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An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca's drug discovery programmes.
Albert JS, Blomberg N, Breeze AL, Brown AJ, Burrows JN, Edwards PD, Folmer RH, Geschwindner S, Griffen EJ, Kenny PW, Nowak T, Olsson LL, Sanganee H, Shapiro AB. Albert JS, et al. Among authors: kenny pw. Curr Top Med Chem. 2007;7(16):1600-29. doi: 10.2174/156802607782341091. Curr Top Med Chem. 2007. PMID: 17979771 Review.
Structure-based design of protein tyrosine phosphatase-1B inhibitors.
Black E, Breed J, Breeze AL, Embrey K, Garcia R, Gero TW, Godfrey L, Kenny PW, Morley AD, Minshull CA, Pannifer AD, Read J, Rees A, Russell DJ, Toader D, Tucker J. Black E, et al. Among authors: kenny pw. Bioorg Med Chem Lett. 2005 May 16;15(10):2503-7. doi: 10.1016/j.bmcl.2005.03.068. Bioorg Med Chem Lett. 2005. PMID: 15863305
Design of compound libraries for fragment screening.
Blomberg N, Cosgrove DA, Kenny PW, Kolmodin K. Blomberg N, et al. Among authors: kenny pw. J Comput Aided Mol Des. 2009 Aug;23(8):513-25. doi: 10.1007/s10822-009-9264-5. Epub 2009 Mar 13. J Comput Aided Mol Des. 2009. PMID: 19283339
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: kenny pw. J Med Chem. 2012 Oct 25;55(20):8827-37. doi: 10.1021/jm301119s. Epub 2012 Oct 11. J Med Chem. 2012. PMID: 22984809
Dipeptidyl nitrile inhibitors of Cathepsin L.
Asaad N, Bethel PA, Coulson MD, Dawson JE, Ford SJ, Gerhardt S, Grist M, Hamlin GA, James MJ, Jones EV, Karoutchi GI, Kenny PW, Morley AD, Oldham K, Rankine N, Ryan D, Wells SL, Wood L, Augustin M, Krapp S, Simader H, Steinbacher S. Asaad N, et al. Among authors: kenny pw. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3. doi: 10.1016/j.bmcl.2009.05.071. Epub 2009 May 27. Bioorg Med Chem Lett. 2009. PMID: 19515558
Design of selective Cathepsin inhibitors.
Bethel PA, Gerhardt S, Jones EV, Kenny PW, Karoutchi GI, Morley AD, Oldham K, Rankine N, Augustin M, Krapp S, Simader H, Steinbacher S. Bethel PA, et al. Among authors: kenny pw. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4622-5. doi: 10.1016/j.bmcl.2009.06.090. Epub 2009 Jun 27. Bioorg Med Chem Lett. 2009. PMID: 19616430
45 results