Covalent Compounds

Covalent screening has become an integral part of Drug Discovery process and is now playing an essential role in hit finding, development of novel screening techniques, identification of new protein targets and assessment of their drugability. Successful drug development campaigns featuring a transition to the covalent binder solidify covalent compounds as a powerful tools for drug design.

In spite of high interest within last few years, the number of commercially accessible covalent binders remains extremely 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 readily accessible covalent compounds that can be confidently synthesized within 4 weeks only.