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Page 1
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. Wilson DM, et al. Among authors: brough s. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6890-6. doi: 10.1016/j.bmcl.2013.09.090. Epub 2013 Oct 5. Bioorg Med Chem Lett. 2013. PMID: 24269482
1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.
Porter RA, Chan WN, Coulton S, Johns A, Hadley MS, Widdowson K, Jerman JC, Brough SJ, Coldwell M, Smart D, Jewitt F, Jeffrey P, Austin N. Porter RA, et al. Among authors: brough sj. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1907-10. doi: 10.1016/s0960-894x(01)00343-2. Bioorg Med Chem Lett. 2001. PMID: 11459658
Discovery of small molecule antagonists of TRPV1.
Rami HK, Thompson M, Wyman P, Jerman JC, Egerton J, Brough S, Stevens AJ, Randall AD, Smart D, Gunthorpe MJ, Davis JB. Rami HK, et al. Among authors: brough s. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3631-4. doi: 10.1016/j.bmcl.2004.05.028. Bioorg Med Chem Lett. 2004. PMID: 15203132
Switching between agonists and antagonists at CRTh2 in a series of highly potent and selective biaryl phenoxyacetic acids.
Luker T, Bonnert R, Schmidt J, Sargent C, Paine SW, Thom S, Pairaudeau G, Patel A, Mohammed R, Akam E, Dougall I, Davis AM, Abbott P, Brough S, Millichip I, McInally T. Luker T, et al. Among authors: brough s. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3616-21. doi: 10.1016/j.bmcl.2011.04.101. Epub 2011 Apr 28. Bioorg Med Chem Lett. 2011. PMID: 21592791
Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.
Gianotti M, Botta M, Brough S, Carletti R, Castiglioni E, Corti C, Dal-Cin M, Delle Fratte S, Korajac D, Lovric M, Merlo G, Mesic M, Pavone F, Piccoli L, Rast S, Roscic M, Sava A, Smehil M, Stasi L, Togninelli A, Wigglesworth MJ. Gianotti M, et al. Among authors: brough s. J Med Chem. 2010 Nov 11;53(21):7778-95. doi: 10.1021/jm100856p. J Med Chem. 2010. PMID: 20942472
The discovery of CCR3/H1 dual antagonists with reduced hERG risk.
Bahl A, Barton P, Bowers K, Brough S, Evans R, Luckhurst CA, Mochel T, Perry MW, Rigby A, Riley RJ, Sanganee H, Sisson A, Springthorpe B. Bahl A, et al. Among authors: brough s. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6688-93. doi: 10.1016/j.bmcl.2012.08.124. Epub 2012 Sep 15. Bioorg Med Chem Lett. 2012. PMID: 23031591
Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor.
Gunthorpe MJ, Hannan SL, Smart D, Jerman JC, Arpino S, Smith GD, Brough S, Wright J, Egerton J, Lappin SC, Holland VA, Winborn K, Thompson M, Rami HK, Randall A, Davis JB. Gunthorpe MJ, et al. Among authors: brough s. J Pharmacol Exp Ther. 2007 Jun;321(3):1183-92. doi: 10.1124/jpet.106.116657. Epub 2007 Mar 28. J Pharmacol Exp Ther. 2007. PMID: 17392405
72 results