Assay Detail
Functional
CHEMBL686879
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Ikr current in isolated guinea pig myocytes during a 0.5 s voltage clamp step from -50 to -10 mV.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| 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
Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.60 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL128007 | — | — | 1 | 7.00 |
| CHEMBL340353 | — | — | 1 | 6.00 |
| CHEMBL332826 | — | — | 1 | 5.82 |
| CHEMBL127701 | — | — | 1 | 5.62 |
| CHEMBL339327 | — | — | 1 | 5.40 |
| CHEMBL9387 | L-365260 | — | 1 | 5.30 |
| CHEMBL16900 | L-768673 | — | 1 | 5.22 |
| CHEMBL338109 | — | — | 1 | 5.06 |
| CHEMBL70380 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL128007 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL340353 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL332826 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL127701 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL339327 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL9387 | L-365260 | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL16900 | L-768673 | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL338109 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL70380 | — | IC50 | = | 10000.0 | nM | 5.00 |