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Assay Detail

CHEMBL702541

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

Binding
Binding affinity for ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand, bound to synaptic membranes prepared from rat cerebral cortex
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Synthesis and AMPA receptor antagonistic activity of a novel class of quinoxalinecarboxylic acid with a substituted phenyl group at the C-7 position.
Takano Y, Shiga F, Asano J, Ando N, Uchiki H, Anraku T.
Bioorg Med Chem Lett (2003) 13 : 3521 -3525
PubMed 14505662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 6.90 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118369 1 7.80
CHEMBL538777 1 7.80
CHEMBL554662 1 7.75
CHEMBL555657 1 7.70
CHEMBL116565 1 7.66
CHEMBL118641 1 7.66
CHEMBL323648 1 7.57
CHEMBL117771 1 7.54
CHEMBL545051 1 7.52
CHEMBL115912 1 7.52
CHEMBL331103 1 7.52
CHEMBL445313 1 7.50
CHEMBL332816 1 7.33
CHEMBL119625 ZONAMPANEL 2.0 1 7.21
CHEMBL222519 NBQX 1 7.19
CHEMBL1627032 1 7.17
CHEMBL115861 1 7.07
CHEMBL119832 1 7.00
CHEMBL13260 YM-90K 1 7.00
CHEMBL326542 1 6.77
CHEMBL325878 1 6.57
CHEMBL326506 1 6.48
CHEMBL326157 1 6.28
CHEMBL118779 1 6.25
CHEMBL331844 1 6.04
CHEMBL119818 1 5.89
CHEMBL116266 1 5.70
CHEMBL122188 1 5.70
CHEMBL119365 1 5.60
CHEMBL118585 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118369 Ki = 16.0 nM 7.80
CHEMBL538777 Ki = 16.0 nM 7.80
CHEMBL554662 Ki = 18.0 nM 7.75
CHEMBL555657 Ki = 20.0 nM 7.70
CHEMBL116565 Ki = 22.0 nM 7.66
CHEMBL118641 Ki = 22.0 nM 7.66
CHEMBL323648 Ki = 27.0 nM 7.57
CHEMBL117771 Ki = 29.0 nM 7.54
CHEMBL545051 Ki = 30.0 nM 7.52
CHEMBL115912 Ki = 30.0 nM 7.52
CHEMBL331103 Ki = 30.0 nM 7.52
CHEMBL445313 Ki = 32.0 nM 7.50
CHEMBL332816 Ki = 47.0 nM 7.33
CHEMBL119625 ZONAMPANEL Ki = 62.0 nM 7.21
CHEMBL222519 NBQX Ki = 65.0 nM 7.19
CHEMBL1627032 Ki = 67.0 nM 7.17
CHEMBL115861 Ki = 86.0 nM 7.07
CHEMBL119832 Ki = 100.0 nM 7.00
CHEMBL13260 YM-90K Ki = 100.0 nM 7.00
CHEMBL326542 Ki = 170.0 nM 6.77
CHEMBL325878 Ki = 270.0 nM 6.57
CHEMBL326506 Ki = 330.0 nM 6.48
CHEMBL326157 Ki = 530.0 nM 6.28
CHEMBL118779 Ki = 560.0 nM 6.25
CHEMBL331844 Ki = 910.0 nM 6.04
CHEMBL119818 Ki = 1300.0 nM 5.89
CHEMBL116266 Ki = 2000.0 nM 5.70
CHEMBL122188 Ki = 2000.0 nM 5.70
CHEMBL119365 Ki = 2500.0 nM 5.60
CHEMBL118585 Ki = 2600.0 nM 5.58
CHEMBL122128 Ki = 3800.0 nM 5.42
CHEMBL445314 Ki > 10000.0 nM -
CHEMBL117502 Ki > 900.0 nM -