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Assay Detail

CHEMBL699743

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

Binding
Binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand.
10
Total Activities
6
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 (CHEMBL2093871)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.
Conti P, De Amici M, De Sarro G, Rizzo M, Stensbøl TB, Bräuner-Osborne H, Madsen U, Toma L, De Micheli C.
J Med Chem (1999) 42 : 4099 -4107
PubMed 10514280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.42 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276815 (S)-AMPA 1 7.40
CHEMBL125440 3 6.27
CHEMBL275040 KAINIC ACID 2.0 1 5.40
CHEMBL340591 3 4.95
CHEMBL133337 1 4.46
CHEMBL334583 1 4.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276815 (S)-AMPA IC50 = 40.0 nM 7.40
CHEMBL125440 IC50 = 540.0 nM 6.27
CHEMBL125440 IC50 = 1300.0 nM 5.89
CHEMBL275040 KAINIC ACID IC50 = 4000.0 nM 5.40
CHEMBL340591 IC50 = 11200.0 nM 4.95
CHEMBL340591 IC50 = 24700.0 nM 4.61
CHEMBL133337 IC50 = 34900.0 nM 4.46
CHEMBL334583 IC50 = 42600.0 nM 4.37
CHEMBL340591 IC50 > 100000.0 nM -
CHEMBL125440 IC50 > 100000.0 nM -