The invention relates to a method of identifying selective covalently binding inhibitors by using a reversibly inhibiting scaffolds modified by a warhead comprising a fast-reacting Michael acceptor moiety and a linker of different length, determining kinact, and replacing the warhead of the covalently binding inhibitor with the highest kinact by a warhead comprising a moderately reacting Michael acceptor.
METHOD FOR IDENTIFYING PI3 KINASE-ALPHA INHIBITORS / C. Borsari, M. Wymann.
METHOD FOR IDENTIFYING PI3 KINASE-ALPHA INHIBITORS
C. Borsari;
2022
Abstract
The invention relates to a method of identifying selective covalently binding inhibitors by using a reversibly inhibiting scaffolds modified by a warhead comprising a fast-reacting Michael acceptor moiety and a linker of different length, determining kinact, and replacing the warhead of the covalently binding inhibitor with the highest kinact by a warhead comprising a moderately reacting Michael acceptor.
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