Assay Detail
Functional
CHEMBL927779
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha assessed as receptor activation by cell based assay
45
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 6.93 | 9.52 |
| Activity | 21 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL253310 | — | — | 2 | 9.52 |
| CHEMBL427890 | — | — | 2 | 8.52 |
| CHEMBL219586 | GW590735 | 2.0 | 2 | 8.40 |
| CHEMBL252675 | — | — | 2 | 8.30 |
| CHEMBL253486 | — | — | 2 | 7.70 |
| CHEMBL254946 | — | — | 2 | 7.30 |
| CHEMBL254744 | — | — | 2 | 7.22 |
| CHEMBL403637 | — | — | 2 | 7.22 |
| CHEMBL403909 | — | — | 2 | 7.16 |
| CHEMBL253520 | — | — | 2 | 7.10 |
| CHEMBL253923 | — | — | 2 | 7.10 |
| CHEMBL438346 | — | — | 2 | 7.10 |
| CHEMBL253109 | — | — | 2 | 6.50 |
| CHEMBL401562 | — | — | 2 | 6.44 |
| CHEMBL402100 | — | — | 2 | 6.35 |
| CHEMBL401560 | — | — | 2 | 6.00 |
| CHEMBL404467 | — | — | 2 | 6.00 |
| CHEMBL253924 | — | — | 2 | 5.55 |
| CHEMBL253490 | — | — | 2 | 5.52 |
| CHEMBL253522 | — | — | 2 | 5.30 |
| CHEMBL401580 | — | — | 2 | 5.22 |
| CHEMBL254540 | — | — | 1 | - |
| CHEMBL254742 | — | — | 1 | - |
| CHEMBL254743 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL253310 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL427890 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL219586 | GW590735 | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL252675 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL253486 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL254946 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL403637 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL254744 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL403909 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL438346 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL253520 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL253923 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL253109 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL401562 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL402100 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL401560 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL404467 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL253924 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL253490 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL253522 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL401580 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL427890 | — | Activity | = | 72.0 | % | - |
| CHEMBL402100 | — | Activity | = | 79.0 | % | - |
| CHEMBL253520 | — | Activity | = | 114.0 | % | - |
| CHEMBL253310 | — | Activity | = | 115.0 | % | - |
| CHEMBL403637 | — | Activity | = | 121.0 | % | - |
| CHEMBL254744 | — | Activity | = | 100.0 | % | - |
| CHEMBL254946 | — | Activity | = | 87.0 | % | - |
| CHEMBL253109 | — | Activity | = | 125.0 | % | - |
| CHEMBL254540 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL254742 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL254743 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL404467 | — | Activity | = | 1.0 | % | - |
| CHEMBL403909 | — | Activity | = | 134.0 | % | - |
| CHEMBL253486 | — | Activity | = | 133.0 | % | - |
| CHEMBL253923 | — | Activity | = | 120.0 | % | - |
| CHEMBL252675 | — | Activity | = | 138.0 | % | - |
| CHEMBL401560 | — | Activity | = | 133.0 | % | - |
| CHEMBL401562 | — | Activity | = | 102.0 | % | - |
| CHEMBL253490 | — | Activity | = | 135.0 | % | - |
| CHEMBL253924 | — | Activity | = | 97.0 | % | - |
| CHEMBL253522 | — | Activity | = | 107.0 | % | - |
| CHEMBL438346 | — | Activity | = | 94.0 | % | - |
| CHEMBL401580 | — | Activity | = | 133.0 | % | - |
| CHEMBL219586 | GW590735 | Activity | = | 95.0 | % | - |