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Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.
Hu E, Ma J, Biorn C, Lester-Zeiner D, Cho R, Rumfelt S, Kunz RK, Nixey T, Michelsen K, Miller S, Shi J, Wong J, Hill Della Puppa G, Able J, Talreja S, Hwang DR, Hitchcock SA, Porter A, Immke D, Allen JR, Treanor J, Chen H. Hu E, et al. Among authors: shi j. J Med Chem. 2012 May 24;55(10):4776-87. doi: 10.1021/jm3002372. Epub 2012 May 11. J Med Chem. 2012. PMID: 22548439
Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).
Hu E, Kunz RK, Chen N, Rumfelt S, Siegmund A, Andrews K, Chmait S, Zhao S, Davis C, Chen H, Lester-Zeiner D, Ma J, Biorn C, Shi J, Porter A, Treanor J, Allen JR. Hu E, et al. Among authors: shi j. J Med Chem. 2013 Nov 14;56(21):8781-92. doi: 10.1021/jm401234w. Epub 2013 Oct 25. J Med Chem. 2013. PMID: 24102193
Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).
Hu E, Chen N, Bourbeau MP, Harrington PE, Biswas K, Kunz RK, Andrews KL, Chmait S, Zhao X, Davis C, Ma J, Shi J, Lester-Zeiner D, Danao J, Able J, Cueva M, Talreja S, Kornecook T, Chen H, Porter A, Hungate R, Treanor J, Allen JR. Hu E, et al. Among authors: shi j. J Med Chem. 2014 Aug 14;57(15):6632-41. doi: 10.1021/jm500713j. Epub 2014 Aug 4. J Med Chem. 2014. PMID: 25062128
Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A).
Hu E, Andrews K, Chmait S, Zhao X, Davis C, Miller S, Hill Della Puppa G, Dovlatyan M, Chen H, Lester-Zeiner D, Able J, Biorn C, Ma J, Shi J, Treanor J, Allen JR. Hu E, et al. Among authors: shi j. ACS Med Chem Lett. 2014 Mar 28;5(6):700-5. doi: 10.1021/ml5000993. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944747 Free PMC article.
AMG 580: a novel small molecule phosphodiesterase 10A (PDE10A) positron emission tomography tracer.
Chen H, Lester-Zeiner D, Shi J, Miller S, Glaus C, Hu E, Chen N, Able J, Biorn C, Wong J, Ma J, Michelsen K, Hill Della Puppa G, Kazules T, Dou HH, Talreja S, Zhao X, Chen A, Rumfelt S, Kunz RK, Ye H, Thiel OR, Williamson T, Davis C, Porter A, Immke D, Allen JR, Treanor J. Chen H, et al. Among authors: shi j. J Pharmacol Exp Ther. 2015 Feb;352(2):327-37. doi: 10.1124/jpet.114.220517. Epub 2014 Dec 11. J Pharmacol Exp Ther. 2015. PMID: 25502803
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