Assay Detail
Binding
CHEMBL4054229
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Inhibition of full-length human 11beta-HSD1 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 2 hr by scintillation proximity assay
7
Total Activities
7
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 |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis of selective 11β-HSD1 inhibitors based on dammarane scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.57 | 7.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL230006 | ENOXOLONE | 2.0 | 1 | 7.95 |
| CHEMBL4071679 | — | — | 1 | 7.00 |
| CHEMBL4088895 | — | — | 1 | 6.61 |
| CHEMBL4087459 | — | — | 1 | 6.31 |
| CHEMBL4064979 | — | — | 1 | 6.14 |
| CHEMBL4102864 | — | — | 1 | 6.00 |
| CHEMBL4103361 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL230006 | ENOXOLONE | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL4071679 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4088895 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL4087459 | — | IC50 | = | 488.0 | nM | 6.31 |
| CHEMBL4064979 | — | IC50 | = | 729.0 | nM | 6.14 |
| CHEMBL4102864 | — | IC50 | = | 994.0 | nM | 6.00 |
| CHEMBL4103361 | — | IC50 | = | 1047.0 | nM | 5.98 |