… To confirm that the compound really binds covalently to BTK, we … The results indicated that
our compound bound covalently to … of NH 2 in the carboxamide group of compound 26 with an …

… covalent inhibitors of Bruton’s tyrosine kinase (BTK) based on an aminopyrazole carboxamide
… Compared to acrylamide-based covalent reactive groups leading to irreversible protein …

… Bruton's tyrosine kinase (BTK) is a member of the Tec kinase … of potent and selective covalent
irreversible BTK inhibitors. … Bruton's tyrosine kinase (BTK) is a member of the Tec family …

… Bruton’s tyrosine kinase (Btk) is a critical enzyme for the development and function of B
cells… form a covalent bond to a specific cysteine present in Btk, and the carboxylic acid amide …

… The Bruton's tyrosine kinase gene is expressed throughout B cell differentiation, from early
precursor B cell stages preceding immunoglobulin gene rearrangement up to mature B cell …

… covalent inhibitors of Bruton’s tyrosine kinase (BTK), we evaluated multiple techniques
for characterizing covalent inhibitors. Several methods qualitatively support the covalent …

… selective covalent 4-oxo-4,5-dihydro-3H-1-thia-3,5,8-triazaacenaphthylene-2-carboxamide
BTK … a noncatalytic cysteine residue (Cys481) for covalent bond formation. Compound 27 is …

… It selectively binds to Cys481 of the target BTK via a covalent bond, thereby inhibits its
autophosphorylation to block the BCR signaling pathway [17]. Unfortunately, owing to multiple …

… of BTK that covalently binds to Cys481 in the kinase domain. Though covalent BTK inhibitors,
such … For instance, the Michael receptor portions of covalent inhibitors raise the concern of …

… We selected the Bruton Tyrosine Kinase (BTK) as a particularly relevant test case to assess
the suitability of 2-SP warheads in TCI design. BTK plays a key role in signal transduction …