Assay Detail
Binding
CHEMBL1960409
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Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors α/γ dual agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 5.30 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL192518 | — | — | 1 | 6.30 |
| CHEMBL1956364 | — | — | 1 | 6.00 |
| CHEMBL1956363 | — | — | 1 | 5.85 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 5.80 |
| CHEMBL1956362 | — | — | 1 | 5.66 |
| CHEMBL1956366 | — | — | 1 | 5.60 |
| CHEMBL1956368 | — | — | 1 | 5.35 |
| CHEMBL364748 | — | — | 1 | 5.31 |
| CHEMBL1956349 | — | — | 1 | 5.29 |
| CHEMBL1956350 | — | — | 1 | 5.27 |
| CHEMBL1956365 | — | — | 1 | 5.19 |
| CHEMBL1956367 | — | — | 1 | 5.18 |
| CHEMBL1956360 | — | — | 1 | 5.01 |
| CHEMBL1956371 | — | — | 1 | 4.99 |
| CHEMBL1956370 | — | — | 1 | 4.72 |
| CHEMBL1956358 | — | — | 1 | 4.68 |
| CHEMBL1956359 | — | — | 1 | 4.65 |
| CHEMBL1956357 | — | — | 1 | 4.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL192518 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1956364 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1956363 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1956362 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1956366 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1956368 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL364748 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL1956349 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL1956350 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL1956365 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL1956367 | — | EC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL1956360 | — | EC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL1956371 | — | EC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL1956370 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL1956358 | — | EC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL1956359 | — | EC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL1956357 | — | EC50 | = | 24800.0 | nM | 4.61 |