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Items: 18

1.

Discovery of a Potent and Orally Bioavailable Cyclophilin Inhibitor Derived from the Sanglifehrin Macrocycle.

Mackman RL, Steadman VA, Dean DK, Jansa P, Poullennec KG, Appleby T, Austin C, Blakemore CA, Cai R, Cannizzaro C, Chin G, Chiva JC, Dunbar NA, Fliri H, Highton AJ, Hui H, Ji M, Jin H, Karki K, Keats AJ, Lazarides L, Lee YJ, Liclican A, Mish M, Murray B, Pettit SB, Pyun P, Sangi M, Santos R, Sanvoisin J, Schmitz U, Schrier A, Siegel D, Sperandio D, Stepan G, Tian Y, Watt GM, Yang H, Schultz BE.

J Med Chem. 2018 Nov 8;61(21):9473-9499. doi: 10.1021/acs.jmedchem.8b00802. Epub 2018 Aug 22.

PMID:
30074795
2.

Discovery of Potent Cyclophilin Inhibitors Based on the Structural Simplification of Sanglifehrin A.

Steadman VA, Pettit SB, Poullennec KG, Lazarides L, Keats AJ, Dean DK, Stanway SJ, Austin CA, Sanvoisin JA, Watt GM, Fliri HG, Liclican AC, Jin D, Wong MH, Leavitt SA, Lee YJ, Tian Y, Frey CR, Appleby TC, Schmitz U, Jansa P, Mackman RL, Schultz BE.

J Med Chem. 2017 Feb 9;60(3):1000-1017. doi: 10.1021/acs.jmedchem.6b01329. Epub 2017 Jan 31.

PMID:
28075591
3.

Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.

Wilson DM, Apps J, Bailey N, Bamford MJ, Beresford IJ, Brackenborough K, Briggs MA, Brough S, Calver AR, Crook B, Davis RK, Davis RP, Davis S, Dean DK, Harris L, Heslop T, Holland V, Jeffrey P, Panchal TA, Parr CA, Quashie N, Schogger J, Sehmi SS, Stean TO, Steadman JG, Trail B, Wald J, Worby A, Takle AK, Witherington J, Medhurst AD.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6890-6. doi: 10.1016/j.bmcl.2013.09.090. Epub 2013 Oct 5.

PMID:
24269482
4.

The discovery of the benzazepine class of histamine H3 receptor antagonists.

Wilson DM, Apps J, Bailey N, Bamford MJ, Beresford IJ, Briggs MA, Calver AR, Crook B, Davis RP, Davis S, Dean DK, Harris L, Heightman TD, Panchal T, Parr CA, Quashie N, Steadman JG, Schogger J, Sehmi SS, Stean TO, Takle AK, Trail BK, White T, Witherington J, Worby A, Medhurst AD.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6897-901. doi: 10.1016/j.bmcl.2013.09.089. Epub 2013 Oct 5.

PMID:
24161834
5.

Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor.

Abberley L, Bebius A, Beswick PJ, Billinton A, Collis KL, Dean DK, Fonfria E, Gleave RJ, Medhurst SJ, Michel AD, Moses AP, Patel S, Roman SA, Scoccitti T, Smith B, Steadman JG, Walter DS.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6370-4. doi: 10.1016/j.bmcl.2010.09.101. Epub 2010 Sep 22.

PMID:
20934331
6.

Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.

Abdi MH, Beswick PJ, Billinton A, Chambers LJ, Charlton A, Collins SD, Collis KL, Dean DK, Fonfria E, Gleave RJ, Lejeune CL, Livermore DG, Medhurst SJ, Michel AD, Moses AP, Page L, Patel S, Roman SA, Senger S, Slingsby B, Steadman JG, Stevens AJ, Walter DS.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5080-4. doi: 10.1016/j.bmcl.2010.07.033. Epub 2010 Jul 14.

PMID:
20673717
7.

Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.

Beswick PJ, Billinton A, Chambers LJ, Dean DK, Fonfria E, Gleave RJ, Medhurst SJ, Michel AD, Moses AP, Patel S, Roman SA, Roomans S, Senger S, Stevens AJ, Walter DS.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4653-6. doi: 10.1016/j.bmcl.2010.05.107. Epub 2010 Jun 8.

