Assay Detail
Functional
CHEMBL902600
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay
32
Total Activities
32
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 | Intermediate |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 32 | 7.17 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL237305 | — | — | 1 | 8.00 |
| CHEMBL237085 | — | — | 1 | 7.80 |
| CHEMBL392717 | — | — | 1 | 7.66 |
| CHEMBL236664 | — | — | 1 | 7.62 |
| CHEMBL237307 | — | — | 1 | 7.62 |
| CHEMBL235143 | — | — | 1 | 7.62 |
| CHEMBL236876 | — | — | 1 | 7.62 |
| CHEMBL393939 | — | — | 1 | 7.60 |
| CHEMBL237277 | — | — | 1 | 7.60 |
| CHEMBL237306 | — | — | 1 | 7.58 |
| CHEMBL237086 | — | — | 1 | 7.55 |
| CHEMBL237520 | — | — | 1 | 7.55 |
| CHEMBL237485 | — | — | 1 | 7.50 |
| CHEMBL237518 | — | — | 1 | 7.43 |
| CHEMBL392058 | — | — | 1 | 7.38 |
| CHEMBL236877 | — | — | 1 | 7.37 |
| CHEMBL237519 | — | — | 1 | 7.37 |
| CHEMBL238152 | — | — | 1 | 7.36 |
| CHEMBL393938 | — | — | 1 | 7.31 |
| CHEMBL236875 | — | — | 1 | 7.24 |
| CHEMBL238357 | — | — | 1 | 6.94 |
| CHEMBL393940 | — | — | 1 | 6.90 |
| CHEMBL399417 | — | — | 1 | 6.87 |
| CHEMBL236218 | — | — | 1 | 6.80 |
| CHEMBL401236 | — | — | 1 | 6.79 |
| CHEMBL399217 | — | — | 1 | 6.62 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 6.51 |
| CHEMBL237730 | — | — | 1 | 6.46 |
| CHEMBL237484 | — | — | 1 | 6.46 |
| CHEMBL237710 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL237305 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL237085 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL392717 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL236664 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL237307 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL235143 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL236876 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL393939 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL237277 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL237306 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL237086 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL237520 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL237485 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL237518 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL392058 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL237519 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL236877 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL238152 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL393938 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL236875 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL238357 | — | EC50 | = | 116.0 | nM | 6.94 |
| CHEMBL393940 | — | EC50 | = | 125.0 | nM | 6.90 |
| CHEMBL399417 | — | EC50 | = | 135.0 | nM | 6.87 |
| CHEMBL236218 | — | EC50 | = | 158.0 | nM | 6.80 |
| CHEMBL401236 | — | EC50 | = | 163.0 | nM | 6.79 |
| CHEMBL399217 | — | EC50 | = | 238.0 | nM | 6.62 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 308.0 | nM | 6.51 |
| CHEMBL237730 | — | EC50 | = | 345.0 | nM | 6.46 |
| CHEMBL237484 | — | EC50 | = | 348.0 | nM | 6.46 |
| CHEMBL237710 | — | EC50 | = | 479.0 | nM | 6.32 |
| CHEMBL237084 | — | EC50 | = | 1058.0 | nM | 5.98 |
| CHEMBL392718 | — | EC50 | = | 1088.0 | nM | 5.96 |