Assay Detail
Binding
CHEMBL4132698
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 11beta-HSD1 in human liver microsomes using [3H]cortisone as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by scintillation proximity assay
23
Total Activities
23
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
Design, synthesis and in vivo study of novel pyrrolidine-based 11β-HSD1 inhibitors for age-related cognitive dysfunction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.85 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4170932 | — | — | 1 | 7.70 |
| CHEMBL4163698 | — | — | 1 | 7.70 |
| CHEMBL4170544 | — | — | 1 | 7.70 |
| CHEMBL4162610 | — | — | 1 | 7.52 |
| CHEMBL4160328 | — | — | 1 | 7.52 |
| CHEMBL4168636 | — | — | 1 | 7.40 |
| CHEMBL4174155 | — | — | 1 | 7.30 |
| CHEMBL1095047 | — | — | 1 | 7.05 |
| CHEMBL4174368 | — | — | 1 | 7.05 |
| CHEMBL4172177 | — | — | 1 | 6.54 |
| CHEMBL4160886 | — | — | 1 | 6.50 |
| CHEMBL4166243 | — | — | 1 | 6.39 |
| CHEMBL4164290 | — | — | 1 | 5.97 |
| CHEMBL4160714 | — | — | 1 | 5.91 |
| CHEMBL4167147 | — | — | 1 | 5.83 |
| CHEMBL4168826 | — | — | 1 | 5.56 |
| CHEMBL4159148 | — | — | 1 | - |
| CHEMBL4169794 | — | — | 1 | - |
| CHEMBL4159236 | — | — | 1 | - |
| CHEMBL4175606 | — | — | 1 | - |
| CHEMBL4167737 | — | — | 1 | - |
| CHEMBL4160506 | — | — | 1 | - |
| CHEMBL4171112 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4170932 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4163698 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4170544 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4162610 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4160328 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4168636 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4174155 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1095047 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4174368 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4172177 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4160886 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4166243 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4164290 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4160714 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL4167147 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL4168826 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL4159148 | — | IC50 | - | — | - | |
| CHEMBL4169794 | — | IC50 | - | — | - | |
| CHEMBL4159236 | — | IC50 | - | — | - | |
| CHEMBL4175606 | — | IC50 | - | — | - | |
| CHEMBL4167737 | — | IC50 | - | — | - | |
| CHEMBL4160506 | — | IC50 | - | — | - | |
| CHEMBL4171112 | — | IC50 | - | — | - |