Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis
Di Paolo, Julie A, Huang, Tao, Balazs, Mercedesz, Barbosa, James, Barck, Kai H, Bravo, Brandon J, Carano, Richard A D, Darrow, James +23 more·2011·Nature Chemical Biology
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- Efficacy and safety of branebrutinib (BMS-986195), an irreversible Bruton's tyrosine kinase inhibitor, for the treatment of rheumatoid arthritis: a phase 2a, randomised, double-blind, placebo-controlled studyMikkel Østergaard, Espen Andre Haavardsholm, Miroslawa Nowak, Yi Luo, Jessica Landis, Aberra Fura, Chahin Pachaï, Duncan Rotich, Yanlin Wang-Fischer, Leonidas N. Carayannopoulos et al. · 2026 · The Lancet Rheumatology
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- Targeting DAMP Activation of Toll-Like Receptors: Novel Pathways to Treat Rheumatoid Arthritis?Theresa H. Page, Kim S. · 2012 · InTech eBooks
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- Innate and adaptive immunomodulation by Bruton’s tyrosine kinase (BTK) inhibitors: An emerging treatment for multiple sclerosisDejan Jakimovski, Bianca Weinstock‐Guttman, Robert Zivadinov · 2023 · Elsevier eBooks
- Development of 7H-pyrrolo[2,3-d]pyrimidin-4-amine Derivatives Using QSARINS Tool as BTK Inhibitors for the Treatment of Rheumatoid ArthritisShital Manoj Patil, Kalyani Dhirendra Asgaonkar, Pradnya Magdum, Vaishnavi Chinde, Aishwarya M. Edake, Akshata Parashram Naik · 2023 · Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
- Small Molecule Immunosuppressants in Inflammatory DiseaseRoy Fleischmann · 2017 · Elsevier eBooks
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- Resistance to Bruton’s Tyrosine Kinase Signaling Pathway Targeted TherapiesYaya Chu, Mitchell Stuart Cairo, Auke Beishuizen · 2019 · Resistance to targeted anti-cancer therapeutics
- Bayesian machine learning to discover Bruton’s tyrosine kinase inhibitorsJian Wang, Ting Ran, Yadong Chen, Tao Lu · 2019 · Chemical Biology & Drug Design
- Development of piperidinyl dipyrrrolopyridine-based dual inhibitors of Janus kinase and Bruton’s tyrosine kinase: a potential therapeutic probability to deal with rheumatoid arthritisNeelam Pery, Nayab Batool Rizvi, Muhammad Imtiaz Shafiq · 2020 · Journal of Molecular Modeling
- Ibrutinib: a strong candidate for the future of mantle cell lymphoma treatmentLiang Zhang, Kate Juliet Newberry, Michael L. Wang · 2013 · Expert Review of Clinical Immunology
- ReplyLindsay E. Nyhoff, Leslie J. Crofford, Peggy L. Kendall · 2016 · Arthritis & Rheumatology
- Comprehensive Characterization of BTK Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Non-covalent Mechanistic SignaturesAntonia C. Darragh, Andrew M. Hanna, Justin Lipner, Nicole B. Servant, Alastair J. King, Mirza Jahic · 2024 · bioRxiv (Cold Spring Harbor Laboratory)
- Use of Signaling Pathways as Therapeutic Targets for Blood CancerJohanna Mondésir, Pierre Sujobert, Mark Alan Murakami, Marie‐Anne Hospital, Didier Bouscary, Jérôme Tamburini · 2014 · International Journal of Hematologic Oncology
- Novel Potent and Selective Bruton's Tyrosine Kinase (BTK) InhibitorLichuan Liu, Jason S. Halladay, Susan Wong, Melis Coraggio, Matthew Baumgardner, Sashi V. Gopaul, Jason W. Boggs, Peter Kuebler, Xiang Liao, Joseph W. Lubach et al. · 2011
- Investigation of the roles of acid sensing proteins in rheumatoid arthritisFawaz Albloui · 2016 · White Rose eTheses Online (University of Leeds, The University of Sheffield, University of York)
- Protein Kinase Inhibitors for the Treatment of Multiple SclerosisAna Martı́nez, Carmen Gil · 2019 · Royal Society of Chemistry eBooks
- Development of Small Molecule Kinase Degraders as Chemical Biology Probes and Cancer TherapiesDennis Dobrovolsky · 2018 · Digital Access to Scholarship at Harvard (DASH) (Harvard University)
- Discovery and Process Development of BIIB068: A Reversible Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Autoimmune DiseasesBin Ma, Chaomin Li, Brian T. Hopkins, Lloyd C. Franklin, Robbie Chen, Tamera Mack, Daniel B. Patience, William F. Kiesman, Erin M. O’Brien · 2020 · ACS symposium series
- Allosteric regulation of BTK by the PHTH domain and small moleculesNeha Amatya · 2021
