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BioAssay: AID 536862

Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK292 cells after 3 hrs

Antagonist activity at the alpha3beta4 nicotinic acetylcholine receptor (nAChR) is thought to contribute to the antiaddictive properties of several compounds. However, truly selective ligands for the alpha3beta4 nAChR have not been available. We report the discovery and SAR of a novel class of compounds that bind to the alpha3beta4 nAChR and have no measurable affinity for the alpha4beta2 or alpha7 subtype. In functional assays the lead compound antagonized epibatidine-induced Ca(2+) flux in alpha3beta4-transfected cells in a noncompetitive manner. ..more
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 Tested Compounds
 Tested Compounds
All(17)
 
 
Active(17)
 
 
 Tested Substances
 Tested Substances
All(17)
 
 
Active(17)
 
 
AID: 536862
Data Source: ChEMBL (684743)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-09-18
Modify Date: 2014-08-23

Data Table ( Complete ):           View Active Data    View All Data
Targets
Sequence: RecName: Full=Neuronal acetylcholine receptor subunit alpha-3; Flags: Precursor
Description ..   
Protein Family: Neurotransmitter-gated ion-channel ligand binding domain
Comment ..   

Gene:CHRNA3     Related Protein 3D Structures     More BioActivity Data..


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BioActive Compounds: 17
Description:
Title: Novel alpha3beta4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation.

Abstract: Antagonist activity at the alpha3beta4 nicotinic acetylcholine receptor (nAChR) is thought to contribute to the antiaddictive properties of several compounds. However, truly selective ligands for the alpha3beta4 nAChR have not been available. We report the discovery and SAR of a novel class of compounds that bind to the alpha3beta4 nAChR and have no measurable affinity for the alpha4beta2 or alpha7 subtype. In functional assays the lead compound antagonized epibatidine-induced Ca(2+) flux in alpha3beta4-transfected cells in a noncompetitive manner.
(PMID: 20979364)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a defined protein complex, consisting of multiple subunits
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Test Type: In vitro
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ki*Ki PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6Ki activity commentKi activity commentString
7Ki standard flagKi standard flagInteger
8Ki qualifierKi qualifierString
9Ki published valueKi published valueFloatnM
10Ki standard valueKi standard valueFloatnM
11Ki binding domainsKi binding domainsString

* Activity Concentration.

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
Classification
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