Assay Detail
Binding
CHEMBL3371803
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Agonist activity at GAL4-tagged PPARalpha ligand-binding domain (unknown origin) expressed in HEK293T cells incubated for 16 to 19 hrs by beta-lactamase 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 | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Biological evaluation and structural insights for design of subtype-selective peroxisome proliferator activated receptor-α (PPAR-α) agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 8.52 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354987 | — | — | 1 | 9.80 |
| CHEMBL247951 | PEMAFIBRATE | 4.0 | 1 | 9.00 |
| CHEMBL1494365 | — | — | 1 | 8.96 |
| CHEMBL3354989 | — | — | 1 | 8.40 |
| CHEMBL1934476 | — | — | 1 | 8.30 |
| CHEMBL435523 | — | — | 1 | 8.30 |
| CHEMBL1934484 | — | — | 1 | 8.22 |
| CHEMBL3354988 | — | — | 1 | 7.92 |
| CHEMBL21241 | GW7647 | — | 1 | 7.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354987 | — | EC50 | = | 0.16 | nM | 9.80 |
| CHEMBL247951 | PEMAFIBRATE | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1494365 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3354989 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1934476 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL435523 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1934484 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3354988 | — | EC50 | = | 12.1 | nM | 7.92 |
| CHEMBL21241 | GW7647 | EC50 | = | 15.4 | nM | 7.81 |