Assay Detail
Binding
CHEMBL1286451
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse NaV1.8 expressed in HEK293 cells by isotopic efflux assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 10 subunit alpha (CHEMBL5158) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 23 | 6.04 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1277877 | — | — | 1 | 7.25 |
| CHEMBL1271106 | — | — | 1 | 7.24 |
| CHEMBL1278223 | — | — | 1 | 7.18 |
| CHEMBL1277959 | — | — | 1 | 6.96 |
| CHEMBL1277876 | — | — | 1 | 6.68 |
| CHEMBL1278224 | — | — | 1 | 6.62 |
| CHEMBL1278044 | — | — | 1 | 6.33 |
| CHEMBL1276882 | — | — | 1 | 6.32 |
| CHEMBL1277514 | — | — | 1 | 6.31 |
| CHEMBL1277958 | — | — | 1 | 6.19 |
| CHEMBL1278045 | — | — | 1 | 6.14 |
| CHEMBL250699 | — | — | 1 | 6.07 |
| CHEMBL1277513 | — | — | 1 | 6.02 |
| CHEMBL1276881 | — | — | 1 | 5.99 |
| CHEMBL1277512 | — | — | 1 | 5.97 |
| CHEMBL1277606 | — | — | 1 | 5.87 |
| CHEMBL1277700 | — | — | 1 | 5.60 |
| CHEMBL1277607 | — | — | 1 | 5.57 |
| CHEMBL1277792 | — | — | 1 | 5.38 |
| CHEMBL1278138 | — | — | 1 | 5.03 |
| CHEMBL1277699 | — | — | 1 | 4.96 |
| CHEMBL1277608 | — | — | 1 | 4.75 |
| CHEMBL1277793 | — | — | 1 | 4.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1277877 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1271106 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1278223 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1277959 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1277876 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1278224 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1278044 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL1276882 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1277514 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL1277958 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL1278045 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL250699 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL1277513 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL1276881 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL1277512 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL1277606 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL1277700 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1277607 | — | IC50 | = | 2680.0 | nM | 5.57 |
| CHEMBL1277792 | — | IC50 | = | 4140.0 | nM | 5.38 |
| CHEMBL1278138 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL1277699 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1277608 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1277793 | — | IC50 | = | 29100.0 | nM | 4.54 |