Assay Detail
Binding
CHEMBL902596
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
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 alpha (CHEMBL239) ↗| 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 | 5.71 | 6.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL237307 | — | — | 1 | 6.73 |
| CHEMBL237518 | — | — | 1 | 6.50 |
| CHEMBL237519 | — | — | 1 | 6.48 |
| CHEMBL237520 | — | — | 1 | 6.42 |
| CHEMBL237085 | — | — | 1 | 6.33 |
| CHEMBL236876 | — | — | 1 | 6.19 |
| CHEMBL392717 | — | — | 1 | 6.14 |
| CHEMBL236875 | — | — | 1 | 5.95 |
| CHEMBL237484 | — | — | 1 | 5.95 |
| CHEMBL393938 | — | — | 1 | 5.91 |
| CHEMBL237710 | — | — | 1 | 5.83 |
| CHEMBL236877 | — | — | 1 | 5.80 |
| CHEMBL393939 | — | — | 1 | 5.76 |
| CHEMBL236664 | — | — | 1 | 5.75 |
| CHEMBL235143 | — | — | 1 | 5.68 |
| CHEMBL392058 | — | — | 1 | 5.46 |
| CHEMBL237306 | — | — | 1 | 5.38 |
| CHEMBL399217 | — | — | 1 | 5.36 |
| CHEMBL237305 | — | — | 1 | 5.31 |
| CHEMBL236218 | — | — | 1 | 5.31 |
| CHEMBL237086 | — | — | 1 | 5.14 |
| CHEMBL237485 | — | — | 1 | 5.13 |
| CHEMBL401236 | — | — | 1 | 5.03 |
| CHEMBL237277 | — | — | 1 | 5.00 |
| CHEMBL237084 | — | — | 1 | 4.99 |
| CHEMBL238357 | — | — | 1 | 4.99 |
| CHEMBL393940 | — | — | 1 | - |
| CHEMBL237730 | — | — | 1 | - |
| CHEMBL399417 | — | — | 1 | - |
| CHEMBL238152 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL237307 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL237518 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL237519 | — | IC50 | = | 331.0 | nM | 6.48 |
| CHEMBL237520 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL237085 | — | IC50 | = | 463.0 | nM | 6.33 |
| CHEMBL236876 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL392717 | — | IC50 | = | 728.0 | nM | 6.14 |
| CHEMBL236875 | — | IC50 | = | 1127.0 | nM | 5.95 |
| CHEMBL237484 | — | IC50 | = | 1132.0 | nM | 5.95 |
| CHEMBL393938 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL237710 | — | IC50 | = | 1483.0 | nM | 5.83 |
| CHEMBL236877 | — | IC50 | = | 1594.0 | nM | 5.80 |
| CHEMBL393939 | — | IC50 | = | 1749.0 | nM | 5.76 |
| CHEMBL236664 | — | IC50 | = | 1763.0 | nM | 5.75 |
| CHEMBL235143 | — | IC50 | = | 2104.0 | nM | 5.68 |
| CHEMBL392058 | — | IC50 | = | 3487.0 | nM | 5.46 |
| CHEMBL237306 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL399217 | — | IC50 | = | 4352.0 | nM | 5.36 |
| CHEMBL237305 | — | IC50 | = | 4850.0 | nM | 5.31 |
| CHEMBL236218 | — | IC50 | = | 4865.0 | nM | 5.31 |
| CHEMBL237086 | — | IC50 | = | 7154.0 | nM | 5.14 |
| CHEMBL237485 | — | IC50 | = | 7457.0 | nM | 5.13 |
| CHEMBL401236 | — | IC50 | = | 9336.0 | nM | 5.03 |
| CHEMBL237277 | — | IC50 | = | 10034.0 | nM | 5.00 |
| CHEMBL237084 | — | IC50 | = | 10313.0 | nM | 4.99 |
| CHEMBL238357 | — | IC50 | = | 10257.0 | nM | 4.99 |
| CHEMBL393940 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL237730 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL399417 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL238152 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL121 | ROSIGLITAZONE | IC50 | > | 10000.0 | nM | - |
| CHEMBL392718 | — | IC50 | > | 10000.0 | nM | - |