Literature DB >> 21237643

Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773).

Henri Stalder1, Marius C Hoener, Roger D Norcross.   

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 IC(50) of 28 nM at mouse TAAR1.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 21237643     DOI： 10.1016/j.bmcl.2010.12.075

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  18 in total

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