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Page 1
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
Liddle J, Atkinson FL, Barker MD, Carter PS, Curtis NR, Davis RP, Douault C, Dickson MC, Elwes D, Garton NS, Gray M, Hayhow TG, Hobbs CI, Jones E, Leach S, Leavens K, Lewis HD, McCleary S, Neu M, Patel VK, Preston AG, Ramirez-Molina C, Shipley TJ, Skone PA, Smithers N, Somers DO, Walker AL, Watson RJ, Weingarten GG. Liddle J, et al. Among authors: walker al. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6188-94. doi: 10.1016/j.bmcl.2011.07.082. Epub 2011 Aug 12. Bioorg Med Chem Lett. 2011. PMID: 21903390
Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.
Angell RM, Angell TD, Bamborough P, Brown D, Brown M, Buckton JB, Cockerill SG, Edwards CD, Jones KL, Longstaff T, Smee PA, Smith KJ, Somers DO, Walker AL, Willson M. Angell RM, et al. Among authors: walker al. Bioorg Med Chem Lett. 2008 Jan 1;18(1):324-8. doi: 10.1016/j.bmcl.2007.10.043. Epub 2007 Oct 17. Bioorg Med Chem Lett. 2008. PMID: 17981461
Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode.
Angell RM, Bamborough P, Cleasby A, Cockerill SG, Jones KL, Mooney CJ, Somers DO, Walker AL. Angell RM, et al. Among authors: walker al. Bioorg Med Chem Lett. 2008 Jan 1;18(1):318-23. doi: 10.1016/j.bmcl.2007.10.076. Epub 2007 Nov 19. Bioorg Med Chem Lett. 2008. PMID: 18006306
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Angell RM, Angell TD, Bamborough P, Bamford MJ, Chung CW, Cockerill SG, Flack SS, Jones KL, Laine DI, Longstaff T, Ludbrook S, Pearson R, Smith KJ, Smee PA, Somers DO, Walker AL. Angell RM, et al. Among authors: walker al. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4433-7. doi: 10.1016/j.bmcl.2008.06.028. Epub 2008 Jun 12. Bioorg Med Chem Lett. 2008. PMID: 18602262
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.
Angell R, Aston NM, Bamborough P, Buckton JB, Cockerill S, deBoeck SJ, Edwards CD, Holmes DS, Jones KL, Laine DI, Patel S, Smee PA, Smith KJ, Somers DO, Walker AL. Angell R, et al. Among authors: walker al. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4428-32. doi: 10.1016/j.bmcl.2008.06.048. Epub 2008 Jun 18. Bioorg Med Chem Lett. 2008. PMID: 18614366
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).
Seal J, Lamotte Y, Donche F, Bouillot A, Mirguet O, Gellibert F, Nicodeme E, Krysa G, Kirilovsky J, Beinke S, McCleary S, Rioja I, Bamborough P, Chung CW, Gordon L, Lewis T, Walker AL, Cutler L, Lugo D, Wilson DM, Witherington J, Lee K, Prinjha RK. Seal J, et al. Among authors: walker al. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. doi: 10.1016/j.bmcl.2012.02.041. Epub 2012 Feb 24. Bioorg Med Chem Lett. 2012. PMID: 22437115
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E. Gosmini R, et al. Among authors: walker al, walker md. J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24. J Med Chem. 2014. PMID: 25249180
94 results