Assay Detail
Binding
CHEMBL4383858
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of red tracer binding to human ERG expressed in membranes preincubated for 10 to 15 mins followed by tracer addition measured after 3 hrs by fluorescence polarization assay
4
Total Activities
4
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
First-in-class DAPK1/CSF1R dual inhibitors: Discovery of 3,5-dimethoxy-N-(4-(4-methoxyphenoxy)-2-((6-morpholinopyridin-3-yl)amino)pyrimidin-5-yl)benzamide as a potential anti-tauopathies agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.39 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL536480 | — | — | 1 | 8.00 |
| CHEMBL4461911 | — | — | 1 | 4.77 |
| CHEMBL103 | PROGESTERONE | 4.0 | 1 | - |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL536480 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4461911 | — | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL103 | PROGESTERONE | IC50 | - | — | - | |
| CHEMBL1355736 | THEOPHYLLINE | IC50 | - | — | - |