Assay Detail
Functional
CHEMBL888368
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human recombinant PPARalpha by GAL4 transactivation assay
36
Total Activities
36
Compounds Tested
1
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 and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 36 | 7.81 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL245866 | — | — | 1 | 9.00 |
| CHEMBL246281 | — | — | 1 | 9.00 |
| CHEMBL427701 | — | — | 1 | 9.00 |
| CHEMBL246070 | — | — | 1 | 9.00 |
| CHEMBL247951 | PEMAFIBRATE | 4.0 | 1 | 9.00 |
| CHEMBL398118 | — | — | 1 | 8.70 |
| CHEMBL391622 | — | — | 1 | 8.70 |
| CHEMBL391620 | — | — | 1 | 8.70 |
| CHEMBL247748 | — | — | 1 | 8.52 |
| CHEMBL398117 | — | — | 1 | 8.52 |
| CHEMBL428574 | — | — | 1 | 8.30 |
| CHEMBL248527 | — | — | 1 | 8.30 |
| CHEMBL429824 | — | — | 1 | 8.15 |
| CHEMBL245865 | — | — | 1 | 8.10 |
| CHEMBL248325 | — | — | 1 | 8.05 |
| CHEMBL248324 | — | — | 1 | 8.00 |
| CHEMBL247952 | — | — | 1 | 8.00 |
| CHEMBL248326 | — | — | 1 | 8.00 |
| CHEMBL246282 | — | — | 1 | 7.96 |
| CHEMBL247749 | — | — | 1 | 7.70 |
| CHEMBL245464 | — | — | 1 | 7.64 |
| CHEMBL246069 | — | — | 1 | 7.62 |
| CHEMBL248117 | — | — | 1 | 7.52 |
| CHEMBL248526 | — | — | 1 | 7.30 |
| CHEMBL245465 | — | — | 1 | 7.00 |
| CHEMBL395924 | — | — | 1 | 7.00 |
| CHEMBL392811 | — | — | 1 | 6.92 |
| CHEMBL394296 | — | — | 1 | 6.89 |
| CHEMBL392810 | — | — | 1 | 6.80 |
| CHEMBL245664 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL245866 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL247951 | PEMAFIBRATE | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL246070 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL427701 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL246281 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL398118 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL391622 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL391620 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL247748 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL398117 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL428574 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL248527 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL429824 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL245865 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL248325 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL248324 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL248326 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL247952 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL246282 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL247749 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL245464 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL246069 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL248117 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL248526 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL245465 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL395924 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL392811 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL394296 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL392810 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL245664 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL248118 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL246510 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL247919 | — | EC50 | = | 630.0 | nM | 6.20 |
| CHEMBL248119 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL247918 | — | EC50 | - | — | - | |
| CHEMBL247917 | — | EC50 | - | — | - |