Assay Detail
Binding
CHEMBL3880277
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK293 cells assessed as decrease in tail current amplitude by whole cell patch clamp method
13
Total Activities
13
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
Use of acacetin and related compounds as potassium channel inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 4.73 | 5.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3968881 | — | — | 1 | 5.39 |
| CHEMBL301692 | — | — | 1 | 4.89 |
| CHEMBL16312 | 4'-METHOXYFLAVONE | — | 1 | 4.66 |
| CHEMBL243664 | ACACETIN | — | 1 | 4.49 |
| CHEMBL2442379 | — | — | 1 | 4.24 |
| CHEMBL311498 | CIANIDANOL | 4.0 | 1 | - |
| CHEMBL3939799 | — | — | 1 | - |
| CHEMBL226335 | RUTIN | 3.0 | 1 | - |
| CHEMBL8260 | BAICALEIN | 2.0 | 1 | - |
| CHEMBL3948644 | — | — | 1 | - |
| CHEMBL3984354 | — | — | 1 | - |
| CHEMBL350958 | APIGENIN DIMETHYLETHER | — | 1 | - |
| CHEMBL3924648 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3968881 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL301692 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL16312 | 4'-METHOXYFLAVONE | IC50 | = | 21900.0 | nM | 4.66 |
| CHEMBL243664 | ACACETIN | IC50 | = | 32400.0 | nM | 4.49 |
| CHEMBL2442379 | — | IC50 | = | 57900.0 | nM | 4.24 |
| CHEMBL311498 | CIANIDANOL | IC50 | - | — | - | |
| CHEMBL3939799 | — | IC50 | - | — | - | |
| CHEMBL226335 | RUTIN | IC50 | - | — | - | |
| CHEMBL8260 | BAICALEIN | IC50 | - | — | - | |
| CHEMBL3948644 | — | IC50 | - | — | - | |
| CHEMBL3984354 | — | IC50 | - | — | - | |
| CHEMBL350958 | APIGENIN DIMETHYLETHER | IC50 | - | — | - | |
| CHEMBL3924648 | — | IC50 | - | — | - |