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Page 1
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).
Edmonds DJ, Kung DW, Kalgutkar AS, Filipski KJ, Ebner DC, Cabral S, Smith AC, Aspnes GE, Bhattacharya SK, Borzilleri KA, Brown JA, Calabrese MF, Caspers NL, Cokorinos EC, Conn EL, Dowling MS, Eng H, Feng B, Fernando DP, Genung NE, Herr M, Kurumbail RG, Lavergne SY, Lee EC, Li Q, Mathialagan S, Miller RA, Panteleev J, Polivkova J, Rajamohan F, Reyes AR, Salatto CT, Shavnya A, Thuma BA, Tu M, Ward J, Withka JM, Xiao J, Cameron KO. Edmonds DJ, et al. Among authors: eng h. J Med Chem. 2018 Mar 22;61(6):2372-2383. doi: 10.1021/acs.jmedchem.7b01641. Epub 2018 Feb 28. J Med Chem. 2018. PMID: 29466005
Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors.
Bhattacharya SK, Aspnes GE, Bagley SW, Boehm M, Brosius AD, Buckbinder L, Chang JS, Dibrino J, Eng H, Frederick KS, Griffith DA, Griffor MC, Guimarães CR, Guzman-Perez A, Han S, Kalgutkar AS, Klug-McLeod J, Garcia-Irizarry C, Li J, Lippa B, Price DA, Southers JA, Walker DP, Wei L, Xiao J, Zawistoski MP, Zhao X. Bhattacharya SK, et al. Among authors: eng h. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7523-9. doi: 10.1016/j.bmcl.2012.10.039. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2012. PMID: 23153798
Demonstration of the innate electrophilicity of 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine (BETP), a small-molecule positive allosteric modulator of the glucagon-like peptide-1 receptor.
Eng H, Sharma R, McDonald TS, Edmonds DJ, Fortin JP, Li X, Stevens BD, Griffith DA, Limberakis C, Nolte WM, Price DA, Jackson M, Kalgutkar AS. Eng H, et al. Drug Metab Dispos. 2013 Aug;41(8):1470-9. doi: 10.1124/dmd.113.052183. Epub 2013 May 7. Drug Metab Dispos. 2013. PMID: 23653442
Undesired versus designed enzymatic cleavage of linkers for liver targeting.
Chirapu SR, Bauman JN, Eng H, Goosen TC, Strelevitz TJ, Sinha SC, Dow RL, Finn MG. Chirapu SR, et al. Among authors: eng h. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1144-7. doi: 10.1016/j.bmcl.2013.12.126. Epub 2014 Jan 8. Bioorg Med Chem Lett. 2014. PMID: 24461291 Free PMC article.
564 results