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BioAssay: AID 595475

Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells

A new series of potential GABA uptake inhibitors starting from of 1H-imidazol-4-ylacetic acid with the carboxylic acid side chain originating from different positions and varying in length have been synthesized and tested for the inhibitory potency at the four GABA uptake transporters mGAT1-4 stably expressed in HEK cells. Further two bicyclic compounds with a rigidified carboxylic acid side chain were included in this study. The results of the biological tests indicated that most I ..more
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 Tested Compounds
 Tested Compounds
All(22)
 
 
Active(11)
 
 
Unspecified(11)
 
 
 Tested Substances
 Tested Substances
All(22)
 
 
Active(11)
 
 
Unspecified(11)
 
 
AID: 595475
Data Source: ChEMBL (745626)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2014-05-24

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Sodium- and chloride-dependent GABA transporter 3; Short=GAT-3; AltName: Full=Sodium- and chloride-dependent GABA transporter 4; Short=GAT-4; AltName: Full=Solute carrier family 6 member 11
Description ..   
Protein Family: Na(+)- and Cl(-)-dependent GABA transporter 3; solute-binding domain
Comment ..   

Gene:SLC6A11     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 11
Description:
Title: Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.

Abstract: A new series of potential GABA uptake inhibitors starting from of 1H-imidazol-4-ylacetic acid with the carboxylic acid side chain originating from different positions and varying in length have been synthesized and tested for the inhibitory potency at the four GABA uptake transporters mGAT1-4 stably expressed in HEK cells. Further two bicyclic compounds with a rigidified carboxylic acid side chain were included in this study. The results of the biological tests indicated that most I
(PMID: 21353350)
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: Binding

Assay Data Source: Scientific Literature

Assay Test Type: In vitro

BAO: Assay Format: cell-based format

Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6IC50 activity commentIC50 activity commentString
7IC50 standard flagIC50 standard flagInteger
8IC50 qualifierIC50 qualifierString
9IC50 published valueIC50 published valueFloat
10IC50 standard valueIC50 standard valueFloatnM
11IC50 data validityIC50 data validityString
12IC50 binding domainsIC50 binding domainsString
13IC50 activity commentIC50 activity commentString
14IC50 standard flagIC50 standard flagInteger
15IC50 qualifierIC50 qualifierString
16IC50 published valueIC50 published valueFloatμM
17IC50 standard valueIC50 standard valueFloatnM
18IC50 data validityIC50 data validityString
19IC50 binding domainsIC50 binding domainsString

* Activity Concentration.

Data Table (Concise)
Classification
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