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) (English)
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In:
Journal of Medicinal Chemistry
;
62
, 7
;
3228-3250
;
2019
- Article (Journal) / Electronic Resource
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Title: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)
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Additional title:J. Med. Chem.
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Contributors:Watterson, Scott H. ( author ) / Liu, Qingjie ( author ) / Beaudoin Bertrand, Myra ( author ) / Batt, Douglas G. ( author ) / Li, Ling ( author ) / Pattoli, Mark A. ( author ) / Skala, Stacey ( author ) / Cheng, Lihong ( author ) / Obermeier, Mary T. ( author ) / Moore, Robin ( author )
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Published in:Journal of Medicinal Chemistry ; 62, 7 ; 3228-3250
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Publisher:
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Publication date:2019-04-11
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ISSN:
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Coden:
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DOI:
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Type of media:Article (Journal)
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Type of material:Electronic Resource
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Language:English
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Source:
Table of contents – Volume 62, Issue 7
The tables of contents are generated automatically and are based on the data records of the individual contributions available in the index of the TIB portal. The display of the Tables of Contents may therefore be incomplete.
- 3171
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Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer TherapyLuan, Yepeng / Li, Jerry / Bernatchez, Jean A. / Li, Rongshi et al. | 2019
- 3184
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Battle against Vancomycin-Resistant Bacteria: Recent Developments in Chemical StrategiesDhanda, Geetika / Sarkar, Paramita / Samaddar, Sandip / Haldar, Jayanta et al. | 2019
- 3206
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State of the Art in Respiratory Syncytial Virus Drug Discovery and DevelopmentCockerill, G. Stuart / Good, James A. D. / Mathews, Neil et al. | 2019
- 3228
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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)Watterson, Scott H. / Liu, Qingjie / Beaudoin Bertrand, Myra / Batt, Douglas G. / Li, Ling / Pattoli, Mark A. / Skala, Stacey / Cheng, Lihong / Obermeier, Mary T. / Moore, Robin et al. | 2019
- 3251
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Resurrecting the Condemned: Identification of N‑Benzoxaborole Benzofuran GSK8175 as a Clinical Candidate with Reduced Metabolic LiabilityZhan, Peng / Kang, Dongwei / Liu, Xinyong et al. | 2019
- 3254
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Design of N‑Benzoxaborole Benzofuran GSK8175Optimization of Human Pharmacokinetics Inspired by Metabolites of a Failed Clinical HCV InhibitorChong, Pek Y. / Shotwell, J. Brad / Miller, John / Price, Daniel J. / Maynard, Andy / Voitenleitner, Christian / Mathis, Amanda / Williams, Shawn / Pouliot, Jeffrey J. / Creech, Katrina et al. | 2019
- 3268
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Phenotypic Screening-Based Identification of 3,4-Disubstituted Piperidine Derivatives as Macrophage M2 Polarization Modulators: An Opportunity for Treating Multiple SclerosisWeng, Qinjie / Che, Jinxin / Zhang, Zhikang / Zheng, Jiahuan / Zhan, Wenhu / Lin, Sendong / Tian, Tian / Wang, Jincheng / Gai, Renhua / Hu, Yongzhou et al. | 2019
