Assay Detail
Functional
CHEMBL947731
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARgamma transactivation expressed in human HePG2 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Modulation of PPAR receptor subtype selectivity of the ligands: aliphatic chain vs aromatic ring as a spacer between pharmacophore and the lipophilic moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 6.88 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL592054 | IMIGLITAZAR | 3.0 | 1 | 8.40 |
| CHEMBL481551 | — | — | 1 | 7.82 |
| CHEMBL520272 | — | — | 1 | 7.51 |
| CHEMBL186179 | MURAGLITAZAR | 3.0 | 1 | 7.05 |
| CHEMBL481550 | — | — | 1 | 7.00 |
| CHEMBL481549 | — | — | 1 | 6.37 |
| CHEMBL481683 | — | — | 1 | 6.35 |
| CHEMBL482334 | — | — | 1 | 6.25 |
| CHEMBL270960 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL592054 | IMIGLITAZAR | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL481551 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL520272 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL186179 | MURAGLITAZAR | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL481550 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL481549 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL481683 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL482334 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL270960 | — | EC50 | = | 6850.0 | nM | 5.16 |