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Bioorg Med Chem Lett. 2013 Mar 1;23(5):1228-31. doi: 10.1016/j.bmcl.2013.01.005. Epub 2013 Jan 11.

1-(4-Phenylpiperazin-1-yl)-2-(1H-pyrazol-1-yl)ethanones as novel CCR1 antagonists.

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1
ChemoCentryx, Inc., 850 Maude Avenue, Mountain View, CA 94043, USA.

Abstract

A novel series of CCR1 antagonists based on the 1-(4-phenylpiperazin-1-yl)-2-(1H-pyrazol-1-yl)ethanone scaffold was identified by screening a compound library utilizing CCR1-expressing human THP-1 cells. SAR studies led to the discovery of the highly potent and selective CCR1 antagonist 14 (CCR1 binding IC(50)=4 nM using [(125)I]-CCL3 as the chemokine ligand). Compound 14 displayed promising pharmacokinetic and toxicological profiles in preclinical species.

PMID:
23374868
DOI:
10.1016/j.bmcl.2013.01.005
[Indexed for MEDLINE]

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