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Page 1
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).
Duffey MO, Vos TJ, Adams R, Alley J, Anthony J, Barrett C, Bharathan I, Bowman D, Bump NJ, Chau R, Cullis C, Driscoll DL, Elder A, Forsyth N, Frazer J, Guo J, Guo L, Hyer ML, Janowick D, Kulkarni B, Lai SJ, Lasky K, Li G, Li J, Liao D, Little J, Peng B, Qian MG, Reynolds DJ, Rezaei M, Scott MP, Sells TB, Shinde V, Shi QJ, Sintchak MD, Soucy F, Sprott KT, Stroud SG, Nestor M, Visiers I, Weatherhead G, Ye Y, D'Amore N. Duffey MO, et al. Among authors: lai sj. J Med Chem. 2012 Jan 12;55(1):197-208. doi: 10.1021/jm2011172. Epub 2011 Dec 5. J Med Chem. 2012. PMID: 22070629
Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.
Kym PR, Iyengar R, Souers AJ, Lynch JK, Judd AS, Gao J, Freeman J, Mulhern M, Zhao G, Vasudevan A, Wodka D, Blackburn C, Brown J, Che JL, Cullis C, Lai SJ, LaMarche MJ, Marsilje T, Roses J, Sells T, Geddes B, Govek E, Patane M, Fry D, Dayton BD, Brodjian S, Falls D, Brune M, Bush E, Shapiro R, Knourek-Segel V, Fey T, McDowell C, Reinhart GA, Preusser LC, Marsh K, Hernandez L, Sham HL, Collins CA. Kym PR, et al. Among authors: lai sj. J Med Chem. 2005 Sep 22;48(19):5888-91. doi: 10.1021/jm050598r. J Med Chem. 2005. PMID: 16161992
Identification of aminopiperidine benzamides as MCHr1 antagonists.
Vasudevan A, Verzal MK, Wodka D, Souers AJ, Blackburn C, Che JL, Lai S, Brodjian S, Falls DH, Dayton BD, Govek E, Daniels T, Geddes B, Marsh KC, Hernandez LE, Collins CA, Kym PR. Vasudevan A, et al. Bioorg Med Chem Lett. 2005 Jul 15;15(14):3412-6. doi: 10.1016/j.bmcl.2005.05.023. Bioorg Med Chem Lett. 2005. PMID: 15950463
Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies.
Yu M, Lizarzaburu M, Motani A, Fu Z, Du X, Liu JJ, Jiao X, Lai S, Fan P, Fu A, Liu Q, Murakoshi M, Nara F, Oda K, Okuyama R, Reagan JD, Watanabe N, Yamazaki M, Xiong Y, Zhang Y, Zhuang R, Lin DC, Houze JB, Medina JC, Li L. Yu M, et al. ACS Med Chem Lett. 2013 May 1;4(9):829-34. doi: 10.1021/ml4000854. eCollection 2013 Sep 12. ACS Med Chem Lett. 2013. PMID: 24900757 Free PMC article.
Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394.
Dransfield PJ, Pattaropong V, Lai S, Fu Z, Kohn TJ, Du X, Cheng A, Xiong Y, Komorowski R, Jin L, Conn M, Tien E, DeWolf WE Jr, Hinklin RJ, Aicher TD, Kraser CF, Boyd SA, Voegtli WC, Condroski KR, Veniant-Ellison M, Medina JC, Houze J, Coward P. Dransfield PJ, et al. ACS Med Chem Lett. 2016 May 23;7(7):714-8. doi: 10.1021/acsmedchemlett.6b00140. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437083 Free PMC article.
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
Liu J, Li AR, Wang Y, Johnson MG, Su Y, Shen W, Wang X, Lively S, Brown M, Lai S, Gonzalez Lopez De Turiso F, Xu Q, Van Lengerich B, Schmitt M, Fu Z, Sun Y, Lawlis S, Seitz L, Danao J, Wait J, Ye Q, Tang HL, Grillo M, Collins TL, Sullivan TJ, Medina JC. Liu J, et al. ACS Med Chem Lett. 2011 Mar 2;2(5):326-30. doi: 10.1021/ml1002234. eCollection 2011 May 12. ACS Med Chem Lett. 2011. PMID: 24900313 Free PMC article.
Phenylalanine derivatives as GPR142 agonists for the treatment of type II diabetes.
Du X, Kim YJ, Lai S, Chen X, Lizarzaburu M, Turcotte S, Fu Z, Liu Q, Zhang Y, Motani A, Oda K, Okuyama R, Nara F, Murakoshi M, Fu A, Reagan JD, Fan P, Xiong Y, Shen W, Li L, Houze J, Medina JC. Du X, et al. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6218-23. doi: 10.1016/j.bmcl.2012.08.015. Epub 2012 Aug 10. Bioorg Med Chem Lett. 2012. PMID: 22926069
5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.
Kohn TJ, Du X, Lai S, Xiong Y, Komorowski R, Veniant M, Fu Z, Jiao X, Pattaropong V, Chow D, Cardozo M, Jin L, Conn M, DeWolf WE Jr, Kraser CF, Hinklin RJ, Boys ML, Medina JC, Houze J, Dransfield P, Coward P. Kohn TJ, et al. ACS Med Chem Lett. 2016 Jun 1;7(7):666-70. doi: 10.1021/acsmedchemlett.6b00145. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437074 Free PMC article.
175 results