Assay Detail
Binding
CHEMBL3804567
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Inhibition of human Nav1.5 expressed in HEK293 cells by whole cell-patch clamp method
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 5 subunit alpha (CHEMBL1980) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.32 | 6.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | 4.0 | 1 | 6.19 |
| CHEMBL3798493 | — | — | 1 | 6.00 |
| CHEMBL3797315 | — | — | 1 | 5.70 |
| CHEMBL3800069 | — | — | 1 | 5.60 |
| CHEMBL3798363 | — | — | 1 | 5.55 |
| CHEMBL3797498 | — | — | 1 | 5.51 |
| CHEMBL3800304 | — | — | 1 | 5.47 |
| CHEMBL3798039 | — | — | 1 | 5.36 |
| CHEMBL3798258 | — | — | 1 | 5.30 |
| CHEMBL3799617 | — | — | 1 | 5.29 |
| CHEMBL3799838 | — | — | 1 | 4.85 |
| CHEMBL3799551 | — | — | 1 | 4.82 |
| CHEMBL3799939 | — | — | 1 | 4.79 |
| CHEMBL3798393 | — | — | 1 | 4.72 |
| CHEMBL3799790 | — | — | 1 | 4.64 |
| CHEMBL3798774 | — | — | 1 | - |
| CHEMBL3798228 | — | — | 1 | - |
| CHEMBL3797267 | — | — | 1 | - |
| CHEMBL3799205 | — | — | 1 | - |
| CHEMBL3798320 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL3798493 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3797315 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3800069 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3798363 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3797498 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3800304 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3798039 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL3798258 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3799617 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3799838 | — | IC50 | = | 14200.0 | nM | 4.85 |
| CHEMBL3799551 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3799939 | — | IC50 | = | 16400.0 | nM | 4.79 |
| CHEMBL3798393 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3799790 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL3798774 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3798228 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3797267 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3799205 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3798320 | — | IC50 | > | 33000.0 | nM | - |