Assay Detail
Functional
CHEMBL696667
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity against rat ionotropic glutamate receptor ionotropic kainate in xenopus oocytes
24
Total Activities
24
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, 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 | 24 | 5.61 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222519 | NBQX | — | 1 | 7.05 |
| CHEMBL65293 | — | — | 1 | 6.82 |
| CHEMBL65729 | — | — | 1 | 6.80 |
| CHEMBL294792 | — | — | 1 | 6.52 |
| CHEMBL13260 | YM-90K | — | 1 | 6.52 |
| CHEMBL64684 | — | — | 1 | 6.22 |
| CHEMBL302611 | — | — | 1 | 5.89 |
| CHEMBL65989 | — | — | 1 | 5.85 |
| CHEMBL62472 | — | — | 1 | 5.68 |
| CHEMBL64104 | — | — | 1 | 5.52 |
| CHEMBL412897 | — | — | 1 | 5.40 |
| CHEMBL61957 | — | — | 1 | 5.30 |
| CHEMBL304631 | — | — | 1 | 5.10 |
| CHEMBL65005 | — | — | 1 | 5.00 |
| CHEMBL65723 | — | — | 1 | 5.00 |
| CHEMBL66298 | — | — | 1 | 4.82 |
| CHEMBL293661 | — | — | 1 | 4.82 |
| CHEMBL64073 | — | — | 1 | 4.19 |
| CHEMBL62352 | — | — | 1 | 4.00 |
| CHEMBL303799 | — | — | 1 | - |
| CHEMBL303821 | — | — | 1 | - |
| CHEMBL64395 | — | — | 1 | - |
| CHEMBL65452 | — | — | 1 | - |
| CHEMBL62922 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222519 | NBQX | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL65293 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL65729 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL294792 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL13260 | YM-90K | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL64684 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL302611 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL65989 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL62472 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL64104 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL412897 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL61957 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL304631 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL65005 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL65723 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL66298 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL293661 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL64073 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL62352 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL303799 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL303821 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL64395 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL65452 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL62922 | — | IC50 | > | 300000.0 | nM | - |