In recent years, the number of drug candidates with a covalent mechanism of action
progressing through clinical trials or being approved by the FDA has increased significantly …

The use of covalent inhibitors in the field of drug discovery has attracted considerable
attention in the 2000s. As a result, more than 50 covalent drugs are currently on the market …

In the history of therapeutics, covalent drugs occupy a very distinct category. While
representing a significant fraction of the drugs on the market, very few have been …

Covalent drugs haveproved to be successful therapies for various indications, but largely
owing to safety concerns, they are rarely considered when initiating a target-directed drug …

Covalent inhibitors are recognized as an important component in drug discovery and
therapeutics. Since the first appearance of covalent inhibitors in the late 18th century, the …

Highlights•High potencies and prolonged effects achievable with covalent drugs may result
in less frequent dosing and improved therapeutic margins for patients.•Covalent inhibition …

Introduction: The design of target-specific covalent inhibitors is conceptually attractive
because of increased biochemical efficiency through covalency and increased duration of …

In the first decade of targeted covalent inhibition, scientists have successfully reversed the
previous trend that had impeded the use of covalent inhibition in drug development …

Covalent inhibition is a rapidly growing discipline within drug discovery. Many historical
covalent inhibitors were discovered by serendipity, with such a mechanism of action often …

Covalent enzyme inhibitors are widely applied as biochemical tools and therapeutic agents.
As a complement to categorization of these inhibitors by reactive group or modification site …