Assay Detail
Toxicity
CHEMBL914758
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of hERG expressed in HEK293 cells assessed as effect on ionic current by patch clamp assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.07 | 5.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL224918 | — | — | 1 | 5.77 |
| CHEMBL387971 | — | — | 1 | 5.28 |
| CHEMBL223971 | — | — | 1 | 4.94 |
| CHEMBL225334 | — | — | 1 | 4.28 |
| CHEMBL445404 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL224918 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL387971 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL223971 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL225334 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL445404 | — | IC50 | > | 150000.0 | nM | - |