BIONET Covalent Fragment Library

BIONET Covalent Fragments

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.

Examples of Key Organics Chloroacetamide fragments

Examples of Key Organics Acrylamide fragments

Other chemical classes are available including Epoxides; Terminal alkynes; Nitro alkyls; Isothiocyanates; 2-Chloropyridines; Michael acceptors; Aldehydes; Boronic acids; Alkyl Halides and Activated nitriles.

Stock Quantities and re-supply for follow up research.

Typically, about 95% of the compounds in our collection are available in >20mg stock quantities and over 93% of the compounds are available in >100mg stock quantities. Indeed a large proportion of our collection is available in gram quantities; this means we can ensure a very high level of re-supply of originally tested compounds.

Advantages of purchasing directly from BIONET:

Fragment integrity & formats:

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