Assay Detail
Functional
CHEMBL802067
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transcriptional repression activity in HEP G2 cells expressing glucocorticoid receptor compared to Dexamethasone
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.78 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 8.68 |
| CHEMBL97206 | — | — | 1 | 8.40 |
| CHEMBL317578 | — | — | 1 | 8.22 |
| CHEMBL99123 | — | — | 1 | 8.05 |
| CHEMBL330638 | — | — | 1 | 7.75 |
| CHEMBL100219 | — | — | 1 | 7.75 |
| CHEMBL327757 | — | — | 1 | 7.64 |
| CHEMBL95644 | — | — | 1 | 7.24 |
| CHEMBL419158 | — | — | 1 | 7.17 |
| CHEMBL99046 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL97206 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL317578 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL99123 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL330638 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL100219 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL327757 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL95644 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL419158 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL99046 | — | IC50 | = | 123.0 | nM | 6.91 |