Assay Detail
Binding
CHEMBL3803792
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG assessed as reduction in channel current by automated patch-clamp electrophysiology assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Design and synthesis of new potent anticancer benzothiazole amides and ureas featuring pyridylamide moiety and possessing dual B-Raf(V600E) and C-Raf kinase inhibitory activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.40 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 8.48 |
| CHEMBL3799621 | — | — | 1 | 4.32 |
| CHEMBL3799746 | — | — | 1 | - |
| CHEMBL3797601 | — | — | 1 | - |
| CHEMBL3798983 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 3.31 | nM | 8.48 |
| CHEMBL3799621 | — | IC50 | = | 48380.0 | nM | 4.32 |
| CHEMBL3799746 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3797601 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3798983 | — | IC50 | > | 100000.0 | nM | - |