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Assay Detail

CHEMBL749508

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Binding
Tested for the affinity to the glycine site -NMDA receptor using [3H]Gly as radioligand.
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate [NMDA] receptor (CHEMBL2094124)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

N-sulfonyl derivatives of 6,7-dichloro 3,4-dihydro-3-oxo-quinoxalinecarboxylate as glycine-site NMDA and AMPA antagonists
Hays SJ, Boxer PA, Taylor CP, Vartanian MG, Robichaud LJ, Nielsen E
Bioorg Med Chem Lett (1993) 3 : 77 -80
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.59 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50267 1 7.17
CHEMBL126035 1 6.92
CHEMBL167548 1 6.44
CHEMBL130213 6,7-DICHLORO-3-HYDROXY-2-QUINOXALINECARBOXYLIC ACID 1 6.34
CHEMBL155265 DNQX 1 6.08
CHEMBL222519 NBQX 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50267 IC50 = 68.0 nM 7.17
CHEMBL126035 IC50 = 120.0 nM 6.92
CHEMBL167548 IC50 = 360.0 nM 6.44
CHEMBL130213 6,7-DICHLORO-3-HYDROXY-2-QUINOXALINECARBOXYLIC ACID IC50 = 460.0 nM 6.34
CHEMBL155265 DNQX IC50 = 840.0 nM 6.08
CHEMBL222519 NBQX IC50 > 100000.0 nM -