Assay Detail
Binding
CHEMBL4841563
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in CHO-K1 cells with holding potential -80 mV incubated for 5 mins by patch-clamp assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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, synthesis, and biological evaluation of novel somatostatin receptor subtype-2 agonists: Optimization for potency and risk mitigation of hERG and phospholipidosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.59 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4849848 | — | — | 1 | 6.22 |
| CHEMBL4863880 | — | — | 1 | 6.10 |
| CHEMBL4854239 | — | — | 1 | 6.05 |
| CHEMBL4872591 | — | — | 1 | 6.00 |
| CHEMBL4878248 | — | — | 1 | 5.77 |
| CHEMBL4845867 | — | — | 1 | 5.77 |
| CHEMBL4860633 | — | — | 1 | 5.77 |
| CHEMBL4845931 | — | — | 1 | 5.77 |
| CHEMBL4862717 | — | — | 1 | 5.72 |
| CHEMBL4861425 | — | — | 1 | 5.70 |
| CHEMBL4858892 | — | — | 1 | 5.66 |
| CHEMBL4851978 | — | — | 1 | 5.52 |
| CHEMBL4866325 | — | — | 1 | 5.43 |
| CHEMBL4870834 | — | — | 1 | 5.31 |
| CHEMBL4878917 | — | — | 1 | 5.31 |
| CHEMBL4853282 | — | — | 1 | 5.24 |
| CHEMBL4854548 | — | — | 1 | 5.14 |
| CHEMBL4876263 | — | — | 1 | 5.12 |
| CHEMBL4873269 | — | — | 1 | 5.08 |
| CHEMBL4862195 | — | — | 1 | 5.07 |
| CHEMBL4862497 | — | — | 1 | - |
| CHEMBL4856293 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4849848 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4863880 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4854239 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4872591 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4878248 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4845867 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4860633 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4845931 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4862717 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4861425 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4858892 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4851978 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4866325 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4870834 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4878917 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4853282 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4854548 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL4876263 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4873269 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL4862195 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4862497 | — | IC50 | - | — | - | |
| CHEMBL4856293 | — | IC50 | - | — | - |