Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay
Hall, Justin, Brault, Amy, Vincent, Fabien, Weng, Shawn, Wang, Hong, Dumlao, Darren, Aulabaugh, Ann, Aivazian, Dikran, Castro, Dana, Chen, Ming, Culp, Jeffrey, Dower, Ken, Gardner, Joseph, Hawrylik, Steven, Golenbock, Douglas, Hepworth, David, Horn, Mark, Jones, Lyn, Jones, Peter, Latz, Eicke, Li, Jing, Lin, Lih-Ling, Lin, Wen, Lin, David, Lovering, Frank, Niljanskul, Nootaree, Nistler, Ryan, Pierce, Betsy, Plotnikova, Olga, Schmitt, Daniel, Shanker, Suman, Smith, James, Snyder, William, Subashi, Timothy, Trujillo, John, Tyminski, Edyta, Wang, Guoxing, Wong, Jimson, Lefker, Bruce, Dakin, Leslie, Leach, Karen
Published in PloS one (21.09.2017)
Published in PloS one (21.09.2017)
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Visible-Light-Driven Photocatalytic Initiation of Radical Thiol–Ene Reactions Using Bismuth Oxide
Fadeyi, Olugbeminiyi O, Mousseau, James J, Feng, Yiqing, Allais, Christophe, Nuhant, Philippe, Chen, Ming Z, Pierce, Betsy, Robinson, Ralph
Published in Organic letters (04.12.2015)
Published in Organic letters (04.12.2015)
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Discovery of Clinical Candidate 1‑{[(2S,3S,4S)‑3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin‑1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design
Lee, Katherine L, Ambler, Catherine M, Anderson, David R, Boscoe, Brian P, Bree, Andrea G, Brodfuehrer, Joanne I, Chang, Jeanne S, Choi, Chulho, Chung, Seungwon, Curran, Kevin J, Day, Jacqueline E, Dehnhardt, Christoph M, Dower, Ken, Drozda, Susan E, Frisbie, Richard K, Gavrin, Lori K, Goldberg, Joel A, Han, Seungil, Hegen, Martin, Hepworth, David, Hope, Heidi R, Kamtekar, Satwik, Kilty, Iain C, Lee, Arthur, Lin, Lih-Ling, Lovering, Frank E, Lowe, Michael D, Mathias, John P, Morgan, Heidi M, Murphy, Elizabeth A, Papaioannou, Nikolaos, Patny, Akshay, Pierce, Betsy S, Rao, Vikram R, Saiah, Eddine, Samardjiev, Ivan J, Samas, Brian M, Shen, Marina W. H, Shin, Julia H, Soutter, Holly H, Strohbach, Joseph W, Symanowicz, Peter T, Thomason, Jennifer R, Trzupek, John D, Vargas, Richard, Vincent, Fabien, Yan, Jiangli, Zapf, Christoph W, Wright, Stephen W
Published in Journal of medicinal chemistry (13.07.2017)
Published in Journal of medicinal chemistry (13.07.2017)
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Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)
Fensome, Andrew, Ambler, Catherine M, Arnold, Eric, Banker, Mary Ellen, Brown, Matthew F, Chrencik, Jill, Clark, James D, Dowty, Martin E, Efremov, Ivan V, Flick, Andrew, Gerstenberger, Brian S, Gopalsamy, Ariamala, Hayward, Matthew M, Hegen, Martin, Hollingshead, Brett D, Jussif, Jason, Knafels, John D, Limburg, David C, Lin, David, Lin, Tsung H, Pierce, Betsy S, Saiah, Eddine, Sharma, Raman, Symanowicz, Peter T, Telliez, Jean-Baptiste, Trujillo, John I, Vajdos, Felix F, Vincent, Fabien, Wan, Zhao-Kui, Xing, Li, Yang, Xiaojing, Yang, Xin, Zhang, Liying
Published in Journal of medicinal chemistry (11.10.2018)
Published in Journal of medicinal chemistry (11.10.2018)
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Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1
Fensome, Andrew, Ambler, Catherine M., Arnold, Eric, Banker, Mary Ellen, Clark, James D., Dowty, Martin E., Efremov, Ivan V., Flick, Andrew, Gerstenberger, Brian S., Gifford, Roger S., Gopalsamy, Ariamala, Hegen, Martin, Jussif, Jason, Limburg, David C., Lin, Tsung H., Pierce, Betsy S., Sharma, Raman, Trujillo, John I., Vajdos, Felix F., Vincent, Fabien, Wan, Zhao-Kui, Xing, Li, Yang, Xiaojing, Yang, Xin
Published in Bioorganic & medicinal chemistry (15.05.2020)
Published in Bioorganic & medicinal chemistry (15.05.2020)
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Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells
