BIONET Covalent Fragment Library

Drugs that covalently bond to their biological targets have a long history in drug discovery. There is an increased interest in covalent therapeutics in the literature and recent years have witnessed a significant increase in the number of drug candidates with covalent mechanism of action progressing through clinical trials or being approved; moreover, about 30% of marketed drugs are covalent binders. Screening fragments has its challenges, principally, the requirement for sensitive biophysical assays due to the low affinity of typical fragment hits. Fragments that can form a covalent bond with their target protein can overcome this challenge due to the increased affinity between the fragment and the target.

Key Organics has assembled a collection of covalent fragments containing cysteine-reactive electrophiles such as chloroacetamides and acrylamides.