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Page 1
Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors.
Garton NS, Barker MD, Davis RP, Douault C, Hooper-Greenhill E, Jones E, Lewis HD, Liddle J, Lugo D, McCleary S, Preston AGS, Ramirez-Molina C, Neu M, Shipley TJ, Somers DO, Watson RJ, Wilson DM. Garton NS, et al. Among authors: jones e. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4606-4612. doi: 10.1016/j.bmcl.2016.08.070. Epub 2016 Aug 23. Bioorg Med Chem Lett. 2016. PMID: 27578246
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: jones e. 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
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.
Christopher JA, Atkinson FL, Bax BD, Brown MJ, Champigny AC, Chuang TT, Jones EJ, Mosley JE, Musgrave JR. Christopher JA, et al. Among authors: jones ej. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2230-4. doi: 10.1016/j.bmcl.2009.02.098. Epub 2009 Feb 28. Bioorg Med Chem Lett. 2009. PMID: 19303774
Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation.
Liddle J, Hutchinson JP, Kitchen S, Rowland P, Neu M, Cecconie T, Holmes DS, Jones E, Korczynska J, Koumantou D, Lea JD, Nickels L, Pemberton M, Phillipou A, Schneck JL, Sheehan H, Tinworth CP, Uings I, Wojno-Picon J, Young RJ, Stratikos E. Liddle J, et al. Among authors: jones e. J Med Chem. 2020 Mar 26;63(6):3348-3358. doi: 10.1021/acs.jmedchem.9b02123. Epub 2020 Mar 9. J Med Chem. 2020. PMID: 32109056
A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.
Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H, Eberhard D, Hutchinson S, Jones E, Katso R, Leveridge M, Mander PK, Mosley J, Ramirez-Molina C, Rowland P, Schofield CJ, Sheppard RJ, Smith JE, Swales C, Tanner R, Thomas P, Tumber A, Drewes G, Oppermann U, Patel DJ, Lee K, Wilson DM. Kruidenier L, et al. Among authors: jones e. Nature. 2012 Aug 16;488(7411):404-8. doi: 10.1038/nature11262. Nature. 2012. PMID: 22842901 Free PMC article.
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
Demont EH, Bamborough P, Chung CW, Craggs PD, Fallon D, Gordon LJ, Grandi P, Hobbs CI, Hussain J, Jones EJ, Le Gall A, Michon AM, Mitchell DJ, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ. Demont EH, et al. ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5. doi: 10.1021/ml5002932. eCollection 2014 Nov 13. ACS Med Chem Lett. 2014. PMID: 25408830 Free PMC article.
Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins.
Preston A, Atkinson S, Bamborough P, Chung CW, Craggs PD, Gordon L, Grandi P, Gray JRJ, Jones EJ, Lindon M, Michon AM, Mitchell DJ, Prinjha RK, Rianjongdee F, Rioja I, Seal J, Taylor S, Wall I, Watson RJ, Woolven J, Demont EH. Preston A, et al. J Med Chem. 2020 Sep 10;63(17):9070-9092. doi: 10.1021/acs.jmedchem.0c00605. Epub 2020 Aug 20. J Med Chem. 2020. PMID: 32691591
Kruidenier et al. reply.
Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H, Eberhard D, Hutchinson S, Jones E, Katso R, Leveridge M, Mander PK, Mosley J, Ramirez-Molina C, Rowland P, Schofield CJ, Sheppard RJ, Smith JE, Swales C, Tanner R, Thomas P, Tumber A, Drewes G, Oppermann U, Patel DJ, Lee K, Wilson DM. Kruidenier L, et al. Among authors: jones e. Nature. 2014 Oct 2;514(7520):E2. doi: 10.1038/nature13689. Nature. 2014. PMID: 25279927 No abstract available.
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.
Demont EH, Chung CW, Furze RC, Grandi P, Michon AM, Wellaway C, Barrett N, Bridges AM, Craggs PD, Diallo H, Dixon DP, Douault C, Emmons AJ, Jones EJ, Karamshi BV, Locke K, Mitchell DJ, Mouzon BH, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ, Bamborough P. Demont EH, et al. J Med Chem. 2015 Jul 23;58(14):5649-73. doi: 10.1021/acs.jmedchem.5b00772. Epub 2015 Jul 9. J Med Chem. 2015. PMID: 26155854
6,441 results