Assay Detail
Binding
CHEMBL3743280
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 11beta-HSD1 in human liver microsomes assessed as conversion of [3H]-cortisone to [3H]-cortisol after 30 mins by scintillation proximity assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Searching for novel applications of the benzohomoadamantane scaffold in medicinal chemistry: Synthesis of novel 11β-HSD1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.95 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1095047 | — | — | 1 | 8.40 |
| CHEMBL3740482 | — | — | 1 | 6.46 |
| CHEMBL3740225 | — | — | 1 | 6.00 |
| CHEMBL3741800 | — | — | 1 | - |
| CHEMBL3739923 | — | — | 1 | - |
| CHEMBL3742167 | — | — | 1 | - |
| CHEMBL3740274 | — | — | 1 | - |
| CHEMBL3739953 | — | — | 1 | - |
| CHEMBL3741346 | — | — | 1 | - |
| CHEMBL3741550 | — | — | 1 | - |
| CHEMBL3741900 | — | — | 1 | - |
| CHEMBL3741686 | — | — | 1 | - |
| CHEMBL3742271 | — | — | 1 | - |
| CHEMBL3740407 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1095047 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3740482 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3740225 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3741800 | — | IC50 | - | — | - | |
| CHEMBL3739923 | — | IC50 | - | — | - | |
| CHEMBL3742167 | — | IC50 | - | — | - | |
| CHEMBL3740274 | — | IC50 | - | — | - | |
| CHEMBL3739953 | — | IC50 | - | — | - | |
| CHEMBL3741346 | — | IC50 | - | — | - | |
| CHEMBL3741550 | — | IC50 | - | — | - | |
| CHEMBL3741900 | — | IC50 | - | — | - | |
| CHEMBL3741686 | — | IC50 | - | — | - | |
| CHEMBL3742271 | — | IC50 | - | — | - | |
| CHEMBL3740407 | — | IC50 | - | — | - |