Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …

Covalent chemistry is a versatile approach for expanding the ligandability of the human
proteome. Activity-based protein profiling (ABPP) can infer the specific residues modified by …

An important consideration in drug discovery is the prioritization of tractable protein targets
that are not only amenable to binding small molecules, but also alter disease biology in …

Cyanamides have emerged as privileged scaffolds in covalent inhibitors of deubiquitinating
enzymes (DUBs). However, many compounds with a cyanopyrrolidine warhead show cross …

High-affinity monovalent ligands for lectins are challenging to develop due to weak binding
interactions. This study investigates the potential of rationally designed covalent ligands …

Molecular glues that engage protein complexes have transformed the study of cell biology
and have had a direct impact on clinical oncology. However, the identification of new glue …

Covalent hits for drug discovery campaigns are neither fantastic beasts nor mythical
creatures, they can be routinely identified through electrophile-first screening campaigns …

Based on current challenges of poor targeting and limited choices in chemical control
methods of cyanobacterial blooms (CBs), identifying new targets is an urgent and formidable …

Chemical proteomics has advanced small molecule ligand discovery by providing insights
into protein-ligand binding mechanism and enabling medicinal chemistry optimization of …

Recent progress in the realm of covalent inhibitors and covalent drugs, placing a distinct
emphasis on precisely defining the scope and outlining key objectives. The scope of this …