Soft Electrophiles

Recent research has shown that covalent inhibitors have a number ofadvantages in drug discovery, especially for targets where complete inactivation is required. ASINEX has, therefore, crafted a unique set of molecules containing mild electrophilic moieties that covalently interact with amino acid residues in the target protein. The diversity of our compounds for covalent drug discovery ranges from natural product-like scaffolds to macrocycles, creating multiple opportunities in hit generation for a selected target. All our soft electrophile compounds possess a reactive “warhead” which is designed to interact with a nucleophilic residue at the binding site while the remaining part of the compound is deemed to govern specific recognition.Examples of efficient electrophilic warheads include chloroacetamides, acrylamides, epoxides, nitriles, and electron-deficient ketones.
The Asinex covalent library encompasses a legacy of extensive enrichment of our compound collection with novel drug-like chemotypes based on natural product-inspired chemistry. New entities are added to the library on a regular basis to increase the number of freshly synthesized compounds that comprise this set. Due to the intrinsic reactivity of molecules containing a covalent reactive group we have implemented rigorous quality control and efficient compound management logistics (storage and handling) to ensure consistent screening results.

A number of smaller, more focused libraries (Signature Libraries) are also available for screening:

SL#019 Soft Electrophiles-1 (acrylamide derivatives)
SL#020 Soft Electrophiles-2 (heterocyclic cinnaminc acid derivatives)
SL#022 Soft Electrophiles-3 (kinase-oriented cinnaminc acid derivatives)
SL#027 Soft Electrophiles-4 (ɑ-oxyketone and spiro-lactone derivatives)
SL#037 Soft Electrophiles-5 (heteroaromatic nitrile derivatives)
Please visit our online catalog for available Covalent libraries or contact our customer support team for any additional information.