Assay Detail
Binding
CHEMBL5500987
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARgamma transfected in African green monkey COS-7 cells co-transfected with pGL4.35 and pBIND reporter gene plasmid assessed as receptor transactivation incubated for 16 hrs by luciferase reporter gene assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 5.51 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 6.70 |
| CHEMBL4091374 | LANIFIBRANOR | 3.0 | 1 | 6.22 |
| CHEMBL5532117 | — | — | 1 | 5.75 |
| CHEMBL5517725 | — | — | 1 | 5.58 |
| CHEMBL5558175 | — | — | 1 | 5.46 |
| CHEMBL5556754 | — | — | 1 | 5.44 |
| CHEMBL5558110 | — | — | 1 | 5.43 |
| CHEMBL5559025 | — | — | 1 | 5.39 |
| CHEMBL5505899 | — | — | 1 | 5.30 |
| CHEMBL5542787 | — | — | 1 | 5.27 |
| CHEMBL5517671 | — | — | 1 | 5.14 |
| CHEMBL5517672 | — | — | 1 | 5.07 |
| CHEMBL264374 | BEZAFIBRATE | 3.0 | 1 | 4.88 |
| CHEMBL5523522 | — | — | 1 | - |
| CHEMBL5556504 | — | — | 1 | - |
| CHEMBL5556927 | — | — | 1 | - |
| CHEMBL5558844 | — | — | 1 | - |
| CHEMBL5531993 | — | — | 1 | - |
| CHEMBL5549754 | — | — | 1 | - |
| CHEMBL5559347 | — | — | 1 | - |
| CHEMBL5505922 | — | — | 1 | - |
| CHEMBL5555531 | — | — | 1 | - |
| CHEMBL5557966 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4091374 | LANIFIBRANOR | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5532117 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5517725 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5558175 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL5556754 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL5558110 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL5559025 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5505899 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5542787 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL5517671 | — | EC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL5517672 | — | EC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL264374 | BEZAFIBRATE | EC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL5523522 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5556504 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5556927 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5558844 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5531993 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5549754 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5559347 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5505922 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5555531 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5557966 | — | EC50 | > | 10000.0 | nM | - |