- Medicinal Attributes of Heterocyclic Compounds in Rheumatoid Arthritis: Recent Developments and SAR StudiesVikram Jeet Singh, Bharti Sharma, Pooja A. Chawla · 2022 · Current Topics in Medicinal Chemistry
- Literature Search and ReviewDoug Auld, Wendy Lea, Mindy I. Davis, Anton M. Simeonov · 2011 · Assay and Drug Development Technologies
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- Drug PropertiesSiamak Cyrus Khojasteh, Harvey Wong, Donglu Zhang, Cornelis E. C. A. Hop · 2022 · Springer eBooks
- A structure-based approach to kinase inhibition based on the natural product (-)-TAN-2483BJordan A. J. McCone · 2020
- Pharmacologic Features of Drugs Targeting Bruton's Tyrosine Kinase ( BTK )Joel McCay and, John G. Gribben · 2023
- Recent Progress of Irreversible BTK InhibitorsWenxi Zhao · 2024 · Transactions on Materials Biotechnology and Life Sciences
- Structure-based design of novel pyrrolo[1,2-a]quinoxalin-4(5H)-one derivatives as potent noncovalent Bruton's tyrosine kinase (BTK) inhibitorsChaoquan Tian, Wenjie Liao, Zhixiao Yu, Hongguang Du, Haoming Song, Wenyi Mei, Zhenjiang Zhao, Yanyan Diao, Zhuo Chen, Honglin Li · 2025 · Bioorganic & Medicinal Chemistry Letters
- Molecular regulation of IL-2 inducible T-cell kinase (Itk) and the Tec kinases: A combined experimental and computational study, with emphasis on the N-terminal Pleckstrin Homology domainScott E. Boyken · 2013
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- Targeting Bruton’s Tyrosine Kinase in CLL: Selectivity, Resistance Mechanisms, and Emerging Therapeutic StrategiesEduardo Bravo, Claudia C. Pastrana, Erica N. Lamkin, Katarzyna Ciurko, Justin Taylor · 2026 · Cells
- Tearing Down Scientific Boundaries: Frontiers in Medicinal Chemistry 2026Pascal Heitel, Philipp Barbie, Alessia Gambardella, Marta Pinto, Felix Pape, Anika Tarasewicz, Gerhard Heßler, Bernhard Wünsch, Matthias Schiedel, Christina Lamers · 2026 · ChemMedChem
- Bruton's Tyrosine Kinase Inhibitors: Mechanisms, Efficacy, Toxicities and Applications for the Treatment of Human DiseasesMiao Sun, Dengju LI, Jia Wei · 2026 · MedComm
- Neuron myelination is accelerated by Bruton’s tyrosine kinase inhibition via microglial extracellular vesiclesMatteo Tartaglia, Arianna Ioni, Mariassunta De Luca, Laura Vilardo, Igea D’Agnano, Antonella Conte, Cristina Limatola, Myriam Catalano · 2026 · Frontiers in Cellular Neuroscience
- BindingDB Entry 50002514: Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis.BindingDB · 2020 · UC San Diego
- BindingDB Entry 50000272: Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.BindingDB · 2019 · UC San Diego
- BindingDB Entry 50001805: The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.BindingDB · 2020 · UC San Diego
- BindingDB Entry 50017377: Emerging small-molecule inhibitors of the Bruton's tyrosine kinase (BTK): Current development.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50023582: Design, Synthesis, and Biological Evaluation of Pyrrolo[1,2-a]quinoxalin-4(5H)-one Derivatives as Potent and Orally Available Noncovalent Bruton's Tyrosine Kinase (BTK) Inhibitors.BindingDB · 2026 · UC San Diego
- BindingDB Entry 7945: Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA-Encoded Chemical Library.BindingDB · 2017 · UC San Diego
- BindingDB Entry 50016662: Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50011293: Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.BindingDB · 2022 · UC San Diego
- BindingDB Entry 50045492: Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.BindingDB · 2016 · UC San Diego
- BindingDB Entry 50008819: Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50046859: Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.BindingDB · 2017 · UC San Diego
- BindingDB Entry 50007921: The Exploration of Chirality for Improved Druggability within the Human Kinome.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50010916: Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50008415: Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50012032: Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.BindingDB · 2022 · UC San Diego
- BindingDB Entry 50011454: Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.BindingDB · 2022 · UC San Diego
