Assay Detail
Binding
CHEMBL4768835
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARgammaDEF receptor expressed in african green monkey COS7 cells transfected with pGal5-TK-pGL3/pRenilla-CMV assessed as intrinsic activity measured after 39 hrs by dual luciferase reporter assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification and development of non-cytotoxic cell death modulators: Impact of sartans and derivatives on PPARγ activation and on growth of imatinib-resistant chronic myelogenous leukemia cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 5.40 | 5.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 5.80 |
| CHEMBL1014 | CANDESARTAN CILEXETIL | 4.0 | 1 | 5.38 |
| CHEMBL1017 | TELMISARTAN | 4.0 | 1 | 5.37 |
| CHEMBL4785781 | — | — | 1 | 5.04 |
| CHEMBL1016 | CANDESARTAN | 3.0 | 1 | - |
| CHEMBL1513 | IRBESARTAN | 4.0 | 1 | - |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | - |
| CHEMBL1200692 | OLMESARTAN MEDOXOMIL | 4.0 | 1 | - |
| CHEMBL1516 | OLMESARTAN | 3.0 | 1 | - |
| CHEMBL4790305 | — | — | 1 | - |
| CHEMBL4786095 | — | — | 1 | - |
| CHEMBL4776997 | — | — | 1 | - |
| CHEMBL4789282 | — | — | 1 | - |
| CHEMBL4797861 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL595 | PIOGLITAZONE | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1014 | CANDESARTAN CILEXETIL | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1017 | TELMISARTAN | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4785781 | — | EC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL1016 | CANDESARTAN | EC50 | - | — | - | |
| CHEMBL1513 | IRBESARTAN | EC50 | - | — | - | |
| CHEMBL191 | LOSARTAN | EC50 | - | — | - | |
| CHEMBL1200692 | OLMESARTAN MEDOXOMIL | EC50 | - | — | - | |
| CHEMBL1516 | OLMESARTAN | EC50 | - | — | - | |
| CHEMBL4790305 | — | EC50 | - | — | - | |
| CHEMBL4786095 | — | EC50 | - | — | - | |
| CHEMBL4776997 | — | EC50 | - | — | - | |
| CHEMBL4789282 | — | EC50 | - | — | - | |
| CHEMBL4797861 | — | EC50 | - | — | - |