Assay Detail
Binding
CHEMBL3880655
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK293 cells assessed as reduction in outward tail current after 5 mins at -80 mV holding potential by patch clamp assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Agents for preventing and treating disorders involving modulation of the RYR receptors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.75 | 6.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2440857 | — | — | 1 | 6.33 |
| CHEMBL536480 | — | — | 1 | 6.30 |
| CHEMBL3958409 | — | — | 1 | 5.60 |
| CHEMBL3909873 | — | — | 1 | 5.36 |
| CHEMBL3933375 | — | — | 1 | 5.15 |
| CHEMBL2105757 | ALADORIAN SODIUM | -1.0 | 1 | - |
| CHEMBL3932540 | — | — | 1 | - |
| CHEMBL3965149 | — | — | 1 | - |
| CHEMBL3943880 | — | — | 1 | - |
| CHEMBL3980215 | — | — | 1 | - |
| CHEMBL3918523 | — | — | 1 | - |
| CHEMBL3915771 | — | — | 1 | - |
| CHEMBL3955655 | — | — | 1 | - |
| CHEMBL3963470 | — | — | 1 | - |
| CHEMBL3954519 | — | — | 1 | - |
| CHEMBL3892659 | — | — | 1 | - |
| CHEMBL2440854 | — | — | 1 | - |
| CHEMBL3958287 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2440857 | — | IC50 | = | 463.0 | nM | 6.33 |
| CHEMBL536480 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3958409 | — | IC50 | = | 2496.0 | nM | 5.60 |
| CHEMBL3909873 | — | IC50 | = | 4406.0 | nM | 5.36 |
| CHEMBL3933375 | — | IC50 | = | 7029.0 | nM | 5.15 |
| CHEMBL2105757 | ALADORIAN SODIUM | IC50 | - | — | - | |
| CHEMBL3932540 | — | IC50 | - | — | - | |
| CHEMBL3965149 | — | IC50 | - | — | - | |
| CHEMBL3943880 | — | IC50 | - | — | - | |
| CHEMBL3980215 | — | IC50 | - | — | - | |
| CHEMBL3918523 | — | IC50 | - | — | - | |
| CHEMBL3915771 | — | IC50 | - | — | - | |
| CHEMBL3955655 | — | IC50 | - | — | - | |
| CHEMBL3963470 | — | IC50 | - | — | - | |
| CHEMBL3954519 | — | IC50 | - | — | - | |
| CHEMBL3892659 | — | IC50 | - | — | - | |
| CHEMBL2440854 | — | IC50 | - | — | - | |
| CHEMBL3958287 | — | IC50 | - | — | - |