Assay Detail
Binding
CHEMBL5240451
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at human PPARgamma in human RT112/84 transfected with NLuc-fused FABP4 assessed as reduction in PPARgamma transactivation incubated for 6 to 18 hrs by Nano-Glo luciferase assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | RT112/84 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.22 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5289955 | — | — | 1 | 8.70 |
| CHEMBL5267263 | — | — | 1 | 8.38 |
| CHEMBL5273393 | — | — | 1 | 8.32 |
| CHEMBL5282503 | — | — | 1 | 8.30 |
| CHEMBL5281842 | — | — | 1 | 8.18 |
| CHEMBL5268912 | — | — | 1 | 8.13 |
| CHEMBL5271038 | — | — | 1 | 8.08 |
| CHEMBL5272194 | — | — | 1 | 7.85 |
| CHEMBL5286386 | — | — | 1 | 7.82 |
| CHEMBL5285688 | — | — | 1 | 7.42 |
| CHEMBL5291018 | — | — | 1 | 7.27 |
| CHEMBL5277957 | — | — | 1 | 7.04 |
| CHEMBL5287868 | — | — | 1 | 7.03 |
| CHEMBL5283176 | — | — | 1 | 6.74 |
| CHEMBL5288593 | — | — | 1 | 5.98 |
| CHEMBL5278668 | — | — | 1 | 5.95 |
| CHEMBL5282181 | — | — | 1 | 5.66 |
| CHEMBL5287866 | — | — | 1 | 5.28 |
| CHEMBL5273751 | — | — | 1 | 5.13 |
| CHEMBL5282748 | — | — | 1 | - |
| CHEMBL5287514 | — | — | 1 | - |
| CHEMBL5281604 | — | — | 1 | - |
| CHEMBL5272116 | — | — | 1 | - |
| CHEMBL5273188 | — | — | 1 | - |
| CHEMBL5286808 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5289955 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5267263 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5273393 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5282503 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5281842 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL5268912 | — | IC50 | = | 7.35 | nM | 8.13 |
| CHEMBL5271038 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5272194 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5286386 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5285688 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5291018 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5277957 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5287868 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5283176 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL5288593 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL5278668 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL5282181 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5287866 | — | IC50 | = | 5250.0 | nM | 5.28 |
| CHEMBL5273751 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL5282748 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5287514 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5281604 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5272116 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5273188 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5286808 | — | IC50 | > | 5000.0 | nM | - |