Assay Detail
Functional
CHEMBL861276
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effect on blockade of Kv1.2 channel
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Potassium voltage-gated channel subfamily A member 2 (CHEMBL2086) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A new class of blockers of the voltage-gated potassium channel Kv1.3 via modification of the 4- or 7-position of khellinone.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 5.48 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL426482 | — | — | 1 | 5.85 |
| CHEMBL382154 | — | — | 1 | 5.60 |
| CHEMBL203909 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL426482 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL382154 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL203909 | — | EC50 | = | 10000.0 | nM | 5.00 |