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BioAssay: AID 143072

Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]glycine as the radioligand.

A series of alpha-amino-3-(phosphonoalkyl)-2-quinoxalinepropanoic acids was synthesized and evaluated for NMDA receptor affinity using a [3H] CPP binding assay. Functional antagonism of the NMDA receptor complex was evaluated in vitro using a stimulated [3H]TCP binding assay and in vivo by employing an NMDA-induced seizure model. Some analogues also were evaluated in the [3H]-glycine binding more ..
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 Tested Compounds
 Tested Compounds
All(7)
 
 
Active(4)
 
 
Unspecified(3)
 
 
 Tested Substances
 Tested Substances
All(7)
 
 
Active(4)
 
 
Unspecified(3)
 
 
 Related BioAssays
 Related BioAssays
AID: 143072
Data Source: ChEMBL (140311)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-21
Modify Date: 2014-05-19

Data Table ( Complete ):           Active    All
BioActive Compounds: 4
Description:
Title: Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.

Abstract: A series of alpha-amino-3-(phosphonoalkyl)-2-quinoxalinepropanoic acids was synthesized and evaluated for NMDA receptor affinity using a [3H] CPP binding assay. Functional antagonism of the NMDA receptor complex was evaluated in vitro using a stimulated [3H]TCP binding assay and in vivo by employing an NMDA-induced seizure model. Some analogues also were evaluated in the [3H]-glycine binding assay. Several compounds of the AP-6 type show potent and selective NMDA antagonistic activity both in vitro and in vivo. In particular alpha-amino-7-chloro-3-(phosphonomethyl)-2-quinoxalinepropanoic acid (1) displayed an ED50 of 1.1 mg/kg ip in the NMDA lethality model. Noteworthy is alpha-amino-6,7-dichloro-3-(phosphonomethyl)-2-quinoxalinepropanoic++ + acid (3) with a unique dual activity, displaying in the NMDA receptor binding assay an IC50 of 3.4 nM and in the glycine binding assay an IC50 of 0.61 microM.
(PMID: 8093907)
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: 104302
Target Type: PROTEIN COMPLEX GROUP
Pref Name: Glutamate NMDA receptor
Synonyms: GluN2D;Glutamate receptor ionotropic; NMDA 2D;Glutamate [NMDA] receptor subunit epsilon-4;N-methyl D-aspartate receptor subtype 2D;NMDAR2D;NR2D;GluN1;Glutamate receptor ionotropic; NMDA 1;Glutamate [NMDA] receptor subunit zeta-1;N-methyl-D-aspartate receptor subunit NR1;NMD-R1;GluN2A;Glutamate receptor ionotropic; NMDA 2A;Glutamate [NMDA] receptor subunit epsilon-1;N-methyl D-aspartate receptor subtype 2A;NMDAR2A;NR2A;GluN2B;Glutamate receptor ionotropic; NMDA 2B;Glutamate [NMDA] receptor subunit epsilon-2;N-methyl D-aspartate receptor subtype 2B;NMDAR2B;NR2B;GluN2C;Glutamate receptor ionotropic; NMDA 2C;Glutamate [NMDA] receptor subunit epsilon-3;N-methyl D-aspartate receptor subtype 2C;NMDAR2C;NR2C;GluN3A;Glutamate receptor chi-1;Glutamate receptor ionotropic; NMDA 3A;N-methyl-D-aspartate receptor;N-methyl-D-aspartate receptor subtype 3A;NMDAR-L;NMDAR-L1;NMDAR3A;NR3A;GluN3B;Glutamate receptor ionotropic; NMDA 3B;N-methyl-D-aspartate receptor subtype 3B;NMDAR3B;NR3B;
Gene Name: GluN2D;Grin2d;Grin1;Nmdar1;Grin2a;Grin2b;Grin2c;Grin3a;Grin3b;
Protein Accession: Q62645;P35439;Q00959;Q00960;Q00961;Q9R1M7;Q8VHN2;
Protein GI: 18202594;548379;3915771;548372;548374;51701631;51701630;
Organism: Rattus norvegicus
Tax ID: 10116
Target Classification: ion channel lgic glut nmda
Confidence: Multiple homologous protein targets may be assigned
Relationship Type: Homologous protein target assigned
Categorized Comment
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)
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