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BioAssay: AID 595474

Inhibition of mouse GAT2-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(19)
 
 
Active(5)
 
 
Unspecified(14)
 
 
 Tested Substances
 Tested Substances
All(19)
 
 
Active(5)
 
 
Unspecified(14)
 
 
AID: 595474
Data Source: ChEMBL (745625)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2014-08-23

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Sodium- and chloride-dependent GABA transporter 2; Short=GAT-2; AltName: Full=Sodium- and chloride-dependent GABA transporter 3; Short=GAT-3; AltName: Full=Solute carrier family 6 member 13
Description ..   
Protein Family: Na(+)- and Cl(-)-dependent GABA transporter 2; solute-binding domain
Comment ..   

Gene:SLC6A13     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 5
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 - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
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
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)
Data Table ( Complete ):     View Active Data    View All Data
Classification
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