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
Fragment-to-Hit-to-Lead Discovery of a Novel Pyridylurea Scaffold of ATP Competitive Dual Targeting Type II Topoisomerase Inhibiting Antibacterial Agents
Basarab, Gregory S, Manchester, John I, Bist, Shanta, Boriack-Sjodin, P. Ann, Dangel, Brian, Illingworth, Ruth, Sherer, Brian A, Sriram, Shubha, Uria-Nickelsen, Maria, Eakin, Ann E
Published in Journal of medicinal chemistry (14.11.2013)
Published in Journal of medicinal chemistry (14.11.2013)
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Journal Article
Optimization of Pyrrolamide Topoisomerase II Inhibitors Toward Identification of an Antibacterial Clinical Candidate (AZD5099)
Basarab, Gregory S, Hill, Pamela J, Garner, C. Edwin, Hull, Ken, Green, Oluyinka, Sherer, Brian A, Dangel, P. Brian, Manchester, John I, Bist, Shanta, Hauck, Sheila, Zhou, Fei, Uria-Nickelsen, Maria, Illingworth, Ruth, Alm, Richard, Rooney, Mike, Eakin, Ann E
Published in Journal of medicinal chemistry (24.07.2014)
Published in Journal of medicinal chemistry (24.07.2014)
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Journal Article
Pyrrolamide DNA Gyrase Inhibitors: Fragment-Based Nuclear Magnetic Resonance Screening To Identify Antibacterial Agents
Eakin, Ann E, Green, Oluyinka, Hales, Neil, Walkup, Grant K, Bist, Shanta, Singh, Alok, Mullen, George, Bryant, Joanna, Embrey, Kevin, Gao, Ning, Breeze, Alex, Timms, Dave, Andrews, Beth, Uria-Nickelsen, Maria, Demeritt, Julie, Loch, James T., III, Hull, Ken, Blodgett, April, Illingworth, Ruth N, Prince, Bryan, Boriack-Sjodin, P. Ann, Hauck, Sheila, MacPherson, Lawrence J, Ni, Haihong, Sherer, Brian
Published in Antimicrobial Agents and Chemotherapy (01.03.2012)
Published in Antimicrobial Agents and Chemotherapy (01.03.2012)
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Journal Article
Pyrrolamide DNA gyrase inhibitors: Optimization of antibacterial activity and efficacy
Sherer, Brian A., Hull, Kenneth, Green, Oluyinka, Basarab, Gregory, Hauck, Sheila, Hill, Pamela, Loch, James T., Mullen, George, Bist, Shanta, Bryant, Joanna, Boriack-Sjodin, Ann, Read, Jon, DeGrace, Nancy, Uria-Nickelsen, Maria, Illingworth, Ruth N., Eakin, Ann E.
Published in Bioorganic & medicinal chemistry letters (15.12.2011)
Published in Bioorganic & medicinal chemistry letters (15.12.2011)
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Journal Article
Discovery of M5049: A Novel Selective Toll-Like Receptor 7/8 Inhibitor for Treatment of Autoimmunity
Vlach, Jaromir, Bender, Andrew T, Przetak, Melinda, Pereira, Albertina, Deshpande, Aditee, Johnson, Theresa L, Reissig, Sonja, Tzvetkov, Evgeni, Musil, Djordje, Morse, Noune Tahmassian, Haselmayer, Philipp, Zimmerli, Simone C, Okitsu, Shinji L, Walsky, Robert L, Sherer, Brian
Published in The Journal of pharmacology and experimental therapeutics (01.03.2021)
Published in The Journal of pharmacology and experimental therapeutics (01.03.2021)
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Journal Article
Discovery of quinazoline HPK1 inhibitors with high cellular potency
Toure, Momar, Johnson, Theresa, Li, Bin, Schmidt, Ralf, Ma, Hong, Neagu, Constantin, Lopez, Andrea Unzue, Wang, Yanping, Guler, Satenig, Xiao, YuFang, Henkes, Renate, Ho, Kevin, Zhang, Susan, Chu, Chia Lin, Gundra, Uma Mahesh, Porichis, Filippos, Li, Long, Maurer, Christine Katharina, Fang, Zhizhou, Musil, Djordje, DiPoto, Maria, Friis, Emily, Jones, Reinaldo, Jones, Christopher, Cummings, James, Chekler, Eugene, Tanzer, Eva Maria, Huck, Bayard, Sherer, Brian
Published in Bioorganic & medicinal chemistry (07.09.2023)
Published in Bioorganic & medicinal chemistry (07.09.2023)
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Journal Article
Discovery of potent and selective reversible Bruton’s tyrosine kinase inhibitors
Qiu, Hui, Ali, Zahid, Bender, Andrew, Caldwell, Richard, Chen, Yi-Ying, Fang, Zhizhou, Gardberg, Anna, Glaser, Nina, Goettsche, Anja, Goutopoulos, Andreas, Grenningloh, Roland, Hanschke, Bettina, Head, Jared, Johnson, Theresa, Jones, Christopher, Jones, Reinaldo, Kulkarni, Shashank, Maurer, Christine, Morandi, Federica, Neagu, Constantin, Poetzsch, Sven, Potnick, Justin, Schmidt, Ralf, Roe, Katherine, Viacava Follis, Ariele, Wing, Carolyn, Zhu, Xiaohua, Sherer, Brian
Published in Bioorganic & medicinal chemistry (15.06.2021)
