Assay Detail
Functional
CHEMBL928498
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha by GAL4 transactivation assay
11
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 6.92 | 7.92 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL398677 | — | — | 1 | 7.92 |
| CHEMBL253416 | — | — | 2 | 7.54 |
| CHEMBL254054 | — | — | 1 | 7.54 |
| CHEMBL399629 | — | — | 1 | 7.52 |
| CHEMBL253851 | — | — | 1 | 6.72 |
| CHEMBL253417 | — | — | 1 | 6.71 |
| CHEMBL282686 | TESAGLITAZAR | 3.0 | 1 | 6.38 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 5.00 |
| CHEMBL252995 | — | — | 1 | - |
| CHEMBL252996 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL398677 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL253416 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL254054 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL399629 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL253416 | — | EC50 | = | 114.0 | nM | 6.94 |
| CHEMBL253851 | — | EC50 | = | 189.0 | nM | 6.72 |
| CHEMBL253417 | — | EC50 | = | 194.0 | nM | 6.71 |
| CHEMBL282686 | TESAGLITAZAR | EC50 | = | 414.0 | nM | 6.38 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL252995 | — | Activity | - | — | - | |
| CHEMBL252996 | — | Activity | - | — | - |