Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy
Miller, Michael M, Banville, Jacques, Friends, Todd J, Gagnon, Mark, Hangeland, Jon J, Lavallée, Jean-François, Martel, Alain, O’Grady, Harold, Rémillard, Roger, Ruediger, Edward, Tremblay, François, Posy, Shana L, Allegretto, Nick J, Guarino, Victor R, Harden, David G, Harper, Timothy W, Hartl, Karen, Josephs, Jonathan, Malmstrom, Sarah, Watson, Carol, Yang, Yanou, Zhang, Ge, Wong, Pancras, Yang, Jing, Bouvier, Michel, Seiffert, Dietmar A, Wexler, Ruth R, Lawrence, R. Michael, Priestley, E. Scott, Marinier, Anne
Published in Journal of medicinal chemistry (22.08.2019)
Published in Journal of medicinal chemistry (22.08.2019)
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In vitro Characterization of a small molecule inhibitor of the alanine serine cysteine transporter ‐1 (SLC7A10)
Brown, Jeffrey M., Hunihan, Lisa, Prack, Margaret M., Harden, David G., Bronson, Joanne, Dzierba, Carolyn D., Gentles, Robert G., Hendricson, Adam, Krause, Rudy, Macor, John E., Westphal, Ryan S.
Published in Journal of neurochemistry (01.04.2014)
Published in Journal of neurochemistry (01.04.2014)
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Triazolopyrimidines identified as reversible myeloperoxidase inhibitors
Duclos, Franck, Abell, Lynn M., Harden, David G., Pike, Kristen, Nowak, Kimberly, Locke, Gregory A., Duke, Gerald J., Liu, Xiaoqin, Fernando, Gayani, Shaw, Scott A., Vokits, Benjamin P., Wurtz, Nicholas R., Viet, Andrew, Valente, Meriah N., Stachura, Sylwia, Sleph, Paul, Khan, Javed A., Gao, Ji, Dongre, Ashok R., Zhao, Lei, Wexler, Ruth R., Gordon, David A., Kick, Ellen K.
Published in MedChemComm (01.11.2017)
Published in MedChemComm (01.11.2017)
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A Small Molecule Inhibitor Selectively Induces Apoptosis in Cells Transformed by High Risk Human Papilloma Viruses
Sheaffer, Amy K, Lee, Min S, Qi, Huilin, Chaniewski, Susan, Zheng, Xiaofan, Farr, Glen A, Esposito, Kim, Harden, David, Lei, Ming, Schweizer, Liang, Friborg, Jacques, Agler, Michele, McPhee, Fiona, Gentles, Robert, Beno, Brett R, Chupak, Lou, Mason, Stephen
Published in PloS one (09.06.2016)
Published in PloS one (09.06.2016)
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A thallium-sensitive, fluorescence-based assay for detecting and characterizing potassium channel modulators in mammalian cells
Weaver, C David, Harden, David, Dworetzky, Steven I, Robertson, Barbara, Knox, Ronald J
Published in Journal of biomolecular screening (01.12.2004)
Published in Journal of biomolecular screening (01.12.2004)
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Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists
McDonald, Ivar M., Mate, Robert A., Zusi, F. Christopher, Huang, Hong, Post-Munson, Debra J., Ferrante, Meredith A., Gallagher, Lizbeth, Bertekap, Robert L., Knox, Ronald J., Robertson, Barbara J., Harden, David G., Morgan, Daniel G., Lodge, Nicholas J., Dworetzky, Steven I., Olson, Richard E., Macor, John E.
Published in Bioorganic & medicinal chemistry letters (15.03.2013)
Published in Bioorganic & medicinal chemistry letters (15.03.2013)
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Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain
Wu, Yong-Jin, Conway, Charles M., Sun, Li-Qiang, Machet, Frederic, Chen, Jie, Chen, Ping, He, Huan, Bourin, Clotilde, Calandra, Vincenzo, Polino, Joseph L., Davis, Carl D., Heman, Karen, Gribkoff, Valentin K., Boissard, Christopher G., Knox, Ronald J., Thompson, Mark W., Fitzpatrick, William, Weaver, David, Harden, David G., Natale, Joanne, Dworetzky, Steven I., Starrett, John E.
