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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. 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. 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. 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
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.
Westaway SM, Brown SL, Fell SC, Johnson CN, MacPherson DT, Mitchell DJ, Myatt JW, Stanway SJ, Seal JT, Stemp G, Thompson M, Lawless K, McKay F, Muir AI, Barford JM, Cluff C, Mahmood SR, Matthews KL, Mohamed S, Smith B, Stevens AJ, Bolton VJ, Jarvie EM, Sanger GJ. Westaway SM, et al. Among authors: muir ai. J Med Chem. 2009 Feb 26;52(4):1180-9. doi: 10.1021/jm801332q. J Med Chem. 2009. PMID: 19191554
28 results