- 3286
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Selective Inhibitors of Helicobacter pylori Methylthioadenosine Nucleosidase and Human Methylthioadenosine PhosphorylaseHarijan, Rajesh K. / Hoff, Oskar / Ducati, Rodrigo G. / Firestone, Ross S. / Hirsch, Brett M. / Evans, Gary B. / Schramm, Vern L. / Tyler, Peter C. et al. | 2019
- 3297
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Development of a Highly Potent Analogue and a Long-Acting Analogue of Oxytocin for the Treatment of Social Impairment-Like BehaviorsIchinose, Wataru / Cherepanov, Stanislav M. / Shabalova, Anna A. / Yokoyama, Shigeru / Yuhi, Teruko / Yamaguchi, Hiroaki / Watanabe, Ayu / Yamamoto, Yasuhiko / Okamoto, Hiroshi / Horike, Shinichi et al. | 2019
- 3311
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Anticancer Cyclometalated Iridium(III) Complexes with Planar Ligands: Mitochondrial DNA Damage and Metabolism DisturbanceCao, Jian-Jun / Zheng, Yue / Wu, Xiao-Wen / Tan, Cai-Ping / Chen, Mu-He / Wu, Na / Ji, Liang-Nian / Mao, Zong-Wan et al. | 2019
- 3323
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Synthesis, Characterization, and Evaluation of Near-IR Boron Dipyrromethene Bioconjugates for Labeling of Adenocarcinomas by Selectively Targeting the Epidermal Growth Factor ReceptorKaufman, Nichole E. M. / Meng, Qianli / Griffin, Kaitlin E. / Singh, Sitanshu S. / Dahal, Achyut / Zhou, Zehua / Fronczek, Frank R. / Mathis, J. Michael / Jois, Seetharama D. / Vicente, M. Graça H. et al. | 2019
- 3336
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Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a “Tail Switching” Strategy on a Piperazinyl Azetidine SkeletonChen, Zhen / Mori, Wakana / Deng, Xiaoyun / Cheng, Ran / Ogasawara, Daisuke / Zhang, Genwei / Schafroth, Michael A. / Dahl, Kenneth / Fu, Hualong / Hatori, Akiko et al. | 2019
- 3354
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De Novo Designed Amphipathic α‑Helical Antimicrobial Peptides Incorporating Dab and Dap Residues on the Polar Face To Treat the Gram-Negative Pathogen, Acinetobacter baumanniiMant, Colin T. / Jiang, Ziqing / Gera, Lajos / Davis, Tim / Nelson, Kirsten L. / Bevers, Shaun / Hodges, Robert S. et al. | 2019
- 3367
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Novel 1‑Methyl‑1H‑pyrazole-5-carboxamide Derivatives with Potent Anthelmintic ActivityLe, Thuy G. / Kundu, Abhijit / Ghoshal, Atanu / Nguyen, Nghi H. / Preston, Sarah / Jiao, Yaqing / Ruan, Banfeng / Xue, Lian / Huang, Fei / Keiser, Jennifer et al. | 2019
- 3381
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Fragment Hits: What do They Look Like and How do They Bind?Giordanetto, Fabrizio / Jin, Chentian / Willmore, Lindsay / Feher, Miklos / Shaw, David E. et al. | 2019
- 3395
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Pt(IV) Bifunctional Prodrug Containing 2‑(2-Propynyl)octanoato Axial Ligand: Induction of Immunogenic Cell Death on Colon CancerSabbatini, Maurizio / Zanellato, Ilaria / Ravera, Mauro / Gabano, Elisabetta / Perin, Elena / Rangone, Beatrice / Osella, Domenico et al. | 2019
- 3407
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Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase InhibitorsShirai, Fumiyuki / Tsumura, Takeshi / Yashiroda, Yoko / Yuki, Hitomi / Niwa, Hideaki / Sato, Shin / Chikada, Tsubasa / Koda, Yasuko / Washizuka, Kenichi / Yoshimoto, Nobuko et al. | 2019
- 3428
