Assay Detail
Functional
CHEMBL2182444
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat GluK1 receptor expressed in Xenopus oocytes by two-electrode voltage-clamp at membrane potential -60 to -80 mV electrophysiology assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | Oocyte |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, kainate 1 (CHEMBL2919) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 9.64 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2178920 | — | — | 1 | 9.72 |
| CHEMBL2178919 | — | — | 1 | 9.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2178920 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL2178919 | — | IC50 | = | 0.28 | nM | 9.55 |