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BioAssay: AID 143070

Inhibition of [3H]MDL-105,519 binding to NMDA receptor glycine-binding site

Potent antagonists at the glycine-binding site of NMDA receptors, as well as dual antagonists acting also at AMPA receptors have been identified in a series of 5-arylaminomethylquinoxaline-2,3-diones. A study of the structure-activity relationship of these compounds is reported here. ..more
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 Tested Compounds
 Tested Compounds
All(10)
 
 
Active(10)
 
 
 Tested Substances
 Tested Substances
All(10)
 
 
Active(10)
 
 
 Related BioAssays
 Related BioAssays
AID: 143070
Data Source: ChEMBL (140309)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-20
Modify Date: 2013-11-11

Data Table ( Complete ):           Active    All
Targets
Sequence: RecName: Full=Glutamate receptor ionotropic, NMDA 2B; Short=GluN2B; AltName: Full=Glutamate [NMDA] receptor subunit epsilon-2; AltName: Full=N-methyl D-aspartate receptor subtype 2B; Short=NMDAR2B; Short=NR2B; Flags: Precursor
Description ..   
Protein Family: N-terminal leucine/isoleucine/valine-binding protein (LIVBP)-like domain of the NR2 subunit of NMDA receptor family
Comment ..   

Gene:GRIN2B     Related Protein 3D Structures     More BioActivity Data..


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BioActive Compounds: 10
Description:
Title: 5-Aminomethylquinoxaline-2,3-diones. Part II: N-aryl derivatives as novel NMDA/glycine and AMPA antagonists.

Abstract: Potent antagonists at the glycine-binding site of NMDA receptors, as well as dual antagonists acting also at AMPA receptors have been identified in a series of 5-arylaminomethylquinoxaline-2,3-diones. A study of the structure-activity relationship of these compounds is reported here.
(PMID: 9871631)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 104302

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface 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 valueFloatnM
10IC50 standard valueIC50 standard valueFloatnM
11IC50 activity commentIC50 activity commentString
12IC50 standard flagIC50 standard flagInteger
13IC50 qualifierIC50 qualifierString
14IC50 published valueIC50 published valueFloatμM
15IC50 standard valueIC50 standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Classification
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