Cloned (Comment) | Organism |
---|---|
HEK-293 cells stably transfected with 17beta-HSD10 | Homo sapiens |
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 | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
mitochondrion | - |
Homo sapiens | 5739 | - |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
17beta-estradiol + NAD+ | - |
Homo sapiens | estrone + NADH + H+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
17beta-HSD10 | - |
Homo sapiens |
17beta-hydroxysteroid dehydrogenase type 10 | - |
Homo sapiens |
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 | 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 |