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Assay Detail

CHEMBL880848

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Compound was evaluated for its binding affinity for the glycine binding site on N-methyl-D-aspartate glutamate receptor by using [3H]MDL-105519 binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, NMDA 1 (CHEMBL2015)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors.
Ametamey SM, Kokic M, Carrey-Rémy N, Bläuenstein P, Willmann M, Bischoff S, Schmutz M, Schubiger PA, Auberson YP.
Bioorg Med Chem Lett (2000) 10 : 75 -78
PubMed 10636248 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.91 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86313 1 8.30
CHEMBL167952 1 8.22
CHEMBL82963 1 8.10
CHEMBL354295 1 8.10
CHEMBL162675 1 8.05
CHEMBL82626 1 7.50
CHEMBL164231 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86313 IC50 = 5.0 nM 8.30
CHEMBL167952 IC50 = 6.0 nM 8.22
CHEMBL82963 IC50 = 8.0 nM 8.10
CHEMBL354295 IC50 = 8.0 nM 8.10
CHEMBL162675 IC50 = 9.0 nM 8.05
CHEMBL82626 IC50 = 32.0 nM 7.50
CHEMBL164231 IC50 = 76.0 nM 7.12