Assay Detail
Binding
CHEMBL829790
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]AMPA (5 nM) from ionotropic glutamate receptor AMPA of rat cerebral cortex synaptic membrane preparation
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| 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 7-imidazolyl-6-trifluoromethyl quinoxalinecarboxylic acid with a substituted phenyl group and improved its good physicochemical properties by introduced CF3 group.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.43 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL361515 | — | — | 1 | 8.28 |
| CHEMBL183997 | — | — | 1 | 7.89 |
| CHEMBL188018 | — | — | 1 | 7.80 |
| CHEMBL185450 | — | — | 1 | 7.70 |
| CHEMBL185386 | — | — | 1 | 7.70 |
| CHEMBL116565 | — | — | 1 | 7.66 |
| CHEMBL362139 | — | — | 1 | 7.64 |
| CHEMBL181598 | — | — | 1 | 7.54 |
| CHEMBL187333 | — | — | 1 | 7.52 |
| CHEMBL426253 | — | — | 1 | 7.46 |
| CHEMBL119625 | ZONAMPANEL | 2.0 | 1 | 7.21 |
| CHEMBL180562 | — | — | 1 | 7.07 |
| CHEMBL13260 | YM-90K | — | 1 | 7.00 |
| CHEMBL425351 | — | — | 1 | 6.72 |
| CHEMBL118779 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL361515 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL183997 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL188018 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL185450 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL185386 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL116565 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL362139 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL181598 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL187333 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL426253 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL119625 | ZONAMPANEL | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL180562 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL13260 | YM-90K | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL425351 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL118779 | — | Ki | = | 560.0 | nM | 6.25 |