Assay Detail
Binding
CHEMBL4605649
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG incubated for 4 hrs by competitive fluorescence tracer binding based assay
8
Total Activities
8
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
Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.17 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4637502 | — | — | 1 | 7.10 |
| CHEMBL4642144 | — | — | 1 | 7.00 |
| CHEMBL4632471 | — | — | 1 | 6.47 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.35 |
| CHEMBL4633367 | — | — | 1 | 6.11 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 6.11 |
| CHEMBL4640297 | — | — | 1 | 5.30 |
| CHEMBL4638981 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4637502 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4642144 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4632471 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4633367 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4640297 | — | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL4638981 | — | IC50 | = | 12100.0 | nM | 4.92 |