90% OF PRODUCTS IN STOCK
ASSURED QUALITY GUARANTEED
SAME DAY DESPATCH
KG PRICING ON REQUEST
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.
Covalent Fragments On Demand
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 enumerated libraries of Covalent Fragments to compliment our off-the-shelf libraries.
We have designed the following:
- Acrylamides - 1518 compounds
- Acylcyanamides - 1273 compounds
- Alpha- beta- unsaturated esters - 566 compounds
- Chloro acetamides - 1365 compounds
- Cyano acrylamides (alpha- beta- unsaturated cyanamide) - 621 compounds
- N,N-dimethyl acrylamides (alpha- beta- unsaturated amide) - 617 compounds
- Vinyl sulfonamides - 1632 compounds
Other designs with different parameters and warheads can be provided on request.
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:
- Ease of purchasing directly through our online shop, by phone, or via e-mail
- Usually dispatched within 1 working day, from stock
- Dedicated customer relations department, real-time response
Fragment integrity & formats:
- Minimum Purity of fragments is >90% by LC-MS and/or 1H NMR with the majority being > 95%. Analytical data for every compound purchased can be provided on request.
- Fragment compounds are available in milligram or micromole amounts in powder form plated to your requirements. Bulk amounts available on request
Database Download
To download all the latest BIONET Fragment databases.
Also to receive our updates please register here.