There has been tremendous progress in covalent inhibitors as evidenced by the ascent of
innovative electrophilic warheads with suppressed non‐specific reactivity but enhanced …

Over the past decade targeted covalent inhibitors have undergone a renaissance due to the
clinical validation and regulatory approval of several small molecule therapeutics that are …

Covalent drugs exert potent and durable activity by chemical modification of the
endogenous target protein in vivo. To maximize the pharmacological efficacy while …

Covalent targeting has experienced a revival in the last decade, especially in the area of
protein kinase inhibitor development. Generally, covalent inhibitors make use of an …

Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

There is a resurging interest in compounds that engage their target through covalent
interactions. Cysteine's thiol is endowed with enhanced reactivity, making it the nucleophile …

Targeted covalent inhibitors have become an integral part of a number of therapeutic
protocols and are the subject of intense research. The mechanism of action of these …

Covalent probes coupled with chemical proteomics represent a powerful method for
investigating small molecule and protein interactions. However, the creation of a reactive …

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 inhibitors have recently seen a revival in medicinal chemistry. Inhibitors
addressing non-catalytic cysteine residues with weakly reactive electrophiles have been …