Assay Detail
Functional
CHEMBL2216558
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at GAL4-fused PPARgamma assessed as transcriptional activity by cell based assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 6.26 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2204595 | — | — | 1 | 8.33 |
| CHEMBL2204597 | — | — | 1 | 7.38 |
| CHEMBL2204598 | — | — | 1 | 7.15 |
| CHEMBL186179 | MURAGLITAZAR | 3.0 | 1 | 7.00 |
| CHEMBL2204596 | — | — | 1 | 6.75 |
| CHEMBL2204600 | — | — | 1 | 6.51 |
| CHEMBL2204594 | — | — | 1 | 6.48 |
| CHEMBL181954 | NAVEGLITAZAR | 2.0 | 1 | 6.40 |
| CHEMBL24038 | RAGAGLITAZAR | 2.0 | 1 | 6.22 |
| CHEMBL2204599 | — | — | 1 | 6.17 |
| CHEMBL2204602 | — | — | 1 | 6.16 |
| CHEMBL2204610 | — | — | 1 | 6.10 |
| CHEMBL2204593 | — | — | 1 | 6.05 |
| CHEMBL24458 | — | — | 1 | 6.00 |
| CHEMBL282686 | TESAGLITAZAR | 3.0 | 1 | 5.89 |
| CHEMBL2204603 | — | — | 1 | 5.89 |
| CHEMBL2204604 | — | — | 1 | 5.66 |
| CHEMBL2204605 | — | — | 1 | 5.11 |
| CHEMBL2204608 | — | — | 1 | 5.06 |
| CHEMBL2204609 | — | — | 1 | 4.80 |
| CHEMBL66206 | — | — | 1 | - |
| CHEMBL2204607 | — | — | 1 | - |
| CHEMBL2204606 | — | — | 1 | - |
| CHEMBL2204601 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2204595 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL2204597 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2204598 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL186179 | MURAGLITAZAR | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2204596 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2204600 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2204594 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL181954 | NAVEGLITAZAR | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL24038 | RAGAGLITAZAR | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2204599 | — | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL2204602 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2204610 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2204593 | — | EC50 | = | 890.0 | nM | 6.05 |
| CHEMBL24458 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL282686 | TESAGLITAZAR | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2204603 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2204604 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2204605 | — | EC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL2204608 | — | EC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL2204609 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL66206 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL2204607 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL2204606 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL2204601 | — | EC50 | > | 25000.0 | nM | - |