Assay Detail
Functional
CHEMBL2182445
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat GluK1 receptor expressed in Xenopus oocytes at membrane potential -60 mV by two-electrode voltage-clamp electrophysiology assay
6
Total Activities
6
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 | 6 | 7.73 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2178920 | — | — | 1 | 9.48 |
| CHEMBL2178919 | — | — | 1 | 9.09 |
| CHEMBL313747 | JORO SPIDER TOXIN 3 | — | 1 | 7.72 |
| CHEMBL2178917 | NEPHILA SPIDER TOXIN 3 | — | 1 | 6.79 |
| CHEMBL2178918 | — | — | 1 | 5.59 |
| CHEMBL1098240 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2178920 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL2178919 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL313747 | JORO SPIDER TOXIN 3 | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2178917 | NEPHILA SPIDER TOXIN 3 | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL2178918 | — | IC50 | = | 2575.0 | nM | 5.59 |
| CHEMBL1098240 | — | IC50 | - | — | - |