Assay Detail
Functional
CHEMBL821189
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Blockade of peak steady-state K+ currents of voltage-gated potassium channel subunit Kv1.3 in mouse fibroblasts L929 at 50 uM
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Potassium voltage-gated channel subfamily A member 3 (CHEMBL4818) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Angular methoxy-substituted furo- and pyranoquinolinones as blockers of the voltage-gated potassium channel Kv1.3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.56 | 6.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281622 | CP-339818 | — | 1 | 6.64 |
| CHEMBL9653 | — | — | 1 | 6.55 |
| CHEMBL277417 | — | — | 1 | 5.30 |
| CHEMBL282441 | — | — | 1 | 5.00 |
| CHEMBL278779 | KOKUSAGININE | — | 1 | 4.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281622 | CP-339818 | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL9653 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL277417 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL282441 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL278779 | KOKUSAGININE | IC50 | = | 49000.0 | nM | 4.31 |