Assay Detail
Binding
CHEMBL5041208
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.7 stably expressed in cells with train pulses to -20 mV at 0.1 Hz and holding potential of -95 mV by 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 9 subunit alpha (CHEMBL4296) ↗| 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 | 7.08 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5074400 | — | — | 1 | 7.70 |
| CHEMBL5086465 | — | — | 1 | 7.57 |
| CHEMBL5093139 | — | — | 1 | 7.52 |
| CHEMBL5085021 | — | — | 1 | 7.50 |
| CHEMBL5074736 | — | — | 1 | 7.38 |
| CHEMBL5088003 | — | — | 1 | 7.37 |
| CHEMBL3318147 | — | — | 1 | 7.36 |
| CHEMBL5080941 | — | — | 1 | 7.20 |
| CHEMBL5089216 | — | — | 1 | 7.19 |
| CHEMBL5086606 | — | — | 1 | 7.13 |
| CHEMBL5088224 | — | — | 1 | 7.12 |
| CHEMBL5078424 | — | — | 1 | 7.08 |
| CHEMBL5091568 | — | — | 1 | 7.04 |
| CHEMBL5093042 | — | — | 1 | 7.04 |
| CHEMBL5083009 | — | — | 1 | 7.01 |
| CHEMBL5075309 | — | — | 1 | 7.00 |
| CHEMBL5092073 | — | — | 1 | 6.96 |
| CHEMBL5085091 | — | — | 1 | 6.95 |
| CHEMBL5076349 | — | — | 1 | 6.74 |
| CHEMBL5075738 | — | — | 1 | 6.66 |
| CHEMBL5092367 | — | — | 1 | 6.65 |
| CHEMBL5076456 | — | — | 1 | 6.63 |
| CHEMBL5090054 | — | — | 1 | 6.62 |
| CHEMBL5078519 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5074400 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5086465 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5093139 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5085021 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5074736 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5088003 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3318147 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5080941 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5089216 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL5086606 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5088224 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5078424 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5091568 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5093042 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5083009 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5075309 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5092073 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5085091 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL5076349 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL5075738 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL5092367 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL5076456 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL5090054 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5078519 | — | IC50 | = | 253.0 | nM | 6.60 |