Assay Detail
Binding
CHEMBL958789
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Inhibition of human recombinant 17beta-HSD2 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol
18
Total Activities
18
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
17-beta-hydroxysteroid dehydrogenase type 2 (CHEMBL2789) ↗| 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 | 18 | 5.37 | 6.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL150 | KAEMPFEROL | 1.0 | 1 | 6.44 |
| CHEMBL50 | QUERCETIN | 3.0 | 1 | 5.81 |
| CHEMBL131921 | BIOCHANIN | — | 1 | 5.00 |
| CHEMBL9352 | NARINGENIN | — | 1 | 4.84 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 4.78 |
| CHEMBL194399 | ENDOSULFAN | — | 1 | - |
| CHEMBL51483 | GOSSYPOL | 3.0 | 1 | - |
| CHEMBL230006 | ENOXOLONE | 2.0 | 1 | - |
| CHEMBL8145 | DAIDZEIN | 2.0 | 1 | - |
| CHEMBL117 | CHRYSIN | — | 1 | - |
| CHEMBL275638 | FLAVONE | 2.0 | 1 | - |
| CHEMBL399121 | HESPERETIN | 0.5 | 1 | - |
| CHEMBL274318 | FLAVANONE | — | 1 | - |
| CHEMBL73933 | 4'-HYDROXY-FLAVANONE | — | 1 | - |
| CHEMBL75897 | 2'-HYDROXY-FLAVANONE | — | 1 | - |
| CHEMBL28 | APIGENIN | — | 1 | - |
| CHEMBL276915 | 7-HYDROXYFLAVONE | — | 1 | - |
| CHEMBL195033 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL150 | KAEMPFEROL | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL50 | QUERCETIN | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL131921 | BIOCHANIN | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL9352 | NARINGENIN | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL44 | GENISTEIN | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL194399 | ENDOSULFAN | IC50 | - | — | - | |
| CHEMBL51483 | GOSSYPOL | IC50 | - | — | - | |
| CHEMBL230006 | ENOXOLONE | IC50 | - | — | - | |
| CHEMBL8145 | DAIDZEIN | IC50 | - | — | - | |
| CHEMBL117 | CHRYSIN | IC50 | - | — | - | |
| CHEMBL275638 | FLAVONE | IC50 | - | — | - | |
| CHEMBL399121 | HESPERETIN | IC50 | - | — | - | |
| CHEMBL274318 | FLAVANONE | IC50 | - | — | - | |
| CHEMBL73933 | 4'-HYDROXY-FLAVANONE | IC50 | - | — | - | |
| CHEMBL75897 | 2'-HYDROXY-FLAVANONE | IC50 | - | — | - | |
| CHEMBL28 | APIGENIN | IC50 | > | 20000.0 | nM | - |
| CHEMBL276915 | 7-HYDROXYFLAVONE | IC50 | > | 20000.0 | nM | - |
| CHEMBL195033 | — | IC50 | - | — | - |