New chemical warheads for covalent drug discovery

Over the past two decades, the pharmaceutical industry has witnessed an exponential growth in approved covalent drugs. The majority of such drugs incorporate a chemical warhead, a mild electrophilic reactive functional group that forms covalent bonds in a reversible or irreversible manner with nucleophilic aminoacid residues. The aim of this proposal is to assess the viability of a new chemical warhead in the discovery of novel kinase inhibitors.