Relative Selectivity of Covalent Inhibitors Requires Assessment of Inactivation Kinetics and Cellular Occupancy: A Case Study of Ibrutinib and Acalabrutinib
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Last updated 04 abril 2025

Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK)

Frontiers Bruton's Tyrosine Kinase Inhibitors Impair FcγRIIA-Driven Platelet Responses to Bacteria in Chronic Lymphocytic Leukemia

Kinetic mechanisms of covalent inhibition - ScienceDirect

A Perspective on the Kinetics of Covalent and Irreversible Inhibition

Case Study - COVALfinder to Study Irreversible EGFR Drugs

Proteomics and Beyond: Cell Decision-Making Shaped by Reactive Electrophiles: Trends in Biochemical Sciences

BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies, Journal of Hematology & Oncology
Btk turnover in Ramos cells. Target occupancy as a function of time

Structure-Function Relationships of Covalent and Non-Covalent BTK Inhibitors. - Abstract - Europe PMC
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