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Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton?s Tyrosine Kinase

Journal Article · · J. Med. Chem.

Research Organization:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Organization:
DOE - Office Of Science; INDUSTRY
OSTI ID:
1902355
Journal Information:
J. Med. Chem., Journal Name: J. Med. Chem. Journal Issue: (21) Vol. 65
Country of Publication:
United States
Language:
ENGLISH

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The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo journal February 2012
Discovery of a Potent and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase with Oral Anti-Inflammatory Activity journal April 2021
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A Fast and Clean BTK Inhibitor journal May 2020
Pharmacodynamic Analysis of BTK Inhibition in Patients with Chronic Lymphocytic Leukemia Treated with Acalabrutinib journal February 2020
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Simultaneous Inhibition of PI3Kδ and PI3Kα Induces ABC-DLBCL Regression by Blocking BCR-Dependent and -Independent Activation of NF-κB and AKT journal January 2017
Tec Kinases Mediate Sustained Calcium Influx via Site-specific Tyrosine Phosphorylation of the Phospholipase Cγ Src Homology 2-Src Homology 3 Linker journal June 2004
Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase journal January 2007
Bruton’s tyrosine kinase (BTK) inhibitors in treating cancer: a patent review (2010-2018) journal March 2019
Medicinal Chemistry Strategies for the Development of Bruton’s Tyrosine Kinase Inhibitors against Resistance journal May 2022
Discovery of Pteridine-7(8H)-one Derivatives as Potent and Selective Inhibitors of Bruton’s Tyrosine Kinase (BTK) journal January 2022
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase journal February 2020
Bruton's tyrosine kinase (Btk) inhibitor tirabrutinib suppresses osteoclastic bone resorption journal June 2019
Regioselective Derivatizations of a Tribrominated Atropisomeric Benzamide Scaffold journal January 2015
Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma journal January 2010
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase journal August 2019
Second-generation inhibitors of Bruton tyrosine kinase journal September 2016
Discovery of the Bruton’s Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one, by Fragment-Based Drug Design journal August 2021
Bruton's Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: A potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints journal February 2013
Targeting Bruton's tyrosine kinase in B cell malignancies journal March 2014
Bruton Tyrosine Kinase Inhibitors journal November 2019
Spebrutinib (CC-292) Affects Markers of B Cell Activation, Chemotaxis, and Osteoclasts in Patients with Rheumatoid Arthritis: Results from a Mechanistic Study journal November 2019
Developing Irreversible Inhibitors of the Protein Kinase Cysteinome journal February 2013
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Btk Inhibitors: A Medicinal Chemistry and Drug Delivery Perspective journal July 2021
Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success journal November 2009
Discovery of Reversible Covalent Bruton’s Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib) journal March 2022

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