Assay Detail
Binding
CHEMBL902597
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
32
Total Activities
32
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 novel and potent amide linked PPARgamma/delta dual agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.60 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL237307 | — | — | 1 | 8.30 |
| CHEMBL237085 | — | — | 1 | 8.15 |
| CHEMBL393939 | — | — | 1 | 8.15 |
| CHEMBL237485 | — | — | 1 | 8.10 |
| CHEMBL237306 | — | — | 1 | 8.10 |
| CHEMBL237520 | — | — | 1 | 8.10 |
| CHEMBL392717 | — | — | 1 | 8.10 |
| CHEMBL236664 | — | — | 1 | 8.05 |
| CHEMBL237086 | — | — | 1 | 8.05 |
| CHEMBL236875 | — | — | 1 | 8.00 |
| CHEMBL236876 | — | — | 1 | 7.92 |
| CHEMBL236877 | — | — | 1 | 7.92 |
| CHEMBL237518 | — | — | 1 | 7.92 |
| CHEMBL237277 | — | — | 1 | 7.89 |
| CHEMBL393938 | — | — | 1 | 7.82 |
| CHEMBL237519 | — | — | 1 | 7.77 |
| CHEMBL392058 | — | — | 1 | 7.75 |
| CHEMBL393940 | — | — | 1 | 7.70 |
| CHEMBL235143 | — | — | 1 | 7.57 |
| CHEMBL238152 | — | — | 1 | 7.46 |
| CHEMBL236218 | — | — | 1 | 7.43 |
| CHEMBL238357 | — | — | 1 | 7.41 |
| CHEMBL237305 | — | — | 1 | 7.33 |
| CHEMBL401236 | — | — | 1 | 7.30 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.17 |
| CHEMBL399217 | — | — | 1 | 7.02 |
| CHEMBL399417 | — | — | 1 | 7.01 |
| CHEMBL237710 | — | — | 1 | 6.94 |
| CHEMBL237730 | — | — | 1 | 6.90 |
| CHEMBL237084 | — | — | 1 | 6.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL237307 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL237085 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL393939 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL237485 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL237306 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL237520 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL392717 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL236664 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL237086 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL236875 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL236876 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL236877 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL237518 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL237277 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL393938 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL237519 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL392058 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL393940 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL235143 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL238152 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL236218 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL238357 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL237305 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL401236 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL121 | ROSIGLITAZONE | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL399217 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL399417 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL237710 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL237730 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL237084 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL237484 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL392718 | — | IC50 | = | 258.0 | nM | 6.59 |