Assay Detail
Binding
CHEMBL889303
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Transactivation of human PPARgamma in CV-1 cells by GAL4 reporter assay
12
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CV-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Co-crystal structure guided array synthesis of PPARgamma inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 6.90 | 9.20 |
| Activity | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL106666 | GW7845 | — | 2 | 9.20 |
| CHEMBL395527 | — | — | 2 | 6.20 |
| CHEMBL230731 | — | — | 2 | 6.20 |
| CHEMBL230259 | — | — | 2 | 6.00 |
| CHEMBL267996 | — | — | 1 | - |
| CHEMBL398185 | — | — | 1 | - |
| CHEMBL230804 | — | — | 1 | - |
| CHEMBL266742 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL106666 | GW7845 | EC50 | = | 0.631 | nM | 9.20 |
| CHEMBL395527 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL230731 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL230259 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL267996 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL398185 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL230804 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL266742 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL230731 | — | Activity | = | 29.0 | % | - |
| CHEMBL395527 | — | Activity | = | 27.0 | % | - |
| CHEMBL230259 | — | Activity | = | 37.0 | % | - |
| CHEMBL106666 | GW7845 | Activity | = | 92.0 | % | - |