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Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1.
Yeh VS, Beno DW, Brodjian S, Brune ME, Cullen SC, Dayton BD, Dhaon MK, Falls HD, Gao J, Grihalde N, Hajduk P, Hansen TM, Judd AS, King AJ, Klix RC, Larson KJ, Lau YY, Marsh KC, Mittelstadt SW, Plata D, Rozema MJ, Segreti JA, Stoner EJ, Voorbach MJ, Wang X, Xin X, Zhao G, Collins CA, Cox BF, Reilly RM, Kym PR, Souers AJ. Yeh VS, et al. Among authors: king aj. J Med Chem. 2012 Feb 23;55(4):1751-7. doi: 10.1021/jm201524g. Epub 2012 Feb 10. J Med Chem. 2012. PMID: 22263872
Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.
Voight EA, Gomtsyan AR, Daanen JF, Perner RJ, Schmidt RG, Bayburt EK, DiDomenico S, McDonald HA, Puttfarcken PS, Chen J, Neelands TR, Bianchi BR, Han P, Reilly RM, Franklin PH, Segreti JA, Nelson RA, Su Z, King AJ, Polakowski JS, Baker SJ, Gauvin DM, Lewis LR, Mikusa JP, Joshi SK, Faltynek CR, Kym PR, Kort ME. Voight EA, et al. Among authors: king aj. J Med Chem. 2014 Sep 11;57(17):7412-24. doi: 10.1021/jm500916t. Epub 2014 Aug 21. J Med Chem. 2014. PMID: 25100568
A-1048400 is a novel, orally active, state-dependent neuronal calcium channel blocker that produces dose-dependent antinociception without altering hemodynamic function in rats.
Scott VE, Vortherms TA, Niforatos W, Swensen AM, Neelands T, Milicic I, Banfor PN, King A, Zhong C, Simler G, Zhan C, Bratcher N, Boyce-Rustay JM, Zhu CZ, Bhatia P, Doherty G, Mack H, Stewart AO, Jarvis MF. Scott VE, et al. Biochem Pharmacol. 2012 Feb 1;83(3):406-18. doi: 10.1016/j.bcp.2011.10.019. Epub 2011 Nov 16. Biochem Pharmacol. 2012. PMID: 22153861
860 results