Biocompatible reactions: advances in kinetic target-guided synthesis

Interest in developing biocompatible reactions continues to grow almost unabated. This results from its relevance to all aspects of drug discovery, ranging from lead discovery via combinatorial chemistry, target-guided synthesis, to proteomics and DNA research. This review summarizes important findings in the development of noncovalent inhibitors of biomolecules using biocompatible reactions through kinetic target-guided synthesis (KTGS). KTGS is an attractive area of research capable of probing the macromolecular complexity and dynamics of biomolecules. It is an unconventional drug discovery approach wherein a biological target is actively engaged in assembling its own bidentate ligand from an array of building blocks. The review showcases the various types of biocompatible reactions used for the identification of inhibitors via KTGS.