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Page 1
Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.
Scott JS, Birch AM, Brocklehurst KJ, Broo A, Brown HS, Butlin RJ, Clarke DS, Davidsson O, Ertan A, Goldberg K, Groombridge SD, Hudson JA, Laber D, Leach AG, Macfaul PA, McKerrecher D, Pickup A, Schofield P, Svensson PH, Sörme P, Teague J. Scott JS, et al. Among authors: macfaul pa. J Med Chem. 2012 Jun 14;55(11):5361-79. doi: 10.1021/jm300310c. Epub 2012 May 17. J Med Chem. 2012. PMID: 22545772
5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.
Morley AD, Kenny PW, Burton B, Heald RA, Macfaul PA, Mullett J, Page K, Porres SS, Ribeiro LR, Smith P, Ward S, Wilkinson TJ. Morley AD, et al. Among authors: macfaul pa. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1658-61. doi: 10.1016/j.bmcl.2009.01.110. Epub 2009 Feb 6. Bioorg Med Chem Lett. 2009. PMID: 19231183
Novel inhibitors of the alphavbeta3 integrin--lead identification strategy.
Elliot D, Henshaw E, MacFaul PA, Morley AD, Newham P, Oldham K, Page K, Rankine N, Sharpe P, Ting A, Wood CM. Elliot D, et al. Among authors: macfaul pa. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4832-5. doi: 10.1016/j.bmcl.2009.06.041. Epub 2009 Jun 13. Bioorg Med Chem Lett. 2009. PMID: 19574045
Selective non zinc binding inhibitors of MMP13.
De Savi C, Morley AD, Ting A, Nash I, Karabelas K, Wood CM, James M, Norris SJ, Karoutchi G, Rankine N, Hamlin G, Macfaul PA, Ryan D, Baker SV, Hargreaves D, Gerhardt S. De Savi C, et al. Among authors: macfaul pa. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4215-9. doi: 10.1016/j.bmcl.2011.05.075. Epub 2011 May 27. Bioorg Med Chem Lett. 2011. PMID: 21669521
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.
Dossetter AG, Beeley H, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Kenny PW, Krapp S, Martin S, MacFaul PA, McGuire TM, Gutierrez PM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Vickers M. Dossetter AG, et al. Among authors: macfaul pa. J Med Chem. 2012 Jul 26;55(14):6363-74. doi: 10.1021/jm3007257. Epub 2012 Jul 10. J Med Chem. 2012. PMID: 22742641
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Dossetter AG, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, MacFaul PA, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C. Dossetter AG, et al. Among authors: macfaul pa. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5563-8. doi: 10.1016/j.bmcl.2012.07.012. Epub 2012 Jul 15. Bioorg Med Chem Lett. 2012. PMID: 22858142
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.
Crawford JJ, Kenny PW, Bowyer J, Cook CR, Finlayson JE, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, Martin S, Macfaul PA, McDermott BP, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Dossetter AG. Crawford JJ, et al. Among authors: macfaul pa. J Med Chem. 2012 Oct 25;55(20):8827-37. doi: 10.1021/jm301119s. Epub 2012 Oct 11. J Med Chem. 2012. PMID: 22984809
35 results