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From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.
Santella JB 3rd, Gardner DS, Yao W, Shi C, Reddy P, Tebben AJ, DeLucca GV, Wacker DA, Watson PS, Welch PK, Wadman EA, Davies P, Solomon KA, Graden DM, Yeleswaram S, Mandlekar S, Kariv I, Decicco CP, Ko SS, Carter PH, Duncia JV. Santella JB 3rd, et al. Among authors: graden dm. Bioorg Med Chem Lett. 2008 Jan 15;18(2):576-85. doi: 10.1016/j.bmcl.2007.11.067. Epub 2007 Nov 22. Bioorg Med Chem Lett. 2008. PMID: 18096386
N-in-1 dosing pharmacokinetics in drug discovery: experience, theoretical and practical considerations.
He K, Qian M, Wong H, Bai SA, He B, Brogdon B, Grace JE, Xin B, Wu J, Ren SX, Zeng H, Deng Y, Graden DM, Olah TV, Unger SE, Luettgen JM, Knabb RM, Pinto DJ, Lam PY, Duan J, Wexler RR, Decicco CP, Christ DD, Grossman SJ. He K, et al. Among authors: graden dm. J Pharm Sci. 2008 Jul;97(7):2568-80. doi: 10.1002/jps.21196. J Pharm Sci. 2008. PMID: 17914718
Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.
De Lucca GV, Kim UT, Vargo BJ, Duncia JV, Santella JB 3rd, Gardner DS, Zheng C, Liauw A, Wang Z, Emmett G, Wacker DA, Welch PK, Covington M, Stowell NC, Wadman EA, Das AM, Davies P, Yeleswaram S, Graden DM, Solomon KA, Newton RC, Trainor GL, Decicco CP, Ko SS. De Lucca GV, et al. Among authors: graden dm. J Med Chem. 2005 Mar 24;48(6):2194-211. doi: 10.1021/jm049530m. J Med Chem. 2005. PMID: 15771462