Assay Detail
Binding
CHEMBL4139881
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Transactivation of human Gal4-fused PPARgamma LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 7.33 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL107367 | FARGLITAZAR | 2.0 | 1 | 8.85 |
| CHEMBL186179 | MURAGLITAZAR | 3.0 | 1 | 8.52 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 8.40 |
| CHEMBL4171153 | — | — | 1 | 8.00 |
| CHEMBL4174996 | — | — | 1 | 7.70 |
| CHEMBL4159590 | — | — | 1 | 7.70 |
| CHEMBL4164063 | — | — | 1 | 7.52 |
| CHEMBL4162949 | — | — | 1 | 7.52 |
| CHEMBL4163242 | — | — | 1 | 7.30 |
| CHEMBL4159869 | — | — | 1 | 7.10 |
| CHEMBL4167504 | — | — | 1 | 6.70 |
| CHEMBL4160416 | — | — | 1 | 6.70 |
| CHEMBL4164343 | — | — | 1 | 6.00 |
| CHEMBL4174713 | — | — | 1 | 6.00 |
| CHEMBL4160661 | — | — | 1 | 6.00 |
| CHEMBL4170881 | — | — | 1 | - |
| CHEMBL4160945 | — | — | 1 | - |
| CHEMBL4167789 | — | — | 1 | - |
| CHEMBL4174598 | — | — | 1 | - |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL107367 | FARGLITAZAR | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL186179 | MURAGLITAZAR | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4171153 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4174996 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4159590 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4164063 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4162949 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4163242 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4159869 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4167504 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4160416 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4164343 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4174713 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4160661 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4170881 | — | EC50 | < | 10.0 | nM | - |
| CHEMBL4160945 | — | EC50 | < | 10.0 | nM | - |
| CHEMBL4167789 | — | EC50 | < | 10.0 | nM | - |
| CHEMBL4174598 | — | EC50 | < | 10.0 | nM | - |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | - | — | - |