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Assay Detail

CHEMBL751465

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

Binding
Binding potency for NMDA site of the glutamate receptor complex using rat brain cortical membranes in a competitive binding assay with [3H]CPP as the radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Competitive NMDA receptor antagonists: synthesis of -ketophosphonate-substituted piperidine carboxylic acid derivatives
Whitten JP, Cube RV, Baron BM, McDonald IA
Bioorg Med Chem Lett (1993) 3 : 19 -22
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.67 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305487 1 8.49
CHEMBL67689 1 8.12
CHEMBL308011 1 7.82
CHEMBL281190 1 7.40
CHEMBL303393 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305487 IC50 = 3.2 nM 8.49
CHEMBL67689 IC50 = 7.6 nM 8.12
CHEMBL308011 IC50 = 15.0 nM 7.82
CHEMBL281190 IC50 = 40.0 nM 7.40
CHEMBL303393 IC50 = 320.0 nM 6.50