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Assay Detail

CHEMBL703571

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

Binding
The compound was tested for binding affinity against Kainate binding site using [3H]kainate as radioligand
8
Total Activities
8
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 kainate (CHEMBL2109241)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Pyrrolylquinoxalinediones: Dicarboxylates as highly potent AMPA receptor antagonists
Lubisch W, Behl B, Hofmann H, Teschendorf H
Bioorg Med Chem Lett (1997) 7 : 2441 -2446
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.47 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL84142 1 6.16
CHEMBL82375 1 5.92
CHEMBL309831 1 5.44
CHEMBL13260 YM-90K 1 5.32
CHEMBL79454 1 5.30
CHEMBL314248 1 5.24
CHEMBL293613 1 5.23
CHEMBL310503 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL84142 Ki = 700.0 nM 6.16
CHEMBL82375 Ki = 1200.0 nM 5.92
CHEMBL309831 Ki = 3600.0 nM 5.44
CHEMBL13260 YM-90K Ki = 4800.0 nM 5.32
CHEMBL79454 Ki = 5000.0 nM 5.30
CHEMBL314248 Ki = 5700.0 nM 5.24
CHEMBL293613 Ki = 5900.0 nM 5.23
CHEMBL310503 Ki = 6700.0 nM 5.17