Assay Detail
Binding
CHEMBL3738365
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG assessed as reduction in IKr current
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
Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.55 | 4.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3735329 | — | — | 1 | 4.68 |
| CHEMBL2105762 | OMARIGLIPTIN | 4.0 | 1 | 4.41 |
| CHEMBL2425070 | — | — | 1 | - |
| CHEMBL3735281 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3735329 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL2105762 | OMARIGLIPTIN | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL2425070 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3735281 | — | IC50 | > | 60000.0 | nM | - |