Assay Detail
Binding
CHEMBL933078
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Inhibition of PPARalpha
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| IC50 | 18 | 6.19 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL255389 | — | — | 1 | 7.10 |
| CHEMBL271240 | — | — | 1 | 6.44 |
| CHEMBL257517 | — | — | 1 | 6.34 |
| CHEMBL272336 | — | — | 1 | 6.32 |
| CHEMBL404646 | — | — | 1 | 6.28 |
| CHEMBL403847 | — | — | 1 | 6.16 |
| CHEMBL411118 | — | — | 1 | 6.14 |
| CHEMBL248906 | — | — | 1 | 6.13 |
| CHEMBL256468 | — | — | 1 | 6.10 |
| CHEMBL429734 | — | — | 1 | 6.07 |
| CHEMBL272962 | — | — | 1 | 5.89 |
| CHEMBL255388 | — | — | 1 | 5.85 |
| CHEMBL271739 | — | — | 1 | 5.62 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
| CHEMBL257891 | — | — | 1 | - |
| CHEMBL272774 | — | — | 1 | - |
| CHEMBL272963 | — | — | 1 | - |
| CHEMBL404451 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL255389 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL271240 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL257517 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL272336 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL404646 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL403847 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL411118 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL248906 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL256468 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL429734 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL272962 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL255388 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL271739 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL121 | ROSIGLITAZONE | IC50 | > | 15000.0 | nM | - |
| CHEMBL257891 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL272774 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL272963 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL404451 | — | IC50 | > | 15000.0 | nM | - |