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Exploring 2-Sulfonylpyrimidine Warheads as Acrylamide Surrogates for Targeted Covalent Inhibition: A BTK Story

Moraru R, Valle-Argos B, Minton A, … Baud MGJ · J Med Chem 2024 · J Med Chem 67(16):13572-13593

BTK Tyrosine kinase Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling PhosphoSens

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More publications on BTK

Bruton's tyrosine kinase inhibition reduces disease severity in a model of secondary progressive autoimmune demyelination

Evonuk KS, Wang S, Mattie J, … Marušić S · Acta Neuropathol Commun 2023

Controlling Ibrutinib's Conformations about Its Heterobiaryl Axis to Increase BTK Selectivity

Toenjes ST, Heydari BS, Albright ST, … Gustafson JL · ACS Med Chem Lett 2023

Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition

Liclican A, Serafini L, Xing W, … Feng JY · Biochim Biophys Acta Gen Subj 2020

Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

Guo WH, Qi X, Yu X, … Wang J · Nat Commun 2020

Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA-Encoded Chemical Library

Cuozzo JW, Centrella PA, Gikunju D, … Clark MA · Chembiochem 2017

Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans

Evans EK, Tester R, Aslanian S, … Westlin WF · J Pharmacol Exp Ther 2013

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