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Literature summary for 1.1.1.64 extracted from

  • Maltais, R.; Fournier, M.A.; Poirier, D.
    Development of 3-substituted-androsterone derivatives as potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 3 (2011), Bioorg. Med. Chem., 19, 4652-4668.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in HEK-293 cell Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3alpha,5alpha)-3-[[trans-2,5-dimethyl-4-[[2-(trifluoromethyl)-phenyl]sulfonyl]piperazin-1-yl]methyl]-3-hydroxyandrostan-17-one strong inhibition of isoform 17beta-HSD3 overexpressed in HEK-293 cells Homo sapiens
(3R,5S,8R,9S,10S,13S,14S)-3'-benzyl-10,13-dimethyltetradecahydro-2'H-spiro[cyclopenta[a]phenanthrene-3,5'-[1,3]oxazolidine]-2',17(2H)-dione strong inhibition of isoform 17beta-HSD3 overexpressed in HEK-293 cells. 44% inhibition at 0.1 microM in homogenized cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P37058
-
-

Synonyms

Synonyms Comment Organism
17beta-HSD3
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000006
-
assay uses homogenized cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens (3alpha,5alpha)-3-[[trans-2,5-dimethyl-4-[[2-(trifluoromethyl)-phenyl]sulfonyl]piperazin-1-yl]methyl]-3-hydroxyandrostan-17-one