Potent and selective Bruton’s tyrosine kinase inhibitors: Discovery of GDC-0834
Young, Wendy B., Barbosa, James, Blomgren, Peter, Bremer, Meire C., Crawford, James J., Dambach, Donna, Gallion, Steve, Hymowitz, Sarah G., Kropf, Jeffrey E., Lee, Seung H., Liu, Lichuan, Lubach, Joseph W., Macaluso, Jen, Maciejewski, Pat, Maurer, Brigitte, Mitchell, Scott A., Ortwine, Daniel F., Di Paolo, Julie, Reif, Karin, Scheerens, Heleen, Schmitt, Aaron, Sowell, C. Gregory, Wang, Xiaojing, Wong, Harvey, Xiong, Jin-Ming, Xu, Jianjun, Zhao, Zhongdong, Currie, Kevin S.
Published in Bioorganic & medicinal chemistry letters (15.03.2015)
Published in Bioorganic & medicinal chemistry letters (15.03.2015)
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Significant Species Difference in Amide Hydrolysis of GDC-0834, a Novel Potent and Selective Bruton's Tyrosine Kinase Inhibitor
LICHUAN LIU, HALLADAY, Jason S, KUEBLER, Peter, DAVIS, John C, CHARLENE LIAO, X, LUBACH, Joseph W, DEESE, Alan, SOWELL, C. Gregory, CURRIE, Kevin S, YOUNG, Wendy B, KHOJASTEH, S. Cyrus, HOP, Cornelis E. C. A, SHIN, Young, WONG, Harvey, WONG, Susan, CORAGGIO, Melis, LA, Hank, BAUMGARDNER, Matthew, LE, Hoa, GOPAUL, Sashi, BOGGS, Jason
Published in Drug metabolism and disposition (01.10.2011)
Published in Drug metabolism and disposition (01.10.2011)
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Characterization of the mechanism of action of lanraplenib, a novel spleen tyrosine kinase inhibitor, in models of lupus nephritis
Pohlmeyer, Christopher W, Shang, Ching, Han, Pei, Cui, Zhi-Hua, Jones, Randall M, Clarke, Astrid S, Murray, Bernard P, Lopez, David A, Newstrom, David W, Inzunza, M David, Matzkies, Franziska G, Currie, Kevin S, Di Paolo, Julie A
Published in BMC rheumatology (30.03.2021)
Published in BMC rheumatology (30.03.2021)
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Small-molecule agents for the treatment of inflammatory bowel disease
Currie, Kevin S., Patel, Leena, Sedillo, Kassandra F.
Published in Bioorganic & medicinal chemistry letters (15.08.2019)
Published in Bioorganic & medicinal chemistry letters (15.08.2019)
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Discovery of GS-9973, a Selective and Orally Efficacious Inhibitor of Spleen Tyrosine Kinase
Currie, Kevin S, Kropf, Jeffrey E, Lee, Tony, Blomgren, Peter, Xu, Jianjun, Zhao, Zhongdong, Gallion, Steve, Whitney, J. Andrew, Maclin, Deborah, Lansdon, Eric B, Maciejewski, Patricia, Rossi, Ann Marie, Rong, Hong, Macaluso, Jennifer, Barbosa, James, Di Paolo, Julie A, Mitchell, Scott A
Published in Journal of medicinal chemistry (08.05.2014)
Published in Journal of medicinal chemistry (08.05.2014)
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Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis
Reif, Karin, Currie, Kevin S, Di Paolo, Julie A, Huang, Tao, Balazs, Mercedesz, Barbosa, James, Barck, Kai H, Bravo, Brandon J, Carano, Richard A D, Darrow, James, Davies, Douglas R, DeForge, Laura E, Diehl, Lauri, Ferrando, Ronald, Gallion, Steven L, Giannetti, Anthony M, Gribling, Peter, Hurez, Vincent, Hymowitz, Sarah G, Jones, Randall, Kropf, Jeffrey E, Lee, Wyne P, Maciejewski, Patricia M, Mitchell, Scott A, Rong, Hong, Staker, Bart L, Whitney, J Andrew, Yeh, Sherry, Young, Wendy B, Yu, Christine, Zhang, Juan
Published in Nature chemical biology (01.01.2011)
Published in Nature chemical biology (01.01.2011)
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Journal Article
Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases
Blomgren, Peter, Chandrasekhar, Jayaraman, Di Paolo, Julie A, Fung, Wanchi, Geng, Guoju, Ip, Carmen, Jones, Randall, Kropf, Jeffrey E, Lansdon, Eric B, Lee, Seung, Lo, Jennifer R, Mitchell, Scott A, Murray, Bernard, Pohlmeyer, Chris, Schmitt, Aaron, Suekawa-Pirrone, Kimberly, Wise, Sarah, Xiong, Jin-Ming, Xu, Jianjun, Yu, Helen, Zhao, Zhongdong, Currie, Kevin S
Published in ACS medicinal chemistry letters (09.04.2020)
Published in ACS medicinal chemistry letters (09.04.2020)
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Journal Article
Effects of GS-9876, a novel spleen tyrosine kinase inhibitor, on platelet function and systemic hemostasis
Clarke, Astrid S., Rousseau, Emma, Wang, Kelly, Kim, Ji-Yun, Murray, Bernard P., Bannister, Roy, Matzkies, Franziska, Currie, Kevin S., Di Paolo, Julie A.
