Assay Detail
Binding
CHEMBL2405919
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Inhibition of human 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 | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6.60 | 8.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2402457 | — | — | 1 | 8.03 |
| CHEMBL230006 | ENOXOLONE | 2.0 | 1 | 7.54 |
| CHEMBL2402475 | — | — | 1 | 6.93 |
| CHEMBL2402464 | — | — | 1 | 6.78 |
| CHEMBL2402458 | — | — | 1 | 6.60 |
| CHEMBL2402461 | — | — | 1 | 6.58 |
| CHEMBL2402452 | — | — | 1 | 6.48 |
| CHEMBL2402453 | — | — | 1 | 6.39 |
| CHEMBL2402473 | — | — | 1 | 6.11 |
| CHEMBL2402471 | — | — | 1 | 6.04 |
| CHEMBL490353 | — | — | 1 | 5.91 |
| CHEMBL512447 | — | — | 1 | 5.85 |
| CHEMBL2402465 | — | — | 1 | - |
| CHEMBL2402444 | — | — | 1 | - |
| CHEMBL489140 | KAURENOIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2402457 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL230006 | ENOXOLONE | IC50 | = | 29.1 | nM | 7.54 |
| CHEMBL2402475 | — | IC50 | = | 116.4 | nM | 6.93 |
| CHEMBL2402464 | — | IC50 | = | 165.4 | nM | 6.78 |
| CHEMBL2402458 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL2402461 | — | IC50 | = | 266.1 | nM | 6.58 |
| CHEMBL2402452 | — | IC50 | = | 330.8 | nM | 6.48 |
| CHEMBL2402453 | — | IC50 | = | 407.3 | nM | 6.39 |
| CHEMBL2402473 | — | IC50 | = | 770.6 | nM | 6.11 |
| CHEMBL2402471 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL490353 | — | IC50 | = | 1236.0 | nM | 5.91 |
| CHEMBL512447 | — | IC50 | = | 1417.0 | nM | 5.85 |
| CHEMBL2402465 | — | IC50 | = | 403700.0 | nM | - |
| CHEMBL2402444 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL489140 | KAURENOIC ACID | IC50 | - | — | - |