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BioAssay: AID 146770

Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in Xenopus oocytes

Epibatidine is a potent but nonselective nAChR agonist. Its biological effects appear to be mediated largely by alpha4beta2 nAChRs. Surprisingly, only a limited number of epibatidine analogues have been synthesized and evaluated in in vitro assays. Even fewer analogues have received in vivo pharmacological evaluation. In this paper, SAR studies directed toward epibatidine analogues will be reviewed. ..more
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 Tested Compounds
 Tested Compounds
All(6)
 
 
Active(5)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(6)
 
 
Active(5)
 
 
Unspecified(1)
 
 
AID: 146770
Data Source: ChEMBL (144014)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-20
Modify Date: 2014-05-19

Data Table ( Complete ):           Active    All
Targets
Sequence: RecName: Full=Neuronal acetylcholine receptor subunit beta-4; AltName: Full=Neuronal acetylcholine receptor non-alpha-2 chain; Short=N-alpha 2; Flags: Precursor
Description ..   
Protein Family: Neurotransmitter-gated ion-channel ligand binding domain
Comment ..   

Gene:CHRNB4     Related Protein 3D Structures     More BioActivity Data..


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BioActive Compounds: 5
Description:
Title: Epibatidine structure-activity relationships.

Abstract: Epibatidine is a potent but nonselective nAChR agonist. Its biological effects appear to be mediated largely by alpha4beta2 nAChRs. Surprisingly, only a limited number of epibatidine analogues have been synthesized and evaluated in in vitro assays. Even fewer analogues have received in vivo pharmacological evaluation. In this paper, SAR studies directed toward epibatidine analogues will be reviewed.
(PMID: 15050621)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Functional

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Target Type: Target is a defined protein complex, consisting of multiple subunits

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
2EC50 activity commentEC50 activity commentString
3EC50 standard flagEC50 standard flagInteger
4EC50 qualifierEC50 qualifierString
5EC50 published valueEC50 published valueFloat%
6EC50 standard valueEC50 standard valueFloat%
7EC50 binding domainsEC50 binding domainsString
8EC50 activity commentEC50 activity commentString
9EC50 standard flagEC50 standard flagInteger
10EC50 qualifierEC50 qualifierString
11EC50 published valueEC50 published valueFloatnM
12EC50 standard valueEC50 standard valueFloatnM
13EC50 binding domainsEC50 binding domainsString

* Activity Concentration.

Data Table (Concise)
Classification
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