Assay Detail
Binding
CHEMBL980390
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Displacement of [3H]darglitazone from human PPARgamma by scintillation proximity assay
24
Total Activities
24
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
Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.61 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL104850 | — | — | 1 | 7.54 |
| CHEMBL477095 | — | — | 1 | 6.73 |
| CHEMBL479002 | — | — | 1 | 6.59 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 6.56 |
| CHEMBL478725 | — | — | 1 | 6.53 |
| CHEMBL478335 | — | — | 1 | 6.23 |
| CHEMBL477323 | — | — | 1 | 5.80 |
| CHEMBL513904 | — | — | 1 | 5.70 |
| CHEMBL476896 | — | — | 1 | 5.66 |
| CHEMBL477094 | — | — | 1 | 5.58 |
| CHEMBL477298 | — | — | 1 | 5.55 |
| CHEMBL476897 | — | — | 1 | 5.55 |
| CHEMBL478334 | — | — | 1 | 5.51 |
| CHEMBL477318 | — | — | 1 | 5.40 |
| CHEMBL514696 | — | — | 1 | 4.96 |
| CHEMBL479001 | — | — | 1 | 4.92 |
| CHEMBL477941 | — | — | 1 | 4.92 |
| CHEMBL515181 | — | — | 1 | 4.66 |
| CHEMBL478726 | — | — | 1 | 4.58 |
| CHEMBL515972 | — | — | 1 | 4.55 |
| CHEMBL477940 | — | — | 1 | 4.28 |
| CHEMBL516129 | — | — | 1 | - |
| CHEMBL478563 | — | — | 1 | - |
| CHEMBL477690 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL104850 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL477095 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL479002 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL121 | ROSIGLITAZONE | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL478725 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL478335 | — | IC50 | = | 587.0 | nM | 6.23 |
| CHEMBL477323 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL513904 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL476896 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL477094 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL477298 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL476897 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL478334 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL477318 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL514696 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL479001 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL477941 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL515181 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL478726 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL515972 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL477940 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL516129 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL478563 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL477690 | — | IC50 | > | 50000.0 | nM | - |