Assay Detail
Binding
CHEMBL5730840
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive Binding Assay: PPARγ binding is measured by a TR-FRET competitive binding assay using Invitrogen LanthaScreen TR-FRET PPARγ Competitive Binding Assay (Invitrogen #4894). This assay uses a terbium-labeled anti-GST antibody to label the GST tagged human PPARγ ligand binding domain (LBD). A fluorescent small molecule pan-PPAR ligand tracer binds to the LBD causing energy transfer from the antibody to the ligand resulting in a high TR-FRET ratio. Competition binding by PPARγ ligands displace the tracer from the LBD causing a lower FRET signal between the antibody and tracer. The TR-FRET ratio is determined by reading the fluorescence emission at 490 and 520 nm using a Synergy2 plate reader (BioTek).
69
Total Activities
23
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
PPAR-sparing compounds for the treatment of metabolic diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 4.83 | 6.90 |
| kon | 23 | - | - |
| k_off | 23 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 3 | 6.90 |
| CHEMBL5810408 | — | — | 3 | 5.43 |
| CHEMBL5983135 | — | — | 3 | 5.10 |
| CHEMBL5816647 | — | — | 3 | 4.96 |
| CHEMBL5800435 | — | — | 3 | 4.93 |
| CHEMBL146624 | MITOGLITAZONE | 2.0 | 3 | 4.58 |
| CHEMBL5998602 | — | — | 3 | 4.56 |
| CHEMBL6065015 | — | — | 3 | 4.56 |
| CHEMBL5877552 | — | — | 3 | 4.52 |
| CHEMBL6002856 | — | — | 3 | 4.23 |
| CHEMBL5848996 | — | — | 3 | 4.21 |
| CHEMBL5745167 | — | — | 3 | 4.01 |
| CHEMBL5893157 | — | — | 3 | - |
| CHEMBL6000671 | — | — | 3 | - |
| CHEMBL5963202 | — | — | 3 | - |
| CHEMBL6032353 | — | — | 3 | - |
| CHEMBL5968108 | — | — | 3 | - |
| CHEMBL5768185 | — | — | 3 | - |
| CHEMBL5841115 | — | — | 3 | - |
| CHEMBL5798146 | — | — | 3 | - |
| CHEMBL5829708 | — | — | 3 | - |
| CHEMBL5971366 | — | — | 3 | - |
| CHEMBL5943071 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL5810408 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL5983135 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL5816647 | — | IC50 | = | 10900.0 | nM | 4.96 |
| CHEMBL5800435 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL146624 | MITOGLITAZONE | IC50 | = | 26600.0 | nM | 4.58 |
| CHEMBL6065015 | — | IC50 | = | 27700.0 | nM | 4.56 |
| CHEMBL5998602 | — | IC50 | = | 27700.0 | nM | 4.56 |
| CHEMBL5877552 | — | IC50 | = | 30500.0 | nM | 4.52 |
| CHEMBL6002856 | — | IC50 | = | 58900.0 | nM | 4.23 |
| CHEMBL5848996 | — | IC50 | = | 61400.0 | nM | 4.21 |
| CHEMBL5745167 | — | IC50 | = | 98500.0 | nM | 4.01 |
| CHEMBL5798146 | — | k_off | = | - | s-1 | - |
| CHEMBL5971366 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL5829708 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL5829708 | — | kon | = | - | — | - |
| CHEMBL5829708 | — | k_off | = | - | s-1 | - |
| CHEMBL5816647 | — | kon | = | - | — | - |
| CHEMBL5816647 | — | k_off | = | - | s-1 | - |
| CHEMBL5810408 | — | kon | = | - | — | - |
| CHEMBL5810408 | — | k_off | = | - | s-1 | - |
| CHEMBL5841115 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL146624 | MITOGLITAZONE | kon | = | - | — | - |
| CHEMBL146624 | MITOGLITAZONE | k_off | = | - | s-1 | - |
| CHEMBL121 | ROSIGLITAZONE | kon | = | - | — | - |
| CHEMBL121 | ROSIGLITAZONE | k_off | = | - | s-1 | - |
| CHEMBL6002856 | — | kon | = | - | — | - |
| CHEMBL6002856 | — | k_off | = | - | s-1 | - |
| CHEMBL5943071 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5943071 | — | kon | = | - | — | - |
| CHEMBL5943071 | — | k_off | = | - | s-1 | - |
| CHEMBL5963202 | — | kon | = | - | — | - |
| CHEMBL5968108 | — | kon | = | - | — | - |
| CHEMBL5768185 | — | k_off | = | - | s-1 | - |
| CHEMBL5968108 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL6032353 | — | k_off | = | - | s-1 | - |
| CHEMBL6032353 | — | kon | = | - | — | - |
| CHEMBL6032353 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL5848996 | — | k_off | = | - | s-1 | - |
| CHEMBL5848996 | — | kon | = | - | — | - |
| CHEMBL5963202 | — | k_off | = | - | s-1 | - |
| CHEMBL5798146 | — | kon | = | - | — | - |
| CHEMBL5963202 | — | IC50 | = | 164300.0 | nM | - |
| CHEMBL5968108 | — | k_off | = | - | s-1 | - |
| CHEMBL5768185 | — | IC50 | = | 190800.0 | nM | - |
| CHEMBL5768185 | — | kon | = | - | — | - |
| CHEMBL5983135 | — | kon | = | - | — | - |
| CHEMBL6065015 | — | kon | = | - | — | - |
| CHEMBL6065015 | — | k_off | = | - | s-1 | - |
| CHEMBL5798146 | — | IC50 | > | 250000.0 | nM | - |