Assay Detail
Binding
CHEMBL4813111
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Inhibition of human Nav1.5 by automated voltage clamp electrophysiology
29
Total Activities
26
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 5 subunit alpha (CHEMBL1980) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of aryl sulfonamides as novel and potent inhibitors of Na<sub>V</sub>1.5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.93 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4864812 | — | — | 1 | 7.51 |
| CHEMBL4854735 | — | — | 3 | 7.41 |
| CHEMBL4849813 | — | — | 2 | 6.62 |
| CHEMBL4863095 | — | — | 1 | 6.58 |
| CHEMBL4853170 | — | — | 1 | 6.34 |
| CHEMBL4860097 | — | — | 1 | 6.33 |
| CHEMBL4865860 | — | — | 1 | 6.21 |
| CHEMBL4876448 | — | — | 1 | 6.17 |
| CHEMBL4859414 | — | — | 1 | 6.16 |
| CHEMBL4872374 | — | — | 1 | 6.12 |
| CHEMBL4867480 | — | — | 1 | 5.96 |
| CHEMBL4867340 | — | — | 1 | 5.93 |
| CHEMBL4870820 | — | — | 1 | 5.89 |
| CHEMBL4850129 | — | — | 1 | 5.81 |
| CHEMBL4850942 | — | — | 1 | 5.37 |
| CHEMBL4862429 | — | — | 1 | 5.34 |
| CHEMBL4846327 | — | — | 1 | 5.33 |
| CHEMBL4863596 | — | — | 1 | 5.30 |
| CHEMBL4855375 | — | — | 1 | 5.20 |
| CHEMBL4877705 | — | — | 1 | 5.15 |
| CHEMBL4867251 | — | — | 1 | 5.11 |
| CHEMBL4857167 | — | — | 1 | 4.88 |
| CHEMBL4849208 | — | — | 1 | 4.60 |
| CHEMBL4862578 | — | — | 1 | 4.59 |
| CHEMBL4872687 | — | — | 1 | - |
| CHEMBL4865549 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4864812 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4854735 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4854735 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4854735 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4849813 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4863095 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4849813 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4853170 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4860097 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4865860 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4876448 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4859414 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4872374 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4867480 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4867340 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL4870820 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL4850129 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4850942 | — | IC50 | = | 4320.0 | nM | 5.37 |
| CHEMBL4862429 | — | IC50 | = | 4580.0 | nM | 5.34 |
| CHEMBL4846327 | — | IC50 | = | 4650.0 | nM | 5.33 |
| CHEMBL4863596 | — | IC50 | = | 5040.0 | nM | 5.30 |
| CHEMBL4855375 | — | IC50 | = | 6330.0 | nM | 5.20 |
| CHEMBL4877705 | — | IC50 | = | 7140.0 | nM | 5.15 |
| CHEMBL4867251 | — | IC50 | = | 7830.0 | nM | 5.11 |
| CHEMBL4857167 | — | IC50 | = | 13210.0 | nM | 4.88 |
| CHEMBL4849208 | — | IC50 | = | 25050.0 | nM | 4.60 |
| CHEMBL4862578 | — | IC50 | = | 25490.0 | nM | 4.59 |
| CHEMBL4872687 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4865549 | — | IC50 | > | 30000.0 | nM | - |