Assay Detail
Functional
CHEMBL980388
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 5.35 | 6.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL477095 | — | — | 1 | 6.21 |
| CHEMBL104850 | — | — | 1 | 6.17 |
| CHEMBL478725 | — | — | 1 | 6.00 |
| CHEMBL477298 | — | — | 1 | 5.80 |
| CHEMBL477323 | — | — | 1 | 5.64 |
| CHEMBL479002 | — | — | 1 | 5.55 |
| CHEMBL476897 | — | — | 1 | 5.55 |
| CHEMBL476896 | — | — | 1 | 5.40 |
| CHEMBL477318 | — | — | 1 | 5.30 |
| CHEMBL478334 | — | — | 1 | 5.30 |
| CHEMBL477094 | — | — | 1 | 4.96 |
| CHEMBL516129 | — | — | 1 | 4.92 |
| CHEMBL515181 | — | — | 1 | 4.92 |
| CHEMBL478726 | — | — | 1 | 4.80 |
| CHEMBL515972 | — | — | 1 | 4.60 |
| CHEMBL479001 | — | — | 1 | 4.54 |
| CHEMBL513904 | — | — | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
| CHEMBL477940 | — | — | 1 | - |
| CHEMBL477941 | — | — | 1 | - |
| CHEMBL478563 | — | — | 1 | - |
| CHEMBL478335 | — | — | 1 | - |
| CHEMBL514696 | — | — | 1 | - |
| CHEMBL477690 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL477095 | — | EC50 | = | 623.0 | nM | 6.21 |
| CHEMBL104850 | — | EC50 | = | 684.0 | nM | 6.17 |
| CHEMBL478725 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL477298 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL477323 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL479002 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL476897 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL476896 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL477318 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL478334 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL477094 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL516129 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL515181 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL478726 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL515972 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL479001 | — | EC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL513904 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL121 | ROSIGLITAZONE | EC50 | > | 12000.0 | nM | - |
| CHEMBL477940 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL477941 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL478563 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL478335 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL514696 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL477690 | — | EC50 | > | 30000.0 | nM | - |