Assay Detail
Binding
CHEMBL697363
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Displacement of [3H]AMPA from Ionotropic glutamate receptor AMPA of rat cortical membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, AMPA (CHEMBL2093871) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.83 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19955 | — | — | 1 | 7.64 |
| CHEMBL282030 | — | — | 1 | 7.46 |
| CHEMBL283350 | — | — | 1 | 7.36 |
| CHEMBL277340 | — | — | 1 | 7.26 |
| CHEMBL277711 | — | — | 1 | 7.03 |
| CHEMBL19892 | FANAPANEL | 2.0 | 1 | 6.85 |
| CHEMBL277281 | — | — | 1 | 6.82 |
| CHEMBL273569 | — | — | 1 | 6.80 |
| CHEMBL281393 | — | — | 1 | 6.78 |
| CHEMBL19194 | — | — | 1 | 6.62 |
| CHEMBL13260 | YM-90K | — | 1 | 6.46 |
| CHEMBL19857 | — | — | 1 | 6.24 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | 6.22 |
| CHEMBL279116 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19955 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL282030 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL283350 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL277340 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL277711 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL19892 | FANAPANEL | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL277281 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL273569 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL281393 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL19194 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL13260 | YM-90K | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL19857 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL279116 | — | IC50 | = | 760.0 | nM | 6.12 |