Assay Detail
Binding
CHEMBL1909112
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 5.70 | 7.48 |
| Ki | 871 | 5.74 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 2 | 7.52 |
| CHEMBL305660 | EBASTINE | 4.0 | 2 | 7.44 |
| CHEMBL17157 | TERFENADINE | 4.0 | 2 | 7.15 |
| CHEMBL41 | FLUOXETINE | 4.0 | 2 | 7.09 |
| CHEMBL841 | LOPERAMIDE | 4.0 | 2 | 7.07 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 2 | 6.84 |
| CHEMBL404849 | SULOCTIDIL | 4.0 | 2 | 6.80 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | 2.0 | 2 | 6.63 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 2 | 6.62 |
| CHEMBL1108 | DROPERIDOL | 4.0 | 2 | 6.61 |
| CHEMBL43064 | CINNARIZINE | 2.0 | 2 | 6.42 |
| CHEMBL64894 | GENTIAN VIOLET | 4.0 | 2 | 6.38 |
| CHEMBL723 | CARVEDILOL | 4.0 | 2 | 6.38 |
| CHEMBL75880 | PERHEXILINE | 4.0 | 2 | 6.33 |
| CHEMBL81 | RALOXIFENE | 4.0 | 2 | 6.32 |
| CHEMBL1221512 | — | — | 2 | 6.31 |
| CHEMBL357995 | BOPINDOLOL | 2.0 | 2 | 6.26 |
| CHEMBL954 | ENCLOMIPHENE | 3.0 | 2 | 6.24 |
| CHEMBL633 | AMIODARONE | 4.0 | 2 | 6.22 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 2 | 6.17 |
| CHEMBL114 | SAQUINAVIR | 4.0 | 2 | 6.17 |
| CHEMBL772 | RESERPINE | 4.0 | 2 | 6.15 |
| CHEMBL19215 | METERGOLINE | 2.0 | 2 | 6.14 |
| CHEMBL1626 | CLEMASTINE | 4.0 | 2 | 6.11 |
| CHEMBL219916 | DOMPERIDONE | 3.0 | 2 | 6.03 |
| CHEMBL1729 | CISAPRIDE | 4.0 | 2 | 6.00 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 2 | 6.00 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 2 | 5.99 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 2 | 5.97 |
| CHEMBL728 | PROCHLORPERAZINE | 4.0 | 2 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL305660 | EBASTINE | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL305660 | EBASTINE | IC50 | = | 39.5 | nM | 7.40 |
| CHEMBL17157 | TERFENADINE | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL41 | FLUOXETINE | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL841 | LOPERAMIDE | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL841 | LOPERAMIDE | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL404849 | SULOCTIDIL | Ki | = | 159.6 | nM | 6.80 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL404849 | SULOCTIDIL | IC50 | = | 174.9 | nM | 6.76 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL30008 | FLUNARIZINE | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL1108 | DROPERIDOL | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL30008 | FLUNARIZINE | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL1108 | DROPERIDOL | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL43064 | CINNARIZINE | Ki | = | 377.0 | nM | 6.42 |
| CHEMBL64894 | GENTIAN VIOLET | Ki | = | 419.0 | nM | 6.38 |
| CHEMBL43064 | CINNARIZINE | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL723 | CARVEDILOL | Ki | = | 415.0 | nM | 6.38 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL64894 | GENTIAN VIOLET | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL75880 | PERHEXILINE | Ki | = | 465.8 | nM | 6.33 |
| CHEMBL81 | RALOXIFENE | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL1221512 | — | Ki | = | 493.0 | nM | 6.31 |
| CHEMBL75880 | PERHEXILINE | IC50 | = | 510.6 | nM | 6.29 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 527.0 | nM | 6.28 |
| CHEMBL1221512 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL357995 | BOPINDOLOL | Ki | = | 548.0 | nM | 6.26 |
| CHEMBL954 | ENCLOMIPHENE | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL633 | AMIODARONE | Ki | = | 595.0 | nM | 6.22 |
| CHEMBL357995 | BOPINDOLOL | IC50 | = | 601.0 | nM | 6.22 |
| CHEMBL954 | ENCLOMIPHENE | IC50 | = | 636.0 | nM | 6.20 |
| CHEMBL633 | AMIODARONE | IC50 | = | 663.0 | nM | 6.18 |
| CHEMBL114 | SAQUINAVIR | Ki | = | 677.0 | nM | 6.17 |
| CHEMBL415 | CLOMIPRAMINE | Ki | = | 677.0 | nM | 6.17 |
| CHEMBL772 | RESERPINE | Ki | = | 706.0 | nM | 6.15 |
| CHEMBL19215 | METERGOLINE | Ki | = | 723.0 | nM | 6.14 |
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 742.0 | nM | 6.13 |
| CHEMBL114 | SAQUINAVIR | IC50 | = | 755.0 | nM | 6.12 |
| CHEMBL1626 | CLEMASTINE | Ki | = | 774.0 | nM | 6.11 |
| CHEMBL772 | RESERPINE | IC50 | = | 774.0 | nM | 6.11 |
| CHEMBL19215 | METERGOLINE | IC50 | = | 792.0 | nM | 6.10 |
| CHEMBL1626 | CLEMASTINE | IC50 | = | 849.0 | nM | 6.07 |
| CHEMBL219916 | DOMPERIDONE | Ki | = | 944.0 | nM | 6.03 |
| CHEMBL1729 | CISAPRIDE | Ki | = | 1012.0 | nM | 6.00 |