Discovery of a Potent and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase with Oral Anti-Inflammatory Activity

Pharmacodynamic analysis of BTK inhibition in patients with chronic lymphocytic leukemia treated with acalabrutinib

(2020) Anfal Alsadhan et al.   CLINICAL CANCER RESEARCH

Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

(2020) Daniela Angst et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2020) Albert Liclican et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Fenebrutinib versus Placebo or Adalimumab in Rheumatoid Arthritis: A Randomized, Double-Blind, Phase II Trial (ANDES Study)

(2020) Stanley Cohen et al.   Arthritis & Rheumatology

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)

(2019) Scott H. Watterson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bruton’s tyrosine kinase (BTK) inhibitors in treating cancer: a patent review (2010-2018)

(2019) Yifan Feng et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Review of Bruton tyrosine kinase inhibitors for the treatment of relapsed or refractory mantle cell lymphoma

(2019) C. Owen et al.   Current Oncology

Placebo-Controlled Trial of an Oral BTK Inhibitor in Multiple Sclerosis

(2019) Xavier Montalban et al.   NEW ENGLAND JOURNAL OF MEDICINE

Switch-like activation of Bruton’s tyrosine kinase by membrane-mediated dimerization

(2019) Jean K. Chung et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

(2019) Yunhang Guo et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Role of Bruton's Tyrosine Kinase in Immune Cell Signaling and Systemic Autoimmunity

(2018) Jasper Rip et al.   CRITICAL REVIEWS IN IMMUNOLOGY

Progress with covalent small-molecule kinase inhibitors

(2018) Zheng Zhao et al.   DRUG DISCOVERY TODAY

Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development

(2018) James J. Crawford et al.   JOURNAL OF MEDICINAL CHEMISTRY

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 Locked Atropisomers

(2016) Scott H. Watterson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia

(2016) John C. Byrd et al.   NEW ENGLAND JOURNAL OF MEDICINE

Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma

(2014) Hong Wu et al.   ACS Chemical Biology

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Irreversible Protein Kinase Inhibitors: Balancing the Benefits and Risks

(2012) Tjeerd Barf et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Src, Syk, and Tec family kinases: Distinct types of molecular switches

(2010) J. Michael Bradshaw   CELLULAR SIGNALLING

Targeted covalent drugs of the kinase family

(2010) Juswinder Singh et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

The Challenge of Atropisomerism in Drug Discovery

(2009) Jonathan Clayden et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION