Identification and Preliminary Characterization of a Potent, Safe, and Orally Efficacious Inhibitor of Acyl-CoA:Diacylglycerol Acyltransferase 1
β Scribed by Yeh, Vince S. C.; Beno, David W. A.; Brodjian, Sevan; Brune, Michael E.; Cullen, Steven C.; Dayton, Brian D.; Dhaon, Madhup K.; Falls, Hugh D.; Gao, Ju; Grihalde, Nelson; Hajduk, Philip; Hansen, T. Matthew; Judd, Andrew S.; King, Andrew J.; Klix, Russel C.; Larson, Kelly J.; Lau, Yau Y.; Marsh, Kennan C.; Mittelstadt, Scott W.; Plata, Dan; Rozema, Michael J.; Segreti, Jason A.; Stoner, Eric J.; Voorbach, Martin J.; Wang, Xiaojun; Xin, Xili; Zhao, Gang; Collins, Christine A.; Cox, Bryan F.; Reilly, Regina M.; Kym, Philip R.; Souers, Andrew J.
- Book ID
- 127119136
- Publisher
- American Chemical Society
- Year
- 2012
- Tongue
- English
- Weight
- 484 KB
- Volume
- 55
- Category
- Article
- ISSN
- 0022-2623
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## Abstract Structureβactivity relationship studies lead to the discovery of compound (I), which shows potent ACAT inhibitory activity (IC~50~ = 12 nM) and good pharmacokinetic profile in mice.