Assay Detail
Functional
CHEMBL760002
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In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells
13
Total Activities
13
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 gamma (CHEMBL235) ↗| 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 | 13 | 7.13 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL94306 | — | — | 1 | 7.85 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.70 |
| CHEMBL94397 | — | — | 1 | 7.64 |
| CHEMBL328615 | — | — | 1 | 7.57 |
| CHEMBL318684 | — | — | 1 | 7.33 |
| CHEMBL92130 | — | — | 1 | 7.16 |
| CHEMBL96451 | — | — | 1 | 7.07 |
| CHEMBL96143 | — | — | 1 | 6.97 |
| CHEMBL97529 | — | — | 1 | 6.91 |
| CHEMBL94496 | — | — | 1 | 6.78 |
| CHEMBL420441 | — | — | 1 | 6.78 |
| CHEMBL300629 | — | — | 1 | 6.52 |
| CHEMBL96758 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL94306 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL94397 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL328615 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL318684 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL92130 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL96451 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL96143 | — | EC50 | = | 106.0 | nM | 6.97 |
| CHEMBL97529 | — | EC50 | = | 123.0 | nM | 6.91 |
| CHEMBL94496 | — | EC50 | = | 167.0 | nM | 6.78 |
| CHEMBL420441 | — | EC50 | = | 165.0 | nM | 6.78 |
| CHEMBL300629 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL96758 | — | EC50 | = | 353.0 | nM | 6.45 |