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Assay Detail

CHEMBL697885

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

Binding
Binding affinity by measuring displacement of [3H]AMPA from Ionotropic glutamate receptor AMPA in rat cortical slice preparation
7
Total Activities
7
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

Excitatory amino acid receptor atagonists: synthesis and pharmacology of 3-(carboxymethoxy)isoxazoles derived from AMPA
Madsen U, Andresen L, Poulsen G, Rasmussen T, Ebert B, Krogsgaard-Larsen P, Brehm L
Bioorg Med Chem Lett (1993) 3 : 1649 -1654
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.62 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13378 (R,S)-AMPA 1 7.40
CHEMBL275040 KAINIC ACID 2.0 1 5.40
CHEMBL291274 1 4.05
CHEMBL46859 1 -
CHEMBL280585 1 -
CHEMBL45051 1 -
CHEMBL42885 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13378 (R,S)-AMPA IC50 = 40.0 nM 7.40
CHEMBL275040 KAINIC ACID IC50 = 4000.0 nM 5.40
CHEMBL291274 IC50 = 90000.0 nM 4.05
CHEMBL46859 IC50 > 100000.0 nM -
CHEMBL280585 IC50 > 100000.0 nM -
CHEMBL45051 IC50 > 100000.0 nM -
CHEMBL42885 IC50 > 100000.0 nM -