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Page 1
The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain.
Giblin GM, Bit RA, Brown SH, Chaignot HM, Chowdhury A, Chessell IP, Clayton NM, Coleman T, Hall A, Hammond B, Hurst DN, Michel AD, Naylor A, Novelli R, Scoccitti T, Spalding D, Tang SP, Wilson AW, Wilson R. Giblin GM, et al. Among authors: bit ra. Bioorg Med Chem Lett. 2007 Jan 15;17(2):385-9. doi: 10.1016/j.bmcl.2006.10.041. Epub 2006 Oct 20. Bioorg Med Chem Lett. 2007. PMID: 17084082
Discovery of novel biaryl heterocyclic EP1 receptor antagonists.
Hall A, Bit RA, Brown SH, Chaignot HM, Chessell IP, Coleman T, Giblin GM, Hurst DN, Kilford IR, Lewell XQ, Michel AD, Mohamed S, Naylor A, Novelli R, Skinner L, Spalding DJ, Tang SP, Wilson RJ. Hall A, et al. Among authors: bit ra. Bioorg Med Chem Lett. 2006 May 15;16(10):2666-71. doi: 10.1016/j.bmcl.2006.02.014. Epub 2006 Feb 28. Bioorg Med Chem Lett. 2006. PMID: 16503138
Novel methylene-linked heterocyclic EP1 receptor antagonists.
Hall A, Bit RA, Brown SH, Chowdhury A, Giblin GM, Hurst DN, Kilford IR, Lewell X, Naylor A, Scoccitti T. Hall A, et al. Among authors: bit ra. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1592-7. doi: 10.1016/j.bmcl.2008.01.071. Epub 2008 Jan 19. Bioorg Med Chem Lett. 2008. PMID: 18262416
Pyrazolopyridazine alpha-2-delta-1 ligands for the treatment of neuropathic pain.
Myatt JW, Healy MP, Bravi GS, Billinton A, Johnson CN, Matthews KL, Jandu KS, Meng W, Hersey A, Livermore DG, Douault CB, Witherington J, Bit RA, Rowedder JE, Brown JD, Clayton NM. Myatt JW, et al. Among authors: bit ra. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4683-8. doi: 10.1016/j.bmcl.2010.05.026. Epub 2010 May 31. Bioorg Med Chem Lett. 2010. PMID: 20566291
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: bit ra. 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: bit ra. J Med Chem. 2011 Oct 13;54(19):6724-33. doi: 10.1021/jm200609t. Epub 2011 Sep 9. J Med Chem. 2011. PMID: 21838322
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.
Wellaway CR, Amans D, Bamborough P, Barnett H, Bit RA, Brown JA, Carlson NR, Chung CW, Cooper AWJ, Craggs PD, Davis RP, Dean TW, Evans JP, Gordon L, Harada IL, Hirst DJ, Humphreys PG, Jones KL, Lewis AJ, Lindon MJ, Lugo D, Mahmood M, McCleary S, Medeiros P, Mitchell DJ, O'Sullivan M, Le Gall A, Patel VK, Patten C, Poole DL, Shah RR, Smith JE, Stafford KAJ, Thomas PJ, Vimal M, Wall ID, Watson RJ, Wellaway N, Yao G, Prinjha RK. Wellaway CR, et al. Among authors: bit ra. J Med Chem. 2020 Jan 23;63(2):714-746. doi: 10.1021/acs.jmedchem.9b01670. Epub 2020 Jan 6. J Med Chem. 2020. PMID: 31904959
Structure-based design of peptidomimetic antagonists of p56(lck) SH2 domain.
Hobbs CJ, Bit RA, Cansfield AD, Harris B, Hill CH, Hilyard KL, Kilford IR, Kitas E, Kroehn A, Lovell P, Pole D, Rugman P, Sherborne BS, Smith IE, Vesey DR, Walmsley DL, Whittaker D, Williams G, Wilson F, Banner D, Surgenor A, Borkakoti N. Hobbs CJ, et al. Among authors: bit ra. Bioorg Med Chem Lett. 2002 May 20;12(10):1365-9. doi: 10.1016/s0960-894x(02)00167-1. Bioorg Med Chem Lett. 2002. PMID: 11992778
16 results