Receptor‐Assisted Combinatorial Chemistry: Thermodynamics and Kinetics in Drug Discovery

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Abstract
Current drug discovery using combinatorial chemistry involves synthesis followed by screening, but emerging methods involve receptor‐assistance to combine these steps. Adding stoichiometric amounts of receptor during library synthesis alters the kinetics or thermodynamics of the synthesis in a way that identifies the best‐binding library members. Three main methods have emerged thus far in receptor‐assisted combinatorial chemistry: dynamic combinatorial libraries, receptor‐accelerated synthesis, and a new method, pseudo‐dynamic libraries. Pseudo‐dynamic libraries apply both thermodynamics and kinetics to amplify library members to easily observable levels, and attain selectivity heretofore unseen in receptor‐assisted systems.

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