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(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. J Med Chem. 2012 Jul 26;55(14):6363-74. doi: 10.1021/jm3007257. Epub 2012 Jul 10. J Med Chem. 2012. PMID: 22742641
Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists.
McCoull W, Barton P, Brown AJ, Bowker SS, Cameron J, Clarke DS, Davies RD, Dossetter AG, Ertan A, Fenwick M, Green C, Holmes JL, Martin N, Masters D, Moore JE, Newcombe NJ, Newton C, Pointon H, Robb GR, Sheldon C, Stokes S, Morgan D. McCoull W, et al. Among authors: dossetter ag. J Med Chem. 2014 Jul 24;57(14):6128-40. doi: 10.1021/jm500610n. Epub 2014 Jul 8. J Med Chem. 2014. PMID: 24967667
Learning Medicinal Chemistry Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) Rules from Cross-Company Matched Molecular Pairs Analysis (MMPA).
Kramer C, Ting A, Zheng H, Hert J, Schindler T, Stahl M, Robb G, Crawford JJ, Blaney J, Montague S, Leach AG, Dossetter AG, Griffen EJ. Kramer C, et al. Among authors: dossetter ag. J Med Chem. 2018 Apr 26;61(8):3277-3292. doi: 10.1021/acs.jmedchem.7b00935. Epub 2017 Sep 28. J Med Chem. 2018. PMID: 28956609
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: dossetter ag. J Med Chem. 2012 Oct 25;55(20):8827-37. doi: 10.1021/jm301119s. Epub 2012 Oct 11. J Med Chem. 2012. PMID: 22984809
The discovery of benzanilides as c-Met receptor tyrosine kinase inhibitors by a directed screening approach.
Allen JV, Bardelle C, Blades K, Buttar D, Chapman L, Colclough N, Dossetter AG, Garner AP, Girdwood A, Lambert C, Leach AG, Law B, Major J, Plant H, Slater AM. Allen JV, et al. Among authors: dossetter ag. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5224-9. doi: 10.1016/j.bmcl.2011.07.047. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21835616
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. 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
Chemists: AI Is Here; Unite To Get the Benefits.
Griffen EJ, Dossetter AG, Leach AG. Griffen EJ, et al. Among authors: dossetter ag. J Med Chem. 2020 Aug 27;63(16):8695-8704. doi: 10.1021/acs.jmedchem.0c00163. Epub 2020 Jun 11. J Med Chem. 2020. PMID: 32459965 Review.
22 results