Assay Detail
Binding
CHEMBL957999
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Inhibition of human recombinant 17beta-HSD1 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol
36
Total Activities
35
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
17-beta-hydroxysteroid dehydrogenase type 1 (CHEMBL3181) ↗| 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 | 35 | 5.62 | 7.57 |
| Ki | 1 | 8.52 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL371948 | — | — | 2 | 8.52 |
| CHEMBL407968 | — | — | 1 | 7.57 |
| CHEMBL373383 | — | — | 1 | 6.77 |
| CHEMBL28 | APIGENIN | — | 1 | 6.15 |
| CHEMBL150 | KAEMPFEROL | 1.0 | 1 | 5.98 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 5.66 |
| CHEMBL9352 | NARINGENIN | — | 1 | 5.30 |
| CHEMBL276915 | 7-HYDROXYFLAVONE | — | 1 | 5.28 |
| CHEMBL470948 | — | — | 1 | 5.24 |
| CHEMBL530555 | — | — | 1 | 4.72 |
| CHEMBL1628094 | — | — | 1 | 4.48 |
| CHEMBL469909 | — | — | 1 | 4.33 |
| CHEMBL194399 | ENDOSULFAN | — | 1 | 4.32 |
| CHEMBL117 | CHRYSIN | — | 1 | - |
| CHEMBL8145 | DAIDZEIN | 2.0 | 1 | - |
| CHEMBL50 | QUERCETIN | 3.0 | 1 | - |
| CHEMBL471998 | — | — | 1 | - |
| CHEMBL131921 | BIOCHANIN | — | 1 | - |
| CHEMBL399121 | HESPERETIN | 0.5 | 1 | - |
| CHEMBL230006 | ENOXOLONE | 2.0 | 1 | - |
| CHEMBL511844 | — | — | 1 | - |
| CHEMBL472508 | — | — | 1 | - |
| CHEMBL512532 | — | — | 1 | - |
| CHEMBL469911 | — | — | 1 | - |
| CHEMBL513427 | — | — | 1 | - |
| CHEMBL51483 | GOSSYPOL | 3.0 | 1 | - |
| CHEMBL472167 | — | — | 1 | - |
| CHEMBL274318 | FLAVANONE | — | 1 | - |
| CHEMBL446912 | — | — | 1 | - |
| CHEMBL488681 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL371948 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL407968 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL371948 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL373383 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL28 | APIGENIN | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL150 | KAEMPFEROL | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL44 | GENISTEIN | IC50 | = | 2210.0 | nM | 5.66 |
| CHEMBL9352 | NARINGENIN | IC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL276915 | 7-HYDROXYFLAVONE | IC50 | = | 5250.0 | nM | 5.28 |
| CHEMBL470948 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL530555 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL1628094 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL469909 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL194399 | ENDOSULFAN | IC50 | = | 48250.0 | nM | 4.32 |
| CHEMBL195033 | — | IC50 | - | — | - | |
| CHEMBL73933 | 4'-HYDROXY-FLAVANONE | IC50 | - | — | - | |
| CHEMBL75897 | 2'-HYDROXY-FLAVANONE | IC50 | - | — | - | |
| CHEMBL512535 | — | IC50 | - | — | - | |
| CHEMBL275638 | FLAVONE | IC50 | - | — | - | |
| CHEMBL117 | CHRYSIN | IC50 | - | — | - | |
| CHEMBL8145 | DAIDZEIN | IC50 | - | — | - | |
| CHEMBL50 | QUERCETIN | IC50 | - | — | - | |
| CHEMBL471998 | — | IC50 | - | — | - | |
| CHEMBL131921 | BIOCHANIN | IC50 | - | — | - | |
| CHEMBL399121 | HESPERETIN | IC50 | - | — | - | |
| CHEMBL230006 | ENOXOLONE | IC50 | - | — | - | |
| CHEMBL511844 | — | IC50 | - | — | - | |
| CHEMBL472508 | — | IC50 | - | — | - | |
| CHEMBL512532 | — | IC50 | - | — | - | |
| CHEMBL469911 | — | IC50 | - | — | - | |
| CHEMBL513427 | — | IC50 | - | — | - | |
| CHEMBL51483 | GOSSYPOL | IC50 | - | — | - | |
| CHEMBL472167 | — | IC50 | - | — | - | |
| CHEMBL274318 | FLAVANONE | IC50 | - | — | - | |
| CHEMBL446912 | — | IC50 | - | — | - | |
| CHEMBL488681 | — | IC50 | - | — | - |