Assay Detail
Binding
CHEMBL3122503
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-methyltrienolone from human androgen 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 | 6.78 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3120319 | — | — | 1 | 8.22 |
| CHEMBL3120318 | — | — | 1 | 8.01 |
| CHEMBL3120317 | — | — | 1 | 6.62 |
| CHEMBL3120320 | — | — | 1 | 6.38 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 5.85 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 5.60 |
| CHEMBL3120316 | — | — | 1 | - |
| CHEMBL382564 | — | — | 1 | - |
| CHEMBL3120315 | — | — | 1 | - |
| CHEMBL3120323 | — | — | 1 | - |
| CHEMBL3120322 | — | — | 1 | - |
| CHEMBL3120321 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3120319 | — | Ki | = | 5.98 | nM | 8.22 |
| CHEMBL3120318 | — | Ki | = | 9.74 | nM | 8.01 |
| CHEMBL3120317 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL3120320 | — | Ki | = | 418.0 | nM | 6.38 |
| CHEMBL384467 | DEXAMETHASONE | Ki | = | 1410.0 | nM | 5.85 |
| CHEMBL131 | PREDNISOLONE | Ki | = | 2520.0 | nM | 5.60 |
| CHEMBL3120316 | — | Ki | - | — | - | |
| CHEMBL382564 | — | Ki | - | — | - | |
| CHEMBL3120315 | — | Ki | - | — | - | |
| CHEMBL3120323 | — | Ki | - | — | - | |
| CHEMBL3120322 | — | Ki | - | — | - | |
| CHEMBL3120321 | — | Ki | - | — | - |