Assay Detail
Functional
CHEMBL928500
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha at 100 uM by GAL4 transactivation assay relative to WY 14,643
11
Total Activities
10
Compounds Tested
1
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 | 11 | 7.58 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 8.40 |
| CHEMBL253416 | — | — | 2 | 8.11 |
| CHEMBL398677 | — | — | 1 | 7.96 |
| CHEMBL254054 | — | — | 1 | 7.85 |
| CHEMBL399629 | — | — | 1 | 7.72 |
| CHEMBL282686 | TESAGLITAZAR | 3.0 | 1 | 7.43 |
| CHEMBL253851 | — | — | 1 | 7.32 |
| CHEMBL253417 | — | — | 1 | 7.19 |
| CHEMBL252995 | — | — | 1 | 6.82 |
| CHEMBL252996 | — | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL253416 | — | EC50 | = | 7.85 | nM | 8.11 |
| CHEMBL398677 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL253416 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL254054 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL399629 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL282686 | TESAGLITAZAR | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL253851 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL253417 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL252995 | — | EC50 | = | 152.0 | nM | 6.82 |
| CHEMBL252996 | — | EC50 | = | 195.0 | nM | 6.71 |