Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue 6, Pages 2666-2670Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm100022r
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Biaryl cyclohexene carboxylic acids were discovered as full and potent niacin receptor (GPR109A) agonists. Compound le (MK-6892) displayed excellent receptor activity, good PK across species, remarkably clean off-target profiles, good ancillary pharmacology, and superior therapeutic window over niacin regarding the FFA reduction versus vasodilation in rats and dogs.
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