Assay Detail
Binding
CHEMBL1648956
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transrepression activity at glucocorticoid receptor in IL-1beta-stimulated human HepG2 cells assessed as inhibition of AP1 response element-induced IL-6 production by ELISA
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct 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 |
|---|---|---|---|
| IC50 | 15 | 7.57 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1644760 | — | — | 2 | 8.80 |
| CHEMBL1644759 | — | — | 1 | 7.80 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 7.64 |
| CHEMBL1644756 | — | — | 1 | 7.44 |
| CHEMBL1644761 | — | — | 1 | 7.43 |
| CHEMBL258191 | — | — | 1 | 7.23 |
| CHEMBL1644757 | — | — | 1 | 7.19 |
| CHEMBL1644755 | — | — | 1 | - |
| CHEMBL1644758 | — | — | 1 | - |
| CHEMBL1644764 | — | — | 1 | - |
| CHEMBL1644754 | — | — | 1 | - |
| CHEMBL1644765 | — | — | 1 | - |
| CHEMBL1644763 | — | — | 1 | - |
| CHEMBL1644762 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1644760 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1644759 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL131 | PREDNISOLONE | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1644756 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1644761 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL258191 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1644757 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1644760 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1644755 | — | IC50 | - | — | - | |
| CHEMBL1644758 | — | IC50 | - | — | - | |
| CHEMBL1644764 | — | IC50 | - | — | - | |
| CHEMBL1644754 | — | IC50 | - | — | - | |
| CHEMBL1644765 | — | IC50 | - | — | - | |
| CHEMBL1644763 | — | IC50 | - | — | - | |
| CHEMBL1644762 | — | IC50 | - | — | - |