Assay Detail
Binding
CHEMBL4232415
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Agonist activity at human PPARalpha after 22 to 24 hrs by luciferase reporter gene assay
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
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-guided evolution of a 2-phenyl-4-carboxyquinoline chemotype into PPARα selective agonists: New leads for oculovascular conditions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 5.50 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219586 | GW590735 | 2.0 | 1 | 7.92 |
| CHEMBL4237642 | — | — | 1 | 5.68 |
| CHEMBL4240338 | — | — | 1 | 5.29 |
| CHEMBL4237449 | — | — | 1 | 5.25 |
| CHEMBL4240680 | — | — | 1 | 4.60 |
| CHEMBL1565327 | — | — | 1 | 4.28 |
| CHEMBL38508 | — | — | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219586 | GW590735 | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4237642 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4240338 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4237449 | — | EC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4240680 | — | EC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL1565327 | — | EC50 | = | 52400.0 | nM | 4.28 |
| CHEMBL38508 | — | EC50 | - | — | - | |
| CHEMBL121 | ROSIGLITAZONE | EC50 | - | — | - |