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Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate.
Ratcliffe P, Adam JM, Baker J, Bursi R, Campbell R, Clark JK, Cottney JE, Deehan M, Easson AM, Ecker D, Edwards D, Epemolu O, Evans L, Fields R, Francis S, Harradine P, Jeremiah F, Kiyoi T, McArthur D, Morrison A, Passier P, Pick J, Schnabel PG, Schulz J, Steinbrede H, Walker G, Westwood P, Wishart G, Udo de Haes J. Ratcliffe P, et al. Among authors: campbell r. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2541-6. doi: 10.1016/j.bmcl.2011.02.023. Epub 2011 Feb 12. Bioorg Med Chem Lett. 2011. PMID: 21411321
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.
Kiyoi T, Adam JM, Clark JK, Davies K, Easson AM, Edwards D, Feilden H, Fields R, Francis S, Jeremiah F, McArthur D, Morrison AJ, Prosser A, Ratcliffe PD, Schulz J, Wishart G, Baker J, Campbell R, Cottney JE, Deehan M, Epemolu O, Evans L. Kiyoi T, et al. Among authors: campbell r. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1748-53. doi: 10.1016/j.bmcl.2011.01.082. Epub 2011 Jan 22. Bioorg Med Chem Lett. 2011. PMID: 21316962
Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain.
Adam JM, Clark JK, Davies K, Everett K, Fields R, Francis S, Jeremiah F, Kiyoi T, Maidment M, Morrison A, Ratcliffe P, Prosser A, Schulz J, Wishart G, Baker J, Boyce S, Campbell R, Cottney JE, Deehan M, Martin I. Adam JM, et al. Among authors: campbell r. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2932-7. doi: 10.1016/j.bmcl.2012.02.048. Epub 2012 Feb 23. Bioorg Med Chem Lett. 2012. PMID: 22421020
Design, synthesis, and structure-activity relationships of indole-3-heterocycles as agonists of the CB1 receptor.
Morrison AJ, Adam JM, Baker JA, Campbell RA, Clark JK, Cottney JE, Deehan M, Easson AM, Fields R, Francis S, Jeremiah F, Keddie N, Kiyoi T, McArthur DR, Meyer K, Ratcliffe PD, Schulz J, Wishart G, Yoshiizumi K. Morrison AJ, et al. Among authors: campbell ra. Bioorg Med Chem Lett. 2011 Jan 1;21(1):506-9. doi: 10.1016/j.bmcl.2010.10.093. Epub 2010 Oct 25. Bioorg Med Chem Lett. 2011. PMID: 21075630
A novel series of positive modulators of the AMPA receptor: structure-based lead optimization.
Jamieson C, Campbell RA, Cumming IA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Maclean JK, Martin F, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L. Jamieson C, et al. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6072-5. doi: 10.1016/j.bmcl.2010.08.063. Epub 2010 Aug 15. Bioorg Med Chem Lett. 2010. PMID: 20817521 Free article.
Structure based evolution of a novel series of positive modulators of the AMPA receptor.
Jamieson C, Maclean JK, Brown CI, Campbell RA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L. Jamieson C, et al. Bioorg Med Chem Lett. 2011 Jan 15;21(2):805-11. doi: 10.1016/j.bmcl.2010.11.098. Epub 2010 Nov 25. Bioorg Med Chem Lett. 2011. PMID: 21190850 Free article.
A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies.
Jamieson C, Basten S, Campbell RA, Cumming IA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Maclean JK, Moir EM, Morrow JA, Papakosta M, Rankovic Z, Smith L. Jamieson C, et al. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5753-6. doi: 10.1016/j.bmcl.2010.07.138. Epub 2010 Aug 13. Bioorg Med Chem Lett. 2010. PMID: 20805031 Free article.
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
Gehling VS, Vaswani RG, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Dakin LA, Cook AS, Gagnon A, Harmange JC, Audia JE, Cummings RT, Normant E, Trojer P, Albrecht BK. Gehling VS, et al. Among authors: campbell r. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3644-9. doi: 10.1016/j.bmcl.2015.06.056. Epub 2015 Jun 19. Bioorg Med Chem Lett. 2015. PMID: 26189078
Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
Vaswani RG, Gehling VS, Dakin LA, Cook AS, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Cantone N, Cummings RT, Normant E, Bellon SF, Albrecht BK, Harmange JC, Trojer P, Audia JE, Zhang Y, Justin N, Chen S, Wilson JR, Gamblin SJ. Vaswani RG, et al. Among authors: campbell r. J Med Chem. 2016 Nov 10;59(21):9928-9941. doi: 10.1021/acs.jmedchem.6b01315. Epub 2016 Oct 28. J Med Chem. 2016. PMID: 27739677 Free PMC article.
N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.
Sidduri A, Tilley JW, Hull K, Lou JP, Kaplan G, Sheffron A, Chen L, Campbell R, Guthrie R, Huang TN, Huby N, Rowan K, Schwinge V, Renzetti LM. Sidduri A, et al. Among authors: campbell r. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2475-8. doi: 10.1016/s0960-894x(02)00386-4. Bioorg Med Chem Lett. 2002. PMID: 12161161
4,533 results