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Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist.
Kim SH, Han S, Zhao J, Wang S, Kusnetzow AK, Reinhart G, Fowler MA, Markison S, Johns M, Luo R, Struthers RS, Zhu Y, Betz SF. Kim SH, et al. Among authors: reinhart g. ACS Med Chem Lett. 2024 Mar 19;15(4):478-485. doi: 10.1021/acsmedchemlett.3c00514. eCollection 2024 Apr 11. ACS Med Chem Lett. 2024. PMID: 38628803
3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.
Tucci FC, Zhu YF, Struthers RS, Guo Z, Gross TD, Rowbottom MW, Acevedo O, Gao Y, Saunders J, Xie Q, Reinhart GJ, Liu XJ, Ling N, Bonneville AK, Chen T, Bozigian H, Chen C. Tucci FC, et al. J Med Chem. 2005 Feb 24;48(4):1169-78. doi: 10.1021/jm049218c. J Med Chem. 2005. PMID: 15715483
Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor.
Chen C, Wu D, Guo Z, Xie Q, Reinhart GJ, Madan A, Wen J, Chen T, Huang CQ, Chen M, Chen Y, Tucci FC, Rowbottom M, Pontillo J, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS. Chen C, et al. J Med Chem. 2008 Dec 11;51(23):7478-85. doi: 10.1021/jm8006454. J Med Chem. 2008. PMID: 19006286
251 results