Assay Detail
Functional
CHEMBL886574
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 6.60 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL107367 | FARGLITAZAR | 2.0 | 1 | 9.22 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.46 |
| CHEMBL429823 | — | — | 1 | 7.44 |
| CHEMBL247925 | — | — | 1 | 7.28 |
| CHEMBL246272 | — | — | 1 | 7.17 |
| CHEMBL246473 | — | — | 1 | 6.97 |
| CHEMBL248530 | — | — | 1 | 6.87 |
| CHEMBL394948 | — | — | 1 | 6.66 |
| CHEMBL245674 | — | — | 1 | 6.64 |
| CHEMBL248906 | — | — | 1 | 6.60 |
| CHEMBL397120 | — | — | 1 | 6.57 |
| CHEMBL246270 | — | — | 1 | 6.53 |
| CHEMBL247720 | — | — | 1 | 6.51 |
| CHEMBL245656 | — | — | 1 | 6.45 |
| CHEMBL395191 | — | — | 1 | 6.41 |
| CHEMBL394947 | — | — | 1 | 6.38 |
| CHEMBL396694 | — | — | 1 | 6.12 |
| CHEMBL247926 | — | — | 1 | 6.08 |
| CHEMBL428748 | — | — | 1 | 6.04 |
| CHEMBL394968 | — | — | 1 | 5.93 |
| CHEMBL396696 | — | — | 1 | 5.92 |
| CHEMBL394967 | — | — | 1 | 5.86 |
| CHEMBL247719 | — | — | 1 | 5.75 |
| CHEMBL371120 | — | — | 1 | 5.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL107367 | FARGLITAZAR | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL429823 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL247925 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL246272 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL246473 | — | EC50 | = | 108.0 | nM | 6.97 |
| CHEMBL248530 | — | EC50 | = | 136.0 | nM | 6.87 |
| CHEMBL394948 | — | EC50 | = | 221.0 | nM | 6.66 |
| CHEMBL245674 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL248906 | — | EC50 | = | 249.0 | nM | 6.60 |
| CHEMBL397120 | — | EC50 | = | 267.0 | nM | 6.57 |
| CHEMBL246270 | — | EC50 | = | 295.0 | nM | 6.53 |
| CHEMBL247720 | — | EC50 | = | 307.0 | nM | 6.51 |
| CHEMBL245656 | — | EC50 | = | 359.0 | nM | 6.45 |
| CHEMBL395191 | — | EC50 | = | 391.0 | nM | 6.41 |
| CHEMBL394947 | — | EC50 | = | 412.0 | nM | 6.38 |
| CHEMBL396694 | — | EC50 | = | 759.0 | nM | 6.12 |
| CHEMBL247926 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL428748 | — | EC50 | = | 901.0 | nM | 6.04 |
| CHEMBL394968 | — | EC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL396696 | — | EC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL394967 | — | EC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL247719 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL371120 | — | EC50 | = | 3600.0 | nM | 5.44 |