Assay Detail
Functional
CHEMBL935699
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha expressed in HEK293 cells assessed as luciferase activity by GAL4 transactivation assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 7.18 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL255309 | — | — | 1 | 8.40 |
| CHEMBL257165 | — | — | 1 | 8.30 |
| CHEMBL403432 | — | — | 1 | 8.22 |
| CHEMBL256142 | — | — | 1 | 8.10 |
| CHEMBL256358 | — | — | 1 | 8.00 |
| CHEMBL401534 | — | — | 1 | 7.80 |
| CHEMBL258212 | — | — | 1 | 7.75 |
| CHEMBL255872 | — | — | 1 | 7.64 |
| CHEMBL257180 | — | — | 1 | 7.55 |
| CHEMBL256569 | — | — | 1 | 7.40 |
| CHEMBL257164 | — | — | 1 | 7.36 |
| CHEMBL257345 | — | — | 1 | 7.25 |
| CHEMBL255271 | — | — | 1 | 7.05 |
| CHEMBL445942 | — | — | 1 | 6.77 |
| CHEMBL258428 | — | — | 1 | 6.68 |
| CHEMBL256134 | — | — | 1 | 6.63 |
| CHEMBL255097 | — | — | 1 | 6.24 |
| CHEMBL186179 | MURAGLITAZAR | 3.0 | 1 | 5.85 |
| CHEMBL402956 | — | — | 1 | 5.31 |
| CHEMBL255251 | — | — | 1 | 5.25 |
| CHEMBL256505 | — | — | 1 | - |
| CHEMBL255930 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL255309 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL257165 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL403432 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL256142 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL256358 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL401534 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL258212 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL255872 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL257180 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL256569 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL257164 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL257345 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL255271 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL445942 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL258428 | — | EC50 | = | 209.0 | nM | 6.68 |
| CHEMBL256134 | — | EC50 | = | 235.0 | nM | 6.63 |
| CHEMBL255097 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL186179 | MURAGLITAZAR | EC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL402956 | — | EC50 | = | 4920.0 | nM | 5.31 |
| CHEMBL255251 | — | EC50 | = | 5570.0 | nM | 5.25 |
| CHEMBL256505 | — | EC50 | > | 7500.0 | nM | - |
| CHEMBL255930 | — | EC50 | = | 165000.0 | nM | - |