Published in Bioorganic & medicinal chemistry letters (15.11.2013)
Published in Bioorganic & medicinal chemistry letters (15.11.2013)
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Journal Article
Identification of small molecules that selectively inhibit diacylglycerol lipase-α activity
Appiah, Kingsley K, Blat, Yuval, Robertson, Barbara J, Pearce, Bradley C, Pedicord, Donna L, Gentles, Robert G, Yu, Xuan-Chuan, Mseeh, Faika, Nguyen, Nghi, Swaffield, Jonathan C, Harden, David G, Westphal, Ryan S, Banks, Martyn N, O'Connell, Jonathan C
Published in Journal of biomolecular screening (01.04.2014)
Published in Journal of biomolecular screening (01.04.2014)
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Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels
Gentles, Robert G., Grant-Young, Katherine, Hu, Shuanghua, Huang, Yazhong, Poss, Michael A., Andres, Charles, Fiedler, Tracey, Knox, Ronald, Lodge, Nicholas, Weaver, C. David, Harden, David G.
Published in Bioorganic & medicinal chemistry (01.10.2008)
Published in Bioorganic & medicinal chemistry (01.10.2008)
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BL-1249 [(5,6,7,8-Tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine]: A Putative Potassium Channel Opener with Bladder-Relaxant Properties
Tertyshnikova, Svetlana, Knox, Ronald J, Plym, Mary Jane, Thalody, George, Griffin, Corinne, Neelands, Torben, Harden, David G, Signor, Laura, Weaver, David, Myers, Robert A, Lodge, Nicholas J
Published in The Journal of pharmacology and experimental therapeutics (01.04.2005)
Published in The Journal of pharmacology and experimental therapeutics (01.04.2005)
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Fluorine Substitution Can Block CYP3A4 Metabolism-Dependent Inhibition: Identification of (S)-N-[1-(4-Fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an Orally Bioavailable KCNQ2 Opener Devoid of CYP3A4 Metabolism-Dependent Inhibition
Wu, Yong-Jin, Davis, Carl D, Dworetzky, Steven, Fitzpatrick, William C, Harden, David, He, Huan, Knox, Ronald J, Newton, Amy E, Philip, Thomas, Polson, Craig, Sivarao, Digavalli V, Sun, Li-Qiang, Tertyshnikova, Svetlana, Weaver, David, Yeola, Suresh, Zoeckler, Mary, Sinz, Michael W
Published in Journal of medicinal chemistry (28.08.2003)
Published in Journal of medicinal chemistry (28.08.2003)
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(S)-N-[1-(3-Morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: An Orally Bioavailable KCNQ2 Opener with Significant Activity in a Cortical Spreading Depression Model of Migraine
Wu, Yong-Jin, Boissard, Christopher G, Greco, Corinne, Gribkoff, Valentin K, Harden, David G, He, Huan, L'Heureux, Alexandre, Kang, Shing Hong, Kinney, Gene G, Knox, Ronald J, Natale, Joanne, Newton, Amy E, Lehtinen-Oboma, Sanna, Sinz, Michael W, Sivarao, Digavalli V, Starrett, John E, Sun, Li-Qiang, Tertyshnikova, Svetlana, Thompson, Mark W, Weaver, David, Wong, Henry S, Zhang, Lei, Dworetzky, Steven I
Published in Journal of medicinal chemistry (17.07.2003)
Published in Journal of medicinal chemistry (17.07.2003)
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Journal Article
Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine KCa channel blockers
GENTLES, Robert G, SHUANGHUA HU, HARDEN, David G, YAZHONG HUANG, GRANT-YOUNG, Katherine, POSS, Michael A, ANDRES, Charles, FIEDLER, Tracey, KNOX, Ronald, LODGE, Nicholas, WEAVER, C. David
