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BioAssay: AID 595476

Inhibition of mouse GAT4-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(20)
 
 
Active(6)
 
 
Unspecified(14)
 
 
 Tested Substances
 Tested Substances
All(20)
 
 
Active(6)
 
 
Unspecified(14)
 
 
 Related BioAssays
 Related BioAssays
AID: 595476
Data Source: ChEMBL (745627)
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 ):           View Active Data    View All Data
BioActive Compounds: 6
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.

Putative Target:

ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Assay Test Type: In vitro

BAO: Assay Format: cell-based format

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2IC50 activity commentIC50 activity commentString
3IC50 standard flagIC50 standard flagInteger
4IC50 qualifierIC50 qualifierString
5IC50 published valueIC50 published valueFloat
6IC50 standard valueIC50 standard valueFloatnM
7IC50 data validityIC50 data validityString
8IC50 activity commentIC50 activity commentString
9IC50 standard flagIC50 standard flagInteger
10IC50 qualifierIC50 qualifierString
11IC50 published valueIC50 published valueFloatμM
12IC50 standard valueIC50 standard valueFloatnM
13IC50 data validityIC50 data validityString

* Activity Concentration.

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