Assay Detail
Binding
CHEMBL973434
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH
21
Total Activities
12
Compounds Tested
2
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
Structure-based virtual screening for identification of novel 11beta-HSD1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.85 | 7.89 |
| Activity | 9 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL230006 | ENOXOLONE | 2.0 | 1 | 7.89 |
| CHEMBL470532 | — | — | 2 | 6.07 |
| CHEMBL470533 | — | — | 2 | 6.01 |
| CHEMBL452136 | — | — | 2 | 5.96 |
| CHEMBL471720 | — | — | 2 | 5.76 |
| CHEMBL470722 | — | — | 2 | 5.65 |
| CHEMBL35 | FUROSEMIDE | 4.0 | 2 | 5.42 |
| CHEMBL474575 | — | — | 2 | 5.40 |
| CHEMBL449922 | — | — | 2 | 5.28 |
| CHEMBL472612 | — | — | 2 | 5.10 |
| CHEMBL473992 | — | — | 1 | - |
| CHEMBL514305 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL230006 | ENOXOLONE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL470532 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL470533 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL452136 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL471720 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL470722 | — | IC50 | = | 2250.0 | nM | 5.65 |
| CHEMBL35 | FUROSEMIDE | IC50 | = | 3760.0 | nM | 5.42 |
| CHEMBL474575 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL449922 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL472612 | — | IC50 | = | 7980.0 | nM | 5.10 |
| CHEMBL473992 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL514305 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL472612 | — | Activity | - | — | - | |
| CHEMBL35 | FUROSEMIDE | Activity | - | — | - | |
| CHEMBL470532 | — | Activity | - | — | - | |
| CHEMBL449922 | — | Activity | - | — | - | |
| CHEMBL470533 | — | Activity | - | — | - | |
| CHEMBL470722 | — | Activity | - | — | - | |
| CHEMBL474575 | — | Activity | - | — | - | |
| CHEMBL452136 | — | Activity | - | — | - | |
| CHEMBL471720 | — | Activity | - | — | - |