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Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.
Cho YS, Angove H, Brain C, Chen CH, Cheng H, Cheng R, Chopra R, Chung K, Congreve M, Dagostin C, Davis DJ, Feltell R, Giraldes J, Hiscock SD, Kim S, Kovats S, Lagu B, Lewry K, Loo A, Lu Y, Luzzio M, Maniara W, McMenamin R, Mortenson PN, Benning R, O'Reilly M, Rees DC, Shen J, Smith T, Wang Y, Williams G, Woolford AJ, Wrona W, Xu M, Yang F, Howard S. Cho YS, et al. Among authors: congreve m. ACS Med Chem Lett. 2012 May 17;3(6):445-9. doi: 10.1021/ml200241a. eCollection 2012 Jun 14. ACS Med Chem Lett. 2012. PMID: 24900493 Free PMC article.
Fragment-based lead discovery.
Rees DC, Congreve M, Murray CW, Carr R. Rees DC, et al. Among authors: congreve m. Nat Rev Drug Discov. 2004 Aug;3(8):660-72. doi: 10.1038/nrd1467. Nat Rev Drug Discov. 2004. PMID: 15286733 Review. No abstract available.
Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation.
Gill AL, Frederickson M, Cleasby A, Woodhead SJ, Carr MG, Woodhead AJ, Walker MT, Congreve MS, Devine LA, Tisi D, O'Reilly M, Seavers LC, Davis DJ, Curry J, Anthony R, Padova A, Murray CW, Carr RA, Jhoti H. Gill AL, et al. Among authors: congreve ms. J Med Chem. 2005 Jan 27;48(2):414-26. doi: 10.1021/jm049575n. J Med Chem. 2005. PMID: 15658855
Fragment-based lead discovery: leads by design.
Carr RA, Congreve M, Murray CW, Rees DC. Carr RA, et al. Among authors: congreve m. Drug Discov Today. 2005 Jul 15;10(14):987-92. doi: 10.1016/S1359-6446(05)03511-7. Drug Discov Today. 2005. PMID: 16023057 Review.
Application of fragment screening by X-ray crystallography to beta-secretase.
Murray CW, Callaghan O, Chessari G, Cleasby A, Congreve M, Frederickson M, Hartshorn MJ, McMenamin R, Patel S, Wallis N. Murray CW, et al. Among authors: congreve m. J Med Chem. 2007 Mar 22;50(6):1116-23. doi: 10.1021/jm0611962. Epub 2007 Feb 22. J Med Chem. 2007. PMID: 17315856
Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.
Edwards PD, Albert JS, Sylvester M, Aharony D, Andisik D, Callaghan O, Campbell JB, Carr RA, Chessari G, Congreve M, Frederickson M, Folmer RH, Geschwindner S, Koether G, Kolmodin K, Krumrine J, Mauger RC, Murray CW, Olsson LL, Patel S, Spear N, Tian G. Edwards PD, et al. Among authors: congreve m. J Med Chem. 2007 Nov 29;50(24):5912-25. doi: 10.1021/jm070829p. Epub 2007 Nov 7. J Med Chem. 2007. PMID: 17985862
72 results