Assay Detail
Binding
CHEMBL748762
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Displacement of [3H]DCKA from N-methyl-D-aspartate glutamate receptor of rat cortical membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| 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 | 5.82 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277281 | — | — | 1 | 7.08 |
| CHEMBL14712 | — | — | 1 | 6.76 |
| CHEMBL14639 | — | — | 1 | 6.70 |
| CHEMBL14725 | — | — | 1 | 6.34 |
| CHEMBL14649 | — | — | 1 | 6.14 |
| CHEMBL279116 | — | — | 1 | 5.52 |
| CHEMBL14519 | — | — | 1 | 5.36 |
| CHEMBL15002 | — | — | 1 | 5.16 |
| CHEMBL14861 | — | — | 1 | 5.00 |
| CHEMBL277059 | — | — | 1 | 5.00 |
| CHEMBL13260 | YM-90K | — | 1 | 4.98 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | - |
| CHEMBL222519 | NBQX | — | 1 | - |
| CHEMBL273545 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277281 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL14712 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL14639 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL14725 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL14649 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL279116 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL14519 | — | IC50 | = | 4330.0 | nM | 5.36 |
| CHEMBL15002 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL14861 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL277059 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL13260 | YM-90K | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | IC50 | > | 10000.0 | nM | - |
| CHEMBL222519 | NBQX | IC50 | > | 10000.0 | nM | - |
| CHEMBL273545 | — | IC50 | - | nM | - |