Assay Detail
Binding
CHEMBL5041210
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.6 stably expressed in cells with train pulses to -20 mV at 0.1 Hz and holding potential of -85 mV by whole-cell Qube-automated patch clamp assay
24
Total Activities
24
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 8 subunit alpha (CHEMBL5202) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Na<sub>v</sub>1.7 for the Treatment of Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.65 | 7.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3318147 | — | — | 1 | 7.12 |
| CHEMBL5085021 | — | — | 1 | 5.93 |
| CHEMBL5074400 | — | — | 1 | 5.91 |
| CHEMBL5093139 | — | — | 1 | 5.58 |
| CHEMBL5088003 | — | — | 1 | 5.40 |
| CHEMBL5086465 | — | — | 1 | 5.32 |
| CHEMBL5086606 | — | — | 1 | 4.99 |
| CHEMBL5093042 | — | — | 1 | 4.95 |
| CHEMBL5074736 | — | — | 1 | - |
| CHEMBL5080941 | — | — | 1 | - |
| CHEMBL5091568 | — | — | 1 | - |
| CHEMBL5083009 | — | — | 1 | - |
| CHEMBL5075309 | — | — | 1 | - |
| CHEMBL5085091 | — | — | 1 | - |
| CHEMBL5076349 | — | — | 1 | - |
| CHEMBL5075738 | — | — | 1 | - |
| CHEMBL5092367 | — | — | 1 | - |
| CHEMBL5076456 | — | — | 1 | - |
| CHEMBL5078519 | — | — | 1 | - |
| CHEMBL5089216 | — | — | 1 | - |
| CHEMBL5088224 | — | — | 1 | - |
| CHEMBL5078424 | — | — | 1 | - |
| CHEMBL5092073 | — | — | 1 | - |
| CHEMBL5090054 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3318147 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5085021 | — | IC50 | = | 1185.0 | nM | 5.93 |
| CHEMBL5074400 | — | IC50 | = | 1234.0 | nM | 5.91 |
| CHEMBL5093139 | — | IC50 | = | 2609.0 | nM | 5.58 |
| CHEMBL5088003 | — | IC50 | = | 3944.0 | nM | 5.40 |
| CHEMBL5086465 | — | IC50 | = | 4830.0 | nM | 5.32 |
| CHEMBL5086606 | — | IC50 | = | 10330.0 | nM | 4.99 |
| CHEMBL5093042 | — | IC50 | = | 11110.0 | nM | 4.95 |
| CHEMBL5074736 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5080941 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5091568 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5083009 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5075309 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5085091 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5076349 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5075738 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5092367 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5076456 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5078519 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5089216 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5088224 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5078424 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5092073 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL5090054 | — | IC50 | > | 17000.0 | nM | - |