Assay Detail
Binding
CHEMBL3378637
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG by MK-499 displacement binding analysis
12
Total Activities
12
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
Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.60 | 6.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3323073 | — | — | 1 | 6.20 |
| CHEMBL3323072 | — | — | 1 | 6.15 |
| CHEMBL3323075 | — | — | 1 | 5.92 |
| CHEMBL3323074 | — | — | 1 | 5.85 |
| CHEMBL3323078 | — | — | 1 | 5.79 |
| CHEMBL2204935 | — | — | 1 | 5.76 |
| CHEMBL3323076 | — | — | 1 | 5.65 |
| CHEMBL3323077 | — | — | 1 | 5.60 |
| CHEMBL3323079 | — | — | 1 | 5.55 |
| CHEMBL3323080 | — | — | 1 | 5.06 |
| CHEMBL3323084 | — | — | 1 | 4.92 |
| CHEMBL3323082 | — | — | 1 | 4.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3323073 | — | IC50 | = | 625.0 | nM | 6.20 |
| CHEMBL3323072 | — | IC50 | = | 707.0 | nM | 6.15 |
| CHEMBL3323075 | — | IC50 | = | 1205.0 | nM | 5.92 |
| CHEMBL3323074 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL3323078 | — | IC50 | = | 1611.0 | nM | 5.79 |
| CHEMBL2204935 | — | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL3323076 | — | IC50 | = | 2257.0 | nM | 5.65 |
| CHEMBL3323077 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL3323079 | — | IC50 | = | 2845.0 | nM | 5.55 |
| CHEMBL3323080 | — | IC50 | = | 8703.0 | nM | 5.06 |
| CHEMBL3323084 | — | IC50 | = | 11990.0 | nM | 4.92 |
| CHEMBL3323082 | — | IC50 | = | 19560.0 | nM | 4.71 |