Assay Detail
Binding
CHEMBL1286450
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Inhibition of tetrodotoxin-resistant NaV1.8 in rat dorsal root ganglion neurons at holding potential -100 mV by whole-cell patch clamp electrophysiology assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Dorsal root ganglion |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 10 subunit alpha (CHEMBL4017) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.99 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1277877 | — | — | 1 | 7.92 |
| CHEMBL1278223 | — | — | 1 | 7.80 |
| CHEMBL1277959 | — | — | 1 | 7.72 |
| CHEMBL1271106 | — | — | 1 | 7.47 |
| CHEMBL1277514 | — | — | 1 | 7.28 |
| CHEMBL1277958 | — | — | 1 | 7.17 |
| CHEMBL1278044 | — | — | 1 | 7.08 |
| CHEMBL1276882 | — | — | 1 | 7.07 |
| CHEMBL1276881 | — | — | 1 | 7.05 |
| CHEMBL1277606 | — | — | 1 | 6.96 |
| CHEMBL1278045 | — | — | 1 | 6.89 |
| CHEMBL250699 | — | — | 1 | 6.85 |
| CHEMBL1278224 | — | — | 1 | 6.77 |
| CHEMBL1277512 | — | — | 1 | 6.72 |
| CHEMBL1277513 | — | — | 1 | 6.55 |
| CHEMBL1277700 | — | — | 1 | 6.55 |
| CHEMBL1277607 | — | — | 1 | 6.44 |
| CHEMBL1278138 | — | — | 1 | 6.35 |
| CHEMBL1277876 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1277877 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1278223 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1277959 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1271106 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1277514 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1277958 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1278044 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL1276882 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1276881 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1277606 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1278045 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL250699 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1278224 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1277512 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1277513 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1277700 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1277607 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1278138 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1277876 | — | IC50 | = | 550.0 | nM | 6.26 |