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BioAssay: AID 143065

In vitro inhibitory activity to inhibit [3H]glycine binding to NMDA receptor

The in vitro activities of 3-hydroxy-imidazolidin-4-one derivatives demonstrated very restricted structure-activity relationships at the strychnine-insensitive glycine site of the NMDA receptor. The most active compound (3a) was completely unsubstituted and exhibited affinity and efficacy similar to that of D-cycloserine, the prototypical partial agonist at this site. ..more
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 Tested Compounds
 Tested Compounds
All(8)
 
 
Active(5)
 
 
Unspecified(3)
 
 
 Tested Substances
 Tested Substances
All(8)
 
 
Active(5)
 
 
Unspecified(3)
 
 
 Related BioAssays
 Related BioAssays
AID: 143065
Data Source: ChEMBL (140304)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-20
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 5
Description:
Title: Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands.

Abstract: The in vitro activities of 3-hydroxy-imidazolidin-4-one derivatives demonstrated very restricted structure-activity relationships at the strychnine-insensitive glycine site of the NMDA receptor. The most active compound (3a) was completely unsubstituted and exhibited affinity and efficacy similar to that of D-cycloserine, the prototypical partial agonist at this site.
(PMID: 10360746)
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: 12865
Target Type: SINGLE PROTEIN
Pref Name: Glutamate (NMDA) receptor subunit zeta 1
Synonyms: GluN1;Glutamate receptor ionotropic; NMDA 1;Glutamate [NMDA] receptor subunit zeta-1;N-methyl-D-aspartate receptor subunit NR1;NMD-R1;
Gene Name: Grin1;Nmdar1;
Protein Accession: P35439;
Protein GI: 548379;
Organism: Rattus norvegicus
Tax ID: 10116
Target Classification: ion channel lgic glut nmda
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Assay Data Source: Scientific Literature
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 valueFloatμM
10IC50 standard valueIC50 standard valueFloatnM

* Activity Concentration.

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