Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development … L Zhang, A Villalobos, EM Beck, T Bocan, TA Chappie, L Chen, ... Journal of medicinal chemistry 56 (11), 4568-4579, 2013 | 178 | 2013 |
Phosphodiesterase 10A inhibitors: a novel approach to the treatment of the symptoms of schizophrenia. FS Menniti, TA Chappie, JM Humphrey, CJ Schmidt Current opinion in investigational drugs (London, England: 2000) 8 (1), 54-59, 2007 | 159 | 2007 |
Discovery of a series of 6, 7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors TA Chappie, JM Humphrey, MP Allen, KG Estep, CB Fox, LA Lebel, ... Journal of medicinal chemistry 50 (2), 182-185, 2007 | 141 | 2007 |
Current landscape of phosphodiesterase 10A (PDE10A) inhibition TA Chappie, CJ Helal, X Hou Journal of medicinal chemistry 55 (17), 7299-7331, 2012 | 107 | 2012 |
Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia CJ Helal, Z Kang, X Hou, J Pandit, TA Chappie, JM Humphrey, ES Marr, ... Journal of medicinal chemistry 54 (13), 4536-4547, 2011 | 58 | 2011 |
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist MA Sanner, TA Chappie, AR Dunaiskis, AF Fliri, KA Desai, SH Zorn, ... Bioorganic & medicinal chemistry letters 8 (7), 725-730, 1998 | 47 | 1998 |
Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1) ST Murphy, G Alton, S Bailey, SM Baxi, BJ Burke, TA Chappie, J Ermolieff, ... Journal of medicinal chemistry 54 (24), 8490-8500, 2011 | 38 | 2011 |
PDE10A inhibitors—clinical failure or window into antipsychotic drug action? FS Menniti, TA Chappie, CJ Schmidt Frontiers in Neuroscience 14, 600178, 2021 | 31 | 2021 |
Application of structure-based design and parallel chemistry to identify a potent, selective, and brain penetrant phosphodiesterase 2A inhibitor CJ Helal, EP Arnold, TL Boyden, C Chang, TA Chappie, KF Fennell, ... Journal of Medicinal Chemistry 60 (13), 5673-5698, 2017 | 30 | 2017 |
The discovery of a novel phosphodiesterase (PDE) 4B-preferring radioligand for positron emission tomography (PET) imaging L Zhang, L Chen, EM Beck, TA Chappie, RV Coelho, SD Doran, KH Fan, ... Journal of Medicinal Chemistry 60 (20), 8538-8551, 2017 | 28 | 2017 |
Chemoproteomics demonstrates target engagement and exquisite selectivity of the clinical phosphodiesterase 10A inhibitor MP-10 in its native environment JP Schülke, LA McAllister, KF Geoghegan, V Parikh, TA Chappie, ... ACS chemical biology 9 (12), 2823-2832, 2014 | 28 | 2014 |
Novel piperidyl derivatives of quinazoline and isoquinoline J Humphrey, T Chappie, S Liras US Patent App. 11/178,104, 2006 | 28 | 2006 |
Imidazo [5, 1-f][1, 2, 4] triazines for the treatment of neurological disorders CJ Helal, TA Chappie, JM Humphrey, PR Verhoest, Y Eddie US Patent 8,598,155, 2013 | 26 | 2013 |
Identification of a potent, highly selective, and brain penetrant phosphodiesterase 2A inhibitor clinical candidate CJ Helal, E Arnold, T Boyden, C Chang, TA Chappie, E Fisher, M Hajos, ... Journal of medicinal chemistry 61 (3), 1001-1018, 2018 | 25 | 2018 |
Application of diazodecomposition reactions in tandem with [2, 3]-sigmatropic rearrangements to prepare substituted azabicyclic ring systems TA Chappie, RM Weekly, MC McMills Tetrahedron letters 37 (36), 6523-6526, 1996 | 23 | 1996 |
Discovery of potent and selective periphery-restricted quinazoline inhibitors of the cyclic nucleotide phosphodiesterase PDE1 JM Humphrey, M Movsesian, CW Am Ende, SL Becker, TA Chappie, ... Journal of Medicinal Chemistry 61 (10), 4635-4640, 2018 | 21 | 2018 |
Dopamine D3/D2 receptor antagonist PF-4363467 attenuates opioid drug-seeking behavior without concomitant D2 side effects TT Wager, T Chappie, D Horton, RY Chandrasekaran, B Samas, ... ACS chemical neuroscience 8 (1), 165-177, 2017 | 21 | 2017 |
Diastereoselective synthesis of 2, 3, 6-trisubstituted piperidines JM Humphrey, EP Arnold, TA Chappie, JB Feltenberger, A Nagel, ... The Journal of Organic Chemistry 74 (12), 4525-4536, 2009 | 21 | 2009 |
Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline MP Allen, TA Chappie, JM Humphrey, S Liras, WM Whalen US Patent 7,268,142, 2007 | 21 | 2007 |
Discovery of small-molecule CD33 pre-mRNA splicing modulators TA Chappie, M Abdelmessih, CW Ambroise, M Boehm, M Cai, M Green, ... ACS Medicinal Chemistry Letters 13 (1), 55-62, 2022 | 12 | 2022 |