Assay Detail
Binding
CHEMBL696669
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against [3H]AMPA binding to rat cortical membranes
5
Total Activities
5
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 (CHEMBL2094119) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships in a series of 2(1H)-quinolones bearing different acidic function in the 3-position: 6,7-dichloro-2(1H)-oxoquinoline-3-phosphonic acid, a new potent and selective AMPA/kainate antagonist with neuroprotective properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.52 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222519 | NBQX | — | 1 | 7.22 |
| CHEMBL65729 | — | — | 1 | 7.05 |
| CHEMBL294792 | — | — | 1 | 6.82 |
| CHEMBL62472 | — | — | 1 | 6.05 |
| CHEMBL412897 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222519 | NBQX | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL65729 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL294792 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL62472 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL412897 | — | IC50 | = | 3500.0 | nM | 5.46 |