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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. J Med Chem. 2013 Oct 10;56(19):7706-14. doi: 10.1021/jm4011737. Epub 2013 Sep 27. J Med Chem. 2013. PMID: 24028535
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. 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