Assay Detail
Binding
CHEMBL4179762
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Inhibition of human Nav1.7 expressed in HEK cells by automated patchXpress electrophysiology method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 9 subunit alpha (CHEMBL4296) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.77 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4217988 | — | — | 1 | 10.52 |
| CHEMBL4205773 | — | — | 1 | 9.30 |
| CHEMBL4207534 | — | — | 1 | 9.15 |
| CHEMBL4208664 | — | — | 1 | 8.82 |
| CHEMBL2325603 | — | — | 1 | 8.80 |
| CHEMBL4215917 | — | — | 1 | 8.32 |
| CHEMBL2321912 | — | — | 1 | 8.07 |
| CHEMBL2325325 | — | — | 1 | 8.07 |
| CHEMBL4213602 | — | — | 1 | 7.88 |
| CHEMBL4208535 | — | — | 1 | - |
| CHEMBL4213464 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4217988 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4205773 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4207534 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4208664 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2325603 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4215917 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL2321912 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL2325325 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4213602 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL4208535 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4213464 | — | IC50 | < | 4.0 | nM | - |