Assay Detail
Binding
CHEMBL3122504
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 9.46 | 9.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3120318 | — | — | 1 | 9.84 |
| CHEMBL3120320 | — | — | 1 | 9.65 |
| CHEMBL3120319 | — | — | 1 | 9.59 |
| CHEMBL3120317 | — | — | 1 | 9.57 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 9.16 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 8.94 |
| CHEMBL3120316 | — | — | 1 | - |
| CHEMBL382564 | — | — | 1 | - |
| CHEMBL3120315 | — | — | 1 | - |
| CHEMBL3120323 | — | — | 1 | - |
| CHEMBL3120322 | — | — | 1 | - |
| CHEMBL3120321 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3120318 | — | Ki | = | 0.146 | nM | 9.84 |
| CHEMBL3120320 | — | Ki | = | 0.226 | nM | 9.65 |
| CHEMBL3120319 | — | Ki | = | 0.257 | nM | 9.59 |
| CHEMBL3120317 | — | Ki | = | 0.268 | nM | 9.57 |
| CHEMBL384467 | DEXAMETHASONE | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL131 | PREDNISOLONE | Ki | = | 1.14 | nM | 8.94 |
| CHEMBL3120316 | — | Ki | > | 100.0 | nM | - |
| CHEMBL382564 | — | Ki | > | 100.0 | nM | - |
| CHEMBL3120315 | — | Ki | > | 100.0 | nM | - |
| CHEMBL3120323 | — | Ki | > | 100.0 | nM | - |
| CHEMBL3120322 | — | Ki | > | 100.0 | nM | - |
| CHEMBL3120321 | — | Ki | > | 100.0 | nM | - |