Assay Detail
Binding
CHEMBL2446793
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant 11beta-HSD2 expressed in HEK293 cells assessed as inhibition of [1,2,6,7-3H]-cortisol to [3H]cortisone preincubated for 10 mins before substrate addition by scintillation counting
9
Total Activities
9
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 type 2 (CHEMBL3746) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis of sterically encumbered 11β-aminoprogesterone derivatives and evaluation as 11β-hydroxysteroid dehydrogenase inhibitors and mineralocorticoid receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.70 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1563246 | — | — | 1 | 6.40 |
| CHEMBL2440888 | 11BETA-HYDROXYPROGESTERONE | — | 1 | 6.31 |
| CHEMBL2440126 | — | — | 1 | 5.98 |
| CHEMBL2440889 | 11BETA-AMINOPROGESTERONE | — | 1 | 5.66 |
| CHEMBL2440890 | — | — | 1 | 5.62 |
| CHEMBL2440891 | — | — | 1 | 5.57 |
| CHEMBL2440893 | — | — | 1 | 5.38 |
| CHEMBL2440892 | — | — | 1 | 5.23 |
| CHEMBL2440894 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1563246 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2440888 | 11BETA-HYDROXYPROGESTERONE | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2440126 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL2440889 | 11BETA-AMINOPROGESTERONE | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2440890 | — | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL2440891 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL2440893 | — | IC50 | = | 4210.0 | nM | 5.38 |
| CHEMBL2440892 | — | IC50 | = | 5850.0 | nM | 5.23 |
| CHEMBL2440894 | — | IC50 | = | 6760.0 | nM | 5.17 |