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2,654 results

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Page 1
Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists.
Vilums M, Zweemer AJ, Yu Z, de Vries H, Hillger JM, Wapenaar H, Bollen IA, Barmare F, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, Ijzerman AP. Vilums M, et al. Among authors: saunders j. J Med Chem. 2013 Oct 10;56(19):7706-14. doi: 10.1021/jm4011737. Epub 2013 Sep 27. J Med Chem. 2013. PMID: 24028535
Multiple binding sites for small-molecule antagonists at the CC chemokine receptor 2.
Zweemer AJ, Nederpelt I, Vrieling H, Hafith S, Doornbos ML, de Vries H, Abt J, Gross R, Stamos D, Saunders J, Smit MJ, Ijzerman AP, Heitman LH. Zweemer AJ, et al. Among authors: saunders j. Mol Pharmacol. 2013 Oct;84(4):551-61. doi: 10.1124/mol.113.086850. Epub 2013 Jul 22. Mol Pharmacol. 2013. PMID: 23877010
When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists.
Vilums M, Zweemer AJ, Barmare F, van der Gracht AM, Bleeker DC, Yu Z, de Vries H, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, IJzerman AP. Vilums M, et al. Among authors: saunders j. Eur J Med Chem. 2015 Mar 26;93:121-34. doi: 10.1016/j.ejmech.2015.01.063. Epub 2015 Feb 2. Eur J Med Chem. 2015. PMID: 25666912
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents.
Slee DH, Chen Y, Zhang X, Moorjani M, Lanier MC, Lin E, Rueter JK, Williams JP, Lechner SM, Markison S, Malany S, Santos M, Gross RS, Jalali K, Sai Y, Zuo Z, Yang C, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J. Slee DH, et al. Among authors: saunders j. J Med Chem. 2008 Mar 27;51(6):1719-29. doi: 10.1021/jm701185v. Epub 2008 Feb 29. J Med Chem. 2008. PMID: 18307292
Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.
Gross RS, Guo Z, Dyck B, Coon T, Huang CQ, Lowe RF, Marinkovic D, Moorjani M, Nelson J, Zamani-Kord S, Grigoriadis DE, Hoare SR, Crowe PD, Bu JH, Haddach M, McCarthy J, Saunders J, Sullivan R, Chen T, Williams JP. Gross RS, et al. Among authors: saunders j. J Med Chem. 2005 Sep 8;48(18):5780-93. doi: 10.1021/jm049085v. J Med Chem. 2005. PMID: 16134945
2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A(2A) antagonists with reduced hERG liability.
Moorjani M, Zhang X, Chen Y, Lin E, Rueter JK, Gross RS, Lanier MC, Tellew JE, Williams JP, Lechner SM, Malany S, Santos M, Ekhlassi P, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J, Slee DH. Moorjani M, et al. Among authors: saunders j. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1269-73. doi: 10.1016/j.bmcl.2008.01.036. Epub 2008 Jan 13. Bioorg Med Chem Lett. 2008. PMID: 18249540
Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.
Dyck B, Grigoriadis DE, Gross RS, Guo Z, Haddach M, Marinkovic D, McCarthy JR, Moorjani M, Regan CF, Saunders J, Schwaebe MK, Szabo T, Williams JP, Zhang X, Bozigian H, Chen TK. Dyck B, et al. Among authors: saunders j. J Med Chem. 2005 Jun 16;48(12):4100-10. doi: 10.1021/jm050070m. J Med Chem. 2005. PMID: 15943483
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.
Slee DH, Moorjani M, Zhang X, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Jalali K, Sai Y, Zuo Z, Yang C, Wen J, O'Brien Z, Petroski R, Saunders J. Slee DH, et al. Among authors: saunders j. J Med Chem. 2008 Mar 27;51(6):1730-9. doi: 10.1021/jm701187w. Epub 2008 Feb 29. J Med Chem. 2008. PMID: 18307293
Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.
Zhang X, Rueter JK, Chen Y, Moorjani M, Lanier MC, Lin E, Gross RS, Tellew JE, Williams JP, Lechner SM, Markison S, Joswig T, Malany S, Santos M, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J, Slee DH. Zhang X, et al. Among authors: saunders j. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1778-83. doi: 10.1016/j.bmcl.2008.02.032. Epub 2008 Feb 16. Bioorg Med Chem Lett. 2008. PMID: 18329269
2,654 results