Assay Detail
Binding
CHEMBL1035293
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Inhibition of human PPARalpha receptor by scintillation proximity assay
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.08 | 7.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL558083 | — | — | 2 | 7.06 |
| CHEMBL562864 | — | — | 1 | 6.31 |
| CHEMBL672 | FENOFIBRATE | 4.0 | 1 | 6.00 |
| CHEMBL560830 | — | — | 1 | 5.97 |
| CHEMBL552240 | — | — | 1 | 5.58 |
| CHEMBL564902 | — | — | 1 | 5.53 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
| CHEMBL564036 | — | — | 1 | - |
| CHEMBL560160 | — | — | 1 | - |
| CHEMBL549746 | — | — | 1 | - |
| CHEMBL461571 | — | — | 1 | - |
| CHEMBL452051 | — | — | 1 | - |
| CHEMBL559567 | — | — | 1 | - |
| CHEMBL556073 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL558083 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL562864 | — | IC50 | = | 491.0 | nM | 6.31 |
| CHEMBL558083 | — | IC50 | = | 764.0 | nM | 6.12 |
| CHEMBL672 | FENOFIBRATE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL560830 | — | IC50 | = | 1081.0 | nM | 5.97 |
| CHEMBL552240 | — | IC50 | = | 2624.0 | nM | 5.58 |
| CHEMBL564902 | — | IC50 | = | 2981.0 | nM | 5.53 |
| CHEMBL121 | ROSIGLITAZONE | IC50 | > | 50000.0 | nM | - |
| CHEMBL564036 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL560160 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL549746 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL461571 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL452051 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL559567 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL556073 | — | IC50 | > | 15000.0 | nM | - |