Li, Jing, Wang, Bu, Juba, Brian M, Vazquez, Michael, Kortum, Steve W, Pierce, Betsy S, Pacheco, Michael, Roberts, Lee, Strohbach, Joseph W, Jones, Lyn H, Hett, Erik, Thorarensen, Atli, Telliez, Jean-Baptiste, Sharei, Armon, Bunnage, Mark, Gilbert, Jonathan Brian
Published in ACS chemical biology (15.12.2017)
Published in ACS chemical biology (15.12.2017)
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A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation
Mourey, Robert J, Burnette, Barry L, Brustkern, Sarah J, Daniels, J Scott, Hirsch, Jeffrey L, Hood, William F, Meyers, Marvin J, Mnich, Stephen J, Pierce, Betsy S, Saabye, Matthew J, Schindler, John F, South, Sarah A, Webb, Elizabeth G, Zhang, Jian, Anderson, David R
Published in The Journal of pharmacology and experimental therapeutics (01.06.2010)
Published in The Journal of pharmacology and experimental therapeutics (01.06.2010)
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Cellular thermal shift and clickable chemical probe assays for the determination of drug-target engagement in live cells
Xu, Hua, Gopalsamy, Ariamala, Hett, Erik C., Salter, Shores, Aulabaugh, Ann, Kyne, Robert E., Pierce, Betsy, Jones, Lyn H.
Published in Organic & biomolecular chemistry (01.01.2016)
Published in Organic & biomolecular chemistry (01.01.2016)
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Maximizing Lipophilic Efficiency: The Use of Free-Wilson Analysis in the Design of Inhibitors of Acetyl-CoA Carboxylase
Freeman-Cook, Kevin D, Amor, Paul, Bader, Scott, Buzon, Leanne M, Coffey, Steven B, Corbett, Jeffrey W, Dirico, Kenneth J, Doran, Shawn D, Elliott, Richard L, Esler, William, Guzman-Perez, Angel, Henegar, Kevin E, Houser, Janet A, Jones, Christopher S, Limberakis, Chris, Loomis, Katherine, McPherson, Kirk, Murdande, Sharad, Nelson, Kendra L, Phillion, Dennis, Pierce, Betsy S, Song, Wei, Sugarman, Eliot, Tapley, Susan, Tu, Meihua, Zhao, Zhengrong
Published in Journal of medicinal chemistry (26.01.2012)
Published in Journal of medicinal chemistry (26.01.2012)
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Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist
XIANGYANG CHEN, PIERCE, Betsy, WIN NAING, GRAPPERHAUS, Margaret L, PHILLION, Dennis P
Published in Bioorganic & medicinal chemistry letters (15.05.2010)
Published in Bioorganic & medicinal chemistry letters (15.05.2010)
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Journal Article
Benzothiophene inhibitors of MK2. Part 2: Improvements in kinase selectivity and cell potency
Anderson, David R., Meyers, Marvin J., Kurumbail, Ravi G., Caspers, Nicole, Poda, Gennadiy I., Long, Scott A., Pierce, Betsy S., Mahoney, Matthew W., Mourey, Robert J., Parikh, Mihir D.
Published in Bioorganic & medicinal chemistry letters (15.08.2009)
Published in Bioorganic & medicinal chemistry letters (15.08.2009)
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Journal Article
3-Aminopyrazole Inhibitors of CDK2/Cyclin A as Antitumor Agents. 1. Lead Finding
Pevarello, Paolo, Brasca, Maria Gabriella, Amici, Raffaella, Orsini, Paolo, Traquandi, Gabriella, Corti, Luca, Piutti, Claudia, Sansonna, Pietro, Villa, Manuela, Pierce, Betsy S, Pulici, Maurizio, Giordano, Patrizia, Martina, Katia, Fritzen, Edward L, Nugent, Richard A, Casale, Elena, Cameron, Alexander, Ciomei, Marina, Roletto, Fulvia, Isacchi, Antonella, Fogliatto, GianPaolo, Pesenti, Enrico, Pastori, Wilma, Marsiglio, Aurelio, Leach, Karen L, Clare, Paula M, Fiorentini, Francesco, Varasi, Mario, Vulpetti, Anna, Warpehoski, Martha A
Published in Journal of medicinal chemistry (17.06.2004)
Published in Journal of medicinal chemistry (17.06.2004)
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Benzothiophene inhibitors of MK2. Part 1: Structure–activity relationships, assessments of selectivity and cellular potency
Anderson, David R., Meyers, Marvin J., Kurumbail, Ravi G., Caspers, Nicole, Poda, Gennadiy I., Long, Scott A., Pierce, Betsy S., Mahoney, Matthew W., Mourey, Robert J.
