Assay Detail
Functional
CHEMBL933080
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Agonist activity at PPARalpha in HEK293 cells by GAL4 transactivation assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 7.17 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272336 | — | — | 1 | 8.30 |
| CHEMBL257517 | — | — | 1 | 8.10 |
| CHEMBL256468 | — | — | 1 | 8.00 |
| CHEMBL271739 | — | — | 1 | 7.96 |
| CHEMBL404646 | — | — | 1 | 7.40 |
| CHEMBL255389 | — | — | 1 | 7.40 |
| CHEMBL248906 | — | — | 1 | 7.35 |
| CHEMBL429734 | — | — | 1 | 7.22 |
| CHEMBL271240 | — | — | 1 | 7.16 |
| CHEMBL272962 | — | — | 1 | 7.05 |
| CHEMBL403847 | — | — | 1 | 6.85 |
| CHEMBL411118 | — | — | 1 | 6.82 |
| CHEMBL255388 | — | — | 1 | 6.64 |
| CHEMBL404451 | — | — | 1 | 6.01 |
| CHEMBL272963 | — | — | 1 | 5.27 |
| CHEMBL272774 | — | — | 1 | - |
| CHEMBL257891 | — | — | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272336 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL257517 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL256468 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL271739 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL404646 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL255389 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL248906 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL429734 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL271240 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL272962 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL403847 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL411118 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL255388 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL404451 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL272963 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL272774 | — | EC50 | > | 7500.0 | nM | - |
| CHEMBL257891 | — | EC50 | > | 7500.0 | nM | - |
| CHEMBL121 | ROSIGLITAZONE | EC50 | > | 5000.0 | nM | - |