Assay Detail
Binding
CHEMBL4812201
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human Gal4 fused PPARalpha LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 5.71 | 6.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4872922 | — | — | 1 | 6.58 |
| CHEMBL3707395 | ELAFIBRANOR | 4.0 | 1 | 6.12 |
| CHEMBL4853743 | — | — | 1 | 6.10 |
| CHEMBL4856271 | — | — | 1 | 5.99 |
| CHEMBL4855296 | — | — | 1 | 5.78 |
| CHEMBL4873389 | — | — | 1 | 5.76 |
| CHEMBL4875481 | — | — | 1 | 5.73 |
| CHEMBL21241 | GW7647 | — | 1 | 5.68 |
| CHEMBL4861167 | — | — | 1 | 5.55 |
| CHEMBL4872726 | — | — | 1 | 5.51 |
| CHEMBL4869134 | — | — | 1 | 5.48 |
| CHEMBL4869342 | — | — | 1 | 5.38 |
| CHEMBL4848052 | — | — | 1 | 5.35 |
| CHEMBL4853930 | — | — | 1 | 5.34 |
| CHEMBL4852230 | — | — | 1 | 5.28 |
| CHEMBL4847495 | — | — | 1 | - |
| CHEMBL4859752 | — | — | 1 | - |
| CHEMBL4860504 | — | — | 1 | - |
| CHEMBL38943 | GW501516 | 2.0 | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4872922 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3707395 | ELAFIBRANOR | EC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4853743 | — | EC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4856271 | — | EC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL4855296 | — | EC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL4873389 | — | EC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL4875481 | — | EC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL21241 | GW7647 | EC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL4861167 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4872726 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4869134 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4869342 | — | EC50 | = | 4190.0 | nM | 5.38 |
| CHEMBL4848052 | — | EC50 | = | 4440.0 | nM | 5.35 |
| CHEMBL4853930 | — | EC50 | = | 4560.0 | nM | 5.34 |
| CHEMBL4852230 | — | EC50 | = | 5210.0 | nM | 5.28 |
| CHEMBL4847495 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4859752 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4860504 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL38943 | GW501516 | EC50 | - | — | - | |
| CHEMBL121 | ROSIGLITAZONE | EC50 | - | — | - |