Assay Detail
Binding
CHEMBL889305
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRL-49653 stimulated human PPARgamma transactivation in CV-1 cells by GAL4 reporter assay
15
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 |
|---|---|---|---|
| IC50 | 8 | 5.59 | 6.00 |
| Activity | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL398185 | — | — | 2 | 6.00 |
| CHEMBL230259 | — | — | 2 | 5.80 |
| CHEMBL230804 | — | — | 2 | 5.70 |
| CHEMBL395527 | — | — | 2 | 5.60 |
| CHEMBL230731 | — | — | 2 | 5.60 |
| CHEMBL267996 | — | — | 2 | 5.20 |
| CHEMBL266742 | — | — | 2 | 5.20 |
| CHEMBL106666 | GW7845 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL398185 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL230259 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL230804 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL395527 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL230731 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL267996 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL266742 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL267996 | — | Activity | = | 55.0 | % | - |
| CHEMBL395527 | — | Activity | = | 57.0 | % | - |
| CHEMBL230731 | — | Activity | = | 59.0 | % | - |
| CHEMBL398185 | — | Activity | = | 92.0 | % | - |
| CHEMBL230804 | — | Activity | = | 80.0 | % | - |
| CHEMBL266742 | — | Activity | = | 48.0 | % | - |
| CHEMBL106666 | GW7845 | IC50 | < | 10000.0 | nM | - |
| CHEMBL230259 | — | Activity | = | 54.0 | % | - |