Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors
Bachovchin, Daniel A, Mohr, Justin T, Speers, Anna E, Wang, Chu, Berlin, Jacob M, Spicer, Timothy P, Fernandez-Vega, Virneliz, Chase, Peter, Hodder, Peter S, Schürer, Stephan C, Nomura, Daniel K, Rosen, Hugh, Fu, Gregory C, Cravatt, Benjamin F
Published in Nature reviews. Drug discovery (26.04.2011)
Published in Nature reviews. Drug discovery (26.04.2011)
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Journal Article
Selective and Brain Penetrant Neuropeptide Y Y2 Receptor Antagonists Discovered by Whole-Cell High-Throughput Screening
Brothers, Shaun P, Saldanha, S Adrian, Spicer, Timothy P, Cameron, Michael, Mercer, Becky A, Chase, Peter, McDonald, Patricia, Wahlestedt, Claes, Hodder, Peter S
Published in Molecular pharmacology (01.01.2010)
Published in Molecular pharmacology (01.01.2010)
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Journal Article
Discovery, design and synthesis of a selective S1P3 receptor allosteric agonist
Guerrero, Miguel, Poddutoori, Ramulu, Urbano, Mariangela, Peng, Xuemei, Spicer, Timothy P., Chase, Peter S., Hodder, Peter S., Schaeffer, Marie-Therese, Brown, Steven, Rosen, Hugh, Roberts, Edward
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
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Journal Article
Discovery, Synthesis and Characterization of a Highly Muscarinic Acetylcholine Receptor (mAChR)-Selective M5-Orthosteric Antagonist, VU0488130 (ML381): A Novel Molecular Probe
Gentry, Patrick R., Kokubo, Masaya, Bridges, Thomas M., Cho, Hyekyung P., Smith, Emery, Chase, Peter, Hodder, Peter S., Utley, Thomas J., Rajapakse, Anuruddha, Byers, Frank, Niswender, Colleen M., Morrison, Ryan D., Daniels, J. Scott, Wood, Michael R., Conn, P. Jeffrey, Lindsley, Craig W.
Published in ChemMedChem (01.08.2014)
Published in ChemMedChem (01.08.2014)
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Journal Article
Characterization of Selective Exosite-Binding Inhibitors of Matrix Metalloproteinase 13 That Prevent Articular Cartilage Degradation in Vitro
Spicer, Timothy P, Jiang, Jianwen, Taylor, Alexander B, Choi, Jun Yong, Hart, P. John, Roush, William R, Fields, Gregg B, Hodder, Peter S, Minond, Dmitriy
Published in Journal of medicinal chemistry (26.11.2014)
Published in Journal of medicinal chemistry (26.11.2014)
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Journal Article
Transitioning pharmacoperones to therapeutic use: In vivo proof-of-principle and design of high throughput screens
Conn, P. Michael, Smithson, David C., Hodder, Peter S., Stewart, M. David, Behringer, Richard R., Smith, Emery, Ulloa-Aguirre, Alfredo, Janovick, Jo Ann
Published in Pharmacological research (01.05.2014)
Published in Pharmacological research (01.05.2014)
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Journal Article
A high-throughput assay for the identification of drugs against late-stage Plasmodium falciparum gametocytes
Peatey, Christopher L., Spicer, Timothy P., Hodder, Peter S., Trenholme, Katharine R., Gardiner, Donald L.
Published in Molecular and biochemical parasitology (01.12.2011)
Published in Molecular and biochemical parasitology (01.12.2011)
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Journal Article
Development of high throughput screening assays and pilot screen for inhibitors of metalloproteases meprin α and β
Madoux, Franck, Tredup, Claudia, Spicer, Timothy P., Scampavia, Louis, Chase, Peter S., Hodder, Peter S., Fields, Gregg B., Becker-Pauly, Christoph, Minond, Dmitriy
Published in Biopolymers (01.09.2014)
Published in Biopolymers (01.09.2014)
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Journal Article
Selective Inhibitor of Platelet-Activating Factor Acetylhydrolases 1b2 and 1b3 That Impairs Cancer Cell Survival
Chang, Jae Won, Zuhl, Andrea M, Speers, Anna E, Niessen, Sherry, Brown, Steven J, Mulvihill, Melinda M, Fan, Yi Chiao, Spicer, Timothy P, Southern, Mark, Scampavia, Louis, Fernandez-Vega, Virneliz, Dix, Melissa M, Cameron, Michael D, Hodder, Peter S, Rosen, Hugh, Nomura, Daniel K, Kwon, Ohyun, Hsu, Ku-Lung, Cravatt, Benjamin F
Published in ACS chemical biology (17.04.2015)
Published in ACS chemical biology (17.04.2015)
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Journal Article
Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core
Wood, Michael R., Noetzel, Meredith J., Engers, Julie L., Bollinger, Katrina A., Melancon, Bruce J., Tarr, James C., Han, Changho, West, Mary, Gregro, Alison R., Lamsal, Atin, Chang, Sichen, Ajmera, Sonia, Smith, Emery, Chase, Peter, Hodder, Peter S., Bubser, Michael, Jones, Carrie K., Hopkins, Corey R., Emmitte, Kyle A., Niswender, Colleen M., Wood, Michael W., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (01.07.2016)
Published in Bioorganic & medicinal chemistry letters (01.07.2016)
