Assay Detail
Binding
CHEMBL5113061
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at PPARgamma LBD (unknown origin) assessed as recruitment of corepressor NCOR2 to PPARgamma LBD by LanthaScreen TR-FRET assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| EC50 | 27 | 7.94 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5191837 | — | — | 1 | 9.19 |
| CHEMBL5186962 | — | — | 1 | 8.74 |
| CHEMBL5206512 | — | — | 1 | 8.70 |
| CHEMBL5179281 | — | — | 1 | 8.66 |
| CHEMBL5201278 | — | — | 1 | 8.59 |
| CHEMBL5206276 | — | — | 1 | 8.48 |
| CHEMBL5183657 | — | — | 1 | 8.43 |
| CHEMBL2324298 | — | — | 1 | 8.41 |
| CHEMBL5182665 | — | — | 1 | 8.40 |
| CHEMBL5204936 | — | — | 1 | 8.36 |
| CHEMBL5201306 | — | — | 1 | 8.28 |
| CHEMBL5207130 | — | — | 1 | 8.24 |
| CHEMBL5200843 | — | — | 1 | 8.24 |
| CHEMBL5174641 | — | — | 1 | 8.14 |
| CHEMBL5187164 | — | — | 1 | 8.02 |
| CHEMBL5184027 | — | — | 1 | 8.00 |
| CHEMBL5199152 | — | — | 1 | 7.72 |
| CHEMBL5207464 | — | — | 1 | 7.55 |
| CHEMBL5170260 | — | — | 1 | 7.27 |
| CHEMBL5173312 | — | — | 1 | 7.06 |
| CHEMBL5172001 | — | — | 1 | 5.10 |
| CHEMBL2447934 | — | — | 1 | 5.09 |
| CHEMBL5171685 | — | — | 1 | - |
| CHEMBL5201597 | — | — | 1 | - |
| CHEMBL5179111 | — | — | 1 | - |
| CHEMBL5203129 | — | — | 1 | - |
| CHEMBL5169731 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5191837 | — | EC50 | = | 0.65 | nM | 9.19 |
| CHEMBL5186962 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5206512 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5179281 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5201278 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5206276 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5183657 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL2324298 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5182665 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5204936 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5201306 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5207130 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5200843 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5174641 | — | EC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5187164 | — | EC50 | = | 9.6 | nM | 8.02 |
| CHEMBL5184027 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5199152 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5207464 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5170260 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5173312 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5172001 | — | EC50 | = | 7950.0 | nM | 5.10 |
| CHEMBL2447934 | — | EC50 | = | 8050.0 | nM | 5.09 |
| CHEMBL5171685 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL5201597 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL5179111 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL5203129 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL5169731 | — | EC50 | > | 50000.0 | nM | - |