Assay Detail
Binding
CHEMBL5734344
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Luciferase Assay: Medium including test compound was aspirated and washed with PBS. 50 μl PBS including 1 mM Mg++ and Ca++ were then added to each well. The luciferase assay was performed using the LucLite kit according to the manufacturer's instructions (Packard Instruments). Light emission was quantified by counting on a Perkin Elmer Envision reader. To measure 3-galactosidase activity 25 μl supernatant from each transfection lysate was transferred to a new 384 microplate. Beta-galactosidase assays were performed in the microwell plates using a kit from Promega and read in a Perkin Elmer Envision reader. The beta-galactosidase data were used to normalize (transfection efficiency, cell growth etc.) the luciferase data.
63
Total Activities
21
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor delta (CHEMBL3979) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
PPAR agonists, compounds, pharmaceutical compositions, and methods of use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 8.37 | 10.00 |
| kon | 21 | - | - |
| k_off | 21 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5931937 | — | — | 3 | 10.00 |
| CHEMBL5955597 | — | — | 3 | 10.00 |
| CHEMBL4755323 | — | — | 3 | 9.70 |
| CHEMBL5925396 | — | — | 3 | 9.30 |
| CHEMBL5936030 | — | — | 3 | 9.10 |
| CHEMBL5960113 | — | — | 3 | 9.00 |
| CHEMBL5849694 | — | — | 3 | 8.46 |
| CHEMBL5911917 | — | — | 3 | 8.43 |
| CHEMBL5764752 | — | — | 3 | 8.42 |
| CHEMBL5871677 | — | — | 3 | 8.36 |
| CHEMBL5889093 | — | — | 3 | 8.18 |
| CHEMBL6056389 | — | — | 3 | 8.11 |
| CHEMBL5972905 | — | — | 3 | 8.00 |
| CHEMBL5790000 | — | — | 3 | 7.88 |
| CHEMBL5774873 | — | — | 3 | 7.87 |
| CHEMBL6034074 | — | — | 3 | 7.84 |
| CHEMBL5949387 | — | — | 3 | 7.75 |
| CHEMBL5740441 | — | — | 3 | 7.73 |
| CHEMBL5989366 | — | — | 3 | 7.61 |
| CHEMBL6024487 | — | — | 3 | 7.41 |
| CHEMBL5975411 | — | — | 3 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5955597 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5931937 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4755323 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5925396 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5936030 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5960113 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5849694 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5911917 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5764752 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5871677 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5889093 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL6056389 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5972905 | — | EC50 | = | 9.9 | nM | 8.00 |
| CHEMBL5790000 | — | EC50 | = | 13.1 | nM | 7.88 |
| CHEMBL5774873 | — | EC50 | = | 13.5 | nM | 7.87 |
| CHEMBL6034074 | — | EC50 | = | 14.3 | nM | 7.84 |
| CHEMBL5949387 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5740441 | — | EC50 | = | 18.8 | nM | 7.73 |
| CHEMBL5989366 | — | EC50 | = | 24.3 | nM | 7.61 |
| CHEMBL6024487 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5975411 | — | EC50 | = | 227.0 | nM | 6.64 |
| CHEMBL5764752 | — | kon | = | - | — | - |
| CHEMBL5764752 | — | k_off | = | - | s-1 | - |
| CHEMBL6024487 | — | kon | = | - | — | - |
| CHEMBL5960113 | — | kon | = | - | — | - |
| CHEMBL5960113 | — | k_off | = | - | s-1 | - |
| CHEMBL6056389 | — | kon | = | - | — | - |
| CHEMBL6056389 | — | k_off | = | - | s-1 | - |
| CHEMBL5911917 | — | kon | = | - | — | - |
| CHEMBL5911917 | — | k_off | = | - | s-1 | - |
| CHEMBL5955597 | — | kon | = | - | — | - |
| CHEMBL5955597 | — | k_off | = | - | s-1 | - |
| CHEMBL4755323 | — | kon | = | - | — | - |
| CHEMBL4755323 | — | k_off | = | - | s-1 | - |
| CHEMBL5989366 | — | kon | = | - | — | - |
| CHEMBL5931937 | — | k_off | = | - | s-1 | - |
| CHEMBL5931937 | — | kon | = | - | — | - |
| CHEMBL5975411 | — | k_off | = | - | s-1 | - |
| CHEMBL5975411 | — | kon | = | - | — | - |
| CHEMBL5949387 | — | k_off | = | - | s-1 | - |
| CHEMBL5949387 | — | kon | = | - | — | - |
| CHEMBL5889093 | — | kon | = | - | — | - |
| CHEMBL6034074 | — | kon | = | - | — | - |
| CHEMBL5790000 | — | k_off | = | - | s-1 | - |
| CHEMBL5790000 | — | kon | = | - | — | - |
| CHEMBL6034074 | — | k_off | = | - | s-1 | - |
| CHEMBL5871677 | — | kon | = | - | — | - |
| CHEMBL5871677 | — | k_off | = | - | s-1 | - |
| CHEMBL5972905 | — | k_off | = | - | s-1 | - |
| CHEMBL5972905 | — | kon | = | - | — | - |