Assay Detail
Binding
CHEMBL4832965
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Agonist activity at human PPARgamma transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 6.12 | 6.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 6.81 |
| CHEMBL4853605 | — | — | 1 | 6.62 |
| CHEMBL4863779 | — | — | 1 | 6.54 |
| CHEMBL4878808 | — | — | 1 | 6.47 |
| CHEMBL4861711 | — | — | 1 | 6.38 |
| CHEMBL4854359 | — | — | 1 | 6.30 |
| CHEMBL4856081 | — | — | 1 | 6.20 |
| CHEMBL4850352 | — | — | 1 | 6.12 |
| CHEMBL4859884 | — | — | 1 | 5.97 |
| CHEMBL4852747 | — | — | 1 | 5.88 |
| CHEMBL4865961 | — | — | 1 | 5.80 |
| CHEMBL4876536 | — | — | 1 | 5.76 |
| CHEMBL3707395 | ELAFIBRANOR | 4.0 | 1 | 5.40 |
| CHEMBL4858856 | — | — | 1 | 5.40 |
| CHEMBL21241 | GW7647 | — | 1 | - |
| CHEMBL38508 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4853605 | — | EC50 | = | 237.0 | nM | 6.62 |
| CHEMBL4863779 | — | EC50 | = | 285.0 | nM | 6.54 |
| CHEMBL4878808 | — | EC50 | = | 335.0 | nM | 6.47 |
| CHEMBL4861711 | — | EC50 | = | 412.0 | nM | 6.38 |
| CHEMBL4854359 | — | EC50 | = | 503.0 | nM | 6.30 |
| CHEMBL4856081 | — | EC50 | = | 634.0 | nM | 6.20 |
| CHEMBL4850352 | — | EC50 | = | 764.0 | nM | 6.12 |
| CHEMBL4859884 | — | EC50 | = | 1063.0 | nM | 5.97 |
| CHEMBL4852747 | — | EC50 | = | 1323.0 | nM | 5.88 |
| CHEMBL4865961 | — | EC50 | = | 1579.0 | nM | 5.80 |
| CHEMBL4876536 | — | EC50 | = | 1745.0 | nM | 5.76 |
| CHEMBL3707395 | ELAFIBRANOR | EC50 | = | 3962.0 | nM | 5.40 |
| CHEMBL4858856 | — | EC50 | = | 3962.0 | nM | 5.40 |
| CHEMBL21241 | GW7647 | EC50 | - | — | - | |
| CHEMBL38508 | — | EC50 | - | — | - |