Assay Detail
Functional
CHEMBL703566
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against generation of currents by 50 uM kainate in Xenopus oocytes injected with rat brain mRNA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | Oocyte |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, kainate (CHEMBL2094119) ↗| 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 | 12 | 6.96 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14861 | — | — | 1 | 8.70 |
| CHEMBL277059 | — | — | 1 | 8.22 |
| CHEMBL14725 | — | — | 1 | 7.60 |
| CHEMBL277281 | — | — | 1 | 7.52 |
| CHEMBL222519 | NBQX | — | 1 | 7.51 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | 6.64 |
| CHEMBL15002 | — | — | 1 | 6.63 |
| CHEMBL13260 | YM-90K | — | 1 | 6.58 |
| CHEMBL14639 | — | — | 1 | 6.46 |
| CHEMBL14712 | — | — | 1 | 6.05 |
| CHEMBL14649 | — | — | 1 | 5.90 |
| CHEMBL279116 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14861 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL277059 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL14725 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL277281 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL222519 | NBQX | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL15002 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL13260 | YM-90K | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL14639 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL14712 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL14649 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL279116 | — | IC50 | = | 1800.0 | nM | 5.75 |