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Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension.
Tran TA, Kramer B, Shin YJ, Vallar P, Boatman PD, Zou N, Sage CR, Gharbaoui T, Krishnan A, Pal B, Shakya SR, Garrido Montalban A, Adams JW, Ramirez J, Behan DP, Shifrina A, Blackburn A, Leakakos T, Shi Y, Morgan M, Sadeque A, Chen W, Unett DJ, Gaidarov I, Chen X, Chang S, Shu HH, Tung SF, Semple G. Tran TA, et al. Among authors: shin yj. J Med Chem. 2017 Feb 9;60(3):913-927. doi: 10.1021/acs.jmedchem.6b00871. Epub 2017 Jan 19. J Med Chem. 2017. PMID: 28072531
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: shin yj. 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
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. Among authors: shin yj. 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 a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile.
Semple G, Lehmann J, Wong A, Ren A, Bruce M, Shin YJ, Sage CR, Morgan M, Chen WC, Sebring K, Chu ZL, Leonard JN, Al-Shamma H, Grottick AJ, Du F, Liang Y, Demarest K, Jones RM. Semple G, et al. Among authors: shin yj. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-5. doi: 10.1016/j.bmcl.2011.12.092. Epub 2011 Dec 30. Bioorg Med Chem Lett. 2012. PMID: 22264481
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.
Skinner PJ, Cherrier MC, Webb PJ, Shin YJ, Gharbaoui T, Lindstrom A, Hong V, Tamura SY, Dang HT, Pride CC, Chen R, Richman JG, Connolly DT, Semple G. Skinner PJ, et al. Among authors: shin yj. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5620-3. doi: 10.1016/j.bmcl.2007.07.101. Epub 2007 Aug 23. Bioorg Med Chem Lett. 2007. PMID: 17804224
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. Among authors: shin yj. 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
710 results