Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency.
Absztrakt G12C mutant KRas is considered druggable by allele-specific covalent inhibitors due to the nucleophilic character of the oncogenic mutant cysteine at position 12. Discovery of these inhibitors requires the optimization of both covalent and noncovalent interactions. Here, we report covalent fragment…