Assay Detail
Binding
CHEMBL1693471
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Inhibition of human 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [1,2,6,7-[3H]cortisol to cortisone after 10 mins by scintillation counting
12
Total Activities
12
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 new glycyrrhetinic acid derived ring A azepanone, 29-urea and 29-hydroxamic acid derivatives as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.39 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1269273 | — | — | 1 | 8.54 |
| CHEMBL1689172 | — | — | 1 | 7.96 |
| CHEMBL1689280 | — | — | 1 | 7.96 |
| CHEMBL1689282 | — | — | 1 | 7.82 |
| CHEMBL1689283 | — | — | 1 | 7.77 |
| CHEMBL1689279 | — | — | 1 | 7.48 |
| CHEMBL1689284 | — | — | 1 | 7.35 |
| CHEMBL1689173 | — | — | 1 | 6.98 |
| CHEMBL1689277 | — | — | 1 | 6.71 |
| CHEMBL230006 | ENOXOLONE | 2.0 | 1 | 6.59 |
| CHEMBL207413 | ACETOXOLONE | -1.0 | 1 | 6.12 |
| CHEMBL1689281 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1269273 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1689172 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1689280 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1689282 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1689283 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1689279 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1689284 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1689173 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL1689277 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL230006 | ENOXOLONE | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL207413 | ACETOXOLONE | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL1689281 | — | IC50 | > | 4000.0 | nM | - |