Assay Detail
Binding
CHEMBL5113081
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Inverse agonist activity at GAL4-tagged mouse PPARgamma LBD expressed in CHO cells measured after 6 hrs by firefly luciferase reporter assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL2459) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 2 | 8.74 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5207130 | — | — | 1 | 9.85 |
| CHEMBL5187164 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5207130 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL5187164 | — | IC50 | = | 24.0 | nM | 7.62 |