Assay Detail
Binding
CHEMBL3418525
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ERG channel expressed in human embryonic kidney cells assessed as tail current amplitude measured for 3 to 30 mins by PatchXpress electrophysiology assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | kidney |
| 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
Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.30 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3415592 | — | — | 1 | 6.22 |
| CHEMBL3415594 | — | — | 1 | 6.00 |
| CHEMBL3415588 | — | — | 1 | 5.80 |
| CHEMBL3415583 | — | — | 1 | 5.80 |
| CHEMBL3415593 | — | — | 1 | 5.77 |
| CHEMBL3415587 | — | — | 1 | 5.77 |
| CHEMBL3415585 | — | — | 1 | 5.28 |
| CHEMBL3415595 | — | — | 1 | 5.23 |
| CHEMBL3415596 | — | — | 1 | 5.19 |
| CHEMBL3415591 | — | — | 1 | 4.85 |
| CHEMBL3415597 | — | — | 1 | 4.75 |
| CHEMBL3415610 | — | — | 1 | 4.66 |
| CHEMBL3415589 | — | — | 1 | 4.54 |
| CHEMBL3415598 | — | — | 1 | 4.36 |
| CHEMBL3415599 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3415592 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3415594 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3415588 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3415583 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3415593 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3415587 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3415585 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL3415595 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL3415596 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL3415591 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3415597 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3415610 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL3415589 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL3415598 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL3415599 | — | IC50 | > | 30000.0 | nM | - |