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Page 1
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: stemp g. J Med Chem. 2009 Feb 26;52(4):1180-9. doi: 10.1021/jm801332q. J Med Chem. 2009. PMID: 19191554
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. Among authors: stemp g. 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
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: stemp g. 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 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: stemp g. 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
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.
Ahmed M, Briggs MA, Bromidge SM, Buck T, Campbell L, Deeks NJ, Garner A, Gordon L, Hamprecht DW, Holland V, Johnson CN, Medhurst AD, Mitchell DJ, Moss SF, Powles J, Seal JT, Stean TO, Stemp G, Thompson M, Trail B, Upton N, Winborn K, Witty DR. Ahmed M, et al. Among authors: stemp g. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4867-71. doi: 10.1016/j.bmcl.2005.06.107. Bioorg Med Chem Lett. 2005. PMID: 16143522
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.
Westaway SM, Thompson M, Rami HK, Stemp G, Trouw LS, Mitchell DJ, Seal JT, Medhurst SJ, Lappin SC, Biggs J, Wright J, Arpino S, Jerman JC, Cryan JE, Holland V, Winborn KY, Coleman T, Stevens AJ, Davis JB, Gunthorpe MJ. Westaway SM, et al. Among authors: stemp g. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5609-13. doi: 10.1016/j.bmcl.2008.08.105. Epub 2008 Aug 31. Bioorg Med Chem Lett. 2008. PMID: 18809327
The design of 8,8-dimethyl[1,6]naphthyridines as potential anticonvulsant agents.
Austin NE, Hadley MS, Harling JD, Harrington FP, Macdonald GJ, Mitchell DJ, Riley GJ, Stean TO, Stemp G, Stratton SC, Thompson M, Upton N. Austin NE, et al. Among authors: stemp g. Bioorg Med Chem Lett. 2003 May 19;13(10):1627-9. doi: 10.1016/s0960-894x(03)00288-9. Bioorg Med Chem Lett. 2003. PMID: 12729628
50 results