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Assay Detail

CHEMBL746909

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

Binding
Ability to inhibit MK-801 binding to NMDA receptor in the presence of 100 uM of spermidine was determined
17
Total Activities
17
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

Aromatic analogs of arcaine inhibit MK-801 binding to the NMDA receptor.
Sharma TA, Carr AJ, Davis RS, Reynolds IJ, Hamilton AD.
Bioorg Med Chem Lett (1998) 8 : 3459 -3464
PubMed 9934452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.72 5.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432447 1 5.65
CHEMBL117961 1 5.23
CHEMBL115850 1 5.15
CHEMBL333241 1 5.03
CHEMBL117030 1 5.00
CHEMBL325856 1 4.98
CHEMBL118521 1 4.92
CHEMBL118520 1 4.80
CHEMBL117622 1 4.69
CHEMBL117808 1 4.53
CHEMBL117463 1 4.31
CHEMBL116027 1 4.26
CHEMBL115747 1 4.12
CHEMBL102740 ARCAINE 1 4.10
CHEMBL116333 1 4.02
CHEMBL117468 1 -
CHEMBL436361 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432447 IC50 = 2230.0 nM 5.65
CHEMBL117961 IC50 = 5890.0 nM 5.23
CHEMBL115850 IC50 = 7090.0 nM 5.15
CHEMBL333241 IC50 = 9270.0 nM 5.03
CHEMBL117030 IC50 = 9880.0 nM 5.00
CHEMBL325856 IC50 = 10470.0 nM 4.98
CHEMBL118521 IC50 = 12170.0 nM 4.92
CHEMBL118520 IC50 = 15710.0 nM 4.80
CHEMBL117622 IC50 = 20560.0 nM 4.69
CHEMBL117808 IC50 = 29810.0 nM 4.53
CHEMBL117463 IC50 = 49300.0 nM 4.31
CHEMBL116027 IC50 = 55260.0 nM 4.26
CHEMBL115747 IC50 = 75800.0 nM 4.12
CHEMBL102740 ARCAINE IC50 = 79980.0 nM 4.10
CHEMBL116333 IC50 = 95210.0 nM 4.02
CHEMBL117468 IC50 = 112030.0 nM -
CHEMBL436361 IC50 = 110500.0 nM -