Assay Detail
Binding
CHEMBL2216585
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Inhibition of Kv1.3 expressed in mouse L929 cells exposed to depolarizing step pulses from -80 mV to +40 mV by whole cell patch clamp method
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | L929 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Potassium voltage-gated channel subfamily A member 3 (CHEMBL4633) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationship exploration of Kv1.3 blockers based on diphenoxylate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.69 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL444449 | — | — | 1 | 8.70 |
| CHEMBL9653 | — | — | 1 | 6.70 |
| CHEMBL2205330 | — | — | 1 | 6.12 |
| CHEMBL2205325 | — | — | 1 | 6.10 |
| CHEMBL2205323 | — | — | 1 | 6.05 |
| CHEMBL2205327 | — | — | 1 | 5.90 |
| CHEMBL2205329 | — | — | 1 | 5.77 |
| CHEMBL2205326 | — | — | 1 | 5.73 |
| CHEMBL2205320 | — | — | 1 | 5.60 |
| CHEMBL2205321 | — | — | 1 | 5.58 |
| CHEMBL2205328 | — | — | 1 | 5.38 |
| CHEMBL1201294 | DIPHENOXYLATE | 4.0 | 1 | 5.30 |
| CHEMBL2205334 | — | — | 1 | 5.24 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.10 |
| CHEMBL2205324 | — | — | 1 | 4.69 |
| CHEMBL2205337 | — | — | 1 | 4.60 |
| CHEMBL2205332 | — | — | 1 | 4.12 |
| CHEMBL2205331 | — | — | 1 | - |
| CHEMBL2205333 | — | — | 1 | - |
| CHEMBL2205335 | — | — | 1 | - |
| CHEMBL2205322 | — | — | 1 | - |
| CHEMBL2205336 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL444449 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL9653 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2205330 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL2205325 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2205323 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2205327 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL2205329 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2205326 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL2205320 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL2205321 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL2205328 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1201294 | DIPHENOXYLATE | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2205334 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL2205324 | — | IC50 | = | 20500.0 | nM | 4.69 |
| CHEMBL2205337 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL2205332 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL2205331 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2205333 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2205335 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2205322 | — | IC50 | = | 230000.0 | nM | - |
| CHEMBL2205336 | — | IC50 | > | 100000.0 | nM | - |