Assay Detail
Binding
CHEMBL3588589
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG
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
Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.37 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3585954 | — | — | 1 | 5.66 |
| CHEMBL3585956 | — | — | 1 | 5.66 |
| CHEMBL3585955 | — | — | 1 | 5.32 |
| CHEMBL3585953 | — | — | 1 | 5.23 |
| CHEMBL3545367 | LEMBOREXANT | 4.0 | 1 | 5.21 |
| CHEMBL3585946 | — | — | 1 | 5.11 |
| CHEMBL3585951 | — | — | 1 | - |
| CHEMBL3585957 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3585954 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3585956 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3585955 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3585953 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL3545367 | LEMBOREXANT | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3585946 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL3585951 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3585957 | — | IC50 | > | 10000.0 | nM | - |