Covalent Compounds

Covalent screening has become an integral part of Drug Discovery process and started to play essential role in hit finding, development of new screening technics, identification of new protein targets and in assessment of their drugability. A number of successful examples, when converting lead molecule to covalent binders leads to increase of the overall efficacy, acknowledged this approach as a powerful tool for drug design.

In spite of high interest within last few years, the number of commercially accessible covalent binders remains still very limited with poor structural diversity and low attractiveness of core structures.

To create a reliable source of covalent modifiers Enamine has focused on elaboration of parallel synthesis approaches to synthesize series of new valuable covalent compounds. Careful choice of appropriately reactive building blocks, optimization of the reaction conditions and elaboration of HPLC purification methods have already allowed synthesis of thousands of different covalent binders and resulted in enumeration of REAL arrays – new covalent readily accessible compounds that can be confidently synthesized within 4 weeks only.