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  • Title: Identification of novel series of human CCR1 antagonists.
    Author: Xie YF, Sircar I, Lake K, Komandla M, Ligsay K, Li J, Xu K, Parise J, Schneider L, Huang D, Liu J, Sakurai N, Barbosa M, Jack R.
    Journal: Bioorg Med Chem Lett; 2008 Mar 15; 18(6):2215-21. PubMed ID: 18329267.
    Abstract:
    A hit-to-lead optimization process was carried out on the high throughput screening hit compound 1 resulting in the identification of several potent and selective CCR1 receptor antagonists. Compound 37 shows the best overall profile with IC(50) values of <100 nM in binding and functional assays.
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