Assay Detail
Binding
CHEMBL954745
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Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol
14
Total Activities
14
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
Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.11 | 5.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL469909 | — | — | 1 | 5.42 |
| CHEMBL469911 | — | — | 1 | 5.21 |
| CHEMBL472508 | — | — | 1 | 4.70 |
| CHEMBL530555 | — | — | 1 | - |
| CHEMBL488681 | — | — | 1 | - |
| CHEMBL511844 | — | — | 1 | - |
| CHEMBL512532 | — | — | 1 | - |
| CHEMBL513427 | — | — | 1 | - |
| CHEMBL1628094 | — | — | 1 | - |
| CHEMBL472167 | — | — | 1 | - |
| CHEMBL470948 | — | — | 1 | - |
| CHEMBL446912 | — | — | 1 | - |
| CHEMBL512535 | — | — | 1 | - |
| CHEMBL471998 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL469909 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL469911 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL472508 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL530555 | — | IC50 | - | — | - | |
| CHEMBL488681 | — | IC50 | - | — | - | |
| CHEMBL511844 | — | IC50 | - | — | - | |
| CHEMBL512532 | — | IC50 | - | — | - | |
| CHEMBL513427 | — | IC50 | - | — | - | |
| CHEMBL1628094 | — | IC50 | - | — | - | |
| CHEMBL472167 | — | IC50 | - | — | - | |
| CHEMBL470948 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL446912 | — | IC50 | - | — | - | |
| CHEMBL512535 | — | IC50 | - | — | - | |
| CHEMBL471998 | — | IC50 | - | — | - |