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Assay Detail

CHEMBL750507

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

Binding
Binding activity against N-methyl-D-aspartate glutamate receptor in rat brain homogenate using [3H]-glycine as the radioligand.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

4-[(Carboxymethyl)oxy]- and 4-[(carboxymethyl)amino]-5,7-dichloroquinoline-2-carboxylic acid: new antagonists of the strychnine-insensitive glycine binding site on the N-methyl-D-aspartate receptor complex.
Harrison BL, Baron BM, Cousino DM, McDonald IA.
J Med Chem (1990) 33 : 3130 -3132
PubMed 2147957 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.07 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50267 1 7.10
CHEMBL105396 1 7.00
CHEMBL311389 7-CHLOROKYNURENIC ACID -1.0 1 6.40
CHEMBL322777 1 5.05
CHEMBL299155 TRANSTORINE 1.0 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50267 IC50 = 80.0 nM 7.10
CHEMBL105396 IC50 = 100.0 nM 7.00
CHEMBL311389 7-CHLOROKYNURENIC ACID IC50 = 400.0 nM 6.40
CHEMBL322777 IC50 = 9000.0 nM 5.05
CHEMBL299155 TRANSTORINE IC50 = 16000.0 nM 4.80