Assay Detail
Binding
CHEMBL5732273
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.
93
Total Activities
31
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 | 31 | 7.05 | 8.80 |
| kon | 31 | - | - |
| k_off | 31 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3964816 | — | — | 3 | 8.80 |
| CHEMBL3975891 | — | — | 3 | 8.71 |
| CHEMBL4217067 | — | — | 3 | 8.32 |
| CHEMBL3958704 | — | — | 3 | 8.30 |
| CHEMBL3983906 | — | — | 3 | 8.26 |
| CHEMBL5877626 | — | — | 3 | 7.92 |
| CHEMBL4209482 | — | — | 3 | 7.90 |
| CHEMBL3911672 | — | — | 3 | 7.87 |
| CHEMBL3914092 | — | — | 3 | 7.65 |
| CHEMBL5814203 | — | — | 3 | 7.47 |
| CHEMBL3895104 | — | — | 3 | 7.40 |
| CHEMBL6031028 | — | — | 3 | 7.35 |
| CHEMBL5844429 | — | — | 3 | 7.28 |
| CHEMBL5748660 | — | — | 3 | 7.22 |
| CHEMBL3923083 | — | — | 3 | 7.19 |
| CHEMBL4212837 | — | — | 3 | 7.09 |
| CHEMBL6007752 | — | — | 3 | 6.94 |
| CHEMBL5772441 | — | — | 3 | 6.68 |
| CHEMBL4203239 | — | — | 3 | 6.64 |
| CHEMBL5963078 | — | — | 3 | 6.63 |
| CHEMBL5925126 | — | — | 3 | 6.58 |
| CHEMBL3981654 | — | — | 3 | 6.58 |
| CHEMBL4212753 | — | — | 3 | 6.29 |
| CHEMBL5772156 | — | — | 3 | 6.29 |
| CHEMBL5933286 | — | — | 3 | 6.20 |
| CHEMBL4215985 | — | — | 3 | 6.16 |
| CHEMBL5951018 | — | — | 3 | 6.15 |
| CHEMBL5948931 | — | — | 3 | 5.90 |
| CHEMBL5895408 | — | — | 3 | 5.75 |
| CHEMBL4215434 | — | — | 3 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3964816 | — | EC50 | = | 1.59 | nM | 8.80 |
| CHEMBL3975891 | — | EC50 | = | 1.93 | nM | 8.71 |
| CHEMBL4217067 | — | EC50 | = | 4.81 | nM | 8.32 |
| CHEMBL3958704 | — | EC50 | = | 5.06 | nM | 8.30 |
| CHEMBL3983906 | — | EC50 | = | 5.51 | nM | 8.26 |
| CHEMBL5877626 | — | EC50 | = | 11.9 | nM | 7.92 |
| CHEMBL4209482 | — | EC50 | = | 12.6 | nM | 7.90 |
| CHEMBL3911672 | — | EC50 | = | 13.5 | nM | 7.87 |
| CHEMBL3914092 | — | EC50 | = | 22.6 | nM | 7.65 |
| CHEMBL5814203 | — | EC50 | = | 33.6 | nM | 7.47 |
| CHEMBL3895104 | — | EC50 | = | 40.2 | nM | 7.40 |
| CHEMBL6031028 | — | EC50 | = | 45.1 | nM | 7.35 |
| CHEMBL5844429 | — | EC50 | = | 52.1 | nM | 7.28 |
| CHEMBL5748660 | — | EC50 | = | 60.16 | nM | 7.22 |
| CHEMBL3923083 | — | EC50 | = | 64.5 | nM | 7.19 |
| CHEMBL4212837 | — | EC50 | = | 80.4 | nM | 7.09 |
| CHEMBL6007752 | — | EC50 | = | 116.0 | nM | 6.94 |
| CHEMBL5772441 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4203239 | — | EC50 | = | 229.0 | nM | 6.64 |
| CHEMBL5963078 | — | EC50 | = | 233.0 | nM | 6.63 |
| CHEMBL3981654 | — | EC50 | = | 265.0 | nM | 6.58 |
| CHEMBL5925126 | — | EC50 | = | 266.0 | nM | 6.58 |
| CHEMBL4212753 | — | EC50 | = | 511.0 | nM | 6.29 |
| CHEMBL5772156 | — | EC50 | = | 511.8 | nM | 6.29 |
| CHEMBL5933286 | — | EC50 | = | 628.0 | nM | 6.20 |
| CHEMBL4215985 | — | EC50 | = | 694.0 | nM | 6.16 |
| CHEMBL5951018 | — | EC50 | = | 707.0 | nM | 6.15 |
| CHEMBL5948931 | — | EC50 | = | 1265.0 | nM | 5.90 |
| CHEMBL5895408 | — | EC50 | = | 1757.0 | nM | 5.75 |
| CHEMBL4215434 | — | EC50 | = | 1849.0 | nM | 5.73 |
| CHEMBL5963392 | — | EC50 | = | 5544.0 | nM | 5.26 |
| CHEMBL5963392 | — | k_off | = | - | s-1 | - |
| CHEMBL4212837 | — | kon | = | - | — | - |
| CHEMBL5951018 | — | kon | = | - | — | - |
| CHEMBL4209482 | — | kon | = | - | — | - |
| CHEMBL4209482 | — | k_off | = | - | s-1 | - |
| CHEMBL4217067 | — | kon | = | - | — | - |
| CHEMBL4217067 | — | k_off | = | - | s-1 | - |
| CHEMBL5772156 | — | kon | = | - | — | - |
| CHEMBL5772156 | — | k_off | = | - | s-1 | - |
| CHEMBL5748660 | — | kon | = | - | — | - |
| CHEMBL5748660 | — | k_off | = | - | s-1 | - |
| CHEMBL4212837 | — | k_off | = | - | s-1 | - |
| CHEMBL5925126 | — | kon | = | - | — | - |
| CHEMBL5844429 | — | k_off | = | - | s-1 | - |
| CHEMBL5925126 | — | k_off | = | - | s-1 | - |
| CHEMBL5844429 | — | kon | = | - | — | - |
| CHEMBL5772441 | — | kon | = | - | — | - |
| CHEMBL5772441 | — | k_off | = | - | s-1 | - |
| CHEMBL5963078 | — | k_off | = | - | s-1 | - |