specific structural criteria can help relieve the bottleneck that has resulted from the large number of "hits," or potential drug candidates, produced by the comparatively random screening of large, diverse compound collections.
In focused library generation, chemists often know something about the target's active site, and this information can be exploited in the next stage of library design: reagent selection.
While the rationale comes easily, the practice of developing and building focused libraries is far from simple.
Focused libraries require more flexibility, particularly with respect to chemistry. The goal is to make what you really need to screen. Consequently, focused library creation requires more library planning and analysis, often involves more difficult chemistry, and necessitates purification steps because the chemistry is often conducted in solution phase rather than solid phase.
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