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Review
. 2020 Apr 17;21(8):1080-1100.
doi: 10.1002/cbic.201900674. Epub 2020 Feb 4.

Covalent Small Molecules as Enabling Platforms for Drug Discovery

Samuel E Dalton  1 , Sebastien Campos  2
Affiliations
Review

Covalent Small Molecules as Enabling Platforms for Drug Discovery

Samuel E Dalton et al. Chembiochem. .

Abstract

Covalent drugs have experienced significant renewed interest in drug discovery. This resurgence has been accompanied by a better understanding of the reactivity relationships required to engage selective covalent bonds between nucleophilic proteins and electrophilic small molecules. As a result, researchers have come to the realisation that covalent molecules could also represent useful and novel tools aimed at supporting medicinal chemistry programmes. This review surveys the increasing number of drug discovery platforms employing covalent chemistries, and highlights the utility of these techniques for identifying and characterising small molecules and biological targets.

Keywords: ABPP; PROTAC; covalent; fragments; photoaffinity.

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