Assay Detail
Functional
CHEMBL701905
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Agonist activity for Human PPAR gamma receptor in transcriptional activation assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The PPARs: from orphan receptors to drug discovery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 6.81 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL107367 | FARGLITAZAR | 2.0 | 1 | 9.47 |
| CHEMBL106666 | GW7845 | — | 1 | 9.15 |
| CHEMBL278994 | L-796449 | — | 1 | 8.28 |
| CHEMBL434063 | — | — | 1 | 8.21 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.37 |
| CHEMBL320553 | — | — | 1 | 7.36 |
| CHEMBL306229 | — | — | 1 | 7.18 |
| CHEMBL24458 | — | — | 1 | 7.08 |
| CHEMBL293526 | REGLITAZAR | 2.0 | 1 | 7.08 |
| CHEMBL408 | TROGLITAZONE | 4.0 | 1 | 6.26 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 6.24 |
| CHEMBL278590 | GSK-9578 | — | 1 | 6.00 |
| CHEMBL435278 | — | — | 1 | 5.60 |
| CHEMBL153057 | — | — | 1 | 5.26 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 4.22 |
| CHEMBL264374 | BEZAFIBRATE | 3.0 | 1 | 4.22 |
| CHEMBL672 | FENOFIBRATE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL107367 | FARGLITAZAR | EC50 | = | 0.34 | nM | 9.47 |
| CHEMBL106666 | GW7845 | EC50 | = | 0.71 | nM | 9.15 |
| CHEMBL278994 | L-796449 | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL434063 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL320553 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL306229 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL24458 | — | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL293526 | REGLITAZAR | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL408 | TROGLITAZONE | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL595 | PIOGLITAZONE | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL278590 | GSK-9578 | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL435278 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL153057 | — | EC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL264374 | BEZAFIBRATE | EC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL672 | FENOFIBRATE | EC50 | = | 300000.0 | nM | - |