Assay Detail
Binding
CHEMBL911538
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]2-methyl-2-(4-{3-[propyl-(5-pyridin-2-yl-thiophene-2-sulfonyl)-amino]-propyl}-phenoxy)-propionic acid from human PPARgamma by SPA
16
Total Activities
16
Compounds Tested
1
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 gamma (CHEMBL235) ↗| 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 | 16 | 7.56 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL212911 | — | — | 1 | 8.30 |
| CHEMBL213315 | — | — | 1 | 8.22 |
| CHEMBL214921 | — | — | 1 | 8.22 |
| CHEMBL377660 | — | — | 1 | 8.22 |
| CHEMBL215582 | — | — | 1 | 8.22 |
| CHEMBL378068 | — | — | 1 | 7.92 |
| CHEMBL214026 | — | — | 1 | 7.82 |
| CHEMBL215127 | — | — | 1 | 7.75 |
| CHEMBL215701 | — | — | 1 | 7.72 |
| CHEMBL213314 | — | — | 1 | 7.42 |
| CHEMBL212591 | — | — | 1 | 7.23 |
| CHEMBL213361 | — | — | 1 | 7.21 |
| CHEMBL215245 | — | — | 1 | 7.20 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.17 |
| CHEMBL212023 | — | — | 1 | 6.38 |
| CHEMBL215126 | — | — | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL212911 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL213315 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL214921 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL377660 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL215582 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL378068 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL214026 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL215127 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL215701 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL213314 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL212591 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL213361 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL215245 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL121 | ROSIGLITAZONE | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL212023 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL215126 | — | IC50 | = | 1130.0 | nM | 5.95 |