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Journal Article
Target-Based Screen Against a Periplasmic Serine Protease That Regulates Intrabacterial pH Homeostasis in Mycobacterium tuberculosis
Zhao, Nan, Darby, Crystal M, Small, Jennifer, Bachovchin, Daniel A, Jiang, Xiuju, Burns-Huang, Kristin E, Botella, Helene, Ehrt, Sabine, Boger, Dale L, Anderson, Erin D, Cravatt, Benjamin F, Speers, Anna E, Fernandez-Vega, Virneliz, Hodder, Peter S, Eberhart, Christina, Rosen, Hugh, Spicer, Timothy P, Nathan, Carl F
Published in ACS chemical biology (20.02.2015)
Published in ACS chemical biology (20.02.2015)
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Journal Article
Discovery and optimization of a novel series of highly CNS penetrant M-4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core
Wood, Michael R., Noetzel, Meredith J., Engers, Julie L., Bollinger, Katrina A., Melancon, Bruce J., Tarr, James C., Han, Changho, West, Mary, Gregro, Alison R., Lamsal, Atin, Chang, Sichen, Ajmera, Sonia, Smith, Emery, Chase, Peter, Hodder, Peter S., Bubser, Michael, Jones, Carrie K., Hopkins, Corey R., Emmitte, Kyle A., Niswender, Colleen M., Woodf, Michael W., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (01.07.2016)
Published in Bioorganic & medicinal chemistry letters (01.07.2016)
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Journal Article
Discovery, design and synthesis of a selective S1P(3) receptor allosteric agonist
Guerrero, Miguel, Poddutoori, Ramulu, Urbano, Mariangela, Peng, Xuemei, Spicer, Timothy P., Chase, Peter S., Hodder, Peter S., Schaeffer, Marie-Therese, Brown, Steven, Rosen, Hugh, Roberts, Edward
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
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Journal Article
Confirming Target Engagement for Reversible Inhibitors in Vivo by Kinetically Tuned Activity-Based Probes
Adibekian, Alexander, Martin, Brent R, Chang, Jae Won, Hsu, Ku-Lung, Tsuboi, Katsunori, Bachovchin, Daniel A, Speers, Anna E, Brown, Steven J, Spicer, Timothy, Fernandez-Vega, Virneliz, Ferguson, Jill, Hodder, Peter S, Rosen, Hugh, Cravatt, Benjamin F
Published in Journal of the American Chemical Society (27.06.2012)
Published in Journal of the American Chemical Society (27.06.2012)
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Journal Article
NH-1,2,3-Triazole Inhibitors of the VIM-2 Metallo-β-Lactamase
Weide, Timo, Saldanha, S. Adrian, Minond, Dmitriy, Spicer, Timothy P, Fotsing, Joseph R, Spaargaren, Michael, Frère, Jean-Marie, Bebrone, Carine, Sharpless, K. Barry, Hodder, Peter S, Fokin, Valery V
Published in ACS medicinal chemistry letters (08.07.2010)
Published in ACS medicinal chemistry letters (08.07.2010)
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Journal Article
A Substrate-Free Activity-Based Protein Profiling Screen for the Discovery of Selective PREPL Inhibitors
Lone, Anna Mari, Bachovchin, Daniel A, Westwood, David B, Speers, Anna E, Spicer, Timothy P, Fernandez-Vega, Virneliz, Chase, Peter, Hodder, Peter S, Rosen, Hugh, Cravatt, Benjamin F, Saghatelian, Alan
Published in Journal of the American Chemical Society (03.08.2011)
Published in Journal of the American Chemical Society (03.08.2011)
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Journal Article
Discovery of ML326: The first sub-micromolar, selective M5 PAM
Gentry, Patrick R., Bridges, Thomas M., Lamsal, Atin, Vinson, Paige N., Smith, Emery, Chase, Peter, Hodder, Peter S., Engers, Julie L., Niswender, Colleen M., Scott Daniels, J., Jeffrey Conn, P., Wood, Michael R., Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (15.05.2013)
Published in Bioorganic & medicinal chemistry letters (15.05.2013)
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Journal Article
Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition
Wood, Michael R., Noetzel, Meredith J., Tarr, James C., Rodriguez, Alice L., Lamsal, Atin, Chang, Sichen, Foster, Jarrett J., Smith, Emery, Chase, Peter, Hodder, Peter S., Engers, Darren W., Niswender, Colleen M., Brandon, Nicholas J., Wood, Michael W., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (01.09.2016)
Published in Bioorganic & medicinal chemistry letters (01.09.2016)
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Journal Article
Development of a Highly Potent, Novel M5 Positive Allosteric Modulator (PAM) Demonstrating CNS Exposure: 1‑((1H‑Indazol-5-yl)sulfoneyl)‑N‑ethyl‑N‑(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)
Gentry, Patrick R, Kokubo, Masaya, Bridges, Thomas M, Noetzel, Meredith J, Cho, Hyekyung P, Lamsal, Atin, Smith, Emery, Chase, Peter, Hodder, Peter S, Niswender, Colleen M, Daniels, J. Scott, Conn, P. Jeffrey, Lindsley, Craig W, Wood, Michael R
Published in Journal of medicinal chemistry (25.09.2014)
Published in Journal of medicinal chemistry (25.09.2014)
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