Assay Detail
Binding
CHEMBL1059161
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Inhibition of mouse microsomal 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL3910) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.79 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL551949 | — | — | 1 | 8.70 |
| CHEMBL552288 | — | — | 1 | 8.70 |
| CHEMBL550065 | — | — | 1 | 8.70 |
| CHEMBL441687 | GLYCYRRHIZIN | 2.0 | 1 | 8.10 |
| CHEMBL559418 | — | — | 1 | 8.00 |
| CHEMBL549600 | — | — | 1 | 7.82 |
| CHEMBL561207 | — | — | 1 | 6.88 |
| CHEMBL554346 | — | — | 1 | 6.52 |
| CHEMBL552943 | — | — | 1 | 6.40 |
| CHEMBL551889 | — | — | 1 | 6.32 |
| CHEMBL558534 | — | — | 1 | 6.24 |
| CHEMBL562769 | — | — | 1 | 6.13 |
| CHEMBL552225 | — | — | 1 | 5.99 |
| CHEMBL561691 | — | — | 1 | 5.88 |
| CHEMBL556657 | — | — | 1 | 5.85 |
| CHEMBL565187 | — | — | 1 | 5.47 |
| CHEMBL564397 | — | — | 1 | 5.25 |
| CHEMBL563065 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL551949 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL552288 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL550065 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL441687 | GLYCYRRHIZIN | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL559418 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL549600 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL561207 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL554346 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL552943 | — | IC50 | = | 395.0 | nM | 6.40 |
| CHEMBL551889 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL558534 | — | IC50 | = | 576.0 | nM | 6.24 |
| CHEMBL562769 | — | IC50 | = | 732.0 | nM | 6.13 |
| CHEMBL552225 | — | IC50 | = | 1024.0 | nM | 5.99 |
| CHEMBL561691 | — | IC50 | = | 1319.0 | nM | 5.88 |
| CHEMBL556657 | — | IC50 | = | 1404.0 | nM | 5.85 |
| CHEMBL565187 | — | IC50 | = | 3379.0 | nM | 5.47 |
| CHEMBL564397 | — | IC50 | = | 5614.0 | nM | 5.25 |
| CHEMBL563065 | — | IC50 | = | 5843.0 | nM | 5.23 |