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Assay Detail

CHEMBL883545

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

Binding
Inhibition of [3H]dizocilpine binding to N-methyl-D-aspartate (NMDA) receptor complex in rat brain membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel bisbenzamidines and bisbenzimidazolines as noncompetitive NMDA receptor antagonists.
Tao B, Huang TL, Sharma TA, Reynolds IJ, Donkor IO.
Bioorg Med Chem Lett (1999) 9 : 1299 -1304
PubMed 10340618 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.99 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269032 1 5.92
CHEMBL55 PENTAMIDINE 4.0 1 5.59
CHEMBL9185 1 5.30
CHEMBL9126 1 5.27
CHEMBL9479 1 5.20
CHEMBL9516 1 5.11
CHEMBL24250 1 5.08
CHEMBL25526 1 4.93
CHEMBL25403 1 4.78
CHEMBL8892 1 4.74
CHEMBL276449 1 4.45
CHEMBL24029 1 4.34
CHEMBL9531 1 4.18
CHEMBL9391 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269032 IC50 = 1190.0 nM 5.92
CHEMBL55 PENTAMIDINE IC50 = 2590.0 nM 5.59
CHEMBL9185 IC50 = 4990.0 nM 5.30
CHEMBL9126 IC50 = 5320.0 nM 5.27
CHEMBL9479 IC50 = 6290.0 nM 5.20
CHEMBL9516 IC50 = 7840.0 nM 5.11
CHEMBL24250 IC50 = 8350.0 nM 5.08
CHEMBL25526 IC50 = 11700.0 nM 4.93
CHEMBL25403 IC50 = 16500.0 nM 4.78
CHEMBL8892 IC50 = 18200.0 nM 4.74
CHEMBL276449 IC50 = 35600.0 nM 4.45
CHEMBL24029 IC50 = 45800.0 nM 4.34
CHEMBL9531 IC50 = 66000.0 nM 4.18
CHEMBL9391 IC50 > 200000.0 nM -