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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: lee ec. 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
A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity.
Filipski KJ, Bian J, Ebner DC, Lee EC, Li JC, Sammons MF, Wright SW, Stevens BD, Didiuk MT, Tu M, Perreault C, Brown J, Atkinson K, Tan B, Salatto CT, Litchfield J, Pfefferkorn JA, Guzman-Perez A. Filipski KJ, et al. Among authors: lee ec. Bioorg Med Chem Lett. 2012 Jan 1;22(1):415-20. doi: 10.1016/j.bmcl.2011.10.113. Epub 2011 Nov 6. Bioorg Med Chem Lett. 2012. PMID: 22119466
The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus.
Guzman-Perez A, Pfefferkorn JA, Lee EC, Stevens BD, Aspnes GE, Bian J, Didiuk MT, Filipski KJ, Moore D, Perreault C, Sammons MF, Tu M, Brown J, Atkinson K, Litchfield J, Tan B, Samas B, Zavadoski WJ, Salatto CT, Treadway J. Guzman-Perez A, et al. Among authors: lee ec. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8. doi: 10.1016/j.bmcl.2013.03.014. Epub 2013 Mar 13. Bioorg Med Chem Lett. 2013. PMID: 23562063
Identification of a novel conformationally constrained glucagon receptor antagonist.
Lee EC, Tu M, Stevens BD, Bian J, Aspnes G, Perreault C, Sammons MF, Wright SW, Litchfield J, Kalgutkar AS, Sharma R, Didiuk MT, Ebner DC, Filipski KJ, Brown J, Atkinson K, Pfefferkorn JA, Guzman-Perez A. Lee EC, et al. Bioorg Med Chem Lett. 2014 Feb 1;24(3):839-44. doi: 10.1016/j.bmcl.2013.12.090. Epub 2013 Dec 28. Bioorg Med Chem Lett. 2014. PMID: 24418771
Chemical Probe Identification Platform for Orphan GPCRs Using Focused Compound Screening: GPR39 as a Case Example.
Boehm M, Hepworth D, Loria PM, Norquay LD, Filipski KJ, Chin JE, Cameron KO, Brenner M, Bonnette P, Cabral S, Conn E, Ebner DC, Gautreau D, Hadcock J, Lee EC, Mathiowetz AM, Morin M, Rogers L, Smith A, VanVolkenburg M, Carpino PA. Boehm M, et al. Among authors: lee ec. ACS Med Chem Lett. 2013 Sep 16;4(11):1079-84. doi: 10.1021/ml400275z. eCollection 2013 Nov 14. ACS Med Chem Lett. 2013. PMID: 24900608 Free PMC article.
Optimization of amide-based EP3 receptor antagonists.
Lee EC, Futatsugi K, Arcari JT, Bahnck K, Coffey SB, Derksen DR, Kalgutkar AS, Loria PM, Sharma R. Lee EC, et al. Bioorg Med Chem Lett. 2016 Jun 1;26(11):2670-5. doi: 10.1016/j.bmcl.2016.04.009. Epub 2016 Apr 9. Bioorg Med Chem Lett. 2016. PMID: 27107947
Amine promiscuity and toxicology analysis.
Lee EC, Steeno G, Wassermann AM, Zhang L, Shah F, Price DA. Lee EC, et al. Bioorg Med Chem Lett. 2017 Feb 1;27(3):653-657. doi: 10.1016/j.bmcl.2016.11.085. Epub 2016 Nov 29. Bioorg Med Chem Lett. 2017. PMID: 28011216
Bispecific Estrogen Receptor α Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening.
Disch JS, Duffy JM, Lee ECY, Gikunju D, Chan B, Levin B, Monteiro MI, Talcott SA, Lau AC, Zhou F, Kozhushnyan A, Westlund NE, Mullins PB, Yu Y, von Rechenberg M, Zhang J, Arnautova YA, Liu Y, Zhang Y, McRiner AJ, Keefe AD, Kohlmann A, Clark MA, Cuozzo JW, Huguet C, Arora S. Disch JS, et al. J Med Chem. 2021 Apr 22;64(8):5049-5066. doi: 10.1021/acs.jmedchem.1c00127. Epub 2021 Apr 12. J Med Chem. 2021. PMID: 33844532
530 results