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Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).
Murphy ST, Alton G, Bailey S, Baxi SM, Burke BJ, Chappie TA, Ermolieff J, Ferre R, Greasley S, Hickey M, Humphrey J, Kablaoui N, Kath J, Kazmirski S, Kraus M, Kupchinsky S, Li J, Lingardo L, Marx MA, Richter D, Tanis SP, Tran K, Vernier W, Xie Z, Yin MJ, Yu XH. Murphy ST, et al. Among authors: chappie ta. J Med Chem. 2011 Dec 22;54(24):8490-500. doi: 10.1021/jm201019k. Epub 2011 Nov 23. J Med Chem. 2011. PMID: 22040023
Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1.
Humphrey JM, Movsesian M, Am Ende CW, Becker SL, Chappie TA, Jenkinson S, Liras JL, Liras S, Orozco C, Pandit J, Vajdos FF, Vandeput F, Yang E, Menniti FS. Humphrey JM, et al. Among authors: chappie ta. J Med Chem. 2018 May 24;61(10):4635-4640. doi: 10.1021/acs.jmedchem.8b00374. Epub 2018 May 10. J Med Chem. 2018. PMID: 29718668
Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia.
Helal CJ, Kang Z, Hou X, Pandit J, Chappie TA, Humphrey JM, Marr ES, Fennell KF, Chenard LK, Fox C, Schmidt CJ, Williams RD, Chapin DS, Siuciak J, Lebel L, Menniti F, Cianfrogna J, Fonseca KR, Nelson FR, O'Connor R, MacDougall M, McDowell L, Liras S. Helal CJ, et al. Among authors: chappie ta. J Med Chem. 2011 Jul 14;54(13):4536-47. doi: 10.1021/jm2001508. Epub 2011 Jun 8. J Med Chem. 2011. PMID: 21650160
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Helal CJ, Arnold EP, Boyden TL, Chang C, Chappie TA, Fennell KF, Forman MD, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, Mente S, O'Connor RE, Pandit J, Piotrowski M, Schmidt AW, Schmidt CJ, Ueno H, Verhoest PR, Yang EX. Helal CJ, et al. Among authors: chappie ta. J Med Chem. 2017 Jul 13;60(13):5673-5698. doi: 10.1021/acs.jmedchem.7b00397. Epub 2017 Jun 16. J Med Chem. 2017. PMID: 28574706
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 L, Villalobos A, Beck EM, Bocan T, Chappie TA, Chen L, Grimwood S, Heck SD, Helal CJ, Hou X, Humphrey JM, Lu J, Skaddan MB, McCarthy TJ, Verhoest PR, Wager TT, Zasadny K. Zhang L, et al. Among authors: chappie ta. J Med Chem. 2013 Jun 13;56(11):4568-79. doi: 10.1021/jm400312y. Epub 2013 May 28. J Med Chem. 2013. PMID: 23651455
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.
Helal CJ, Arnold E, Boyden T, Chang C, Chappie TA, Fisher E, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Pandit J, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, McGinnis D, O'Connor RE, O'Donnell CJ, Ogden A, Piotrowski M, Schmidt CJ, Seymour PA, Ueno H, Vansell N, Verhoest PR, Yang EX. Helal CJ, et al. Among authors: chappie ta. J Med Chem. 2018 Feb 8;61(3):1001-1018. doi: 10.1021/acs.jmedchem.7b01466. Epub 2018 Jan 16. J Med Chem. 2018. PMID: 29293004
Diastereoselective synthesis of 2,3,6-trisubstituted piperidines.
Humphrey JM, Arnold EP, Chappie TA, Feltenberger JB, Nagel A, Simon W, Suarez-Contreras M, Tom NJ, O'Neill BT. Humphrey JM, et al. Among authors: chappie ta. J Org Chem. 2009 Jun 19;74(12):4525-36. doi: 10.1021/jo9003184. J Org Chem. 2009. PMID: 19441779
19 results