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Page 1
Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1.
Yeh VS, Beno DW, Brodjian S, Brune ME, Cullen SC, Dayton BD, Dhaon MK, Falls HD, Gao J, Grihalde N, Hajduk P, Hansen TM, Judd AS, King AJ, Klix RC, Larson KJ, Lau YY, Marsh KC, Mittelstadt SW, Plata D, Rozema MJ, Segreti JA, Stoner EJ, Voorbach MJ, Wang X, Xin X, Zhao G, Collins CA, Cox BF, Reilly RM, Kym PR, Souers AJ. Yeh VS, et al. Among authors: gao j. J Med Chem. 2012 Feb 23;55(4):1751-7. doi: 10.1021/jm201524g. Epub 2012 Feb 10. J Med Chem. 2012. PMID: 22263872
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.
Souers AJ, Wodka D, Gao J, Lewis JC, Vasudevan A, Gentles R, Brodjian S, Dayton B, Ogiela CA, Fry D, Hernandez LE, Marsh KC, Collins CA, Kym PR. Souers AJ, et al. Among authors: gao j. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4873-7. doi: 10.1016/j.bmcl.2004.07.032. Bioorg Med Chem Lett. 2004. PMID: 15341942
Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity.
Souers AJ, Gao J, Brune M, Bush E, Wodka D, Vasudevan A, Judd AS, Mulhern M, Brodjian S, Dayton B, Shapiro R, Hernandez LE, Marsh KC, Sham HL, Collins CA, Kym PR. Souers AJ, et al. Among authors: gao j. J Med Chem. 2005 Mar 10;48(5):1318-21. doi: 10.1021/jm0490890. J Med Chem. 2005. PMID: 15743174
Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Souers AJ, Gao J, Wodka D, Judd AS, Mulhern MM, Napier JJ, Brune ME, Bush EN, Brodjian SJ, Dayton BD, Shapiro R, Hernandez LE, Marsh KC, Sham HL, Collins CA, Kym PR. Souers AJ, et al. Among authors: gao j. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2752-7. doi: 10.1016/j.bmcl.2005.03.114. Bioorg Med Chem Lett. 2005. PMID: 15911251
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: gao j. J Med Chem. 2005 Sep 22;48(19):5888-91. doi: 10.1021/jm050598r. J Med Chem. 2005. PMID: 16161992
Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.
Vasudevan A, Souers AJ, Freeman JC, Verzal MK, Gao J, Mulhern MM, Wodka D, Lynch JK, Engstrom KM, Wagaw SH, Brodjian S, Dayton B, Falls DH, Bush E, Brune M, Shapiro RD, Marsh KC, Hernandez LE, Collins CA, Kym PR. Vasudevan A, et al. Among authors: gao j. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5293-7. doi: 10.1016/j.bmcl.2005.08.049. Epub 2005 Oct 3. Bioorg Med Chem Lett. 2005. PMID: 16203136
Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.
Kym PR, Souers AJ, Campbell TJ, Lynch JK, Judd AS, Iyengar R, Vasudevan A, Gao J, Freeman JC, Wodka D, Mulhern M, Zhao G, Wagaw SH, Napier JJ, Brodjian S, Dayton BD, Reilly RM, Segreti JA, Fryer RM, Preusser LC, Reinhart GA, Hernandez L, Marsh KC, Sham HL, Collins CA, Polakowski JS. Kym PR, et al. Among authors: gao j. J Med Chem. 2006 Apr 6;49(7):2339-52. doi: 10.1021/jm0512286. J Med Chem. 2006. PMID: 16570930
Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.
Souers AJ, Iyengar RR, Judd AS, Beno DW, Gao J, Zhao G, Brune ME, Napier JJ, Mulhern MM, Lynch JK, Freeman JC, Wodka D, Chen CJ, Falls HD, Brodjian S, Dayton BD, Diaz GJ, Bush EN, Shapiro R, Droz BA, Knourek-Segel V, Hernandez LE, Marsh KC, Reilly RM, Sham HL, Collins CA, Kym PR. Souers AJ, et al. Among authors: gao j. Bioorg Med Chem Lett. 2007 Feb 15;17(4):884-9. doi: 10.1016/j.bmcl.2006.11.061. Epub 2006 Dec 1. Bioorg Med Chem Lett. 2007. PMID: 17188866
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