Assay Detail
Binding
CHEMBL4158630
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.7 expressed in HEK293 cells at holding potential of -125 mV after 10 mins by patchxpress-based electrophysiology assay
41
Total Activities
41
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 9 subunit alpha (CHEMBL4296) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Tarantula Venom-Derived NaV1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 8.40 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4163942 | — | — | 1 | 9.70 |
| CHEMBL4162835 | — | — | 1 | 9.70 |
| CHEMBL4169884 | — | — | 1 | 9.59 |
| CHEMBL4173743 | — | — | 1 | 9.52 |
| CHEMBL4159473 | — | — | 1 | 9.52 |
| CHEMBL4174312 | — | — | 1 | 9.30 |
| CHEMBL4164272 | — | — | 1 | 9.30 |
| CHEMBL4175995 | — | — | 1 | 9.30 |
| CHEMBL4168880 | — | — | 1 | 9.22 |
| CHEMBL4167379 | — | — | 1 | 9.22 |
| CHEMBL4159169 | — | — | 1 | 9.10 |
| CHEMBL4167376 | — | — | 1 | 9.00 |
| CHEMBL4160269 | — | — | 1 | 9.00 |
| CHEMBL4175589 | — | — | 1 | 8.96 |
| CHEMBL4175563 | — | — | 1 | 8.96 |
| CHEMBL4166895 | — | — | 1 | 8.96 |
| CHEMBL4160943 | — | — | 1 | 8.89 |
| CHEMBL4167083 | — | — | 1 | 8.89 |
| CHEMBL4174592 | — | — | 1 | 8.80 |
| CHEMBL4167720 | — | — | 1 | 8.77 |
| CHEMBL4163637 | — | — | 1 | 8.60 |
| CHEMBL4165380 | — | — | 1 | 8.52 |
| CHEMBL4170712 | — | — | 1 | 8.51 |
| CHEMBL4170875 | — | — | 1 | 8.24 |
| CHEMBL4175832 | — | — | 1 | 8.17 |
| CHEMBL4165814 | — | — | 1 | 8.08 |
| CHEMBL4160074 | — | — | 1 | 8.05 |
| CHEMBL4171314 | — | — | 1 | 7.90 |
| CHEMBL4164545 | — | — | 1 | 7.82 |
| CHEMBL4171687 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4163942 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4162835 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4169884 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL4173743 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4159473 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4174312 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4164272 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4175995 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4168880 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4167379 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4159169 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4167376 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4160269 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4166895 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4175563 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4175589 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4160943 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4167083 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4174592 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4167720 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4163637 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4165380 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4170712 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4170875 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4175832 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4165814 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4160074 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4171314 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL4164545 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4171687 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4177466 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL4165596 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4174202 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4175203 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4167979 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4170776 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4172428 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL4174769 | — | IC50 | = | 471.0 | nM | 6.33 |
| CHEMBL4160718 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4164121 | — | IC50 | = | 825.0 | nM | 6.08 |
| CHEMBL4159239 | — | IC50 | > | 1000.0 | nM | - |