PMID:
20579878
8.

Mechanism of action of species-selective P2X(7) receptor antagonists.

Michel AD, Ng SW, Roman S, Clay WC, Dean DK, Walter DS.

Br J Pharmacol. 2009 Apr;156(8):1312-25. doi: 10.1111/j.1476-5381.2009.00135.x. Epub 2009 Mar 20.

9.

Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor.

Witherington J, Abberley L, Bellenie BR, Boatman R, Collis K, Dean DK, Gaiba A, King NP, Shuker N, Steadman JG, Takle AK, Sanger G, Butler S, McKay F, Muir A, Winborn K, Ward RW, Heightman TD.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):684-7. doi: 10.1016/j.bmcl.2008.12.042. Epub 2008 Dec 14.

PMID:
19128969
10.

The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase.

Takle AK, Bamford MJ, Davies S, Davis RP, Dean DK, Gaiba A, Irving EA, King FD, Naylor A, Parr CA, Ray AM, Reith AD, Smith BB, Staton PC, Steadman JG, Stean TO, Wilson DM.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4373-6. doi: 10.1016/j.bmcl.2008.06.070. Epub 2008 Jun 24.

PMID:
18621524
11.

Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation.

Witherington J, Abberley L, Briggs MA, Collis K, Dean DK, Gaiba A, King NP, Kraus H, Shuker N, Steadman JG, Takle AK, Sanger G, Wadsworth G, Butler S, McKay F, Muir A, Winborn K, Heightman TD.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2203-5. doi: 10.1016/j.bmcl.2007.12.021. Epub 2007 Dec 15.

PMID:
18316188
12.

Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification.

Heightman TD, Scott JS, Longley M, Bordas V, Dean DK, Elliott R, Hutley G, Witherington J, Abberley L, Passingham B, Berlanga M, de Los Frailes M, Wise A, Powney B, Muir A, McKay F, Butler S, Winborn K, Gardner C, Darton J, Campbell C, Sanger G.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6584-7. Epub 2007 Sep 25.

PMID:
17942309
13.

The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.

Takle AK, Brown MJ, Davies S, Dean DK, Francis G, Gaiba A, Hird AW, King FD, Lovell PJ, Naylor A, Reith AD, Steadman JG, Wilson DM.

Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81. Epub 2005 Nov 2.

PMID:
16260133
14.

(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.

Bamford MJ, Bailey N, Davies S, Dean DK, Francis L, Panchal TA, Parr CA, Sehmi S, Steadman JG, Takle AK, Townsend JT, Wilson DM.

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3407-11.

PMID:
15955699
15.

(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.

Bamford MJ, Alberti MJ, Bailey N, Davies S, Dean DK, Gaiba A, Garland S, Harling JD, Jung DK, Panchal TA, Parr CA, Steadman JG, Takle AK, Townsend JT, Wilson DM, Witherington J.

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3402-6. Erratum in: Bioorg Med Chem Lett. 2015 Mar 1;25(5):1151.

PMID:
15950465
17.

The contribution of classical (beta1/2-) and atypical beta-adrenoceptors to the stimulation of human white adipocyte lipolysis and right atrial appendage contraction by novel beta3-adrenoceptor agonists of differing selectivities.

Sennitt MV, Kaumann AJ, Molenaar P, Beeley LJ, Young PW, Kelly J, Chapman H, Henson SM, Berge JM, Dean DK, Kotecha NR, Morgan HK, Rami HK, Ward RW, Thompson M, Wilson S, Smith SA, Cawthorne MA, Stock MJ, Arch JR.

J Pharmacol Exp Ther. 1998 Jun;285(3):1084-95. Erratum in: J Pharmacol Exp Ther 1998 Dec;287(3):1135.

PMID:
9618411
18.

Synthesis and antifungal activity of C-16 oximino and vinyl amphotericin B derivatives.

Corbett DF, Dean DK, Greenlees AR, Macpherson DT.

J Antibiot (Tokyo). 1995 Jun;48(6):509-15.

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