Discovery of Affinity‐Based Probes for Btk Occupancy Assays
Qiu, Hui, Caldwell, Richard, Liu‐Bujalski, Lesley, Goutopoulos, Andreas, Jones, Reinaldo, Potnick, Justin, Sherer, Brian, Bender, Andrew, Grenningloh, Roland, Xu, Daigen, Gardberg, Anna, Mochalkin, Igor, Johnson, Theresa, Viacava Follis, Ariele, Head, Jared, Morandi, Federica
Published in ChemMedChem (22.01.2019)
Published in ChemMedChem (22.01.2019)
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Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases
Caldwell, Richard D, Qiu, Hui, Askew, Ben C, Bender, Andrew T, Brugger, Nadia, Camps, Montserrat, Dhanabal, Mohanraj, Dutt, Vikram, Eichhorn, Thomas, Gardberg, Anna S, Goutopoulos, Andreas, Grenningloh, Roland, Head, Jared, Healey, Brian, Hodous, Brian L, Huck, Bayard R, Johnson, Theresa L, Jones, Christopher, Jones, Reinaldo C, Mochalkin, Igor, Morandi, Federica, Nguyen, Ngan, Meyring, Michael, Potnick, Justin R, Santos, Dusica Cvetinovic, Schmidt, Ralf, Sherer, Brian, Shutes, Adam, Urbahns, Klaus, Follis, Ariele Viacava, Wegener, Ansgar A, Zimmerli, Simone C, Liu-Bujalski, Lesley
Published in Journal of medicinal chemistry (12.09.2019)
Published in Journal of medicinal chemistry (12.09.2019)
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Journal Article
Ability of Bruton's Tyrosine Kinase Inhibitors to Sequester Y551 and Prevent Phosphorylation Determines Potency for Inhibition of Fc Receptor but not B-Cell Receptor Signaling
Bender, Andrew T, Gardberg, Anna, Pereira, Albertina, Johnson, Theresa, Wu, Yin, Grenningloh, Roland, Head, Jared, Morandi, Federica, Haselmayer, Philipp, Liu-Bujalski, Lesley
Published in Molecular pharmacology (01.03.2017)
Published in Molecular pharmacology (01.03.2017)
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Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models
Haselmayer, Philipp, Camps, Montserrat, Liu-Bujalski, Lesley, Nguyen, Ngan, Morandi, Federica, Head, Jared, O'Mahony, Alison, Zimmerli, Simone C, Bruns, Lisa, Bender, Andrew T, Schroeder, Patricia, Grenningloh, Roland
Published in The Journal of immunology (1950) (15.05.2019)
Published in The Journal of immunology (1950) (15.05.2019)
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BTK Compositions and Methods for the Production of Pyrimidine and Pyridine Compounds with BTK Inhibitory Activity
NGUYEN NGAN, LIU BUJALSKI LESLEY, GOUTOPOULOS ANDREAS, BRUGGER NADIA, HODOUS BRIAN L, MOCHALKIN IGOR, JONES REINALDO, BANKSTON DONALD, JOHNSON THERESA L, QIU HUI
Year of Publication 01.02.2019
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Year of Publication 01.02.2019
Patent
BTK Compositions and Methods for the Production of Pyrimidine and Pyridine Compounds with BTK Inhibitory Activity
NGUYEN NGAN, LIU BUJALSKI LESLEY, GOUTOPOULOS ANDREAS, BRUGGER NADIA, HODOUS BRIAN L, MOCHALKIN IGOR, JONES REINALDO, BANKSTON DONALD, JOHNSON THERESA L, QIU HUI
Year of Publication 24.07.2018
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Year of Publication 24.07.2018
Patent
PYRIDINES, PYRIMIDINES, AND PYRAZINES, AS BTK INHIBITORS AND USES THEREOF
NGUYEN NGAN, LIU BUJALSKI LESLEY, MOCHALKIN IGOR, JONES REINALDO, CALDWELL RICHARD D, QIU HUI
Year of Publication 01.04.2016
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Year of Publication 01.04.2016
Patent
BTK Compositions and Methods for the Production of Pyrimidine and Pyridine Compounds with BTK Inhibitory Activity
NGUYEN NGAN, LIU BUJALSKI LESLEY, GOUTOPOULOS ANDREAS, BRUGGER NADIA, HODOUS BRIAN L, MOCHALKIN IGOR, JONES REINALDO, BANKSTON DONALD, JOHNSON THERESA L, QIU HUI
Year of Publication 27.02.2017
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Year of Publication 27.02.2017
Patent
PYRANO[3,2-D][1,3]THIAZOLE AS GLYCOSIDASE INHIBITORS
LIU BUJALSKI LESLEY, GOUTOPOULOS ANDREAS, YU HENRY, DONNELLY MARIANNE, QIU HUI
Year of Publication 08.05.2014
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Year of Publication 08.05.2014
Patent
HETEROARYL COMPOUNDS AS BTK INHIBITORSAND USES THEREOF
