Albert JS - Search Results

1

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. Curr Top Med Chem. 2007;7(16):1600-29. doi: 10.2174/156802607782341091. Curr Top Med Chem. 2007. PMID: 17979771 Review.

2

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: albert js. J Med Chem. 2007 Nov 29;50(24):5912-25. doi: 10.1021/jm070829p. Epub 2007 Nov 7. J Med Chem. 2007. PMID: 17985862

3

Discovery of a novel warhead against beta-secretase through fragment-based lead generation.

Geschwindner S, Olsson LL, Albert JS, Deinum J, Edwards PD, de Beer T, Folmer RH. Geschwindner S, et al. Among authors: albert js. J Med Chem. 2007 Nov 29;50(24):5903-11. doi: 10.1021/jm070825k. Epub 2007 Nov 7. J Med Chem. 2007. PMID: 17985861

4

Development of a plate-based optical biosensor fragment screening methodology to identify phosphodiesterase 10A inhibitors.

Geschwindner S, Dekker N, Horsefield R, Tigerström A, Johansson P, Scott CW, Albert JS. Geschwindner S, et al. Among authors: albert js. J Med Chem. 2013 Apr 25;56(8):3228-34. doi: 10.1021/jm301665y. Epub 2013 Apr 9. J Med Chem. 2013. PMID: 23509991

5

Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.

Varnes JG, Geschwindner S, Holmquist CR, Forst J, Wang X, Dekker N, Scott CW, Tian G, Wood MW, Albert JS. Varnes JG, et al. Among authors: albert js. Bioorg Med Chem Lett. 2016 Jan 1;26(1):197-202. doi: 10.1016/j.bmcl.2015.10.100. Epub 2015 Nov 11. Bioorg Med Chem Lett. 2016. PMID: 26597534

6

Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of beta-secretase.

Congreve M, Aharony D, Albert J, Callaghan O, Campbell J, Carr RA, Chessari G, Cowan S, Edwards PD, Frederickson M, McMenamin R, Murray CW, Patel S, Wallis N. Congreve M, et al. J Med Chem. 2007 Mar 22;50(6):1124-32. doi: 10.1021/jm061197u. Epub 2007 Feb 22. J Med Chem. 2007. PMID: 17315857

7

Progress in the development of beta-secretase inhibitors for Alzheimer's disease.

Albert JS. Albert JS. Prog Med Chem. 2009;48:133-61. doi: 10.1016/s0079-6468(09)04804-8. Prog Med Chem. 2009. PMID: 21544959 Review.

8

Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.

Albert JS, Ohnmacht C, Bernstein PR, Rumsey WL, Aharony D, Alelyunas Y, Russell DJ, Potts W, Sherwood SA, Shen L, Dedinas RF, Palmer WE, Russell K. Albert JS, et al. J Med Chem. 2004 Jan 29;47(3):519-29. doi: 10.1021/jm030197g. J Med Chem. 2004. PMID: 14736234

9

Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.

Albert JS, Aharony D, Andisik D, Barthlow H, Bernstein PR, Bialecki RA, Dedinas R, Dembofsky BT, Hill D, Kirkland K, Koether GM, Kosmider BJ, Ohnmacht C, Palmer W, Potts W, Rumsey W, Shen L, Shenvi A, Sherwood S, Warwick PJ, Russell K. Albert JS, et al. J Med Chem. 2002 Aug 29;45(18):3972-83. doi: 10.1021/jm020094i. J Med Chem. 2002. PMID: 12190319

10

Synthesis and SAR of sulfoxide substituted carboxyquinolines as NK3 receptor antagonists.

Xiong H, Kang J, Woods JM, McCauley JP Jr, Koether GM, Albert JS, Hinkley L, Li Y, Gadient RA, Simpson TR. Xiong H, et al. Among authors: albert js. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1896-9. doi: 10.1016/j.bmcl.2010.11.003. Epub 2010 Dec 21. Bioorg Med Chem Lett. 2011. PMID: 21320776

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