Assay Detail
Binding
CHEMBL885568
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]2-methyl-2-(4-{3-[porpyl-(5-pyridin-2yl-thiophene-2-sulfonyl)-amino]-propyl}-phenoxy)-propionic acid from human PPARgamma
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of a novel class of dual PPARgamma/delta agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.81 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL212911 | — | — | 1 | 8.30 |
| CHEMBL238970 | — | — | 1 | 7.80 |
| CHEMBL241478 | — | — | 1 | 7.70 |
| CHEMBL241479 | — | — | 1 | 7.46 |
| CHEMBL241471 | — | — | 1 | 7.34 |
| CHEMBL241472 | — | — | 1 | 7.22 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.17 |
| CHEMBL241299 | — | — | 1 | 7.06 |
| CHEMBL393926 | — | — | 1 | 6.67 |
| CHEMBL241286 | — | — | 1 | 6.46 |
| CHEMBL391470 | — | — | 1 | 6.32 |
| CHEMBL391283 | — | — | 1 | 6.28 |
| CHEMBL392063 | — | — | 1 | 6.25 |
| CHEMBL391264 | — | — | 1 | 6.03 |
| CHEMBL241298 | — | — | 1 | 6.01 |
| CHEMBL241078 | — | — | 1 | 5.96 |
| CHEMBL400024 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL212911 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL238970 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL241478 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL241479 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL241471 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL241472 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL121 | ROSIGLITAZONE | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL241299 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL393926 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL241286 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL391470 | — | IC50 | = | 483.0 | nM | 6.32 |
| CHEMBL391283 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL392063 | — | IC50 | = | 568.0 | nM | 6.25 |
| CHEMBL391264 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL241298 | — | IC50 | = | 979.0 | nM | 6.01 |
| CHEMBL241078 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL400024 | — | IC50 | = | 1530.0 | nM | 5.82 |