Published in Thrombosis research (01.10.2018)
Published in Thrombosis research (01.10.2018)
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A potential therapeutic strategy for chronic lymphocytic leukemia by combining Idelalisib and GS-9973, a novel spleen tyrosine kinase (Syk) inhibitor
Burke, Russell T, Meadows, Sarah, Loriaux, Marc M, Currie, Kevin S, Mitchell, Scott A, Maciejewski, Patricia, Clarke, Astrid S, Dipaolo, Julie A, Druker, Brian J, Lannutti, Brian J, Spurgeon, Stephen E
Published in Oncotarget (28.02.2014)
Published in Oncotarget (28.02.2014)
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Discovery of highly potent and selective Bruton’s tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability
Young, Wendy B., Barbosa, James, Blomgren, Peter, Bremer, Meire C., Crawford, James J., Dambach, Donna, Eigenbrot, Charles, Gallion, Steve, Johnson, Adam R., Kropf, Jeffrey E., Lee, Seung H., Liu, Lichuan, Lubach, Joseph W., Macaluso, Jen, Maciejewski, Pat, Mitchell, Scott A., Ortwine, Daniel F., Di Paolo, Julie, Reif, Karin, Scheerens, Heleen, Schmitt, Aaron, Wang, Xiaojing, Wong, Harvey, Xiong, Jin-Ming, Xu, Jianjun, Yu, Christine, Zhao, Zhongdong, Currie, Kevin S.
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
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Btk-specific inhibition blocks pathogenic plasma cell signatures and myeloid cell-associated damage in IFN α -driven lupus nephritis
Katewa, Arna, Wang, Yugang, Hackney, Jason A, Huang, Tao, Suto, Eric, Ramamoorthi, Nandhini, Austin, Cary D, Bremer, Meire, Chen, Jacob Zhi, Crawford, James J, Currie, Kevin S, Blomgren, Peter, DeVoss, Jason, DiPaolo, Julie A, Hau, Jonathan, Johnson, Adam, Lesch, Justin, DeForge, Laura E, Lin, Zhonghua, Liimatta, Marya, Lubach, Joseph W, McVay, Sami, Modrusan, Zora, Nguyen, Allen, Poon, Chungkee, Wang, Jianyong, Liu, Lichuan, Lee, Wyne P, Wong, Harvey, Young, Wendy B, Townsend, Michael J, Reif, Karin
Published in JCI insight (06.04.2017)
Published in JCI insight (06.04.2017)
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Discovery of Potent and Selective Tricyclic Inhibitors of Bruton’s Tyrosine Kinase with Improved Druglike Properties
Wang, Xiaojing, Barbosa, James, Blomgren, Peter, Bremer, Meire C, Chen, Jacob, Crawford, James J, Deng, Wei, Dong, Liming, Eigenbrot, Charles, Gallion, Steve, Hau, Jonathon, Hu, Huiyong, Johnson, Adam R, Katewa, Arna, Kropf, Jeffrey E, Lee, Seung H, Liu, Lichuan, Lubach, Joseph W, Macaluso, Jen, Maciejewski, Pat, Mitchell, Scott A, Ortwine, Daniel F, DiPaolo, Julie, Reif, Karin, Scheerens, Heleen, Schmitt, Aaron, Wong, Harvey, Xiong, Jin-Ming, Xu, Jianjun, Zhao, Zhongdong, Zhou, Fusheng, Currie, Kevin S, Young, Wendy B
Published in ACS medicinal chemistry letters (08.06.2017)
Published in ACS medicinal chemistry letters (08.06.2017)
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Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation
Farand, Julie, Kropf, Jeffrey E, Blomgren, Peter, Xu, Jianjun, Schmitt, Aaron C, Newby, Zachary E, Wang, Ting, Murakami, Eisuke, Barauskas, Ona, Sudhamsu, Jawahar, Feng, Joy Y, Niedziela-Majka, Anita, Schultz, Brian E, Schwartz, Karen, Viatchenko-Karpinski, Serge, Kornyeyev, Dmytro, Kashishian, Adam, Fan, Peidong, Chen, Xiaowu, Lansdon, Eric B, Ports, Michael O, Currie, Kevin S, Watkins, William J, Notte, Gregory T
Published in ACS medicinal chemistry letters (12.03.2020)
Published in ACS medicinal chemistry letters (12.03.2020)
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Imidazo[1,2-a]pyrazine diaryl ureas: Inhibitors of the receptor tyrosine kinase EphB4
Mitchell, Scott A., Danca, Mihaela Diana, Blomgren, Peter A., Darrow, James W., Currie, Kevin S., Kropf, Jeffrey E., Lee, Seung H., Gallion, Steven L., Xiong, Jin-Ming, Pippin, Douglas A., DeSimone, Robert W., Brittelli, David R., Eustice, David C., Bourret, Aaron, Hill-Drzewi, Melissa, Maciejewski, Patricia M., Elkin, Lisa L.
Published in Bioorganic & medicinal chemistry letters (15.12.2009)
Published in Bioorganic & medicinal chemistry letters (15.12.2009)
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