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64 results

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Page 1
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. Heightman TD, et al. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6584-7. doi: 10.1016/j.bmcl.2007.09.067. Epub 2007 Sep 25. Bioorg Med Chem Lett. 2007. PMID: 17942309
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. Witherington J, et al. Among authors: 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. Bioorg Med Chem Lett. 2008. PMID: 18316188
Identification of small molecule agonists of the motilin receptor.
Heightman TD, Conway E, Corbett DF, Macdonald GJ, Stemp G, Westaway SM, Celestini P, Gagliardi S, Riccaboni M, Ronzoni S, Vaidya K, Butler S, McKay F, Muir A, Powney B, Winborn K, Wise A, Jarvie EM, Sanger GJ. Heightman TD, et al. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6423-8. doi: 10.1016/j.bmcl.2008.10.071. Epub 2008 Oct 19. Bioorg Med Chem Lett. 2008. PMID: 18980843
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. Witherington J, et al. Among authors: 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. Bioorg Med Chem Lett. 2009. PMID: 19128969
The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.
Bailey JM, Scott JS, Basilla JB, Bolton VJ, Boyfield I, Evans DG, Fleury E, Heightman TD, Jarvie EM, Lawless K, Matthews KL, McKay F, Mok H, Muir A, Orlek BS, Sanger GJ, Stemp G, Stevens AJ, Thompson M, Ward J, Vaidya K, Westaway SM. Bailey JM, et al. Among authors: heightman td. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6452-8. doi: 10.1016/j.bmcl.2009.09.027. Epub 2009 Sep 12. Bioorg Med Chem Lett. 2009. PMID: 19804969
The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.
Westaway SM, Brown SL, Conway E, Heightman TD, Johnson CN, Lapsley K, Macdonald GJ, MacPherson DT, Mitchell DJ, Myatt JW, Seal JT, Stanway SJ, Stemp G, Thompson M, Celestini P, Colombo A, Consonni A, Gagliardi S, Riccaboni M, Ronzoni S, Briggs MA, Matthews KL, Stevens AJ, Bolton VJ, Boyfield I, Jarvie EM, Stratton SC, Sanger GJ. Westaway SM, et al. Among authors: heightman td. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6429-36. doi: 10.1016/j.bmcl.2008.10.072. Epub 2008 Oct 19. Bioorg Med Chem Lett. 2008. PMID: 19006669
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. Wilson DM, et al. Among authors: heightman td. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6897-901. doi: 10.1016/j.bmcl.2013.09.089. Epub 2013 Oct 5. Bioorg Med Chem Lett. 2013. PMID: 24161834
Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
Skidmore J, Heer J, Johnson CN, Norton D, Redshaw S, Sweeting J, Hurst D, Cridland A, Vesey D, Wall I, Ahmed M, Rivers D, Myatt J, Giblin G, Philpott K, Kumar U, Stevens A, Bit RA, Haynes A, Taylor S, Watson R, Witherington J, Demont E, Heightman TD. Skidmore J, et al. Among authors: heightman td. J Med Chem. 2014 Dec 26;57(24):10424-42. doi: 10.1021/jm5010336. Epub 2014 Dec 15. J Med Chem. 2014. PMID: 25431977
Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
Demont EH, Arpino S, Bit RA, Campbell CA, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Harrison LA, Haynes A, Heightman TD, Holmes DS, Humphreys PG, Kumar U, Morse MA, Osborne GJ, Panchal T, Philpott KL, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. Among authors: heightman td. J Med Chem. 2011 Oct 13;54(19):6724-33. doi: 10.1021/jm200609t. Epub 2011 Sep 9. J Med Chem. 2011. PMID: 21838322
64 results