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Description: BMS-830216 is a prodrug of BMS-819881 which is a novel and potent antagonist of MCHR1 (Melanin concentrating hormone receptor 1) with minimal hERG activity. It binds to rat MCHR1 with a Ki of 7 nM and is also selective for CYP3A4 activity with an EC50 of 13 uM. BMS-819881 has the potential to be used as an anti-obesity drug. It is currently under investigation in Phase 1 clinical trial for treating obesity as the phosphate ester pro-drug (BMS-830216).
References: J Med Chem. 2014 Sep 25; 57(18):7509-22.
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