Assay Detail
Functional
CHEMBL640420
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonism at AMPA receptor by inhibition of depolarizations induced by 40 uM AMPA in rat cortical slice preparation.
16
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, AMPA (CHEMBL2093871) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Structure-activity studies of 6-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists. 2. Effects of distal acid bioisosteric substitution, absolute stereochemical preferences, and in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.04 | 5.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 2 | 5.75 |
| CHEMBL423498 | — | — | 1 | 5.67 |
| CHEMBL304282 | — | — | 1 | 4.78 |
| CHEMBL433294 | — | — | 1 | 4.72 |
| CHEMBL71755 | — | — | 2 | 4.66 |
| CHEMBL73837 | — | — | 1 | 4.50 |
| CHEMBL307281 | — | — | 1 | - |
| CHEMBL311632 | — | — | 1 | - |
| CHEMBL72413 | — | — | 1 | - |
| CHEMBL70937 | — | — | 1 | - |
| CHEMBL422589 | — | — | 1 | - |
| CHEMBL72592 | — | — | 1 | - |
| CHEMBL72544 | — | — | 1 | - |
| CHEMBL306851 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL423498 | — | IC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL304282 | — | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL433294 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL71755 | — | IC50 | = | 21900.0 | nM | 4.66 |
| CHEMBL73837 | — | IC50 | = | 31400.0 | nM | 4.50 |
| CHEMBL307281 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL311632 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL71755 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL72413 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL70937 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL422589 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL72592 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL72544 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL306851 | — | IC50 | > | 100000.0 | nM | - |