Assay Detail
Binding
CHEMBL1272437
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [1,2-3H]-cortisone to cortisol by scintillation counting
11
Total Activities
11
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 novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.19 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1269877 | — | — | 1 | 7.37 |
| CHEMBL1271410 | — | — | 1 | 7.21 |
| CHEMBL493512 | — | — | 1 | 6.21 |
| CHEMBL1270688 | — | — | 1 | 6.20 |
| CHEMBL230006 | ENOXOLONE | 2.0 | 1 | 6.11 |
| CHEMBL1270093 | — | — | 1 | 6.08 |
| CHEMBL1270994 | — | — | 1 | 6.03 |
| CHEMBL1269273 | — | — | 1 | 6.00 |
| CHEMBL1271303 | — | — | 1 | 5.94 |
| CHEMBL1270589 | — | — | 1 | 5.82 |
| CHEMBL207413 | ACETOXOLONE | -1.0 | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1269877 | — | IC50 | = | 42.7 | nM | 7.37 |
| CHEMBL1271410 | — | IC50 | = | 61.9 | nM | 7.21 |
| CHEMBL493512 | — | IC50 | = | 619.0 | nM | 6.21 |
| CHEMBL1270688 | — | IC50 | = | 626.0 | nM | 6.20 |
| CHEMBL230006 | ENOXOLONE | IC50 | = | 778.0 | nM | 6.11 |
| CHEMBL1270093 | — | IC50 | = | 825.0 | nM | 6.08 |
| CHEMBL1270994 | — | IC50 | = | 929.0 | nM | 6.03 |
| CHEMBL1269273 | — | IC50 | = | 1012.0 | nM | 6.00 |
| CHEMBL1271303 | — | IC50 | = | 1157.0 | nM | 5.94 |
| CHEMBL1270589 | — | IC50 | = | 1508.0 | nM | 5.82 |
| CHEMBL207413 | ACETOXOLONE | IC50 | = | 7138.0 | nM | 5.15 |