Assay Detail
Binding
CHEMBL1272887
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Inhibition of mouse NaV1.8 by electrophysiology
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| 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
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.38 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1270301 | — | — | 1 | 7.58 |
| CHEMBL1269991 | — | — | 1 | 7.50 |
| CHEMBL1271106 | — | — | 1 | 7.24 |
| CHEMBL1269883 | — | — | 1 | 7.09 |
| CHEMBL1270208 | — | — | 1 | 7.06 |
| CHEMBL1270207 | — | — | 1 | 7.06 |
| CHEMBL1271309 | — | — | 1 | 6.72 |
| CHEMBL1271105 | — | — | 1 | 6.55 |
| CHEMBL1270797 | — | — | 1 | 6.54 |
| CHEMBL1270898 | — | — | 1 | 6.47 |
| CHEMBL1270302 | — | — | 1 | 6.47 |
| CHEMBL1270999 | — | — | 1 | 6.40 |
| CHEMBL1271206 | — | — | 1 | 6.28 |
| CHEMBL1271416 | — | — | 1 | 6.21 |
| CHEMBL1271417 | — | — | 1 | 6.21 |
| CHEMBL1270100 | — | — | 1 | 6.17 |
| CHEMBL1270998 | — | — | 1 | 6.06 |
| CHEMBL1270899 | — | — | 1 | 5.85 |
| CHEMBL1271205 | — | — | 1 | 5.82 |
| CHEMBL1271415 | — | — | 1 | 5.72 |
| CHEMBL1270099 | — | — | 1 | 5.58 |
| CHEMBL1270098 | — | — | 1 | 5.10 |
| CHEMBL1271308 | — | — | 1 | 4.96 |
| CHEMBL1269882 | — | — | 1 | - |
| CHEMBL1269990 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1270301 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1269991 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1271106 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL1269883 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL1270208 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL1270207 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL1271309 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1271105 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1270797 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1270898 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL1270302 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL1270999 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1271206 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL1271416 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL1271417 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1270100 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL1270998 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL1270899 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1271205 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1271415 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1270099 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1270098 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL1271308 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1269882 | — | IC50 | < | 30.0 | nM | - |
| CHEMBL1269990 | — | IC50 | < | 30.0 | nM | - |