Published in Bioorganic & medicinal chemistry letters (15.10.2008)
Published in Bioorganic & medicinal chemistry letters (15.10.2008)
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Lichen planus associated with hepatitis C virus: no viral transcripts are found in the lichen planus, and effective therapy for hepatitis C virus does not clear lichen planus
Harden, MAJ David, Skelton, Henry, Smith, COL Kathleen J
Published in Journal of the American Academy of Dermatology (01.11.2003)
Published in Journal of the American Academy of Dermatology (01.11.2003)
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( S)- N-[1-(4-Cyclopropylmethyl-3,4-dihydro-2 H-benzo [1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons
Wu, Yong-Jin, Boissard, Christopher G, Chen, Jie, Fitzpatrick, William, Gao, Qi, Gribkoff, Valentin K, Harden, David G, He, Huan, Knox, Ronald J, Natale, Joanne, Pieschl, Rick L, Starrett, John E, Sun, Li-Qiang, Thompson, Mark, Weaver, David, Wu, Dedong, Dworetzky, Steven I
Published in Bioorganic & medicinal chemistry letters (19.04.2004)
Published in Bioorganic & medicinal chemistry letters (19.04.2004)
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Synthesis and KCNQ2 opener activity of N-(1-benzo[1,3]dioxol-5-yl-ethyl, N-[1-(2,3-dihydro-benzofuran-5-yl)-ethyl, and N-[1-(2,3-dihydro-1 H-indol-5-yl)-ethyl acrylamides
Wu, Yong-Jin, Sun, Li-Qiang, He, Huan, Chen, Jie, Starrett, John E, Dextraze, Pierre, Daris, Jean-Paul, Boissard, Christopher G, Pieschl, Rick L, Gribkoff, Valentin K, Natale, Joanne, Knox, Ronald J, Harden, David G, Thompson, Mark W, Fitzpatrick, William, Weaver, David, Wu, Dedong, Gao, Qi, Dworetzky, Steven I
Published in Bioorganic & medicinal chemistry letters (06.09.2004)
Published in Bioorganic & medicinal chemistry letters (06.09.2004)
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( S, E)- N-[1-(3-Heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity
L’Heureux, Alexandre, Martel, Alain, He, Huan, Chen, Jie, Sun, Li-Qiang, Starrett, John E., Natale, Joanne, Dworetzky, Steven I., Knox, Ronald J., Harden, David G., Weaver, David, Thompson, Mark W., Wu, Yong-Jin
Published in Bioorganic & medicinal chemistry letters (17.01.2005)
Published in Bioorganic & medicinal chemistry letters (17.01.2005)
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Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding
Wong, Pancras C, Seiffert, Dietmar, Bird, J Eileen, Watson, Carol A, Bostwick, Jeffrey S, Giancarli, Mary, Allegretto, Nick, Hua, Ji, Harden, David, Guay, Jocelyne, Callejo, Mario, Miller, Michael M, Lawrence, R Michael, Banville, Jacques, Guy, Julia, Maxwell, Brad D, Priestley, E Scott, Marinier, Anne, Wexler, Ruth R, Bouvier, Michel, Gordon, David A, Schumacher, William A, Yang, Jing
Published in Science translational medicine (04.01.2017)
Published in Science translational medicine (04.01.2017)
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High-Throughput Assessment of Bile Salt Export Pump Inhibition Using RapidFire-MS and DESI-MS
Li, Jie, Morato, Nicolás M., Westover, Lori S., Abeywickrema, Pravien, Geng, Jieping, Piassek, Madison, Harden, David, Strambeanu, Iulia, Shi, Zhicai, Cooks, R. Graham, Meng, Juncai
Published in ACS medicinal chemistry letters (12.09.2024)
Published in ACS medicinal chemistry letters (12.09.2024)
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