Assay Detail
Binding
CHEMBL886015
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Effect on PPARalpha transactivation activity in HEK293 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and evaluation of potent, structurally novel peroxisome proliferator-activated receptor (PPAR) delta-selective agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 6.92 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL387914 | — | — | 1 | 8.09 |
| CHEMBL425666 | — | — | 1 | 7.92 |
| CHEMBL118939 | — | — | 1 | 7.75 |
| CHEMBL229785 | — | — | 1 | 7.72 |
| CHEMBL229837 | — | — | 1 | 7.54 |
| CHEMBL376165 | — | — | 1 | 7.39 |
| CHEMBL229786 | — | — | 1 | 7.16 |
| CHEMBL229778 | — | — | 1 | 7.11 |
| CHEMBL229525 | — | — | 1 | 6.85 |
| CHEMBL229888 | — | — | 1 | 6.68 |
| CHEMBL390116 | — | — | 1 | 6.64 |
| CHEMBL375471 | — | — | 1 | 6.60 |
| CHEMBL229836 | — | — | 1 | 6.55 |
| CHEMBL389903 | — | — | 1 | 6.28 |
| CHEMBL427071 | — | — | 1 | 6.21 |
| CHEMBL229573 | — | — | 1 | 6.09 |
| CHEMBL38943 | GW501516 | 2.0 | 1 | 6.00 |
| CHEMBL229831 | — | — | 1 | 5.92 |
| CHEMBL426371 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL387914 | — | EC50 | = | 8.2 | nM | 8.09 |
| CHEMBL425666 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL118939 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL229785 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL229837 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL376165 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL229786 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL229778 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL229525 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL229888 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL390116 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL375471 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL229836 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL389903 | — | EC50 | = | 520.0 | nM | 6.28 |
| CHEMBL427071 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL229573 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL38943 | GW501516 | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL229831 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL426371 | — | EC50 | > | 10000.0 | nM | - |