Assay Detail
Binding
CHEMBL698739
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Displacement of [3H]-AMPA from Ionotropic glutamate receptor AMPA of rat cortical membranes
14
Total Activities
12
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
Indeno[1,2-b]pyrazin-2,3-diones: a new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.76 | 6.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL420396 | — | — | 1 | 6.73 |
| CHEMBL312610 | — | — | 1 | 6.37 |
| CHEMBL289832 | LICOSTINEL | 2.0 | 1 | 6.12 |
| CHEMBL80649 | — | — | 3 | 6.00 |
| CHEMBL76808 | — | — | 1 | 5.89 |
| CHEMBL306934 | — | — | 1 | 5.75 |
| CHEMBL80267 | — | — | 1 | 5.35 |
| CHEMBL310685 | — | — | 1 | 5.34 |
| CHEMBL308028 | — | — | 1 | 5.16 |
| CHEMBL310024 | — | — | 1 | - |
| CHEMBL80741 | — | — | 1 | - |
| CHEMBL311104 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL420396 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL312610 | — | IC50 | = | 423.0 | nM | 6.37 |
| CHEMBL289832 | LICOSTINEL | IC50 | = | 766.0 | nM | 6.12 |
| CHEMBL80649 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL76808 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL306934 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL80649 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL80267 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL310685 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL308028 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL80649 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL310024 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL80741 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL311104 | — | IC50 | > | 10000.0 | nM | - |