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Journal of Medicinal Chemistry|July 23, 2020
Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune DiseasesBin Ma, Tonika Bohnert, Kevin L Otipoby, et al.ACS Medicinal Chemistry Letters|April 22, 2022
Discovery of Phospholipase D Inhibitors with Improved Drug-like Properties and Central Nervous System PenetranceTricia L May-Dracka, Fang Gao, Brian T Hopkins, et al.Bioorganic & Medicinal Chemistry Letters|December 20, 2022
Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse modelGeorge H Vandeveer, Robert M Arduini, Darren P Baker, et al.Bioorganic & Medicinal Chemistry|May 30, 2019
Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screensBrian T Hopkins, Eris Bame, Noah Bell, et al.Bioorganic & Medicinal Chemistry|July 27, 2021
Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitorsBrian T Hopkins, Eris Bame, Noah Bell, et al.Journal of Medicinal Chemistry|April 7, 2026
Leveraging Kinase Drugs for Neurosciences: Discovery of Selective, CNS-Penetrant Reversible Bruton's Tyrosine Kinase Inhibitors as Therapeutics for NeuroinflammationBrian T Hopkins, Isaac E Marx, Harlod George Vandeveer, et al.Clinical & Translational Immunology|June 18, 2021
Next-generation Bruton's tyrosine kinase inhibitor BIIB091 selectively and potently inhibits B cell and Fc receptor signaling and downstream functions in B cells and myeloid cellsEris Bame, Hao Tang, Jeremy C Burns, et al.Journal of Medicinal Chemistry|November 4, 2021
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple SclerosisBrian T Hopkins, Eris Bame, Bekim Bajrami, et al.Journal of Medicinal Chemistry|May 7, 2024
Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple SclerosisMartin K Himmelbauer, Bekim Bajrami, Rebecca Basile, et al.Pageof 2