PDE10A Inhibitors-Clinical Failure or Window Into Antipsychotic Drug Action?
Menniti, Frank S, Chappie, Thomas A, Schmidt, Christopher J
Published in Frontiers in neuroscience (20.01.2021)
Published in Frontiers in neuroscience (20.01.2021)
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Journal Article
Current Landscape of Phosphodiesterase 10A (PDE10A) Inhibition
Chappie, Thomas A, Helal, Christopher J, Hou, Xinjun
Published in Journal of medicinal chemistry (13.09.2012)
Published in Journal of medicinal chemistry (13.09.2012)
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Journal Article
Design and Selection Parameters to Accelerate the Discovery of Novel Central Nervous System Positron Emission Tomography (PET) Ligands and Their Application in the Development of a Novel Phosphodiesterase 2A PET Ligand
Zhang, Lei, Villalobos, Anabella, Beck, Elizabeth M, Bocan, Thomas, Chappie, Thomas A, Chen, Laigao, Grimwood, Sarah, Heck, Steven D, Helal, Christopher J, Hou, Xinjun, Humphrey, John M, Lu, Jiemin, Skaddan, Marc B, McCarthy, Timothy J, Verhoest, Patrick R, Wager, Travis T, Zasadny, Kenneth
Published in Journal of medicinal chemistry (13.06.2013)
Published in Journal of medicinal chemistry (13.06.2013)
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Journal Article
Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1
Humphrey, John M, Movsesian, Matthew, am Ende, Christopher W, Becker, Stacey L, Chappie, Thomas A, Jenkinson, Stephen, Liras, Jennifer L, Liras, Spiros, Orozco, Christine, Pandit, Jayvardhan, Vajdos, Felix F, Vandeput, Fabrice, Yang, Eddie, Menniti, Frank S
Published in Journal of medicinal chemistry (24.05.2018)
Published in Journal of medicinal chemistry (24.05.2018)
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Journal Article
The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging
Zhang, Lei, Chen, Laigao, Beck, Elizabeth M, Chappie, Thomas A, Coelho, Richard V, Doran, Shawn D, Fan, Kuo-Hsien, Helal, Christopher J, Humphrey, John M, Hughes, Zoe, Kuszpit, Kyle, Lachapelle, Erik A, Lazzaro, John T, Lee, Chewah, Mather, Robert J, Patel, Nandini C, Skaddan, Marc B, Sciabola, Simone, Verhoest, Patrick R, Young, Joseph M, Zasadny, Kenneth, Villalobos, Anabella
Published in Journal of medicinal chemistry (26.10.2017)
Published in Journal of medicinal chemistry (26.10.2017)
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Journal Article
Discovery of Small-Molecule CD33 Pre-mRNA Splicing Modulators
Chappie, Thomas A, Abdelmessih, Mario, Ambroise, Claude W, Boehm, Markus, Cai, Mi, Green, Michael, Guilmette, Edward, Steppan, Claire M, Stevens, Lucy M, Wei, Liuqing, Xi, Simon, Hasson, Samuel A
Published in ACS medicinal chemistry letters (13.01.2022)
Published in ACS medicinal chemistry letters (13.01.2022)
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Journal Article
First-in-Human Evaluation of 18 F-PF-06445974, a PET Radioligand That Preferentially Labels Phosphodiesterase-4B
