Assay Detail
Binding
CHEMBL806152
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex
115
Total Activities
113
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Sodium channel alpha subunits; brain (Types I, II, III) (CHEMBL2096682) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 115 | 5.19 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL841 | LOPERAMIDE | 4.0 | 1 | 6.57 |
| CHEMBL421665 | FLUPERAMIDE | 2.0 | 1 | 6.55 |
| CHEMBL24072 | PRENYLAMINE | 4.0 | 1 | 6.52 |
| CHEMBL43064 | CINNARIZINE | 2.0 | 1 | 6.36 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 1 | 6.22 |
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 6.22 |
| CHEMBL126075 | DILAZEP | 2.0 | 1 | 6.22 |
| CHEMBL1108 | DROPERIDOL | 4.0 | 1 | 6.13 |
| CHEMBL2110608 | — | — | 1 | 6.13 |
| CHEMBL340398 | — | — | 1 | 6.10 |
| CHEMBL1008 | BEPRIDIL | 4.0 | 1 | 6.08 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 1 | 6.00 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 5.92 |
| CHEMBL338667 | DIPERODON | 2.0 | 1 | 5.89 |
| CHEMBL1086 | DIBUCAINE | 4.0 | 1 | 5.85 |
| CHEMBL127300 | HEXOBENDINE | 2.0 | 1 | 5.85 |
| CHEMBL772 | RESERPINE | 4.0 | 1 | 5.80 |
| CHEMBL127123 | PHENACAINE | 2.0 | 1 | 5.77 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | — | 1 | 5.75 |
| CHEMBL1196 | PROPARACAINE | 4.0 | 1 | 5.72 |
| CHEMBL127487 | CYCLOMETHYCAINE | 2.0 | 1 | 5.70 |
| CHEMBL6066837 | (-)-BUTACLAMOL | — | 1 | 5.70 |
| CHEMBL127592 | OXETHAZAINE | 3.0 | 1 | 5.64 |
| CHEMBL126732 | — | — | 1 | 5.62 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 5.62 |
| CHEMBL129529 | BUTACAINE | 2.0 | 1 | 5.57 |
| CHEMBL1200 | BENOXINATE | 4.0 | 1 | 5.54 |
| CHEMBL1294 | QUINIDINE | 4.0 | 1 | 5.50 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.48 |
| CHEMBL7568 | QUINACRINE | 4.0 | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL841 | LOPERAMIDE | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL421665 | FLUPERAMIDE | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL24072 | PRENYLAMINE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL43064 | CINNARIZINE | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL267930 | SPIPERONE | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL30008 | FLUNARIZINE | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL126075 | DILAZEP | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2110608 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL1108 | DROPERIDOL | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL340398 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1008 | BEPRIDIL | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL516 | CYPROHEPTADINE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL338667 | DIPERODON | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1086 | DIBUCAINE | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL127300 | HEXOBENDINE | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL772 | RESERPINE | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL127123 | PHENACAINE | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1196 | PROPARACAINE | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL6066837 | (-)-BUTACLAMOL | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL127487 | CYCLOMETHYCAINE | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL127592 | OXETHAZAINE | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL126732 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL72 | DESIPRAMINE | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL129529 | BUTACAINE | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1200 | BENOXINATE | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL1294 | QUINIDINE | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL7568 | QUINACRINE | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL127643 | DIMETHISOQUIN | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL698 | TETRACAINE | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL936 | DIPHENIDOL | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL492 | ETIDOCAINE | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL51149 | GALLOPAMIL | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL8514 | BUTACLAMOL | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL11 | IMIPRAMINE | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL726 | FLUPHENAZINE | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL339701 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL127734 | CARCAINIUM CHLORIDE | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL282567 | PROADIFEN | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL126628 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL170 | QUININE | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL540140 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL422 | TRIFLUOPERAZINE | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1098 | BUPIVACAINE | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL564 | PROMAZINE | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL6437 | MIANSERIN | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL657 | DIPHENHYDRAMINE | IC50 | = | 6000.0 | nM | 5.22 |