covalent inh. of remote ALK kinase cysteine
thought-provoking proposed MoA
from ceritinib and linker opt.
J. Med. Chem., Jan. 20, 2021
Sichuan University / Tsinghua University, CN
Con B-1
The academic covalent ALKi inhibitor, Con B-1, is thought-provoking initial proof-of-concept that remote kinase cysteines might be targetable from an active-site inhibitor. The authors show that a derivative of…