Assay Detail
Binding
CHEMBL4832967
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARdelta 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 delta (CHEMBL3979) ↗| 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 | 6.15 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38508 | — | — | 1 | 7.75 |
| CHEMBL3707395 | ELAFIBRANOR | 4.0 | 1 | 6.60 |
| CHEMBL4853605 | — | — | 1 | 6.47 |
| CHEMBL4863779 | — | — | 1 | 6.43 |
| CHEMBL4878808 | — | — | 1 | 6.38 |
| CHEMBL4861711 | — | — | 1 | 6.27 |
| CHEMBL4854359 | — | — | 1 | 6.19 |
| CHEMBL4856081 | — | — | 1 | 6.04 |
| CHEMBL4850352 | — | — | 1 | 6.02 |
| CHEMBL4859884 | — | — | 1 | 5.82 |
| CHEMBL4852747 | — | — | 1 | 5.66 |
| CHEMBL4876536 | — | — | 1 | 5.57 |
| CHEMBL4865961 | — | — | 1 | 5.49 |
| CHEMBL4858856 | — | — | 1 | 5.45 |
| CHEMBL21241 | GW7647 | — | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38508 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3707395 | ELAFIBRANOR | EC50 | = | 249.0 | nM | 6.60 |
| CHEMBL4853605 | — | EC50 | = | 341.0 | nM | 6.47 |
| CHEMBL4863779 | — | EC50 | = | 372.0 | nM | 6.43 |
| CHEMBL4878808 | — | EC50 | = | 413.0 | nM | 6.38 |
| CHEMBL4861711 | — | EC50 | = | 539.0 | nM | 6.27 |
| CHEMBL4854359 | — | EC50 | = | 652.0 | nM | 6.19 |
| CHEMBL4856081 | — | EC50 | = | 913.0 | nM | 6.04 |
| CHEMBL4850352 | — | EC50 | = | 958.0 | nM | 6.02 |
| CHEMBL4859884 | — | EC50 | = | 1523.0 | nM | 5.82 |
| CHEMBL4852747 | — | EC50 | = | 2203.0 | nM | 5.66 |
| CHEMBL4876536 | — | EC50 | = | 2679.0 | nM | 5.57 |
| CHEMBL4865961 | — | EC50 | = | 3217.0 | nM | 5.49 |
| CHEMBL4858856 | — | EC50 | = | 3512.0 | nM | 5.45 |
| CHEMBL21241 | GW7647 | EC50 | - | — | - | |
| CHEMBL121 | ROSIGLITAZONE | EC50 | - | — | - |