Expertise of the month: Design and synthesis of novel TCIs

Covalent targeting plays a rising role in Medicinal Chemistry and Chemical Biology.

Targeted Covalent Inhibitors (TCIs) typically arise from structure-based design, starting from optimized reversible ligands which are then modified by attachment of an electrophilic covalent reactive (“warhead”) to address a proximal amino acid. More recently, fragment-based, tethering-based approaches and DNA-encoded libraries featuring electrophilic ligands appear as alternative strategies.

At SpiroChem, we are very active in TCIs discovery :

We will be happy to support your projects.
For more information, please contact Laurence Jung at laurence.jung@spirochem.com