Assay Detail
Functional
CHEMBL763850
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In vitro transactivation of human Peroxisome proliferator activated receptor alpha measured in PPAR-GAL4 chimeric COS-1 cell
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | COS-1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 6.98 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96451 | — | — | 1 | 7.18 |
| CHEMBL318684 | — | — | 1 | 7.09 |
| CHEMBL96143 | — | — | 1 | 7.07 |
| CHEMBL328615 | — | — | 1 | 6.81 |
| CHEMBL420441 | — | — | 1 | 6.75 |
| CHEMBL94496 | — | — | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
| CHEMBL94397 | — | — | 1 | - |
| CHEMBL97529 | — | — | 1 | - |
| CHEMBL96758 | — | — | 1 | - |
| CHEMBL92130 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96451 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL318684 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL96143 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL328615 | — | EC50 | = | 156.0 | nM | 6.81 |
| CHEMBL420441 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL94496 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL121 | ROSIGLITAZONE | EC50 | > | 3000.0 | nM | - |
| CHEMBL94397 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL97529 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL96758 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL92130 | — | EC50 | > | 3000.0 | nM | - |