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Assay Detail

CHEMBL698744

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

Binding
Concentration required for 50% inhibition of [3H]AMPA binding to AMPA receptor in rat cortical slice preparation
6
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

Excitatory amino acid receptor ligands. Synthesis and biological activity of 3-isoxazolol amino acids structurally related to homoibotenic acid.
Christensen IT, Ebert B, Madsen U, Nielsen B, Brehm L, Krogsgaard-Larsen P.
J Med Chem (1992) 35 : 3512 -3519
PubMed 1383544 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.97 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13378 (R,S)-AMPA 1 7.22
CHEMBL268762 1 6.22
CHEMBL10339 1 5.70
CHEMBL325291 1 5.70
CHEMBL113180 1 5.00
CHEMBL9822 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13378 (R,S)-AMPA IC50 = 60.0 nM 7.22
CHEMBL268762 IC50 = 600.0 nM 6.22
CHEMBL10339 IC50 = 2000.0 nM 5.70
CHEMBL325291 IC50 = 2000.0 nM 5.70
CHEMBL113180 IC50 = 10000.0 nM 5.00
CHEMBL9822 IC50 > 100000.0 nM -