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Page 1
Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia.
Layton ME, Kern JC, Hartingh TJ, Shipe WD, Raheem I, Kandebo M, Hayes RP, Huszar S, Eddins D, Ma B, Fuerst J, Wollenberg GK, Li J, Fritzen J, McGaughey GB, Uslaner JM, Smith SM, Coleman PJ, Cox CD. Layton ME, et al. Among authors: kern jc. J Med Chem. 2023 Jan 26;66(2):1157-1171. doi: 10.1021/acs.jmedchem.2c01521. Epub 2023 Jan 9. J Med Chem. 2023. PMID: 36624931 Free PMC article.
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
Fensome A, Adams WR, Adams AL, Berrodin TJ, Cohen J, Huselton C, Illenberger A, Kern JC, Hudak VA, Marella MA, Melenski EG, McComas CC, Mugford CA, Slayden OD, Yudt M, Zhang Z, Zhang P, Zhu Y, Winneker RC, Wrobel JE. Fensome A, et al. Among authors: kern jc. J Med Chem. 2008 Mar 27;51(6):1861-73. doi: 10.1021/jm701080t. Epub 2008 Mar 5. J Med Chem. 2008. PMID: 18318463
Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides.
Moore WJ, Kern JC, Bhat R, Commons TJ, Fukayama S, Goljer I, Krishnamurthy G, Magolda RL, Nogle L, Pitts K, Stauffer B, Trybulski EJ, Welmaker GS, Wilson M, Bodine PV. Moore WJ, et al. Among authors: kern jc. J Med Chem. 2009 Jan 8;52(1):105-16. doi: 10.1021/jm801144h. J Med Chem. 2009. PMID: 19072540
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.
Zhang P, Terefenko E, Kern J, Fensome A, Trybulski E, Unwalla R, Wrobel J, Lockhead S, Zhu Y, Cohen J, Lacava M, Winneker RC, Zhang Z. Zhang P, et al. Bioorg Med Chem. 2007 Oct 15;15(20):6556-64. doi: 10.1016/j.bmc.2007.07.011. Epub 2007 Jul 26. Bioorg Med Chem. 2007. PMID: 17681796
3-(Pyridin-2-yl-ethynyl)benzamide metabotropic glutamate receptor 5 negative allosteric modulators: hit to lead studies.
Gilbert AM, Bursavich MG, Lombardi S, Adedoyin A, Dwyer JM, Hughes Z, Kern JC, Khawaja X, Rosenzweig-Lipson S, Moore WJ, Neal SJ, Olsen M, Rizzo SJ, Springer D. Gilbert AM, et al. Among authors: kern jc. Bioorg Med Chem Lett. 2011 Jan 1;21(1):195-9. doi: 10.1016/j.bmcl.2010.11.038. Epub 2010 Nov 12. Bioorg Med Chem Lett. 2011. PMID: 21126874
39 results