Assay Detail
Binding
CHEMBL933193
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG by FLIPR assay
16
Total Activities
16
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 azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.29 | 5.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272336 | — | — | 1 | 5.89 |
| CHEMBL429734 | — | — | 1 | 5.75 |
| CHEMBL404646 | — | — | 1 | 5.68 |
| CHEMBL257517 | — | — | 1 | 5.50 |
| CHEMBL255389 | — | — | 1 | 5.21 |
| CHEMBL256468 | — | — | 1 | 4.74 |
| CHEMBL411118 | — | — | 1 | 4.27 |
| CHEMBL271240 | — | — | 1 | - |
| CHEMBL257891 | — | — | 1 | - |
| CHEMBL272962 | — | — | 1 | - |
| CHEMBL255388 | — | — | 1 | - |
| CHEMBL271739 | — | — | 1 | - |
| CHEMBL403847 | — | — | 1 | - |
| CHEMBL404451 | — | — | 1 | - |
| CHEMBL272963 | — | — | 1 | - |
| CHEMBL272774 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272336 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL429734 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL404646 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL257517 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL255389 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL256468 | — | IC50 | = | 18100.0 | nM | 4.74 |
| CHEMBL411118 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL271240 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL257891 | — | IC50 | - | — | - | |
| CHEMBL272962 | — | IC50 | - | — | - | |
| CHEMBL255388 | — | IC50 | - | — | - | |
| CHEMBL271739 | — | IC50 | - | — | - | |
| CHEMBL403847 | — | IC50 | - | — | - | |
| CHEMBL404451 | — | IC50 | - | — | - | |
| CHEMBL272963 | — | IC50 | - | — | - | |
| CHEMBL272774 | — | IC50 | - | — | - |