Assay Detail
Functional
CHEMBL699782
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonism at Ionotropic glutamate receptor kainate by inhibition of depolarizations induced by 10 uM kainic acid in rat cortical slice preparation.
18
Total Activities
16
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, kainate (CHEMBL2094119) ↗| 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 | 18 | 4.44 | 5.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL423498 | — | — | 1 | 5.00 |
| CHEMBL71755 | — | — | 3 | 4.54 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | 4.50 |
| CHEMBL433294 | — | — | 1 | 4.15 |
| CHEMBL73837 | — | — | 1 | 4.00 |
| CHEMBL307281 | — | — | 1 | - |
| CHEMBL73356 | — | — | 1 | - |
| CHEMBL311632 | — | — | 1 | - |
| CHEMBL72573 | — | — | 1 | - |
| CHEMBL72413 | — | — | 1 | - |
| CHEMBL304282 | — | — | 1 | - |
| CHEMBL70937 | — | — | 1 | - |
| CHEMBL422589 | — | — | 1 | - |
| CHEMBL72592 | — | — | 1 | - |
| CHEMBL72544 | — | — | 1 | - |
| CHEMBL306851 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL423498 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL71755 | — | IC50 | = | 28900.0 | nM | 4.54 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | IC50 | = | 31700.0 | nM | 4.50 |
| CHEMBL433294 | — | IC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL73837 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL307281 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL306851 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL72544 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL73356 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL72592 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL422589 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL70937 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL304282 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL311632 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL72413 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL71755 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL71755 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL72573 | — | IC50 | > | 100000.0 | nM | - |