Assay Detail
Functional
CHEMBL700787
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Agonist activity for Human PPAR alpha receptor in transcriptional activation assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The PPARs: from orphan receptors to drug discovery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 5.81 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL278994 | L-796449 | — | 1 | 8.39 |
| CHEMBL278590 | GSK-9578 | — | 1 | 7.30 |
| CHEMBL435278 | — | — | 1 | 6.77 |
| CHEMBL107367 | FARGLITAZAR | 2.0 | 1 | 6.35 |
| CHEMBL306229 | — | — | 1 | 6.13 |
| CHEMBL24458 | — | — | 1 | 6.07 |
| CHEMBL293526 | REGLITAZAR | 2.0 | 1 | 5.72 |
| CHEMBL106666 | GW7845 | — | 1 | 5.46 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 5.30 |
| CHEMBL153057 | — | — | 1 | 5.00 |
| CHEMBL672 | FENOFIBRATE | 4.0 | 1 | 4.52 |
| CHEMBL264374 | BEZAFIBRATE | 3.0 | 1 | 4.30 |
| CHEMBL565 | CLOFIBRATE | 4.0 | 1 | 4.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL278994 | L-796449 | EC50 | = | 4.1 | nM | 8.39 |
| CHEMBL278590 | GSK-9578 | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL435278 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL107367 | FARGLITAZAR | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL306229 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL24458 | — | EC50 | = | 850.0 | nM | 6.07 |
| CHEMBL293526 | REGLITAZAR | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL106666 | GW7845 | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL153057 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL672 | FENOFIBRATE | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL264374 | BEZAFIBRATE | EC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL565 | CLOFIBRATE | EC50 | = | 55000.0 | nM | 4.26 |