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ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.
Souers AJ, Leverson JD, Boghaert ER, Ackler SL, Catron ND, Chen J, Dayton BD, Ding H, Enschede SH, Fairbrother WJ, Huang DC, Hymowitz SG, Jin S, Khaw SL, Kovar PJ, Lam LT, Lee J, Maecker HL, Marsh KC, Mason KD, Mitten MJ, Nimmer PM, Oleksijew A, Park CH, Park CM, Phillips DC, Roberts AW, Sampath D, Seymour JF, Smith ML, Sullivan GM, Tahir SK, Tse C, Wendt MD, Xiao Y, Xue JC, Zhang H, Humerickhouse RA, Rosenberg SH, Elmore SW. Souers AJ, et al. Among authors: dayton bd. Nat Med. 2013 Feb;19(2):202-8. doi: 10.1038/nm.3048. Epub 2013 Jan 6. Nat Med. 2013. PMID: 23291630
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: dayton bd. 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
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. J Med Chem. 2005 Mar 10;48(5):1318-21. doi: 10.1021/jm0490890. J Med Chem. 2005. PMID: 15743174
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: dayton bd. J Med Chem. 2012 Feb 23;55(4):1751-7. doi: 10.1021/jm201524g. Epub 2012 Feb 10. J Med Chem. 2012. PMID: 22263872
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: dayton bd. 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
Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.
Judd AS, Souers AJ, Wodka D, Zhao G, Mulhern MM, Iyengar RR, Gao J, Lynch JK, Freeman JC, Falls HD, Brodjian S, Dayton BD, Reilly RM, Gintant G, Limberis JT, Mikhail A, Leitza ST, Houseman KA, Diaz G, Bush EN, Shapiro R, Knourek-Segel V, Hernandez LE, Marsh KC, Sham HL, Collins CA, Kym PR. Judd AS, et al. Among authors: dayton bd. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2365-71. doi: 10.1016/j.bmcl.2006.11.068. Epub 2006 Dec 1. Bioorg Med Chem Lett. 2007. PMID: 17350253
Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor.
Zhao G, Souers AJ, Voorbach M, Falls HD, Droz B, Brodjian S, Lau YY, Iyengar RR, Gao J, Judd AS, Wagaw SH, Ravn MM, Engstrom KM, Lynch JK, Mulhern MM, Freeman J, Dayton BD, Wang X, Grihalde N, Fry D, Beno DW, Marsh KC, Su Z, Diaz GJ, Collins CA, Sham H, Reilly RM, Brune ME, Kym PR. Zhao G, et al. Among authors: dayton bd. J Med Chem. 2008 Feb 14;51(3):380-3. doi: 10.1021/jm7013887. Epub 2008 Jan 10. J Med Chem. 2008. PMID: 18183944
43 results