Publications by authors named "Jonathan Lippy"

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Discovery of pyrrolo[2,1-][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain.
Carolyn D Dzierba, Bireshwar Dasgupta, George Karageorge, Walter Kostich, Brian Hamman, Jonathan S Lippy

Med Chem Res· June 2023

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Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors.
Richard A Hartz, Vijay T Ahuja, Susheel J Nara, C M Vijaya Kumar, Raju K V L P Manepalli, Jonathan S Lippy

J Med Chem· March 2022

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Discovery of ()-1-((2',6-Bis(difluoromethyl)-[2,4'-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain.
Guanglin Luo, Ling Chen, Walter A Kostich, Brian Hamman, Jason Allen, Jonathan Lippy

J Med Chem· March 2022

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Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.
Guanglin Luo, Ling Chen, Walter A Kostich, Brian Hamman, Jason Allen, Jonathan Lippy

J Med Chem· March 2022

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Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.
Richard A Hartz, Vijay T Ahuja, Susheel J Nara, C M Vijaya Kumar, Jeffrey M Brown, Jonathan S Lippy

J Med Chem· August 2021

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An innovative kinome platform to accelerate small-molecule inhibitor discovery and optimization from hits to leads.
Charu Chaudhry, Andrew Tebben, John S Tokarski, Robert Borzilleri, William J Pitts, Jonathan Lippy

Drug Discov Today· May 2021

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Leveraging Automation toward Development of a High-Throughput Gene Expression Profiling Platform.
Jing Chen, Alan Futran, Austin Crithary, Sha Li, Alex Wolicki, Jonathan Lippy

SLAS Discov· March 2021

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Rapid Compound Integrity Assessment for High-Throughput Screening Hit Triaging.
Wilson Z Shou, Samuel W Gerritz, David Harden, R Michael Lawrence, Peter Chase, Jonathan S Lippy

SLAS Discov· February 2021

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Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent.
Upender Velaparthi, Chetan Padmakar Darne, Jayakumar Warrier, Peiying Liu, Hasibur Rahaman, Jonathan Lippy

ACS Med Chem Lett· February 2020

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Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.
Steven H Spergel, Michael E Mertzman, James Kempson, Junqing Guo, Sylwia Stachura, Jonathan S Lippy

ACS Med Chem Lett· March 2019

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Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents.
Yong Zhang, Yufen Zhao, Andrew J Tebben, Steven Sheriff, Max Ruzanov, Jonathan Lippy

ACS Med Chem Lett· November 2018

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Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.
Qingjie Liu, Douglas G Batt, Charu Chaudhry, Jonathan S Lippy, Mark A Pattoli

Bioorg Med Chem Lett· October 2018

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Miniaturized High-Throughput Multiparameter Flow Cytometry Assays Measuring In Vitro Human Dendritic Cell Maturation and T-Cell Activation in Mixed Lymphocyte Reactions.
Yi Fan, Joseph G Naglich, Jennifer D Koenitzer, Humberto Ribeiro, Jonathan Lippy

SLAS Discov· August 2018

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Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI).
Lalgudi S Harikrishnan, Jayakumar Warrier, Andrew J Tebben, Gopikishan Tonukunuru, Sudhakara R Madduri, Jonathan Lippy

Bioorg Med Chem· March 2018

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Leveraging the IncuCyte Technology for Higher-Throughput and Automated Chemotaxis Assays for Target Validation and Compound Characterization.
Jing Chen, Bert Ribeiro, Han Li, Larnie Myer, Peter Chase, Jonathan Lippy

SLAS Discov· February 2018

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Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.
John Hynes, Hong Wu, James Kempson, James J-W Duan, Zhonghui Lu, Jonathan S Lippy

Bioorg Med Chem Lett· July 2017

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Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Qingjie Liu, Qing Shi, David Marcoux, Douglas G Batt, Lyndon Cornelius, Jonathan Lippy

J Med Chem· June 2017

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Development of a Human Whole Blood Screening Platform to Monitor JAK/STAT Signaling Using High-Throughput Flow Cytometry.
Mark P Fereshteh, Xin Li, Sha Li, Yi Fan, Rosemary Zhang, Jonathan Lippy

J Biomol Screen· September 2016

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Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.
Walter Kostich, Brian D Hamman, Yu-Wen Li, Sreenivasulu Naidu, Kumaran Dandapani, Jonathan Lippy

J Pharmacol Exp Ther· September 2016

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Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.
Guanglin Luo, Ling Chen, Catherine R Burton, Hong Xiao, Prasanna Sivaprakasam, Jonathan Lippy

J Med Chem· February 2016

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Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).
Qingjie Liu, Douglas G Batt, Jonathan S Lippy, Neha Surti, Andrew J Tebben

Bioorg Med Chem Lett· October 2015

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Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.
Amy C Hart, Gretchen M Schroeder, Honghe Wan, James Grebinski, Jennifer Inghrim, Jonathan Lippy

ACS Med Chem Lett· August 2015

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Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.
Honghe Wan, Gretchen M Schroeder, Amy C Hart, Jennifer Inghrim, James Grebinski, Jonathan Lippy

ACS Med Chem Lett· August 2015

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9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.
Kurt Zimmermann, Xiaopeng Sang, Harold A Mastalerz, Walter L Johnson, Guifen Zhang, Jonathan Lippy

Bioorg Med Chem Lett· July 2015

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Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core.
Prasanna Sivaprakasam, Xiaojun Han, Rita L Civiello, Swanee Jacutin-Porte, Kevin Kish, Jonathan S Lippy

Bioorg Med Chem Lett· May 2015

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