Assay Detail
Binding
CHEMBL959182
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Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Selective, potent PPARgamma agonists with cyclopentenone core structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 6.24 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL278590 | GSK-9578 | — | 1 | 6.60 |
| CHEMBL520508 | — | — | 1 | 6.30 |
| CHEMBL485179 | — | — | 1 | 6.30 |
| CHEMBL485155 | — | — | 1 | 6.00 |
| CHEMBL472071 | — | — | 1 | 6.00 |
| CHEMBL519854 | — | — | 1 | - |
| CHEMBL511989 | — | — | 1 | - |
| CHEMBL38943 | GW501516 | 2.0 | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL278590 | GSK-9578 | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL520508 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL485179 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL485155 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL472071 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL519854 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL511989 | — | EC50 | - | — | - | |
| CHEMBL38943 | GW501516 | EC50 | > | 10000.0 | nM | - |
| CHEMBL121 | ROSIGLITAZONE | EC50 | > | 10000.0 | nM | - |