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Assay Detail

CHEMBL644192

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

Binding
Binding affinity against AMPA receptor using [3H]- AMPA radioligand
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor ionotropic AMPA (CHEMBL2096670)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Homology modeling of the ampa receptor: A quantitative predictive tool for the design of novel antagonists
Hesson DP, Sturgess MA
Bioorg Med Chem Lett (1997) 7 : 1437 -1442
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.15 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222519 NBQX 1 7.28
CHEMBL293206 1 7.10
CHEMBL122054 1 6.82
CHEMBL32908 1 6.82
CHEMBL121771 1 6.78
CHEMBL155265 DNQX 1 6.70
CHEMBL9790 1 6.47
CHEMBL33751 1 6.24
CHEMBL286103 1 6.20
CHEMBL330795 1 6.16
CHEMBL32123 1 5.87
CHEMBL23044 1 5.70
CHEMBL607705 1 5.14
CHEMBL341000 1 4.62
CHEMBL122559 1 4.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222519 NBQX IC50 = 52.0 nM 7.28
CHEMBL293206 IC50 = 80.0 nM 7.10
CHEMBL122054 IC50 = 153.0 nM 6.82
CHEMBL32908 IC50 = 150.0 nM 6.82
CHEMBL121771 IC50 = 166.0 nM 6.78
CHEMBL155265 DNQX IC50 = 200.0 nM 6.70
CHEMBL9790 IC50 = 340.0 nM 6.47
CHEMBL33751 IC50 = 580.0 nM 6.24
CHEMBL286103 IC50 = 630.0 nM 6.20
CHEMBL330795 IC50 = 700.0 nM 6.16
CHEMBL32123 IC50 = 1350.0 nM 5.87
CHEMBL23044 IC50 = 2000.0 nM 5.70
CHEMBL607705 IC50 = 7200.0 nM 5.14
CHEMBL341000 IC50 = 24000.0 nM 4.62
CHEMBL122559 IC50 = 44000.0 nM 4.36