incorporates an α-chloroacetamide. These warheads show increasing reactivity when matched molecular pairs are reacted with glutathione, with the α-chloroacetamide being the most reactive. All analogs were then docked into the co-crystal structure (8RPC). 2-4 were predicted to maintain the binding mode of TCMDC-135051 (1), forming the same key interactions discussed above, while projecting sufficiently out of the pocket to form covalent bonds with Cys368 (Fig. ).