Assay Detail
Functional
CHEMBL896469
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARdelta in HepG2 cells by GAL4-luciferase reporter gene assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Peroxisome proliferator-activated receptor delta (CHEMBL3979) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and SAR of selective benzothiophene, benzofuran, and indole-based peroxisome proliferator-activated receptor delta agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 6.34 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38943 | GW501516 | 2.0 | 1 | 8.40 |
| CHEMBL231690 | — | — | 1 | 8.40 |
| CHEMBL233976 | — | — | 1 | 7.83 |
| CHEMBL234588 | — | — | 1 | 6.78 |
| CHEMBL234587 | — | — | 1 | 6.76 |
| CHEMBL233978 | — | — | 1 | 6.65 |
| CHEMBL234801 | — | — | 1 | 6.65 |
| CHEMBL234169 | — | — | 1 | 6.64 |
| CHEMBL265868 | — | — | 1 | 6.61 |
| CHEMBL231689 | — | — | 1 | 6.59 |
| CHEMBL391457 | — | — | 1 | 6.52 |
| CHEMBL391068 | — | — | 1 | 6.49 |
| CHEMBL234382 | — | — | 1 | 6.25 |
| CHEMBL391085 | — | — | 1 | 6.20 |
| CHEMBL234170 | — | — | 1 | 6.18 |
| CHEMBL234589 | — | — | 1 | 5.97 |
| CHEMBL393767 | — | — | 1 | 5.86 |
| CHEMBL234799 | — | — | 1 | 5.83 |
| CHEMBL234168 | — | — | 1 | 5.79 |
| CHEMBL234383 | — | — | 1 | 5.65 |
| CHEMBL393765 | — | — | 1 | 5.63 |
| CHEMBL393373 | — | — | 1 | 5.55 |
| CHEMBL231688 | — | — | 1 | 5.51 |
| CHEMBL393766 | — | — | 1 | 5.51 |
| CHEMBL234800 | — | — | 1 | 5.46 |
| CHEMBL234381 | — | — | 1 | 5.20 |
| CHEMBL391084 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38943 | GW501516 | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL231690 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL233976 | — | EC50 | = | 14.7 | nM | 7.83 |
| CHEMBL234588 | — | EC50 | = | 166.0 | nM | 6.78 |
| CHEMBL234587 | — | EC50 | = | 172.0 | nM | 6.76 |
| CHEMBL233978 | — | EC50 | = | 226.0 | nM | 6.65 |
| CHEMBL234801 | — | EC50 | = | 223.0 | nM | 6.65 |
| CHEMBL234169 | — | EC50 | = | 227.0 | nM | 6.64 |
| CHEMBL265868 | — | EC50 | = | 243.0 | nM | 6.61 |
| CHEMBL231689 | — | EC50 | = | 254.0 | nM | 6.59 |
| CHEMBL391457 | — | EC50 | = | 305.0 | nM | 6.52 |
| CHEMBL391068 | — | EC50 | = | 323.0 | nM | 6.49 |
| CHEMBL234382 | — | EC50 | = | 561.0 | nM | 6.25 |
| CHEMBL391085 | — | EC50 | = | 638.0 | nM | 6.20 |
| CHEMBL234170 | — | EC50 | = | 656.0 | nM | 6.18 |
| CHEMBL234589 | — | EC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL393767 | — | EC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL234799 | — | EC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL234168 | — | EC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL234383 | — | EC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL393765 | — | EC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL393373 | — | EC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL231688 | — | EC50 | = | 3080.0 | nM | 5.51 |
| CHEMBL393766 | — | EC50 | = | 3120.0 | nM | 5.51 |
| CHEMBL234800 | — | EC50 | = | 3440.0 | nM | 5.46 |
| CHEMBL234381 | — | EC50 | = | 6360.0 | nM | 5.20 |
| CHEMBL391084 | — | EC50 | - | — | - |