Assay Detail
Binding
CHEMBL911540
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 PPARdelta 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 delta (CHEMBL3979) ↗| 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 | 15 | 8.19 | 8.52 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL212911 | — | — | 1 | 8.52 |
| CHEMBL215701 | — | — | 1 | 8.40 |
| CHEMBL215245 | — | — | 1 | 8.40 |
| CHEMBL214026 | — | — | 1 | 8.40 |
| CHEMBL377660 | — | — | 1 | 8.40 |
| CHEMBL213361 | — | — | 1 | 8.30 |
| CHEMBL213315 | — | — | 1 | 8.30 |
| CHEMBL214921 | — | — | 1 | 8.30 |
| CHEMBL215582 | — | — | 1 | 8.30 |
| CHEMBL213314 | — | — | 1 | 8.22 |
| CHEMBL215127 | — | — | 1 | 8.22 |
| CHEMBL378068 | — | — | 1 | 8.15 |
| CHEMBL212591 | — | — | 1 | 8.10 |
| CHEMBL212023 | — | — | 1 | 8.05 |
| CHEMBL215126 | — | — | 1 | 6.74 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL212911 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL215701 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL215245 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL214026 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL377660 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL213361 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL213315 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL214921 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL215582 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL213314 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL215127 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL378068 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL212591 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL212023 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL215126 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL121 | ROSIGLITAZONE | Activity | - | — | - |