Assay Detail
Binding
CHEMBL2154209
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Transactivation of PPARalpha expressed in HEK293A cells co-expressing GAL4 after 16 to 18 hrs by luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293-A |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Fibrate-derived N-(methylsulfonyl)amides with antagonistic properties on PPARα.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 5.38 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL21241 | GW7647 | — | 1 | 6.70 |
| CHEMBL2153833 | — | — | 1 | 5.80 |
| CHEMBL2153843 | — | — | 1 | 5.15 |
| CHEMBL2153840 | — | — | 1 | 4.97 |
| CHEMBL683 | CLOFIBRIC ACID | 2.0 | 1 | 4.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL21241 | GW7647 | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2153833 | — | EC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL2153843 | — | EC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL2153840 | — | EC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL683 | CLOFIBRIC ACID | EC50 | = | 55000.0 | nM | 4.26 |