Assay Detail
Binding
CHEMBL1648865
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of radiolabeled Dexamethasone from glucocorticoid receptor expressed in baculovirus
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
Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.91 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL258191 | — | — | 1 | 9.22 |
| CHEMBL1644760 | — | — | 2 | 9.05 |
| CHEMBL1644759 | — | — | 1 | 8.77 |
| CHEMBL1644756 | — | — | 1 | 8.46 |
| CHEMBL1644755 | — | — | 1 | 8.35 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 8.28 |
| CHEMBL1644754 | — | — | 1 | 8.24 |
| CHEMBL1644757 | — | — | 1 | 8.22 |
| CHEMBL1644765 | — | — | 1 | 8.00 |
| CHEMBL1644761 | — | — | 1 | 7.80 |
| CHEMBL1644758 | — | — | 1 | 6.47 |
| CHEMBL1644764 | — | — | 1 | 6.38 |
| CHEMBL1644763 | — | — | 1 | 6.36 |
| CHEMBL1644762 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL258191 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1644760 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL1644759 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL1644756 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL1644755 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL131 | PREDNISOLONE | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL1644754 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL1644757 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL1644765 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1644761 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1644760 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL1644758 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL1644764 | — | Ki | = | 416.0 | nM | 6.38 |
| CHEMBL1644763 | — | Ki | = | 436.0 | nM | 6.36 |
| CHEMBL1644762 | — | Ki | - | — | - |