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Literature summary for 1.1.1.62 extracted from
- Synthesis of 17beta-hydroxysteroid dehydrogenase type 10 steroidal inhibitors selectivity, metabolic stability and enhanced potency (2021), Eur. J. Med. Chem., 209, 112909 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| HEK-293 cells stably transfected with 17beta-HSD10 | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 3alpha-hydroxy-3beta-([4-[(2-methoxy-4-methylphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one | - |
Homo sapiens |  |
| 3alpha-hydroxy-3beta-([4-[(3-methoxy-4-methylphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one | - |
Homo sapiens | |
| 3alpha-hydroxy-3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one | - |
Homo sapiens | |
| 3alpha-hydroxy-3beta-([4-[(quinolin-3-yl)methyl]piperazin-1-yl]methyl)-androstan-17-one | - |
Homo sapiens | |
| 3alpha-hydroxy-3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-androstan-17-one | - |
Homo sapiens | |
| 3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-17alpha-pregn-20-yne-3alpha,17-diol | metabolic stability and selectivity of inhibition for 17beta-HSD10 over 17beta-HSD3 | Homo sapiens | |
| 3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-androstane-3alpha,17alpha-diol | metabolic stability and selectivity of inhibition for 17beta-HSD10 over 17beta-HSD3 | Homo sapiens | |
| 3beta-[[4-(3,5-dimethylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one | - |
Homo sapiens | |
| 3beta-[[4-(3-acetylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one | - |
Homo sapiens | |
| 3beta-[[4-([1,1'-biphenyl]-4-carbonyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one | - |
Homo sapiens | |
| 4-(4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]piperazine-1-carbonyl)benzonitrile | - |
Homo sapiens | |
| 4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]-N-[[3-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide | - |
Homo sapiens | |
| N-ethyl-4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]-N-methylpiperazine-1-sulfonamide | - |
Homo sapiens | |
| N-[4-(dimethylsulfamoyl)phenyl]-4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]piperazine-1-carbothioamide | - |
Homo sapiens | |
| [[4-(4-benzoylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one | - |
Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| mitochondrion | - |
Homo sapiens | 5739 | - |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 17beta-estradiol + NAD+ | - |
Homo sapiens | estrone + NADH + H+ | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| 17beta-HSD10 | - |
Homo sapiens |
| 17beta-hydroxysteroid dehydrogenase type 10 | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00014 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 3alpha-hydroxy-3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-androstan-17-one | |
| 0.00042 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 3alpha-hydroxy-3beta-([4-[(3-methoxy-4-methylphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one | |
| 0.00095 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-androstane-3alpha,17alpha-diol | |
| 0.00097 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 3alpha-hydroxy-3beta-([4-[(quinolin-3-yl)methyl]piperazin-1-yl]methyl)-androstan-17-one | |
| 0.00107 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | N-[4-(dimethylsulfamoyl)phenyl]-4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]piperazine-1-carbothioamide | |
| 0.00126 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-17alpha-pregn-20-yne-3alpha,17-diol | |
| 0.0014 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]-N-[[3-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide | |
| 0.0016 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | N-ethyl-4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]-N-methylpiperazine-1-sulfonamide | |
| 0.0017 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 4-(4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]piperazine-1-carbonyl)benzonitrile | |
| 0.00205 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 3beta-[[4-(3,5-dimethylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one | |
| 0.0023 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 3beta-[[4-(3-acetylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one | |
| 0.0026 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 3alpha-hydroxy-3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one | |
| 0.0026 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 3beta-[[4-([1,1'-biphenyl]-4-carbonyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one | |
| 0.00285 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | [[4-(4-benzoylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one | |
| 0.0031 | - |
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells | Homo sapiens | 3alpha-hydroxy-3beta-([4-[(2-methoxy-4-methylphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| drug target | possible role in Alzheimer's disease, inhibition appears to be a therapeutic strategy | Homo sapiens |
| metabolism | the enzyme can oxidize estradiol into estrone, thus reducing concentration of this neuroprotective steroid | Homo sapiens |
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