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15,030 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: brown m. 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 in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.
Cushing TD, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, Chen Y, Duquette J, Fisher B, Gonzalez-Lopez de Turiso F, He X, Henne KR, Hu YL, Hungate R, Johnson MG, Kelly RC, Lucas B, McCarter JD, McGee LR, Medina JC, San Miguel T, Mohn D, Pattaropong V, Pettus LH, Reichelt A, Rzasa RM, Seganish J, Tasker AS, Wahl RC, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang D, Metz DP. Cushing TD, et al. Among authors: brown m. J Med Chem. 2015 Jan 8;58(1):480-511. doi: 10.1021/jm501624r. Epub 2014 Dec 3. J Med Chem. 2015. PMID: 25469863
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: brown m. 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
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. Among authors: brown m. 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.
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. 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
Structure guided design of a series of sphingosine kinase (SphK) inhibitors.
Gustin DJ, Li Y, Brown ML, Min X, Schmitt MJ, Wanska M, Wang X, Connors R, Johnstone S, Cardozo M, Cheng AC, Jeffries S, Franks B, Li S, Shen S, Wong M, Wesche H, Xu G, Carlson TJ, Plant M, Morgenstern K, Rex K, Schmitt J, Coxon A, Walker N, Kayser F, Wang Z. Gustin DJ, et al. Among authors: brown ml. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4608-16. doi: 10.1016/j.bmcl.2013.06.030. Epub 2013 Jun 20. Bioorg Med Chem Lett. 2013. PMID: 23845219
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: brown m. 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
Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.
Kaizerman JA, Aaron W, An S, Austin R, Brown M, Chong A, Huang T, Hungate R, Jiang B, Johnson MG, Lee G, Lucas BS, Orf J, Rong M, Toteva MM, Wickramasinghe D, Xu G, Ye Q, Zhong W, McMinn DL. Kaizerman JA, et al. Among authors: brown m. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4607-10. doi: 10.1016/j.bmcl.2010.06.006. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20594845
Design and synthesis of a novel series of [1-(4-hydroxy-benzyl)-1H-indol-5-yloxy]-acetic acid compounds as potent, selective, thyroid hormone receptor β agonists.
Burkholder TP, Cunningham BE, Clayton JR, Lander PA, Brown ML, Doti RA, Durst GL, Montrose-Rafizadeh C, King C, Osborne HE, Amos RM, Zink RW, Stramm LE, Burris TP, Cardona G, Konkol DL, Reidy C, Christe ME, Genin MJ. Burkholder TP, et al. Among authors: brown ml. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1377-80. doi: 10.1016/j.bmcl.2015.02.062. Epub 2015 Mar 3. Bioorg Med Chem Lett. 2015. PMID: 25752984
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