Assay Detail
Binding
CHEMBL2379025
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at GAL4-fused PPARalpha (unknown origin) expressed in human HepG2 cells by transactivation assay
25
Total Activities
23
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
Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 5.92 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489074 | — | — | 2 | 7.96 |
| CHEMBL489075 | — | — | 1 | 6.82 |
| CHEMBL191275 | — | — | 1 | 6.72 |
| CHEMBL192518 | — | — | 1 | 6.30 |
| CHEMBL2375947 | — | — | 1 | 6.23 |
| CHEMBL472451 | — | — | 1 | 6.23 |
| CHEMBL2375948 | — | — | 1 | 6.20 |
| CHEMBL191060 | — | — | 1 | 6.15 |
| CHEMBL472245 | — | — | 2 | 6.06 |
| CHEMBL2375951 | — | — | 1 | 6.05 |
| CHEMBL472246 | — | — | 1 | 5.95 |
| CHEMBL426632 | — | — | 1 | 5.85 |
| CHEMBL2375946 | — | — | 1 | 5.62 |
| CHEMBL371320 | — | — | 1 | 5.60 |
| CHEMBL2375949 | — | — | 1 | 5.60 |
| CHEMBL2375950 | — | — | 1 | 5.52 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 5.46 |
| CHEMBL471011 | — | — | 1 | 5.44 |
| CHEMBL364748 | — | — | 1 | 5.41 |
| CHEMBL2375952 | — | — | 1 | 5.41 |
| CHEMBL366157 | — | — | 1 | 5.08 |
| CHEMBL190368 | — | — | 1 | 4.87 |
| CHEMBL370054 | — | — | 1 | 4.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489074 | — | EC50 | = | 10.96 | nM | 7.96 |
| CHEMBL489074 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL489075 | — | EC50 | = | 151.36 | nM | 6.82 |
| CHEMBL191275 | — | EC50 | = | 190.55 | nM | 6.72 |
| CHEMBL192518 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL2375947 | — | EC50 | = | 588.84 | nM | 6.23 |
| CHEMBL472451 | — | EC50 | = | 588.84 | nM | 6.23 |
| CHEMBL2375948 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL191060 | — | EC50 | = | 707.95 | nM | 6.15 |
| CHEMBL472245 | — | EC50 | = | 870.96 | nM | 6.06 |
| CHEMBL2375951 | — | EC50 | = | 891.25 | nM | 6.05 |
| CHEMBL472246 | — | EC50 | = | 1122.02 | nM | 5.95 |
| CHEMBL426632 | — | EC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL2375946 | — | EC50 | = | 2398.83 | nM | 5.62 |
| CHEMBL371320 | — | EC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL2375949 | — | EC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL2375950 | — | EC50 | = | 3019.95 | nM | 5.52 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 3460.0 | nM | 5.46 |
| CHEMBL471011 | — | EC50 | = | 3630.78 | nM | 5.44 |
| CHEMBL364748 | — | EC50 | = | 3890.45 | nM | 5.41 |
| CHEMBL472245 | — | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL2375952 | — | EC50 | = | 3890.45 | nM | 5.41 |
| CHEMBL366157 | — | EC50 | = | 8317.64 | nM | 5.08 |
| CHEMBL190368 | — | EC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL370054 | — | EC50 | = | 28840.32 | nM | 4.54 |