Wakabayashi, Yuichi, Stenkrona, Per, Arakawa, Ryosuke, Yan, Xuefeng, Van Buskirk, Maia G, Jenkins, Madeline D, Santamaria, Jose A Montero, Maresca, Kevin P, Takano, Akihiro, Liow, Jeih-San, Chappie, Thomas A, Varrone, Andrea, Nag, Sangram, Zhang, Lei, Hughes, Zoë A, Schmidt, Christopher J, Doran, Shawn D, Mannes, Andrew, Zanotti-Fregonara, Paolo, Ooms, Maarten, Morse, Cheryl L, Zoghbi, Sami S, Halldin, Christer, Pike, Victor W, Innis, Robert B
Published in Journal of Nuclear Medicine (01.12.2022)
Published in Journal of Nuclear Medicine (01.12.2022)
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Journal Article
First-in-Human Evaluation of 18F-PF-06445974, a PET Radioligand That Preferentially Labels Phosphodiesterase-4B
Wakabayashi, Yuichi, Stenkrona, Per, Arakawa, Ryosuke, Yan, Xuefeng, Van Buskirk, Maia G, Jenkins, Madeline D, Santamaria, Jose A Montero, Maresca, Kevin P, Takano, Akihiro, Liow, Jeih-San, Chappie, Thomas A, Varrone, Andrea, Nag, Sangram, Zhang, Lei, Hughes, Zoë A, Schmidt, Christopher J, Doran, Shawn D, Mannes, Andrew, Zanotti-Fregonara, Paolo, Ooms, Maarten, Morse, Cheryl L, Zoghbi, Sami S, Halldin, Christer, Pike, Victor W, Innis, Robert B
Published in The Journal of nuclear medicine (1978) (01.12.2022)
Published in The Journal of nuclear medicine (1978) (01.12.2022)
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Journal Article
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate
Helal, Christopher J, Arnold, Eric, Boyden, Tracey, Chang, Cheng, Chappie, Thomas A, Fisher, Ethan, Hajos, Mihaly, Harms, John F, Hoffman, William E, Humphrey, John M, Pandit, Jayvardhan, Kang, Zhijun, Kleiman, Robin J, Kormos, Bethany L, Lee, Che-Wah, Lu, Jiemin, Maklad, Noha, McDowell, Laura, McGinnis, Dina, O’Connor, Rebecca E, O’Donnell, Christopher J, Ogden, Adam, Piotrowski, Mary, Schmidt, Christopher J, Seymour, Patricia A, Ueno, Hirokazu, Vansell, Nichole, Verhoest, Patrick R, Yang, Edward X
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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Journal Article
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor
Helal, Christopher J, Arnold, Eric P, Boyden, Tracey L, Chang, Cheng, Chappie, Thomas A, Fennell, Kimberly F, Forman, Michael D, Hajos, Mihaly, Harms, John F, Hoffman, William E, Humphrey, John M, Kang, Zhijun, Kleiman, Robin J, Kormos, Bethany L, Lee, Che-Wah, Lu, Jiemin, Maklad, Noha, McDowell, Laura, Mente, Scot, O’Connor, Rebecca E, Pandit, Jayvardhan, Piotrowski, Mary, Schmidt, Anne W, Schmidt, Christopher J, Ueno, Hirokazu, Verhoest, Patrick R, Yang, Edward X
Published in Journal of medicinal chemistry (13.07.2017)
Published in Journal of medicinal chemistry (13.07.2017)
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Journal Article
Discovery of a Series of 6,7-Dimethoxy-4-pyrrolidylquinazoline PDE10A Inhibitors
Chappie, Thomas A., Humphrey, John M., Allen, Martin P., Estep, Kimberly G., Fox, Carol B., Lebel, Lorraine A., Liras, Spiros, Marr, Eric S., Menniti, Frank S., Pandit, Jayvardhan, Schmidt, Christopher J., Tu, Meihua, Williams, Robert D., Yang, Feng V.
