Assay Detail
Binding
CHEMBL818203
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against type IIA sodium channel in CNaIIA-1 cell line expressed in CHO cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium channel protein type 2 subunit alpha (CHEMBL3399) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
A structure-activity relationship study of novel phenylacetamides which are sodium channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.50 | 6.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1423 | PIMOZIDE | 4.0 | 1 | 6.47 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 1 | 6.31 |
| CHEMBL288826 | — | — | 1 | 6.22 |
| CHEMBL36637 | — | — | 1 | 6.16 |
| CHEMBL35818 | — | — | 1 | 6.14 |
| CHEMBL37100 | — | — | 1 | 5.96 |
| CHEMBL37217 | — | — | 1 | 5.92 |
| CHEMBL37974 | — | — | 1 | 5.92 |
| CHEMBL39907 | — | — | 1 | 5.85 |
| CHEMBL36798 | — | — | 1 | 5.82 |
| CHEMBL38095 | — | — | 1 | 5.66 |
| CHEMBL40106 | — | — | 1 | 5.57 |
| CHEMBL282833 | — | — | 1 | 5.57 |
| CHEMBL40788 | — | — | 1 | 5.36 |
| CHEMBL37446 | — | — | 1 | 5.34 |
| CHEMBL290663 | — | — | 1 | 5.28 |
| CHEMBL288029 | — | — | 1 | 5.19 |
| CHEMBL40061 | — | — | 1 | 5.14 |
| CHEMBL40002 | — | — | 1 | 5.00 |
| CHEMBL37379 | — | — | 1 | 4.70 |
| CHEMBL40078 | — | — | 1 | 4.50 |
| CHEMBL34069 | — | — | 1 | 4.40 |
| CHEMBL435767 | — | — | 1 | 4.02 |
| CHEMBL289225 | — | — | 1 | - |
| CHEMBL285029 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1423 | PIMOZIDE | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL30008 | FLUNARIZINE | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL288826 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL36637 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL35818 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL37100 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL37217 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL37974 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL39907 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL36798 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL38095 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL40106 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL282833 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL40788 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL37446 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL290663 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL288029 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL40061 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL40002 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL37379 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL40078 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL34069 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL435767 | — | IC50 | = | 95000.0 | nM | 4.02 |
| CHEMBL289225 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL285029 | — | IC50 | > | 200000.0 | nM | - |