Displacement of [125I]Galanin from human recombinant GAL2 receptor expressed in CHO cells - BioAssay Summary
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. ..more
 _
   
 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 567956
Data Source: ChEMBL (716496)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-09-18
Modify Date: 2013-05-13

Data Table (Complete):           All
Target
Helptop of page
Sequence: RecName: Full=Galanin receptor type 2; Short=GAL2-R; Short=GALR-2
Description ..   
Protein Family: Serpentine type 7TM GPCR chemoreceptor Srw
Comment ..   

Gene:GALR2     Related Protein 3D Structures
Tested Compound:
Description:
Helptop of page
Title: Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773).

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.
(PMID: 21237643)
Categorized Comment
Helptop of page
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 11498

ChEMBL target type: Target is a single protein chain

Result Definitions
Helptop of page
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat%
5Inhibition standard valueInhibition standard valueFloat%

Data Table (Concise)
Helptop of page
Classification
PageFrom: