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Discovery of ((S)-5-(methoxymethyl)-7-(1-methyl-1H-indol-2-yl)-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone as a potent and selective I(Kur) inhibitor.
Finlay HJ, Lloyd J, Vaccaro W, Kover A, Yan L, Bhave G, Prol J, Huynh T, Bhandaru R, Caringal Y, DiMarco J, Gan J, Harper T, Huang C, Conder ML, Sun H, Levesque P, Blanar M, Atwal K, Wexler R. Finlay HJ, et al. Among authors: gan j. J Med Chem. 2012 Apr 12;55(7):3036-48. doi: 10.1021/jm201386u. Epub 2012 Mar 21. J Med Chem. 2012. PMID: 22409629
Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists.
Zhao G, Kwon C, Bisaha SN, Stein PD, Rossi KA, Cao X, Ung T, Wu G, Hung CP, Malmstrom SE, Zhang G, Qu Q, Gan J, Keim WJ, Cullen MJ, Rohrbach KW, Devenny J, Pelleymounter MA, Miller KJ, Robl JA. Zhao G, et al. Among authors: gan j. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3914-9. doi: 10.1016/j.bmcl.2013.04.061. Epub 2013 Apr 29. Bioorg Med Chem Lett. 2013. PMID: 23683593
Cytochrome P450 11A1 bioactivation of a kinase inhibitor in rats: use of radioprofiling, modulation of metabolism, and adrenocortical cell lines to evaluate adrenal toxicity.
Zhang D, Flint O, Wang L, Gupta A, Westhouse RA, Zhao W, Raghavan N, Caceres-Cortes J, Marathe P, Shen G, Zhang Y, Allentoff A, Josephs J, Gan J, Borzilleri R, Humphreys WG. Zhang D, et al. Among authors: gan j. Chem Res Toxicol. 2012 Mar 19;25(3):556-71. doi: 10.1021/tx200524d. Epub 2012 Mar 2. Chem Res Toxicol. 2012. PMID: 22295996
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.
Ahmad S, Ngu K, Miller KJ, Wu G, Hung CP, Malmstrom S, Zhang G, O'Tanyi E, Keim WJ, Cullen MJ, Rohrbach KW, Thomas M, Ung T, Qu Q, Gan J, Narayanan R, Pelleymounter MA, Robl JA. Ahmad S, et al. Among authors: gan j. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33. doi: 10.1016/j.bmcl.2009.12.014. Epub 2009 Dec 6. Bioorg Med Chem Lett. 2010. PMID: 20022752
2,192 results