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Page 1
Agonist lead identification for the high affinity niacin receptor GPR109a.
Gharbaoui T, Skinner PJ, Shin YJ, Averbuj C, Jung JK, Johnson BR, Duong T, Decaire M, Uy J, Cherrier MC, Webb PJ, Tamura SY, Zou N, Rodriguez N, Boatman PD, Sage CR, Lindstrom A, Xu J, Schrader TO, Smith BM, Chen R, Richman JG, Connolly DT, Colletti SL, Tata JR, Semple G. Gharbaoui T, et al. Among authors: semple g. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4914-9. doi: 10.1016/j.bmcl.2007.06.028. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17588745
Novel H3 receptor antagonists with improved pharmacokinetic profiles.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Semple G, Ren A, Pereira G, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Lorea J, Grottick AJ. Santora VJ, et al. Among authors: semple g. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4133-6. doi: 10.1016/j.bmcl.2008.05.086. Epub 2008 May 24. Bioorg Med Chem Lett. 2008. PMID: 18554904
3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.
Semple G, Skinner PJ, Gharbaoui T, Shin YJ, Jung JK, Cherrier MC, Webb PJ, Tamura SY, Boatman PD, Sage CR, Schrader TO, Chen R, Colletti SL, Tata JR, Waters MG, Cheng K, Taggart AK, Cai TQ, Carballo-Jane E, Behan DP, Connolly DT, Richman JG. Semple G, et al. J Med Chem. 2008 Aug 28;51(16):5101-8. doi: 10.1021/jm800258p. Epub 2008 Jul 30. J Med Chem. 2008. PMID: 18665582
Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Semple G, Ren A, Fioravanti B, Pereira G, Calderon I, Choi K, Xiong Y, Shin YJ, Gharbaoui T, Sage CR, Morgan M, Xing C, Chu ZL, Leonard JN, Grottick AJ, Al-Shamma H, Liang Y, Demarest KT, Jones RM. Semple G, et al. Bioorg Med Chem Lett. 2011 May 15;21(10):3134-41. doi: 10.1016/j.bmcl.2011.03.007. Epub 2011 Mar 13. Bioorg Med Chem Lett. 2011. PMID: 21444206
Identification of biaryl sulfone derivatives as antagonists of the histamine H₃ receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916).
Semple G, Santora VJ, Smith JM, Covel JA, Hayashi R, Gallardo C, Ibarra JB, Schultz JA, Park DM, Estrada SA, Hofilena BJ, Smith BM, Ren A, Suarez M, Frazer J, Edwards JE, Hart R, Hauser EK, Lorea J, Grottick AJ. Semple G, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):71-5. doi: 10.1016/j.bmcl.2011.11.075. Epub 2011 Nov 30. Bioorg Med Chem Lett. 2012. PMID: 22172695
Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series.
Han S, Narayanan S, Kim SH, Calderon I, Zhu X, Kawasaki A, Yue D, Lehmann J, Wong A, Buzard DJ, Semple G, Carroll C, Chu ZL, Al-Sharmma H, Shu HH, Tung SF, Unett DJ, Behan DP, Yoon WH, Morgan M, Usmani KA, Chen C, Sadeque A, Leonard JN, Jones RM. Han S, et al. Among authors: semple g. Bioorg Med Chem Lett. 2015 Aug 1;25(15):3034-8. doi: 10.1016/j.bmcl.2015.04.102. Epub 2015 May 23. Bioorg Med Chem Lett. 2015. PMID: 26048791
80 results