Published in Journal of medicinal chemistry (25.01.2007)
Published in Journal of medicinal chemistry (25.01.2007)
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Journal Article
Use of Structure-Based Design to Discover a Potent, Selective, In Vivo Active Phosphodiesterase 10A Inhibitor Lead Series for the Treatment of Schizophrenia
Helal, Christopher J, Kang, Zhijun, Hou, Xinjun, Pandit, Jayvardhan, Chappie, Thomas A, Humphrey, John M, Marr, Eric S, Fennell, Kimberly F, Chenard, Lois K, Fox, Carol, Schmidt, Christopher J, Williams, Robert D, Chapin, Douglas S, Siuciak, Judith, Lebel, Lorraine, Menniti, Frank, Cianfrogna, Julia, Fonseca, Kari R, Nelson, Frederick R, O’Connor, Rebecca, MacDougall, Mary, McDowell, Laura, Liras, Spiros
Published in Journal of medicinal chemistry (14.07.2011)
Published in Journal of medicinal chemistry (14.07.2011)
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Journal Article
Chemoproteomics Demonstrates Target Engagement and Exquisite Selectivity of the Clinical Phosphodiesterase 10A Inhibitor MP-10 in Its Native Environment
Schülke, Jan-Philip, McAllister, Laura A, Geoghegan, Kieran F, Parikh, Vinod, Chappie, Thomas A, Verhoest, Patrick R, Schmidt, Christopher J, Johnson, Douglas S, Brandon, Nicholas J
Published in ACS chemical biology (19.12.2014)
Published in ACS chemical biology (19.12.2014)
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Journal Article
Correction to Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor
Helal, Christopher J, Arnold, Eric P, Boyden, Tracey L, Chang, Cheng, Chappie, Thomas A, Fennell, Kimberly F, Forman, Michael D, Hajos, Mihaly, Harms, John F, Hoffman, William E, Humphrey, John M, Kang, Zhijun, Kleiman, Robin J, Kormos, Bethany L, LaChapelle, Erik A, Lee, Che-Wah, Lu, Jiemin, Maklad, Noha, McDowell, Laura, Mente, Scot, O’Connor, Rebecca E, Pandit, Jayvardhan, Piotrowski, Mary, Schmidt, Anne W, Schmidt, Christopher J, Ueno, Hirokazu, Verhoest, Patrick R, Yang, Edward X
Published in Journal of medicinal chemistry (26.04.2018)
Published in Journal of medicinal chemistry (26.04.2018)
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Journal Article
Discovery of Novel, Potent, and Selective Inhibitors of 3-Phosphoinositide-Dependent Kinase (PDK1)
Murphy, Sean T, Alton, Gordon, Bailey, Simon, Baxi, Sangita M, Burke, Benjamin J, Chappie, Thomas A, Ermolieff, Jacques, Ferre, RoseAnn, Greasley, Samantha, Hickey, Michael, Humphrey, John, Kablaoui, Natasha, Kath, John, Kazmirski, Steven, Kraus, Michelle, Kupchinsky, Stan, Li, John, Lingardo, Laura, Marx, Matthew A, Richter, Dan, Tanis, Steven P, Tran, Khanh, Vernier, William, Xie, Zhi, Yin, Min-Jean, Yu, Xiao-Hong
Published in Journal of medicinal chemistry (22.12.2011)
Published in Journal of medicinal chemistry (22.12.2011)
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Journal Article
Phosphodiesterase 10A inhibitors: a novel approach to the treatment of the symptoms of schizophrenia
Menniti, Frank S, Chappie, Thomas A, Humphrey, John M, Schmidt, Christopher J
Published in Current opinion in investigational drugs (London, England : 2000) (01.01.2007)
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Published in Current opinion in investigational drugs (London, England : 2000) (01.01.2007)
Journal Article
Diastereoselective Synthesis of 2,3,6-Trisubstituted Piperidines
Humphrey, John M, Arnold, Eric P, Chappie, Thomas A, Feltenberger, John B, Nagel, Arthur, Simon, Wendy, Suarez-Contreras, Melani, Tom, Norma J, O’Neill, Brian T
Published in Journal of organic chemistry (19.06.2009)
Published in Journal of organic chemistry (19.06.2009)
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Journal Article
Synthesis of a Pyridoazepine Scaffold via Rhodium-Catalyzed Ring Expansion and Nitroacetamide Condensation
Yang, Eddie, Tucker, Joseph W., Chappie, Thomas A., Weaver, John D., Chapman, Caroline, Duzguner, Remzi, Humphrey, John M.
Published in Organic process research & development (17.02.2023)
Published in Organic process research & development (17.02.2023)
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Journal Article
Dopamine D3/D2 Receptor Antagonist PF-4363467 Attenuates Opioid Drug-Seeking Behavior without Concomitant D2 Side Effects
Wager, Travis T, Chappie, Thomas, Horton, David, Chandrasekaran, Ramalakshmi Y, Samas, Brian, Dunn-Sims, Elizabeth R, Hsu, Cathleen, Nawreen, Nawshaba, Vanase-Frawley, Michelle A, O’Connor, Rebecca E, Schmidt, Christopher J, Dlugolenski, Keith, Stratman, Nancy C, Majchrzak, Mark J, Kormos, Bethany L, Nguyen, David P, Sawant-Basak, Aarti, Mead, Andy N
Published in ACS chemical neuroscience (18.01.2017)
Published in ACS chemical neuroscience (18.01.2017)
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