- BindingDB Entry 50008045: Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50002240: Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.BindingDB · 2020 · UC San Diego
- BindingDB Entry 50045472: Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold.BindingDB · 2016 · UC San Diego
- BindingDB Entry 50007980: Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50000297: Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.BindingDB · 2019 · UC San Diego
- BindingDB Entry 50047871: Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two LockeBindingDB · 2018 · UC San Diego
- BindingDB Entry 50012914: Discovery and Evaluation of Pyrazolo[3,4-BindingDB · 2022 · UC San Diego
- BindingDB Entry 50018849: Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases.BindingDB · 2024 · UC San Diego
- BindingDB Entry 50009603: Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50018682: 4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry.BindingDB · 2024 · UC San Diego
- BindingDB Entry 50003050: Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors.BindingDB · 2020 · UC San Diego
- BindingDB Entry 50046425: Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.BindingDB · 2016 · UC San Diego
- BindingDB Entry 50015799: Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50040780: Rational design of highly selective spleen tyrosine kinase inhibitors.BindingDB · 2013 · UC San Diego
- BindingDB Entry 50040034: Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.BindingDB · 2013 · UC San Diego
- BindingDB Entry 50013934: Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors.BindingDB · 2022 · UC San Diego
- BindingDB Entry 50049042: Discovery of novel BTK inhibitors with carboxylic acids.BindingDB · 2019 · UC San Diego
- BindingDB Entry 50046650: Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).BindingDB · 2016 · UC San Diego
- BindingDB Entry 50001941: Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.BindingDB · 2020 · UC San Diego
- BindingDB Entry 50011285: Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.BindingDB · 2022 · UC San Diego
- BindingDB Entry 50045011: Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors.BindingDB · 2016 · UC San Diego
- BindingDB Entry 50044550: Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.BindingDB · 2015 · UC San Diego
- BindingDB Entry 50003054: Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk.BindingDB · 2020 · UC San Diego
- BindingDB Entry 50002048: Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors.BindingDB · 2020 · UC San Diego
- BindingDB Entry 50016410: Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50046550: Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.BindingDB · 2016 · UC San Diego
- BindingDB Entry 50007714: Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50046163: Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase.BindingDB · 2016 · UC San Diego
- BindingDB Entry 50034114: Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.BindingDB · 2012 · UC San Diego
- BindingDB Entry 50002854: Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.BindingDB · 2020 · UC San Diego
- BindingDB Entry 50017556: Discovery of selective irreversible inhibitors of B-Lymphoid tyrosine kinase (BLK).BindingDB · 2023 · UC San Diego
- BindingDB Entry 50017353: Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50015211: Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50013640: Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry.BindingDB · 2022 · UC San Diego
- BindingDB Entry 50044301: Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.BindingDB · 2015 · UC San Diego
- BindingDB Entry 50010667: 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).BindingDB · 2021 · UC San Diego
- BindingDB Entry 50007369: Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50000587: Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.BindingDB · 2019 · UC San Diego
- BindingDB Entry 50045572: TR-FRET binding assay targeting unactivated form of Bruton's tyrosine kinase.BindingDB · 2016 · UC San Diego
- BindingDB Entry 50000744: Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.BindingDB · 2020 · UC San Diego