Assay Detail
Binding
CHEMBL4056904
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Inhibition of rat NaV1.7 at -125 mV holding potential yielding 20 to 50% inactivation after 3 to 5 mins by PatchXpress automated electrophysiology method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 9 subunit alpha (CHEMBL3312) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of a biarylamide series of potent, state-dependent NaV1.7 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.25 | 5.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4100413 | — | — | 1 | 5.39 |
| CHEMBL4076051 | — | — | 1 | 5.31 |
| CHEMBL4076380 | — | — | 1 | 5.25 |
| CHEMBL4100514 | — | — | 1 | 5.03 |
| CHEMBL4071906 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4100413 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4076051 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4076380 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4100514 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL4071906 | — | IC50 | > | 30000.0 | nM | - |