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Assay Detail

CHEMBL747511

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

Binding
Activity against rat cortical and hippocampal membrane N-methyl-D-aspartate glutamate receptor 1/2A/2B/2C/2D using [3H]CPP
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Hippocampus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex.
Salituro FG, Harrison BL, Baron BM, Nyce PL, Stewart KT, McDonald IA.
J Med Chem (1990) 33 : 2944 -2946
PubMed 2146391 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.47 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50267 1 4.92
CHEMBL417544 1 4.60
CHEMBL278097 1 4.47
CHEMBL50160 1 4.23
CHEMBL299155 TRANSTORINE 1.0 1 4.12
CHEMBL295718 1 -
CHEMBL53744 1 -
CHEMBL311389 7-CHLOROKYNURENIC ACID -1.0 1 -
CHEMBL31344 1 -
CHEMBL278390 INDOLE-2-CARBOXYLIC ACID 1 -
CHEMBL301556 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50267 IC50 = 12000.0 nM 4.92
CHEMBL417544 IC50 = 25000.0 nM 4.60
CHEMBL278097 IC50 = 34000.0 nM 4.47
CHEMBL50160 IC50 = 59000.0 nM 4.23
CHEMBL299155 TRANSTORINE IC50 = 75000.0 nM 4.12
CHEMBL295718 IC50 = 283000.0 nM -
CHEMBL53744 IC50 > 100000.0 nM -
CHEMBL311389 7-CHLOROKYNURENIC ACID IC50 = 162000.0 nM -
CHEMBL31344 IC50 = 358000.0 nM -
CHEMBL278390 INDOLE-2-CARBOXYLIC ACID IC50 = 4200000.0 nM -
CHEMBL301556 IC50 > 1000000.0 nM -