Targeted covalent inhibitors

Targeted covalent inhibitors (TCIs) or Targeted covalent drugs are rationally designed inhibitors that bind and then bond to their target proteins. These inhibitors possess a bond-forming functional group of low chemical reactivity that, following binding to the target protein, is positioned to react rapidly with a proximate nucleophilic residue at the target site to form a bond.[1]

This illustration describes the mechanism by which covalent drugs irreversibly bind and modify the protein, e.g. silencing its activity
  1. ^ Cite error: The named reference Singh_2011 was invoked but never defined (see the help page).