Assay Detail
Binding
CHEMBL1054535
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationships of 9-substituted-9-dihydroerythromycin-based motilin agonists: optimizing for potency and safety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.27 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL584549 | 3 9-DIHYDRO-N-DESMETHYL-N-ISOPROPYLERYTHROMYCIN A | — | 1 | 8.00 |
| CHEMBL532 | ERYTHROMYCIN | 4.0 | 1 | 7.41 |
| CHEMBL572996 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL584549 | 3 9-DIHYDRO-N-DESMETHYL-N-ISOPROPYLERYTHROMYCIN A | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL532 | ERYTHROMYCIN | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL572996 | — | IC50 | = | 411.0 | nM | 6.39 |