Assay Detail
Binding
CHEMBL697365
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Affinity towards Ionotropic glutamate receptor AMPA using [3H]AMPA as ligand on rat cortical membrane preparations
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, AMPA (CHEMBL2093871) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Bioisosteres of 9-carboxymethyl-4-oxo-imidazo[1,2-a]indeno-[1,2-e]pyrazin-2-carboxylic acid derivatives. Progress towards selective, potent in vivo AMPA antagonists with longer durations of action.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.10 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL433424 | — | — | 1 | 8.40 |
| CHEMBL24875 | — | — | 1 | 7.92 |
| CHEMBL25529 | — | — | 1 | 7.89 |
| CHEMBL279018 | — | — | 1 | 7.82 |
| CHEMBL24980 | — | — | 1 | 7.75 |
| CHEMBL25404 | — | — | 1 | 7.52 |
| CHEMBL281030 | — | — | 1 | 7.51 |
| CHEMBL28388 | — | — | 1 | 7.40 |
| CHEMBL281658 | — | — | 1 | 7.00 |
| CHEMBL24507 | — | — | 1 | 6.86 |
| CHEMBL222519 | NBQX | — | 1 | 6.85 |
| CHEMBL278615 | — | — | 1 | 6.83 |
| CHEMBL283446 | — | — | 1 | 6.82 |
| CHEMBL25504 | — | — | 1 | 6.72 |
| CHEMBL25453 | — | — | 1 | 6.63 |
| CHEMBL13260 | YM-90K | — | 1 | 6.46 |
| CHEMBL25687 | — | — | 1 | 6.23 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | 6.22 |
| CHEMBL279116 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL433424 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL24875 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL25529 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL279018 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL24980 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL25404 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL281030 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL28388 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL281658 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL24507 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL222519 | NBQX | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL278615 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL283446 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL25504 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL25453 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL13260 | YM-90K | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL25687 | — | IC50 | = | 586.0 | nM | 6.23 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL279116 | — | IC50 | = | 760.0 | nM | 6.12 |