Assay Detail
Binding
CHEMBL1217015
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Displacement of [3H]AMPA from AMPA receptor in rat cortical membrane
17
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.53 | 7.37 |
| Ki | 8 | 6.17 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1214123 | — | — | 1 | 7.37 |
| CHEMBL13260 | YM-90K | — | 1 | 7.08 |
| CHEMBL119625 | ZONAMPANEL | 2.0 | 1 | 7.02 |
| CHEMBL19892 | FANAPANEL | 2.0 | 1 | 6.92 |
| CHEMBL222519 | NBQX | — | 1 | 6.82 |
| CHEMBL84990 | — | — | 1 | 6.77 |
| CHEMBL84775 | — | — | 1 | 6.54 |
| CHEMBL9790 | — | — | 1 | 6.52 |
| CHEMBL155265 | DNQX | — | 1 | 6.30 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 2 | 6.17 |
| CHEMBL345094 | — | — | 1 | 6.09 |
| CHEMBL27715 | — | — | 1 | 5.80 |
| CHEMBL23044 | — | — | 1 | 5.70 |
| CHEMBL83198 | — | — | 1 | 5.62 |
| CHEMBL342289 | — | — | 1 | 5.30 |
| CHEMBL282672 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1214123 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL13260 | YM-90K | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL119625 | ZONAMPANEL | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL19892 | FANAPANEL | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL222519 | NBQX | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL84990 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL84775 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL9790 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL155265 | DNQX | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL345094 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL27715 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL23044 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL83198 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL342289 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL282672 | — | Ki | > | 100000.0 | nM | - |