Assay Detail
Binding
CHEMBL3707772
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Fluorescence Polarization Ligand Binding Assay: The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-length glucocorticoid (GR) protein. Reagents for this assay are purchased from Invitrogen in a test kit. A fluorescent labeled GR ligand is used as a fluorescent tracer and test compounds compete with the fluorescent tracer for GR binding. The change in polarization value in the presence of test compounds is due to binding of test compounds to GR and is used to determine IC50 and relative binding affinity of test compounds for GR.
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Tricyclic compounds, compositions, and methods
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.31 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3647440 | — | — | 1 | 9.46 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 9.28 |
| CHEMBL3647443 | — | — | 1 | 8.93 |
| CHEMBL3647441 | — | — | 1 | 8.91 |
| CHEMBL3137304 | DAGROCORAT | 2.0 | 1 | 8.88 |
| CHEMBL3647444 | — | — | 1 | 8.72 |
| CHEMBL3647442 | — | — | 1 | 8.69 |
| CHEMBL3647445 | — | — | 1 | 8.67 |
| CHEMBL3647448 | — | — | 1 | 8.34 |
| CHEMBL3647439 | — | — | 1 | 8.15 |
| CHEMBL3647446 | — | — | 1 | 8.10 |
| CHEMBL3647447 | — | — | 1 | 8.04 |
| CHEMBL3137316 | FOSDAGROCORAT | 2.0 | 2 | 7.38 |
| CHEMBL3647449 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3647440 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL131 | PREDNISOLONE | IC50 | = | 0.526 | nM | 9.28 |
| CHEMBL3647443 | — | IC50 | = | 1.18 | nM | 8.93 |
| CHEMBL3647441 | — | IC50 | = | 1.22 | nM | 8.91 |
| CHEMBL3137304 | DAGROCORAT | IC50 | = | 1.31 | nM | 8.88 |
| CHEMBL3647444 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3647442 | — | IC50 | = | 2.06 | nM | 8.69 |
| CHEMBL3647445 | — | IC50 | = | 2.13 | nM | 8.67 |
| CHEMBL3647448 | — | IC50 | = | 4.58 | nM | 8.34 |
| CHEMBL3647439 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3647446 | — | IC50 | = | 8.03 | nM | 8.10 |
| CHEMBL3647447 | — | IC50 | = | 9.12 | nM | 8.04 |
| CHEMBL3137316 | FOSDAGROCORAT | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3137316 | FOSDAGROCORAT | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3647449 | — | IC50 | = | 895.0 | nM | 6.05 |