Assay Detail
Binding
CHEMBL697806
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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
4,10-Dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazin-2-carboxylic acid derivatives: highly potent and selective AMPA receptors antagonists with in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.99 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14861 | — | — | 1 | 8.40 |
| CHEMBL14519 | — | — | 1 | 8.05 |
| CHEMBL277059 | — | — | 1 | 8.05 |
| CHEMBL273545 | — | — | 1 | 7.26 |
| CHEMBL14725 | — | — | 1 | 7.22 |
| CHEMBL14712 | — | — | 1 | 7.07 |
| CHEMBL222519 | NBQX | — | 1 | 6.85 |
| CHEMBL277281 | — | — | 1 | 6.82 |
| CHEMBL14639 | — | — | 1 | 6.68 |
| CHEMBL13260 | YM-90K | — | 1 | 6.46 |
| CHEMBL15002 | — | — | 1 | 6.33 |
| CHEMBL14649 | — | — | 1 | 6.32 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | 6.22 |
| CHEMBL279116 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14861 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL14519 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL277059 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL273545 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL14725 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL14712 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL222519 | NBQX | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL277281 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL14639 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL13260 | YM-90K | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL15002 | — | IC50 | = | 473.0 | nM | 6.33 |
| CHEMBL14649 | — | IC50 | = | 476.0 | nM | 6.32 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL279116 | — | IC50 | = | 760.0 | nM | 6.12 |