Assay Detail
Binding
CHEMBL5343452
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARgamma transfected in african green monkey COS7 cells assessed transactivation incubated for 16 hrs by luciferase assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of the First Subnanomolar PPARα/δ Dual Agonist for the Treatment of Cholestatic Liver Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 37 | 5.89 | 6.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 6.81 |
| CHEMBL5433003 | — | — | 1 | 6.56 |
| CHEMBL5400319 | — | — | 1 | 6.20 |
| CHEMBL5430327 | — | — | 1 | 6.20 |
| CHEMBL5416466 | — | — | 1 | 6.20 |
| CHEMBL5402111 | — | — | 1 | 6.18 |
| CHEMBL5437491 | — | — | 1 | 6.17 |
| CHEMBL5401474 | — | — | 1 | 6.13 |
| CHEMBL5433219 | — | — | 1 | 6.01 |
| CHEMBL5432415 | — | — | 1 | 6.00 |
| CHEMBL5395441 | — | — | 1 | 5.97 |
| CHEMBL5422924 | — | — | 1 | 5.93 |
| CHEMBL5440979 | — | — | 1 | 5.92 |
| CHEMBL5409347 | — | — | 1 | 5.86 |
| CHEMBL5419064 | — | — | 1 | 5.85 |
| CHEMBL5411276 | — | — | 1 | 5.83 |
| CHEMBL5405660 | — | — | 1 | 5.79 |
| CHEMBL5417169 | — | — | 1 | 5.78 |
| CHEMBL5406894 | — | — | 1 | 5.78 |
| CHEMBL5439116 | — | — | 1 | 5.77 |
| CHEMBL5408757 | — | — | 1 | 5.75 |
| CHEMBL5084377 | — | — | 1 | 5.73 |
| CHEMBL5408588 | — | — | 1 | 5.68 |
| CHEMBL5436973 | — | — | 1 | 5.57 |
| CHEMBL5406915 | — | — | 1 | 5.55 |
| CHEMBL5429423 | — | — | 1 | 5.47 |
| CHEMBL5403187 | — | — | 1 | 5.44 |
| CHEMBL5413215 | — | — | 1 | 5.39 |
| CHEMBL5440454 | — | — | 1 | 5.31 |
| CHEMBL5402424 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 154.5 | nM | 6.81 |
| CHEMBL5433003 | — | EC50 | = | 277.3 | nM | 6.56 |
| CHEMBL5400319 | — | EC50 | = | 629.6 | nM | 6.20 |
| CHEMBL5430327 | — | EC50 | = | 627.9 | nM | 6.20 |
| CHEMBL5416466 | — | EC50 | = | 628.8 | nM | 6.20 |
| CHEMBL5402111 | — | EC50 | = | 656.9 | nM | 6.18 |
| CHEMBL5437491 | — | EC50 | = | 681.3 | nM | 6.17 |
| CHEMBL5401474 | — | EC50 | = | 736.4 | nM | 6.13 |
| CHEMBL5433219 | — | EC50 | = | 971.4 | nM | 6.01 |
| CHEMBL5432415 | — | EC50 | = | 996.3 | nM | 6.00 |
| CHEMBL5395441 | — | EC50 | = | 1070.7 | nM | 5.97 |
| CHEMBL5422924 | — | EC50 | = | 1173.7 | nM | 5.93 |
| CHEMBL5440979 | — | EC50 | = | 1204.5 | nM | 5.92 |
| CHEMBL5409347 | — | EC50 | = | 1387.9 | nM | 5.86 |
| CHEMBL5419064 | — | EC50 | = | 1416.4 | nM | 5.85 |
| CHEMBL5411276 | — | EC50 | = | 1487.8 | nM | 5.83 |
| CHEMBL5405660 | — | EC50 | = | 1623.0 | nM | 5.79 |
| CHEMBL5406894 | — | EC50 | = | 1646.0 | nM | 5.78 |
| CHEMBL5417169 | — | EC50 | = | 1656.1 | nM | 5.78 |
| CHEMBL5439116 | — | EC50 | = | 1682.0 | nM | 5.77 |
| CHEMBL5408757 | — | EC50 | = | 1796.0 | nM | 5.75 |
| CHEMBL5084377 | — | EC50 | = | 1868.0 | nM | 5.73 |
| CHEMBL5408588 | — | EC50 | = | 2105.0 | nM | 5.68 |
| CHEMBL5436973 | — | EC50 | = | 2720.1 | nM | 5.57 |
| CHEMBL5406915 | — | EC50 | = | 2786.0 | nM | 5.55 |
| CHEMBL5429423 | — | EC50 | = | 3372.5 | nM | 5.47 |
| CHEMBL5403187 | — | EC50 | = | 3637.8 | nM | 5.44 |
| CHEMBL5413215 | — | EC50 | = | 4060.0 | nM | 5.39 |
| CHEMBL5440454 | — | EC50 | = | 4867.5 | nM | 5.31 |
| CHEMBL5402424 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL5405631 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL5407426 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL5411943 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL5430889 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL5426514 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL5429581 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL5429348 | — | EC50 | > | 5000.0 | nM | - |