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BioAssay: AID 719499

Ago-positive allosteric modulation of rat mGlu5 receptor expressed in HEK293 cells by fluorescence-based calcium flux assay

Herein we report the discovery and SAR of a novel series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on an aryl glycine sulfonamide scaffold. This series represents a rare non-MPEP site mGlu(5) PAM chemotype. ..more
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 Tested Compounds
 Tested Compounds
All(16)
 
 
Active(14)
 
 
Unspecified(2)
 
 
 Tested Substances
 Tested Substances
All(16)
 
 
Active(14)
 
 
Unspecified(2)
 
 
AID: 719499
Data Source: ChEMBL (887242)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-06-29
Modify Date: 2014-05-26

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Metabotropic glutamate receptor 5; Short=mGluR5; Flags: Precursor
Description ..   
Protein Family: Ligand binding domain of the group I metabotropic glutamate receptor
Comment ..   

Gene:GRM5     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 14
Description:
Title: Discovery and SAR of a novel series of non-MPEP site mGlu# PAMs based on an aryl glycine sulfonamide scaffold.

Abstract: Herein we report the discovery and SAR of a novel series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on an aryl glycine sulfonamide scaffold. This series represents a rare non-MPEP site mGlu(5) PAM chemotype.
(PMID: 23142615)
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

BAO: Assay Format: cell-based format

Assay Cell Type: HEK293

Target Type: Target is a single protein chain

Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6EC50 activity commentEC50 activity commentString
7EC50 standard flagEC50 standard flagInteger
8EC50 qualifierEC50 qualifierString
9EC50 published valueEC50 published valueFloat
10EC50 standard valueEC50 standard valueFloatnM
11EC50 activity commentEC50 activity commentString
12EC50 standard flagEC50 standard flagInteger
13EC50 qualifierEC50 qualifierString
14EC50 published valueEC50 published valueFloatnM
15EC50 standard valueEC50 standard valueFloatnM
16EC50 activity commentEC50 activity commentString
17EC50 standard flagEC50 standard flagInteger
18EC50 qualifierEC50 qualifierString
19EC50 published valueEC50 published valueFloatμM
20EC50 standard valueEC50 standard valueFloatnM

* Activity Concentration.

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