Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR)

…, J Li, P Pircher, M Petrowski, I Schulman…

Index: Flatt, Brenton; Martin, Richard; Wang, Tie-Lin; Mahaney, Paige; Murphy, Brett; Gu, Xiao-Hui; Foster, Paul; Li, Jiali; Pircher, Parinaz; Petrowski, Mary; Schulman, Ira; Westin, Stefan; Wrobel, Jay; Yan, Grace; Bischoff, Eric; Daige, Chris; Mohan, Raju Journal of Medicinal Chemistry, 2009 , vol. 52, # 4 p. 904 - 907

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Citation Number: 92

Abstract

Azepino [4, 5-b] indoles have been identified as potent agonists of the farnesoid X receptor (FXR). In vitro and in vivo optimization has led to the discovery of 6m (XL335, WAY-362450) as a potent, selective, and orally bioavailable FXR agonist (EC50= 4 nM, Eff= 149%). Oral ...