Assay Detail
Functional
CHEMBL1019546
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human PPARgamma receptor expressed in Saccharomyces cerevisiae AH109 co-transfected with mouse CBP assessed as inhibition of rosiglitazone-induced LBD-CBP interaction by alpha-galactosidase based yeast two hybrid assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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
Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.13 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL451321 | METAGLIDASEN | — | 1 | 6.66 |
| CHEMBL455856 | — | — | 1 | 6.09 |
| CHEMBL510698 | — | — | 1 | 6.00 |
| CHEMBL375270 | — | — | 1 | 5.48 |
| CHEMBL476008 | — | — | 1 | 5.28 |
| CHEMBL39176 | — | — | 1 | 5.06 |
| CHEMBL515773 | — | — | 1 | 4.82 |
| CHEMBL477417 | — | — | 1 | 4.81 |
| CHEMBL513911 | — | — | 1 | 4.74 |
| CHEMBL476173 | — | — | 1 | 4.73 |
| CHEMBL477627 | — | — | 1 | 4.59 |
| CHEMBL456071 | HALOFENATE | 2.0 | 1 | 4.40 |
| CHEMBL258558 | — | — | 1 | 4.00 |
| CHEMBL284768 | MIFOBATE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL451321 | METAGLIDASEN | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL455856 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL510698 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL375270 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL476008 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL39176 | — | IC50 | = | 8670.0 | nM | 5.06 |
| CHEMBL515773 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL477417 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL513911 | — | IC50 | = | 18400.0 | nM | 4.74 |
| CHEMBL476173 | — | IC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL477627 | — | IC50 | = | 25800.0 | nM | 4.59 |
| CHEMBL456071 | HALOFENATE | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL258558 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL284768 | MIFOBATE | IC50 | = | 140000.0 | nM | - |