Assay Detail
Functional
CHEMBL911539
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CV-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 7.26 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL213315 | — | — | 1 | 8.40 |
| CHEMBL212911 | — | — | 1 | 8.40 |
| CHEMBL214921 | — | — | 1 | 8.30 |
| CHEMBL215582 | — | — | 1 | 8.22 |
| CHEMBL377660 | — | — | 1 | 8.10 |
| CHEMBL378068 | — | — | 1 | 8.05 |
| CHEMBL215127 | — | — | 1 | 7.34 |
| CHEMBL214026 | — | — | 1 | 7.28 |
| CHEMBL215701 | — | — | 1 | 6.99 |
| CHEMBL213314 | — | — | 1 | 6.95 |
| CHEMBL212591 | — | — | 1 | 6.64 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 6.51 |
| CHEMBL213361 | — | — | 1 | 6.45 |
| CHEMBL215245 | — | — | 1 | 6.40 |
| CHEMBL215126 | — | — | 1 | 6.17 |
| CHEMBL212023 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL213315 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL212911 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL214921 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL215582 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL377660 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL378068 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL215127 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL214026 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL215701 | — | EC50 | = | 102.0 | nM | 6.99 |
| CHEMBL213314 | — | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL212591 | — | EC50 | = | 228.0 | nM | 6.64 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 308.0 | nM | 6.51 |
| CHEMBL213361 | — | EC50 | = | 355.0 | nM | 6.45 |
| CHEMBL215245 | — | EC50 | = | 402.0 | nM | 6.40 |
| CHEMBL215126 | — | EC50 | = | 674.0 | nM | 6.17 |
| CHEMBL212023 | — | EC50 | = | 968.0 | nM | 6.01 |