Fragment‐based drug discovery (FBDD) is now established as a complementary approach
to high‐throughput screening (HTS). Contrary to HTS, where large libraries of drug‐like …

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 …

Fragment-based drug discovery (FBDD) has grown and matured to a point where it is
valuable to keep track of its extent and details of application. This Perspective summarizes …

Covalent drugs have experienced significant renewed interest in drug discovery. This
resurgence has been accompanied by a better understanding of the reactivity relationships …

Designing covalent inhibitors is increasingly important, although it remains challenging.
Here, we present covalentizer, a computational pipeline for identifying irreversible inhibitors …

Fragment based drug discovery has long been used for the identification of new ligands and
interest in targeted covalent inhibitors has continued to grow in recent years, with high …

The continuous approval of covalent drugs in recent years for the treatment of diseases has
led to an increased search for covalent agents by medicinal chemists and computational …

Fragment-based drug discovery (FBDD) has become a mainstream technology for the
identification of chemical hit matter in drug discovery programs. To date, the food and drug …

Targeted covalent inhibitors (TCIs) are considered to be an important component in the
toolbox of drug discovery and about 30% of currently marketed drugs are TCIs. Although …

The epidermal growth factor receptor (EGFR) has been shown to be extremely important in
numerous signaling pathways, particularly those involved in cancer progression. Many …