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Discovery and Mechanistic Study of Tailor-Made Quinoline Derivatives as Topoisomerase 1 Poison with Potent Anticancer ActivityKundu, Biswajit / Das, Subhendu K. / Paul Chowdhuri, Srijita / Pal, Sourav / Sarkar, Dipayan / Ghosh, Arijit / Mukherjee, Ayan / Bhattacharya, Debomita / Das, Benu Brata / Talukdar, Arindam et al. | 2019
- 3447
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Design, Synthesis, and Biological Evaluation of Novel Allosteric Protein Disulfide Isomerase InhibitorsYang, Suhui / Shergalis, Andrea / Lu, Dan / Kyani, Anahita / Liu, Ziwei / Ljungman, Mats / Neamati, Nouri et al. | 2019
- 3475
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Discovery and Structural Optimization of Acridones as Broad-Spectrum AntimalarialsDodean, Rozalia A. / Kancharla, Papireddy / Li, Yuexin / Melendez, Victor / Read, Lisa / Bane, Charles E. / Vesely, Brian / Kreishman-Deitrick, Mara / Black, Chad / Li, Qigui et al. | 2019
- 3503
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4‑Aryl Pyrrolidines as a Novel Class of Orally Efficacious Antimalarial Agents. Part 1: Evaluation of 4‑Aryl‑N‑benzylpyrrolidine-3-carboxamidesMeyers, Marvin J. / Liu, Jianguang / Xu, Jing / Leng, Fang / Guan, Jiantong / Liu, Zhijun / McNitt, Sarah A. / Qin, Limei / Dai, Linglin / Ma, Hongwei et al. | 2019
- 3513
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Coagulation Factor XIIIa Inhibitor Tridegin: On the Role of Disulfide Bonds for Folding, Stability, and FunctionBäuml, Charlotte A. / Schmitz, Thomas / Paul George, Ajay Abisheck / Sudarsanam, Monica / Hardes, Kornelia / Steinmetzer, Torsten / Holle, Lori A. / Wolberg, Alisa S. / Pötzsch, Bernd / Oldenburg, Johannes et al. | 2019
- 3524
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Tumor-Targeted Delivery of 6‑Diazo-5-oxo‑l‑norleucine (DON) Using Substituted Acetylated Lysine ProdrugsTenora, Lukáš / Alt, Jesse / Dash, Ranjeet P. / Gadiano, Alexandra J. / Novotná, Kateřina / Veeravalli, Vijayabhaskar / Lam, Jenny / Kirkpatrick, Quinn R. / Lemberg, Kathryn M. / Majer, Pavel et al. | 2019
- 3539
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Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A3 ReceptorYang, Xue / van Veldhoven, Jacobus P. D. / Offringa, Jelle / Kuiper, Boaz J. / Lenselink, Eelke B. / Heitman, Laura H. / van der Es, Daan / IJzerman, Adriaan P. et al. | 2019
- 3553
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Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV‑1 Protease Inhibitor AtazanavirA. M. Subbaiah, Murugaiah / Mandlekar, Sandhya / Desikan, Sridhar / Ramar, Thangeswaran / Subramani, Lakshumanan / Annadurai, Mathiazhagan / Desai, Salil D. / Sinha, Sarmistha / Jenkins, Susan M. / Krystal, Mark R. et al. | 2019
- 3575
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Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part IIZhang, Wei / Lun, Shichun / Liu, Ling-Ling / Xiao, Shiqi / Duan, Guanfu / Gunosewoyo, Hendra / Yang, Fan / Tang, Jie / Bishai, William R. / Yu, Li-Fang et al. | 2019
- 3590
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Potent and Highly Selective Aldo–Keto Reductase 1C3 (AKR1C3) Inhibitors Act as Chemotherapeutic Potentiators in Acute Myeloid Leukemia and T‑Cell Acute Lymphoblastic LeukemiaVerma, Kshitij / Zang, Tianzhu / Penning, Trevor M. / Trippier, Paul C. et al. | 2019
- 3617
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Optimization of Peptidomimetics as Selective Inhibitors for the β‑Catenin/T-Cell Factor Protein–Protein InteractionWang, Zhen / Zhang, Min / Wang, Jin / Ji, Haitao et al. | 2019
- 3636
