Assay Detail
Binding
CHEMBL911536
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid from human PPARalpha by SPA
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.46 | 6.05 |
| Activity | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214921 | — | — | 1 | 6.05 |
| CHEMBL213315 | — | — | 1 | 5.98 |
| CHEMBL215582 | — | — | 1 | 5.88 |
| CHEMBL213314 | — | — | 1 | 5.85 |
| CHEMBL215245 | — | — | 1 | 5.57 |
| CHEMBL377660 | — | — | 1 | 5.42 |
| CHEMBL212911 | — | — | 1 | 5.37 |
| CHEMBL213361 | — | — | 1 | 5.36 |
| CHEMBL214026 | — | — | 1 | 5.28 |
| CHEMBL215701 | — | — | 1 | 5.16 |
| CHEMBL378068 | — | — | 1 | 5.08 |
| CHEMBL215127 | — | — | 1 | 5.05 |
| CHEMBL212591 | — | — | 1 | 4.96 |
| CHEMBL215126 | — | — | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
| CHEMBL212023 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214921 | — | IC50 | = | 897.0 | nM | 6.05 |
| CHEMBL213315 | — | IC50 | = | 1037.0 | nM | 5.98 |
| CHEMBL215582 | — | IC50 | = | 1323.0 | nM | 5.88 |
| CHEMBL213314 | — | IC50 | = | 1398.0 | nM | 5.85 |
| CHEMBL215245 | — | IC50 | = | 2681.0 | nM | 5.57 |
| CHEMBL377660 | — | IC50 | = | 3758.0 | nM | 5.42 |
| CHEMBL212911 | — | IC50 | = | 4257.0 | nM | 5.37 |
| CHEMBL213361 | — | IC50 | = | 4386.0 | nM | 5.36 |
| CHEMBL214026 | — | IC50 | = | 5303.0 | nM | 5.28 |
| CHEMBL215701 | — | IC50 | = | 6932.0 | nM | 5.16 |
| CHEMBL378068 | — | IC50 | = | 8251.0 | nM | 5.08 |
| CHEMBL215127 | — | IC50 | = | 8919.0 | nM | 5.05 |
| CHEMBL212591 | — | IC50 | = | 10897.0 | nM | 4.96 |
| CHEMBL215126 | — | Activity | - | — | - | |
| CHEMBL121 | ROSIGLITAZONE | Activity | - | — | - | |
| CHEMBL212023 | — | Activity | - | — | - |