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Assay Detail

CHEMBL702015

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

Functional
Antagonistic activity against Ca++permeable Ionotropic glutamate receptor AMPA as concentration of compound that reduces the inward current induced by kainate by 50% in Xenopus oocytes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor ionotropic, AMPA (CHEMBL2093871)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Synthesis of diaminobutane derivatives as potent Ca(2+)-permeable AMPA receptor antagonists.
Yoneda Y, Kawajiri S, Sugimura M, Osanai K, Kito F, Ota E, Mimura T.
Bioorg Med Chem Lett (2001) 11 : 2663 -2666
PubMed 11551773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.32 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22366 1 6.72
CHEMBL90950 1 6.60
CHEMBL315554 1 6.41
CHEMBL90895 1 6.28
CHEMBL25101 1 6.16
CHEMBL91247 1 6.14
CHEMBL316188 1 6.13
CHEMBL419685 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22366 IC50 = 190.0 nM 6.72
CHEMBL90950 IC50 = 250.0 nM 6.60
CHEMBL315554 IC50 = 390.0 nM 6.41
CHEMBL90895 IC50 = 530.0 nM 6.28
CHEMBL25101 IC50 = 690.0 nM 6.16
CHEMBL91247 IC50 = 730.0 nM 6.14
CHEMBL316188 IC50 = 740.0 nM 6.13
CHEMBL419685 IC50 = 790.0 nM 6.10