Assay Detail
Binding
CHEMBL1930422
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 6.51 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1927476 | — | — | 1 | 7.50 |
| CHEMBL1927473 | — | — | 1 | 6.25 |
| CHEMBL1927474 | — | — | 1 | 6.15 |
| CHEMBL1927475 | — | — | 1 | 6.13 |
| CHEMBL38943 | GW501516 | 2.0 | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1927476 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1927473 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1927474 | — | EC50 | = | 710.0 | nM | 6.15 |
| CHEMBL1927475 | — | EC50 | = | 735.0 | nM | 6.13 |
| CHEMBL38943 | GW501516 | EC50 | > | 1000.0 | nM | - |
| CHEMBL121 | ROSIGLITAZONE | EC50 | > | 1000.0 | nM | - |