TATE DEVON, NEAGU CONSTANTIN, LIU BUJALSKI LESLEY, MOCHALKIN IGOR, JONES REINALDO, CALDWELL RICHARD D, JOHNSON THERESA L, GARDBERG ANNA, QIU HUI
Year of Publication 03.06.2016
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Year of Publication 03.06.2016
Patent
BTK HETEROARYL COMPOUNDS AS BTK INHIBITORS AND USES THEREOF
NEAGU CONSTANTIN, LIU BUJALSKI LESLEY, GOUTOPOULOS ANDREAS, JONES REINALDO, POTNICK JUSTIN, WON ANNIE CHO, JOHNSON THERESA L, GARDBERG ANNA, QIU HUI, GAILLARD PASCALE, SHERER BRIAN A, CALDWELL RICHARD D, SEENISAMY JEYAPRAKASHNARAYANAN
Year of Publication 14.06.2017
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Year of Publication 14.06.2017
Patent
COMPOSITIONS AND METHODS FOR THE PRODUCTION OF PYRIMIDINE AND PYRIDINE COMPOUNDS WITH BTK INHIBITORY ACTIVITY
NGUYEN NGAN, LIU BUJALSKI LESLEY, GOUTOPOULOS ANDREAS, BRUGGER NADIA, HODOUS BRIAN L, MOCHALKIN IGOR, JONES REINALDO, BANKSTON DONALD, JOHNSON THERESA L, QIU HUI
Year of Publication 28.12.2015
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Year of Publication 28.12.2015
Patent
Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit
Qiu, Hui, Liu-Bujalski, Lesley, Caldwell, Richard D, Follis, Ariele Viacava, Gardberg, Anna, Goutopoulos, Andreas, Grenningloh, Roland, Head, Jared, Johnson, Theresa, Jones, Reinaldo, Mochalkin, Igor, Morandi, Federica, Neagu, Constantin, Sherer, Brian
Published in Bioorganic & medicinal chemistry letters (15.09.2018)
Published in Bioorganic & medicinal chemistry letters (15.09.2018)
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Journal Article
Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk
Caldwell, Richard, Liu-Bujalski, Lesley, Qiu, Hui, Mochalkin, Igor, Jones, Reinaldo, Neagu, Constantin, Goutopoulos, Andreas, Grenningloh, Roland, Johnson, Theresa, Sherer, Brian, Gardberg, Anna, Follis, Ariele Viacava, Morandi, Federica, Head, Jared
Published in Bioorganic & medicinal chemistry letters (15.11.2018)
Published in Bioorganic & medicinal chemistry letters (15.11.2018)
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Journal Article
Btk inhibition treats TLR7/IFN driven murine lupus
Bender, Andrew T, Pereira, Albertina, Fu, Kai, Samy, Eileen, Wu, Yin, Liu-Bujalski, Lesley, Caldwell, Richard, Chen, Yi-Ying, Tian, Hui, Morandi, Federica, Head, Jared, Koehler, Ursula, Genest, Melinda, Okitsu, Shinji L, Xu, Daigen, Grenningloh, Roland
Published in Clinical immunology (Orlando, Fla.) (01.03.2016)
Published in Clinical immunology (Orlando, Fla.) (01.03.2016)
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Journal Article
Selective Wee1 Inhibitors Led to Antitumor Activity In Vitro and Correlated with Myelosuppression
Guler, Satenig, DiPoto, Maria C., Crespo, Alejandro, Caldwell, Richard, Doerfel, Benjamin, Grossmann, Nina, Ho, Kevin, Huck, Bayard, Jones, Christopher CV, Lan, Ruoxi, Musil, Djordje, Potnick, Justin, Schilke, Heike, Sherer, Brian, Simon, Stephanie, Sirrenberg, Christian, Zhang, Zhuo, Liu-Bujalski, Lesley
Published in ACS medicinal chemistry letters (11.05.2023)
Published in ACS medicinal chemistry letters (11.05.2023)
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Journal Article
COMPOSITIONS AND METHODS FOR THE PRODUCTION OF PYRIMIDINE AND PYRIDINE COMPOUNDS WITH BTK INHIBITORY ACTIVITY
NGUYEN NGAN, LIU BUJALSKI LESLEY, GOUTOPOULOS ANDREAS, BRUGGER NADIA, HODOUS BRIAN L, MOCHALKIN IGOR, JONES REINALDO, BANKSTON DONALD, JOHNSON THERESA L, QIU HUI
Year of Publication 20.01.2014
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Year of Publication 20.01.2014
Patent
Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors
Qiu, Hui, Liu-Bujalski, Lesley, Caldwell, Richard D., Viacava Follis, Ariele, Gardberg, Anna, Goutopoulos, Andreas, Grenningloh, Roland, Head, Jared, Johnson, Theresa, Jones, Christopher C.V., Jones, Reinaldo, Mochalkin, Igor, Morandi, Federica, Neagu, Constantin, Potnick, Justin, Sherer, Brian
Published in Bioorganic & medicinal chemistry letters (01.11.2018)
Published in Bioorganic & medicinal chemistry letters (01.11.2018)
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Journal Article