Expedition Medicines: Generative covalent chemistry to unlock difficult targets at scale

Expedition Medicines aims to drug targets lacking conventional binding pockets by learning the rules of how the electrons on small molecules interact with “microenvironments” within proteins to drive formation of covalent bonds.

While covalent chemistry has long been used to crack protein targets without clearly druggable features, it has relied on the discovery of cryptic chemically reactive residues, such as the cysteine in the switch II pocket of mutant KRAS, that are capable of forming covalent bonds...