Assay Detail
Binding
CHEMBL757773
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In vitro transcription activation on human peroxisome proliferator activated receptor-alpha (PPAR alpha)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.67 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL324027 | — | — | 1 | 7.52 |
| CHEMBL331388 | — | — | 1 | 7.36 |
| CHEMBL325844 | — | — | 1 | 7.16 |
| CHEMBL118577 | — | — | 1 | 7.05 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 6.85 |
| CHEMBL118816 | — | — | 1 | 6.85 |
| CHEMBL117796 | — | — | 1 | 6.77 |
| CHEMBL117402 | — | — | 1 | 6.60 |
| CHEMBL293526 | REGLITAZAR | 2.0 | 1 | 5.72 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 4.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL324027 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL331388 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL325844 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL118577 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL118816 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL117796 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL117402 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL293526 | REGLITAZAR | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 15500.0 | nM | 4.81 |