Assay Detail
Binding
CHEMBL4672963
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 10 subunit alpha (CHEMBL5451) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-Amino-N-heteroaryl-nicotimamides as Na1.8 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.60 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4760292 | — | — | 1 | 9.52 |
| CHEMBL4777598 | — | — | 1 | 9.30 |
| CHEMBL4781110 | — | — | 1 | 9.05 |
| CHEMBL4745699 | — | — | 1 | 9.00 |
| CHEMBL4764433 | — | — | 1 | 8.80 |
| CHEMBL4743638 | — | — | 1 | 8.59 |
| CHEMBL4751356 | — | — | 1 | 8.55 |
| CHEMBL4748189 | — | — | 1 | 8.52 |
| CHEMBL4778738 | — | — | 1 | 8.51 |
| CHEMBL4777784 | — | — | 1 | 8.41 |
| CHEMBL4796719 | — | — | 1 | 8.39 |
| CHEMBL4759995 | — | — | 1 | 8.35 |
| CHEMBL4788313 | — | — | 1 | 8.28 |
| CHEMBL4752525 | — | — | 1 | 8.24 |
| CHEMBL4753100 | — | — | 1 | 8.19 |
| CHEMBL4763229 | — | — | 1 | 7.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4760292 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4777598 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4781110 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4745699 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4764433 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4743638 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4751356 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4748189 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4778738 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4777784 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4796719 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4759995 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4788313 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4752525 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4753100 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4763229 | — | IC50 | = | 12.0 | nM | 7.92 |