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Page 1
Small molecule binding sites on the Ras:SOS complex can be exploited for inhibition of Ras activation.
Winter JJ, Anderson M, Blades K, Brassington C, Breeze AL, Chresta C, Embrey K, Fairley G, Faulder P, Finlay MR, Kettle JG, Nowak T, Overman R, Patel SJ, Perkins P, Spadola L, Tart J, Tucker JA, Wrigley G. Winter JJ, et al. Among authors: fairley g. J Med Chem. 2015 Mar 12;58(5):2265-74. doi: 10.1021/jm501660t. Epub 2015 Feb 26. J Med Chem. 2015. PMID: 25695162 Free article.
Diverse heterocyclic scaffolds as allosteric inhibitors of AKT.
Kettle JG, Brown S, Crafter C, Davies BR, Dudley P, Fairley G, Faulder P, Fillery S, Greenwood H, Hawkins J, James M, Johnson K, Lane CD, Pass M, Pink JH, Plant H, Cosulich SC. Kettle JG, et al. Among authors: fairley g. J Med Chem. 2012 Feb 9;55(3):1261-73. doi: 10.1021/jm201394e. Epub 2012 Jan 27. J Med Chem. 2012. PMID: 22248236
Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.
Kettle JG, Ballard P, Bardelle C, Cockerill M, Colclough N, Critchlow SE, Debreczeni J, Fairley G, Fillery S, Graham MA, Goodwin L, Guichard S, Hudson K, Ward RA, Whittaker D. Kettle JG, et al. Among authors: fairley g. J Med Chem. 2015 Mar 26;58(6):2834-44. doi: 10.1021/acs.jmedchem.5b00098. Epub 2015 Mar 12. J Med Chem. 2015. PMID: 25738750
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.
Ward RA, Colclough N, Challinor M, Debreczeni JE, Eckersley K, Fairley G, Feron L, Flemington V, Graham MA, Greenwood R, Hopcroft P, Howard TD, James M, Jones CD, Jones CR, Renshaw J, Roberts K, Snow L, Tonge M, Yeung K. Ward RA, et al. Among authors: fairley g. J Med Chem. 2015 Jun 11;58(11):4790-801. doi: 10.1021/acs.jmedchem.5b00466. Epub 2015 May 28. J Med Chem. 2015. PMID: 25977981
Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point.
Ward RA, Bethel P, Cook C, Davies E, Debreczeni JE, Fairley G, Feron L, Flemington V, Graham MA, Greenwood R, Griffin N, Hanson L, Hopcroft P, Howard TD, Hudson J, James M, Jones CD, Jones CR, Lamont S, Lewis R, Lindsay N, Roberts K, Simpson I, St-Gallay S, Swallow S, Tang J, Tonge M, Wang Z, Zhai B. Ward RA, et al. Among authors: fairley g. J Med Chem. 2017 Apr 27;60(8):3438-3450. doi: 10.1021/acs.jmedchem.7b00267. Epub 2017 Apr 14. J Med Chem. 2017. PMID: 28376306
Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).
Ward RA, Anderton MJ, Bethel P, Breed J, Cook C, Davies EJ, Dobson A, Dong Z, Fairley G, Farrington P, Feron L, Flemington V, Gibbons FD, Graham MA, Greenwood R, Hanson L, Hopcroft P, Howells R, Hudson J, James M, Jones CD, Jones CR, Li Y, Lamont S, Lewis R, Lindsay N, McCabe J, McGuire T, Rawlins P, Roberts K, Sandin L, Simpson I, Swallow S, Tang J, Tomkinson G, Tonge M, Wang Z, Zhai B. Ward RA, et al. Among authors: fairley g. J Med Chem. 2019 Dec 26;62(24):11004-11018. doi: 10.1021/acs.jmedchem.9b01295. Epub 2019 Nov 25. J Med Chem. 2019. PMID: 31710489
Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy.
McCoull W, Boyd S, Brown MR, Coen M, Collingwood O, Davies NL, Doherty A, Fairley G, Goldberg K, Hardaker E, He G, Hennessy EJ, Hopcroft P, Hodgson G, Jackson A, Jiang X, Karmokar A, Lainé AL, Lindsay N, Mao Y, Markandu R, McMurray L, McLean N, Mooney L, Musgrove H, Nissink JWM, Pflug A, Reddy VP, Rawlins PB, Rivers E, Schimpl M, Smith GF, Tentarelli S, Travers J, Troup RI, Walton J, Wang C, Wilkinson S, Williamson B, Winter-Holt J, Yang D, Zheng Y, Zhu Q, Smith PD. McCoull W, et al. Among authors: fairley g. J Med Chem. 2021 Sep 23;64(18):13524-13539. doi: 10.1021/acs.jmedchem.1c00920. Epub 2021 Sep 3. J Med Chem. 2021. PMID: 34478292
Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.
Scott JS, Moss TA, Barlaam B, Davey PRJ, Fairley G, Gangl ET, Greenwood RDR, Hatoum-Mokdad H, Lister AS, Longmire D, Polanski R, Stokes S, Tucker MJ, Varnes JG, Yang B. Scott JS, et al. Among authors: fairley g. ACS Med Chem Lett. 2020 Oct 28;11(12):2519-2525. doi: 10.1021/acsmedchemlett.0c00505. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335676 Free PMC article.
77 results