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C‑6α- vs C‑7α-Substituted Steroidal Aromatase Inhibitors: Which Is Better? Synthesis, Biochemical Evaluation, Docking Studies, and Structure–Activity RelationshipsRoleira, Fernanda M. F. / Varela, Carla / Amaral, Cristina / Costa, Saul C. / Correia-da-Silva, Georgina / Moraca, Federica / Costa, Giosuè / Alcaro, Stefano / Teixeira, Natércia A. A. / Tavares da Silva, Elisiário J. et al. | 2019
- 3658
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Topographical Mapping of Isoform-Selectivity Determinants for J‑Channel-Binding Inhibitors of Sphingosine Kinases 1 and 2Adams, David R. / Tawati, Salha / Berretta, Giacomo / Rivas, Paula Lopez / Baiget, Jessica / Jiang, Zhong / Alsfouk, Aisha / Mackay, Simon P. / Pyne, Nigel J. / Pyne, Susan et al. | 2019
- 3677
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Structure–Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5′-Nucleotidase (CD73) InhibitorsJunker, Anna / Renn, Christian / Dobelmann, Clemens / Namasivayam, Vigneshwaran / Jain, Shanu / Losenkova, Karolina / Irjala, Heikki / Duca, Sierra / Balasubramanian, Ramachandran / Chakraborty, Saibal et al. | 2019
- 3696
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Amino Acid Scanning at P5′ within the Bowman–Birk Inhibitory Loop Reveals Specificity Trends for Diverse Serine ProteasesLi, Choi Yi / de Veer, Simon J. / White, Andrew M. / Chen, Xingchen / Harris, Jonathan M. / Swedberg, Joakim E. / Craik, David J. et al. | 2019
- 3707
-
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar InhibitorsHuang, Yi-You / Yu, Yan-Fa / Zhang, Chen / Chen, Yiping / Zhou, Qian / Li, Zhuoming / Zhou, Sihang / Li, Zhe / Guo, Lei / Wu, Deyan et al. | 2019
- 3722
-
Dopamine D4 Receptor-Selective Compounds Reveal Structure–Activity Relationships that Engender Agonist EfficacyKeck, Thomas M. / Free, R. Benjamin / Day, Marilyn M. / Brown, Sonvia L. / Maddaluna, Michele S. / Fountain, Griffin / Cooper, Charles / Fallon, Brooke / Holmes, Matthew / Stang, Christopher T. et al. | 2019
- 3741
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FragLitesMinimal, Halogenated Fragments Displaying Pharmacophore Doublets. An Efficient Approach to Druggability Assessment and Hit GenerationWood, Daniel J. / Lopez-Fernandez, J. Daniel / Knight, Leanne E. / Al-Khawaldeh, Islam / Gai, Conghao / Lin, Shengying / Martin, Mathew P. / Miller, Duncan C. / Cano, Céline / Endicott, Jane A. et al. | 2019
- 3753
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Defining Structure–Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D1 Receptor AgonistsMartini, Michael L. / Liu, Jing / Ray, Caroline / Yu, Xufen / Huang, Xi-Ping / Urs, Aarti / Urs, Nikhil / McCorvy, John D. / Caron, Marc G. / Roth, Bryan L. et al. | 2019
- 3773
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Discovery of Bisubstrate Inhibitors for Protein N‑Terminal Methyltransferase 1Chen, Dongxing / Dong, Guangping / Noinaj, Nicholas / Huang, Rong et al. | 2019
- 3780
-
Correction to Optimization of Fused Bicyclic Allosteric SHP2 InhibitorsBagdanoff, Jeffrey T. / Chen, Zhouliang / Acker, Michael / Chen, Ying-Nan / Chan, Homan / Dore, Michael / Firestone, Brant / Fodor, Michelle / Fortanet, Jorge / Hentemann, Murphy et al. | 2019
- 3781
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Correction to 6‑Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 InhibitorsSarver, Patrick / Acker, Michael / Bagdanoff, Jeffrey T. / Chen, Zhouliang / Chen, Ying-Nan / Chan, Homan / Firestone, Brant / Fodor, Michelle / Fortanet, Jorge / Hao, Huaixiang et al. | 2019
- 3782
-
Correction to “Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides”Wang, Jiajun / Chou, Shuli / Yang, Zhanyi / Yang, Yang / Wang, Zhihua / Song, Jing / Dou, Xiujing / Shan, Anshan et al. | 2019