Assay Detail
Binding
CHEMBL2405920
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse 11beta-HSD1 expressed in HEK293 cell microsomes assessed as inhibition of [3H]cortisone conversion to [3H]cortisol by scintillation proximity assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL3910) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery and structure-activity relationships of ent-Kaurene diterpenoids as potent and selective 11β-HSD1 inhibitors: potential impact in diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.43 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL230006 | ENOXOLONE | 2.0 | 1 | 8.70 |
| CHEMBL2402444 | — | — | 1 | 6.59 |
| CHEMBL489140 | KAURENOIC ACID | — | 1 | 6.45 |
| CHEMBL512447 | — | — | 1 | 5.81 |
| CHEMBL2402471 | — | — | 1 | 5.55 |
| CHEMBL490353 | — | — | 1 | 5.49 |
| CHEMBL2402465 | — | — | 1 | - |
| CHEMBL2402464 | — | — | 1 | - |
| CHEMBL2402461 | — | — | 1 | - |
| CHEMBL2402458 | — | — | 1 | - |
| CHEMBL2402457 | — | — | 1 | - |
| CHEMBL2402453 | — | — | 1 | - |
| CHEMBL2402452 | — | — | 1 | - |
| CHEMBL2402475 | — | — | 1 | - |
| CHEMBL2402473 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL230006 | ENOXOLONE | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2402444 | — | IC50 | = | 258.6 | nM | 6.59 |
| CHEMBL489140 | KAURENOIC ACID | IC50 | = | 357.0 | nM | 6.45 |
| CHEMBL512447 | — | IC50 | = | 1553.0 | nM | 5.81 |
| CHEMBL2402471 | — | IC50 | = | 2805.0 | nM | 5.55 |
| CHEMBL490353 | — | IC50 | = | 3216.0 | nM | 5.49 |
| CHEMBL2402465 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2402464 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2402461 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2402458 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2402457 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2402453 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2402452 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2402475 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2402473 | — | IC50 | > | 1000.0 | nM | - |