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Page 1
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.
Bruce I, Akhlaq M, Bloomfield GC, Budd E, Cox B, Cuenoud B, Finan P, Gedeck P, Hatto J, Hayler JF, Head D, Keller T, Kirman L, Leblanc C, Le Grand D, McCarthy C, O'Connor D, Owen C, Oza MS, Pilgrim G, Press NE, Sviridenko L, Whitehead L. Bruce I, et al. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5445-50. doi: 10.1016/j.bmcl.2012.07.042. Epub 2012 Jul 17. Bioorg Med Chem Lett. 2012. PMID: 22863202
Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders.
Ladduwahetty T, Gilligan M, Humphries A, Merchant KJ, Fish R, McAlister G, Ivarsson M, Dominguez M, O'Connor D, MacLeod AM. Ladduwahetty T, et al. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12. doi: 10.1016/j.bmcl.2010.04.090. Epub 2010 Apr 24. Bioorg Med Chem Lett. 2010. PMID: 20493697
Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition.
Ellard JM, Madin A, Philps O, Hopkin M, Henderson S, Birch L, O'Connor D, Arai T, Takase K, Morgan L, Reynolds D, Talma S, Howley E, Powney B, Payne AH, Hall A, Gartlon JE, Dawson LA, Castro L, Atkinson PJ. Ellard JM, et al. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5792-6. doi: 10.1016/j.bmcl.2015.10.050. Epub 2015 Oct 17. Bioorg Med Chem Lett. 2015. PMID: 26531152
Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction.
Jones P, Atack JR, Braun MP, Cato BP, Chambers MS, O'Connor D, Cook SM, Hobbs SC, Maxey R, Szekeres HJ, Szeto N, Wafford KA, MacLeod AM. Jones P, et al. Bioorg Med Chem Lett. 2006 Feb 15;16(4):872-5. doi: 10.1016/j.bmcl.2005.11.012. Epub 2005 Nov 21. Bioorg Med Chem Lett. 2006. PMID: 16303300
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
Carling RW, Moore KW, Street LJ, Wild D, Isted C, Leeson PD, Thomas S, O'Connor D, McKernan RM, Quirk K, Cook SM, Atack JR, Wafford KA, Thompson SA, Dawson GR, Ferris P, Castro JL. Carling RW, et al. J Med Chem. 2004 Mar 25;47(7):1807-22. doi: 10.1021/jm031020p. J Med Chem. 2004. PMID: 15027873
2,729 results