| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1362198 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
High throughput screening of the Roche compound library identified benzanilides such as 1 and 2 as antagonists of TAAR1. Optimisation of this hit series led to the first selective TAAR1 antagonist (N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide EPPTB (RO5212773, 9f) having IC50 of 28 nM at mouse TAAR1.
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Related Topics
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Authors
Henri Stalder, Marius C. Hoener, Roger D. Norcross,