Assay Detail
Binding
CHEMBL5113063
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at PPARgamma in human RT112/84-FABP4 cells assessed as reduction in PPARgamma transactivation measured by Nanoluciferase reporter gene assay
27
Total Activities
27
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 Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists <b>BAY-4931</b> and <b>BAY-0069</b>.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.05 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5191837 | — | — | 1 | 9.80 |
| CHEMBL5207130 | — | — | 1 | 9.77 |
| CHEMBL5187164 | — | — | 1 | 9.66 |
| CHEMBL5179281 | — | — | 1 | 9.64 |
| CHEMBL5206512 | — | — | 1 | 9.60 |
| CHEMBL5207464 | — | — | 1 | 9.54 |
| CHEMBL5204936 | — | — | 1 | 9.49 |
| CHEMBL5201278 | — | — | 1 | 9.24 |
| CHEMBL5184027 | — | — | 1 | 8.80 |
| CHEMBL5199152 | — | — | 1 | 8.48 |
| CHEMBL5206276 | — | — | 1 | 8.40 |
| CHEMBL5183657 | — | — | 1 | 8.36 |
| CHEMBL5173312 | — | — | 1 | 8.07 |
| CHEMBL5174641 | — | — | 1 | 7.28 |
| CHEMBL5201306 | — | — | 1 | 6.71 |
| CHEMBL2324298 | — | — | 1 | 6.32 |
| CHEMBL5186962 | — | — | 1 | 5.89 |
| CHEMBL5182665 | — | — | 1 | 5.75 |
| CHEMBL5179111 | — | — | 1 | 5.24 |
| CHEMBL5172001 | — | — | 1 | 5.03 |
| CHEMBL5170260 | — | — | 1 | - |
| CHEMBL5200843 | — | — | 1 | - |
| CHEMBL5203129 | — | — | 1 | - |
| CHEMBL5171685 | — | — | 1 | - |
| CHEMBL5169731 | — | — | 1 | - |
| CHEMBL2447934 | — | — | 1 | - |
| CHEMBL5201597 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5191837 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL5207130 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL5187164 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL5179281 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL5206512 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL5207464 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL5204936 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL5201278 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL5184027 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5199152 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5206276 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5183657 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5173312 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5174641 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5201306 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL2324298 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5186962 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5182665 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5179111 | — | IC50 | = | 5750.0 | nM | 5.24 |
| CHEMBL5172001 | — | IC50 | = | 9350.0 | nM | 5.03 |
| CHEMBL5170260 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5200843 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5203129 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL5171685 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5169731 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2447934 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5201597 | — | IC50 | > | 50000.0 | nM | - |