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420 results

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Page 1
Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors.
Gonzalez-Lopez de Turiso F, Shin Y, Brown M, Cardozo M, Chen Y, Fong D, Hao X, He X, Henne K, Hu YL, Johnson MG, Kohn T, Lohman J, McBride HJ, McGee LR, Medina JC, Metz D, Miner K, Mohn D, Pattaropong V, Seganish J, Simard JL, Wannberg S, Whittington DA, Yu G, Cushing TD. Gonzalez-Lopez de Turiso F, et al. Among authors: johnson mg. J Med Chem. 2012 Sep 13;55(17):7667-85. doi: 10.1021/jm300679u. Epub 2012 Aug 29. J Med Chem. 2012. PMID: 22876881
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
Johnson M, Li AR, Liu J, Fu Z, Zhu L, Miao S, Wang X, Xu Q, Huang A, Marcus A, Xu F, Ebsworth K, Sablan E, Danao J, Kumer J, Dairaghi D, Lawrence C, Sullivan T, Tonn G, Schall T, Collins T, Medina J. Johnson M, et al. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43. doi: 10.1016/j.bmcl.2007.03.106. Epub 2007 Apr 6. Bioorg Med Chem Lett. 2007. PMID: 17448658
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
Li AR, Johnson MG, Liu J, Chen X, Du X, Mihalic JT, Deignan J, Gustin DJ, Duquette J, Fu Z, Zhu L, Marcus AP, Bergeron P, McGee LR, Danao J, Lemon B, Carabeo T, Sullivan T, Ma J, Tang L, Tonn G, Collins TL, Medina JC. Li AR, et al. Among authors: johnson mg. Bioorg Med Chem Lett. 2008 Jan 15;18(2):688-93. doi: 10.1016/j.bmcl.2007.11.060. Epub 2007 Nov 21. Bioorg Med Chem Lett. 2008. PMID: 18061451
An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing.
Tonn GR, Wong SG, Wong SC, Johnson MG, Ma J, Cho R, Floren LC, Kersey K, Berry K, Marcus AP, Wang X, Van Lengerich B, Medina JC, Pearson PG, Wong BK. Tonn GR, et al. Among authors: johnson mg. Drug Metab Dispos. 2009 Mar;37(3):502-13. doi: 10.1124/dmd.108.021931. Epub 2008 Dec 16. Drug Metab Dispos. 2009. PMID: 19088267 Clinical Trial.
Optimization of a series of quinazolinone-derived antagonists of CXCR3.
Liu J, Fu Z, Li AR, Johnson M, Zhu L, Marcus A, Danao J, Sullivan T, Tonn G, Collins T, Medina J. Liu J, et al. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5114-8. doi: 10.1016/j.bmcl.2009.07.032. Epub 2009 Jul 10. Bioorg Med Chem Lett. 2009. PMID: 19632842
Bioactivation of a novel 2-methylindole-containing dual chemoattractant receptor-homologous molecule expressed on T-helper type-2 cells/D-prostanoid receptor antagonist leads to mechanism-based CYP3A inactivation: glutathione adduct characterization and prediction of in vivo drug-drug interaction.
Wong SG, Fan PW, Subramanian R, Tonn GR, Henne KR, Johnson MG, Tadano Lohr M, Wong BK. Wong SG, et al. Among authors: johnson mg. Drug Metab Dispos. 2010 May;38(5):841-50. doi: 10.1124/dmd.109.031344. Epub 2010 Jan 25. Drug Metab Dispos. 2010. PMID: 20100816
Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists.
Lucas BS, Aaron W, An S, Austin RJ, Brown M, Chan H, Chong A, Hungate R, Huang T, Jiang B, Johnson MG, Kaizerman JA, Lee G, McMinn DL, Orf J, Powers JP, Rong M, Toteva MM, Uyeda C, Wickramasinghe D, Xu G, Ye Q, Zhong W. Lucas BS, et al. Among authors: johnson mg. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3618-22. doi: 10.1016/j.bmcl.2010.04.110. Epub 2010 Apr 28. Bioorg Med Chem Lett. 2010. PMID: 20493695
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.
Brown ML, Aaron W, Austin RJ, Chong A, Huang T, Jiang B, Kaizerman JA, Lee G, Lucas BS, McMinn DL, Orf J, Rong M, Toteva MM, Xu G, Ye Q, Zhong W, Degraffenreid MR, Wickramasinghe D, Powers JP, Hungate R, Johnson MG. Brown ML, et al. Among authors: johnson mg. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5206-9. doi: 10.1016/j.bmcl.2011.07.052. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21840217
Discovery of potent and specific CXCR3 antagonists.
Chen X, Mihalic J, Deignan J, Gustin DJ, Duquette J, Du X, Chan J, Fu Z, Johnson M, Li AR, Henne K, Sullivan T, Lemon B, Ma J, Miao S, Tonn G, Collins T, Medina JC. Chen X, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):357-62. doi: 10.1016/j.bmcl.2011.10.120. Epub 2011 Nov 9. Bioorg Med Chem Lett. 2012. PMID: 22130135
Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.
Liu JJ, Wang Y, Johnson MG, Li AR, Shen W, Wang X, Su Y, Brown M, Van Lengerich B, Rickel E, Martin T, Budelsky A, Seitz L, Danao J, Tang HL, Collins T, Medina JC. Liu JJ, et al. Among authors: johnson mg. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1686-9. doi: 10.1016/j.bmcl.2011.12.107. Epub 2011 Dec 30. Bioorg Med Chem Lett. 2012. PMID: 22264478
420 results