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185 results

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Page 1
Exploitation of a Novel Binding Pocket in Human Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Discovered through X-ray Fragment Screening.
Woolford AJ, Pero JE, Aravapalli S, Berdini V, Coyle JE, Day PJ, Dodson AM, Grondin P, Holding FP, Lee LY, Li P, Manas ES, Marino J Jr, Martin AC, McCleland BW, McMenamin RL, Murray CW, Neipp CE, Page LW, Patel VK, Potvain F, Rich S, Rivero RA, Smith K, Somers DO, Trottet L, Velagaleti R, Williams G, Xie R. Woolford AJ, et al. Among authors: patel vk. J Med Chem. 2016 Jun 9;59(11):5356-67. doi: 10.1021/acs.jmedchem.6b00212. Epub 2016 May 20. J Med Chem. 2016. PMID: 27167608
Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2).
Woolford AJ, Day PJ, Bénéton V, Berdini V, Coyle JE, Dudit Y, Grondin P, Huet P, Lee LY, Manas ES, McMenamin RL, Murray CW, Page LW, Patel VK, Potvain F, Rich SJ, Sang Y, Somers DO, Trottet L, Wan Z, Zhang X. Woolford AJ, et al. Among authors: patel vk. J Med Chem. 2016 Dec 8;59(23):10738-10749. doi: 10.1021/acs.jmedchem.6b01427. Epub 2016 Nov 18. J Med Chem. 2016. PMID: 27933945
Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode.
Down K, Amour A, Anderson NA, Barton N, Campos S, Cannons EP, Clissold C, Convery MA, Coward JJ, Doyle K, Duempelfeld B, Edwards CD, Goldsmith MD, Krause J, Mallett DN, McGonagle GA, Patel VK, Rowedder J, Rowland P, Sharpe A, Sriskantharajah S, Thomas DA, Thomson DW, Uddin S, Hamblin JN, Hessel EM. Down K, et al. Among authors: patel vk. J Med Chem. 2021 Sep 23;64(18):13780-13792. doi: 10.1021/acs.jmedchem.1c01102. Epub 2021 Sep 11. J Med Chem. 2021. PMID: 34510892
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.
Humphreys PG, Anderson NA, Bamborough P, Baxter A, Chung CW, Cookson R, Craggs PD, Dalton T, Fournier JCL, Gordon LJ, Gray HF, Gray MW, Gregory R, Hirst DJ, Jamieson C, Jones KL, Kessedjian H, Lugo D, McGonagle G, Patel VK, Patten C, Poole DL, Prinjha RK, Ramirez-Molina C, Rioja I, Seal G, Stafford KAJ, Shah RR, Tape D, Theodoulou NH, Tomlinson L, Ukuser S, Wall ID, Wellaway N, White G. Humphreys PG, et al. Among authors: patel vk. J Med Chem. 2022 Nov 24;65(22):15174-15207. doi: 10.1021/acs.jmedchem.2c01102. Epub 2022 Nov 15. J Med Chem. 2022. PMID: 36378954
Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.
Watson NS, Brown D, Campbell M, Chan C, Chaudry L, Convery MA, Fenwick R, Hamblin JN, Haslam C, Kelly HA, King NP, Kurtis CL, Leach AR, Manchee GR, Mason AM, Mitchell C, Patel C, Patel VK, Senger S, Shah GP, Weston HE, Whitworth C, Young RJ. Watson NS, et al. Among authors: patel vk, patel c. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3784-8. doi: 10.1016/j.bmcl.2006.04.053. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16697194
N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics.
Bamborough P, Angell RM, Bhamra I, Brown D, Bull J, Christopher JA, Cooper AW, Fazal LH, Giordano I, Hind L, Patel VK, Ranshaw LE, Sims MJ, Skone PA, Smith KJ, Vickerstaff E, Washington M. Bamborough P, et al. Among authors: patel vk. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4363-8. doi: 10.1016/j.bmcl.2007.04.029. Epub 2007 Apr 13. Bioorg Med Chem Lett. 2007. PMID: 17600705
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: patel vk. 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
One-Step Synthesis of Photoaffinity Probes for Live-Cell MS-Based Proteomics.
Fallon DJ, Lehmann S, Chung CW, Phillipou A, Eberl C, Fantom KGM, Zappacosta F, Patel VK, Bantscheff M, Schofield CJ, Tomkinson NCO, Bush JT. Fallon DJ, et al. Among authors: patel vk. Chemistry. 2021 Dec 20;27(71):17880-17888. doi: 10.1002/chem.202102036. Epub 2021 Sep 14. Chemistry. 2021. PMID: 34328642 Free article.
185 results