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Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target.
Henley ZA, Amour A, Barton N, Bantscheff M, Bergamini G, Bertrand SM, Convery M, Down K, Dümpelfeld B, Edwards CD, Grandi P, Gore PM, Keeling S, Livia S, Mallett D, Maxwell A, Price M, Rau C, Reinhard FBM, Rowedder J, Rowland P, Taylor JA, Thomas DA, Hessel EM, Hamblin JN. Henley ZA, et al. J Med Chem. 2020 Jan 23;63(2):638-655. doi: 10.1021/acs.jmedchem.9b01585. Epub 2020 Jan 8. J Med Chem. 2020. PMID: 31855425
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. 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
Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists.
Procopiou PA, Barrett JW, Barton NP, Begg M, Clapham D, Copley RC, Ford AJ, Graves RH, Hall DA, Hancock AP, Hill AP, Hobbs H, Hodgson ST, Jumeaux C, Lacroix YM, Miah AH, Morriss KM, Needham D, Sheriff EB, Slack RJ, Smith CE, Sollis SL, Staton H. Procopiou PA, et al. Among authors: barton np. J Med Chem. 2013 Mar 14;56(5):1946-60. doi: 10.1021/jm301572h. Epub 2013 Feb 27. J Med Chem. 2013. PMID: 23409871
A practical drug discovery project at the undergraduate level.
Fray MJ, Macdonald SJ, Baldwin IR, Barton N, Brown J, Campbell IB, Churcher I, Coe DM, Cooper AW, Craven AP, Fisher G, Inglis GG, Kelly HA, Liddle J, Maxwell AC, Patel VK, Swanson S, Wellaway N. Fray MJ, et al. Drug Discov Today. 2013 Dec;18(23-24):1158-72. doi: 10.1016/j.drudis.2013.09.004. Epub 2013 Sep 16. Drug Discov Today. 2013. PMID: 24051399
18 results