Assay Detail
Binding
CHEMBL3888500
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Activity Assay: After 24 h treatment with the medicament, the cells were lysed with a lysis solution (Cell Culture Lysis buffer, Promega) and centrifuged, and the supernatant was collected. The supernatant was reacted with a fluorescence assay kit (Promega) and counted by a fluorometer (Ascent Fluoroskan FL reader, Thermo Labsystems, Finland), and the relative intensity of luciferase was determined. For the assay of the β-galactosidase activity used in the experiment as the internal reference (the internal reference for calibrating the transfection efficiency), 50 μl of the supernatant was transferred into a fresh microplate, treated with a Promega kit, and the value was read with a microplate reader at a wavelength of 405 nm (Bio-tech Instruments Inc., Winooski, Vt., USA) (Sauerberg, P.; Olsen, G. S.; Jeppesen, L.; Mogensen, J. P. et al., J. Med. Chem., 2007, 50, 1495-1503).
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Compounds having activating effect on subtypes of peroxisome proliferator-activated receptors and its preparation method and uses
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 7.46 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 9.00 |
| CHEMBL3932461 | — | — | 1 | 8.40 |
| CHEMBL3920204 | — | — | 1 | 8.30 |
| CHEMBL3972176 | — | — | 1 | 7.89 |
| CHEMBL3976442 | — | — | 1 | 7.66 |
| CHEMBL3905699 | — | — | 1 | 7.60 |
| CHEMBL3914680 | — | — | 1 | 7.33 |
| CHEMBL3892207 | — | — | 1 | 7.05 |
| CHEMBL3946222 | — | — | 1 | 6.16 |
| CHEMBL3904658 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3932461 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3920204 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3972176 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3976442 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3905699 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3914680 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3892207 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3946222 | — | EC50 | = | 692.0 | nM | 6.16 |
| CHEMBL3904658 | — | EC50 | = | 6761.0 | nM | 5.17 |