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Bioorg Med Chem Lett. 2012 Feb 15;22(4):1686-9. doi: 10.1016/j.bmcl.2011.12.107. Epub 2011 Dec 30.

Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.

Author information

1
Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. jiwenl@amgen.com

Abstract

Our first generation CRTH2 and DP dual antagonists, represented by AMG 009, are more potent toward the CRTH2 receptor than to the DP receptor. Here we report our efforts in the discovery of CRTH2 and DP dual antagonists with more balanced potencies to both receptors, such as compound 15.

PMID:
22264478
DOI:
10.1016/j.bmcl.2011.12.107
[Indexed for MEDLINE]

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