Published in Bioorganic & medicinal chemistry (15.06.2021)
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Journal Article
Discovery of potent and selective reversible Bruton?s tyrosine kinase inhibitors
Qiu, Hui, Ali, Zahid, Bender, Andrew, Caldwell, Richard, Chen, Yi-Ying, Fang, Zhizhou, Gardberg, Anna, Glaser, Nina, Goettsche, Anja, Goutopoulos, Andreas, Grenningloh, Roland, Hanschke, Bettina, Head, Jared, Johnson, Theresa, Jones, Christopher, Jones, Reinaldo, Kulkarni, Shashank, Maurer, Christine, Morandi, Federica, Neagu, Constantin, Poetzsch, Sven, Potnick, Justin, Schmidt, Ralf, Roe, Katherine, Follis, Ariele Viacava, Wing, Carolyn, Zhu, Xiaohua, Sherer, Brian
Published in Bioorganic & medicinal chemistry (15.06.2021)
Published in Bioorganic & medicinal chemistry (15.06.2021)
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Journal Article
Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers
DeSelm, Lizbeth, Huck, Bayard, Lan, Ruoxi, Neagu, Constantin, Potnick, Justin, Xiao, Yufang, Chen, Xiaoling, Jones, Reinaldo, Richardson, Thomas E, Heasley, Brian H, Haxell, Thomas, Moore, Joseph, Tian, Hui, Georgi, Katrin, Rohdich, Felix, Sutton, Amanda, Johnson, Theresa, Mochalkin, Igor, Jackson, Jennifer, Lin, Jing, Crowley, Lindsey, Machl, Andreas, Clark, Anderson, Wilker, Erik, Sherer, Brian, Goutopoulos, Andreas
Published in Journal of medicinal chemistry (14.10.2021)
Published in Journal of medicinal chemistry (14.10.2021)
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Journal Article
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
Synthesis and SAR development of quinoline analogs as novel P2X7 receptor antagonists
Xiao, Yufang, Karra, Srinivasa, Goutopoulos, Andreas, Morse, Noune Tahmassian, Zhang, Susan, Dhanabal, Mohanraj, Tian, Hui, Seenisamy, Jeyaprakashnarayanan, Jayadevan, Jayashankaran, Caldwell, Richard, Potnick, Justin, Bleich, Matthew, Chekler, Eugene, Sherer, Brian, Sriraman, Venkataraman
Published in Bioorganic & medicinal chemistry letters (01.07.2019)
Published in Bioorganic & medicinal chemistry letters (01.07.2019)
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Journal Article
Corrigendum to “Discovery of 4-aminopyrimidine analogs as highly potent dual P70S6K/Akt inhibitors” [Bioorgan. Med. Chem. Lett. 50 (2021) 128352]
Xiao, Yufang, Huck, Bayard R., Lan, Ruoxi, DeSelm, Lizbeth, Chen, Xiaoling, Qiu, Hui, Neagu, Constantin, Johnson, Theresa, Mochalkin, Igor, Gardberg, Anna, Jiang, Xuliang, Tian, Hui, Dutt, Vikram, Santos, Dusica, Head, Jared, Jackson, Jennifer, Syed, Sakeena, Lin, Jing, Wilker, Erik, Ma, Jianguo, Clark, Anderson, Machl, Andreas, Bankston, Donald, Jones, Christopher C.V., Goutopoulos, Andreas, Sherer, Brian
Published in Bioorganic & medicinal chemistry letters (01.07.2022)
Published in Bioorganic & medicinal chemistry letters (01.07.2022)
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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
Discovery of 4-aminopyrimidine analogs as highly potent dual P70S6K/Akt inhibitors
Xiao, Yufang, Huck, Bayard R., Lan, Ruoxi, DeSelm, Lizbeth, Chen, Xiaoling, Qiu, Hui, Neagu, Constantin, Johnson, Theresa, Mochalkin, Igor, Gardberg, Anna, Jiang, Xuliang, Tian, Hui, Dutt, Vikram, Santos, Dusica, Head, Jared, Jackson, Jennifer, Syed, Sakeena, Lin, Jing, Wilker, Erik, Ma, Jianguo, Clark, Anderson, Machl, Andreas, Bankston, Donald, Jones, Christopher C.V., Goutopoulos, Andreas, Sherer, Brian
Published in Bioorganic & medicinal chemistry letters (15.10.2021)
Published in Bioorganic & medicinal chemistry letters (15.10.2021)
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Journal Article
Discovery of Covalent Bruton's Tyrosine Kinase Inhibitors with Decreased CYP2C8 Inhibitory Activity
Qiu, Hui, Ali, Zahid, Bowlan, Julian, Caldwell, Richard, Gardberg, Anna, Glaser, Nina, Goutopoulos, Andreas, Head, Jared, Johnson, Theresa, Maurer, Christine, Georgi, Katrin, Grenningloh, Roland, Fang, Zhizhou, Morandi, Federica, Rohdich, Felix, Schmidt, Ralf, Follis, Ariele Viacava, Sherer, Brian
Published in ChemMedChem (14.12.2021)
Published in ChemMedChem (14.12.2021)
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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
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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