Published in Bioorganic & medicinal chemistry letters (15.08.2009)
Published in Bioorganic & medicinal chemistry letters (15.08.2009)
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Journal Article
Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode
Meyers, Marvin J., Pelc, Matthew, Kamtekar, Satwik, Day, Jacqueline, Poda, Gennadiy I., Hall, Molly K., Michener, Marshall L., Reitz, Beverly A., Mathis, Karl J., Pierce, Betsy S., Parikh, Mihir D., Mischke, Deborah A., Long, Scott A., Parlow, John J., Anderson, David R., Thorarensen, Atli
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
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Journal Article
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)-2,2-Difluorocyclopropyl)((1R,5S)-3-(2-(1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841
Fensome, Andrew, Ambler, Catherine M., Arnold, Eric, Banker, Mary Ellen, Brown, Matthew F., Chrencik, Jill, Clark, James D., Dowty, Martin E., Efremov, Ivan V., Flick, Andrew, Gerstenberger, Brian S., Gopalsamy, Ariamala, Hayward, Matthew M., Hegen, Martin, Hollingshead, Brett D., Jussif, Jason, Knafels, John D., Limburg, David C., Lin, David, Lin, Tsung H., Pierce, Betsy S., Saiah, Eddine, Sharma, Raman, Symanowicz, Peter T., Telliez, Jean-Baptiste, Trujillo, John I., Vajdos, Felix F., Vincent, Fabien, Wan, Zhao-Kui, Xing, Li, Yang, Xiaojing, Yang, Xin, Zhang, Liying
Published in Journal of medicinal chemistry (11.10.2018)
Published in Journal of medicinal chemistry (11.10.2018)
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Improved Synthesis of a Macrocyclic Peptide-Like C5aR Antagonist for Intravenous Applications
Feng, Yiqing, Liang, Sidney, Langille, Jonathan, Pierce, Betsy S., Chung, Seungwon, Szeliga, Jan, Wilcox, Glenn, Simonds, Paul, Farley, Kathleen A., Li, Bryan, Garcia-Irizarry, Carmen, Jones, Peter, Lira, Ricardo
Published in Organic process research & development (19.10.2023)
Published in Organic process research & development (19.10.2023)
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Journal Article
Improved Synthesis of a Macrocyclic Peptide-Like C5aR Antagonist for Intravenous Applications
Feng, Yiqing, Liang, Sidney, Langille, Jonathan, Pierce, Betsy S., Chung, SeungWon, Szeliga, Jan, Wilcox, Glenn, Simonds, Paul, Farley, Kathleen A., Li, Bryan, Garcia-Irizarry, Carmen, Jones, Peter, Lira, Ricardo
Published in Organic process research & development (17.11.2023)
Published in Organic process research & development (17.11.2023)
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Cyclic Peptide C5aR1 Antagonist Design Using Solution Conformational Analysis Derived from Residual Dipolar Couplings
Farley, Kathleen A., Che, Ye, Lira, Ricardo, Jones, Peter, Papaioannou, Nikolaos, Hayward, Matthew, Flanagan, Mark E., Langille, Jonathan, Liang, Sidney, Pierce, Betsy S., Ciszewski, Gregory, Bonin, Paul, Vincent, Fabien, Ramsey, Simeon, Hepworth, David
Published in ACS medicinal chemistry letters (29.10.2024)
Published in ACS medicinal chemistry letters (29.10.2024)
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Determination of Antibody–Drug Conjugate Released Payload Species Using Directed in Vitro Assays and Mass Spectrometric Interrogation
Bessire, Andrew J, Ballard, T. Eric, Charati, Manoj, Cohen, Justin, Green, Michael, Lam, My-Hanh, Loganzo, Frank, Nolting, Birte, Pierce, Betsy, Puthenveetil, Sujiet, Roberts, Lee, Schildknegt, Klaas, Subramanyam, Chakrapani
Published in Bioconjugate chemistry (20.07.2016)
Published in Bioconjugate chemistry (20.07.2016)
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Cellular thermal shift and clickable chemical probe assays for the determination of drug-target engagement in live cellsElectronic supplementary information (ESI) available. See DOI: 10.1039/c6ob01078d
Xu, Hua, Gopalsamy, Ariamala, Hett, Erik C, Salter, Shores, Aulabaugh, Ann, Kyne, Robert E, Pierce, Betsy, Jones, Lyn H
Year of Publication 29.06.2016
Year of Publication 29.06.2016
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