Assay Detail
Binding
CHEMBL827807
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against IKr potassium channel
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 55 | 5.96 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 8.82 |
| CHEMBL129583 | — | — | 1 | 8.10 |
| CHEMBL182977 | — | — | 1 | 8.00 |
| CHEMBL327980 | — | — | 1 | 7.70 |
| CHEMBL182646 | — | — | 1 | 7.70 |
| CHEMBL533 | IBUTILIDE | 4.0 | 1 | 7.70 |
| CHEMBL473 | DOFETILIDE | 4.0 | 1 | 7.52 |
| CHEMBL96153 | TERIKALANT | 2.0 | 1 | 7.52 |
| CHEMBL1107 | HALOFANTRINE | 4.0 | 1 | 7.40 |
| CHEMBL17157 | TERFENADINE | 4.0 | 1 | 7.30 |
| CHEMBL362721 | — | — | 1 | 7.05 |
| CHEMBL9484 | CLOFILIUM | 2.0 | 1 | 6.82 |
| CHEMBL362103 | ALMOKALANT | 2.0 | 1 | 6.60 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 6.58 |
| CHEMBL723 | CARVEDILOL | 4.0 | 1 | 6.46 |
| CHEMBL123558 | AZIMILIDE | 3.0 | 1 | 6.40 |
| CHEMBL184461 | — | — | 1 | 6.38 |
| CHEMBL1008 | BEPRIDIL | 4.0 | 1 | 6.37 |
| CHEMBL363295 | TERODILINE | 4.0 | 1 | 6.30 |
| CHEMBL631 | PROPAFENONE | 4.0 | 1 | 6.10 |
| CHEMBL353985 | — | — | 1 | 6.00 |
| CHEMBL505 | CHLORPHENIRAMINE | 4.0 | 1 | 5.96 |
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | 5.96 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 5.85 |
| CHEMBL45816 | MIBEFRADIL | 4.0 | 1 | 5.85 |
| CHEMBL1423 | PIMOZIDE | 4.0 | 1 | 5.77 |
| CHEMBL46516 | FLUSPIRILENE | 3.0 | 1 | 5.64 |
| CHEMBL76 | CHLOROQUINE | 4.0 | 1 | 5.60 |
| CHEMBL416956 | MEFLOQUINE | 4.0 | 1 | 5.58 |
| CHEMBL184412 | DRONEDARONE | 4.0 | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL129583 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL182977 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL327980 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL182646 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL533 | IBUTILIDE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL473 | DOFETILIDE | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL96153 | TERIKALANT | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1107 | HALOFANTRINE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL362721 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL9484 | CLOFILIUM | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL362103 | ALMOKALANT | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL123558 | AZIMILIDE | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL184461 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL1008 | BEPRIDIL | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL363295 | TERODILINE | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL631 | PROPAFENONE | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL353985 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL505 | CHLORPHENIRAMINE | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL511 | PYRILAMINE | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL45816 | MIBEFRADIL | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1423 | PIMOZIDE | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL46516 | FLUSPIRILENE | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL76 | CHLOROQUINE | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL416956 | MEFLOQUINE | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL184412 | DRONEDARONE | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL9387 | L-365260 | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL16900 | L-768673 | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL184014 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL38827 | LUMEFANTRINE | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL87045 | CIFENLINE | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL360861 | NIFEKALANT | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL517 | DISOPYRAMIDE | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL185434 | AROXYBUTYNIN | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL298475 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL186873 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL442717 | DAURICINE | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL17423 | VESNARINONE | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1726 | NISOLDIPINE | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL532 | ERYTHROMYCIN | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL1264 | 5-HYDROXY PROPAFENONE | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL1365 | N-DEPROPYL-PROPAPHENONE | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL1741 | CLARITHROMYCIN | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL1097 | ACECAINIDE | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL193 | NIFEDIPINE | IC50 | = | 280000.0 | nM | - |