Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.1.1.64 extracted from

  • Tchedam Ngatcha, B.; Luu-The, V.; Labrie, F.; Poirier, D.
    Androsterone 3alpha-ether-3beta-substituted and androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase: chemical synthesis and structure-activity relationship (2005), J. Med. Chem., 48, 5257-5268.
    View publication on PubMed
Search for more literature for 1.1.1.64

Inhibitors

Inhibitors Comment Organism Structure
3-(17'-oxo-5'alpha-androstan-3'alpha-oxy)propanoic acid 0.003 mM, 48% inhibition Homo sapiens
3alpha,3beta-O-(1'-oxo-1',3'-propanediyloxy)-5alpha-androstan-17-one 0.003 mM, 53% inhibition Homo sapiens
3alpha-(2'-hydroxypropanoxy)-5alpha-androstan-17-one 0.003 mM, 89% inhibition Homo sapiens
3alpha-(3'-bromopropanoxy)-5alpha-androstan-17-one 0.003 mM, 93% inhibition Homo sapiens
3alpha-(3'-hydroxypropanoxy)-5alpha-androstan-17-one 0.003 mM, 86% inhibition Homo sapiens
3alpha-(prop-2'-enoxy)-5alpha-androstan-17-one 0.003 mM, 95% inhibition Homo sapiens
3alpha-ethoxy-3beta-(phenylmethyl)-5alpha-androstan-17-one 0.003 mM, 92% inhibition, IC50: 352 nM Homo sapiens
3alpha-ethoxy-5alpha-androstan-17-one 0.003 mM, 95% inhibition Homo sapiens
3alpha-hexanoxy-3beta-(phenylmethyl)-5alpha-androstan-17-one 0.003 mM, 28% inhibition Homo sapiens
3alpha-hexanoxy-5alpha-androstan-17-one 0.003 mM, 92% inhibition Homo sapiens
3alpha-hydroxy-3'-phenyl-5alpha-androstan-17-one 0.003 mM, 95% inhibition, IC50: 81 nM Homo sapiens
3alpha-hydroxy-3beta-(3'-hydroxypropyl)-5alpha-androstan-17-one 0.003 mM, 74% inhibition Homo sapiens
3alpha-hydroxy-3beta-(prop-2'-enyl)-5alpha-androstan-17-one 0.003 mM, 76% inhibition Homo sapiens
3alpha-hydroxy-3beta-methyl-5alpha-androstan-17-one 0.003 mM, 93% inhibition Homo sapiens
3alpha-hydroxy-3beta-octyl-5alpha-androstan-17-one 0.003 mM, 92% inhibition, IC50: 147 nM Homo sapiens
3alpha-hydroxy-3beta-phenylethyl-5alpha-androstan-17-one 0.003 mM, 93% inhibition, IC50: 99 nM Homo sapiens
3alpha-hydroxy-3beta-phenylmethyl-5alpha-androstan-17-one 0.003 mM, 94% inhibition, IC50: 57 nM Homo sapiens
3alpha-hydroxy-3beta-phenylpropyl-5alpha-androstan-17-one 0.003 mM, 97% inhibition Homo sapiens
3alpha-hydroxy-3beta-propyl-5alpha-androstan-17-one 0.003 mM, 94% inhibition, IC50: 67 nM Homo sapiens
3alpha-hydroxy-3beta-vinyl-5alpha-androstan-17-one 0.003 mM, 94% inhibition Homo sapiens
3alpha-methoxy-3beta-(2'-phenylethyl)-5alpha-androstan-17-one 0.003 mM, 95% inhibition, IC50: 73 nM Homo sapiens
3alpha-methoxy-3beta-(phenylmethyl)-5alpha-androstan-17-one 0.003 mM, 93% inhibition, IC50: 154 nM Homo sapiens
3alpha-methoxy-5alpha-androstan-17-one 0.003 mM, 94% inhibition Homo sapiens
3alpha-O-(spirotetrahydrofuran-2-yl)-5alpha-androstan-17-one 0.003 mM, 94% inhibition Homo sapiens
3alpha-propanoxy-3beta-(phenylmethyl)-5alpha-androstan-17-one 0.003 mM, 87% inhibition Homo sapiens
3alpha-propanoxy-5alpha-androstan-17-one 0.003 mM, 93% inhibition Homo sapiens
3beta,3alpha-O-(1'-oxo-1',3'-propanediyloxy)-5alpha-androstan-17-one 0.003 mM, 93% inhibition Homo sapiens
3beta-(2'-cyclohexylethyl)-3alpha-methoxy-5alpha-androstan-17-one 0.003 mM, 88% inhibition, IC50: 354 nM Homo sapiens
3beta-cyclohexyl-3alpha-hydroxy-5alpha-androstan-17-one 0.003 mM, 95% inhibition, IC50: 97 nM Homo sapiens
3beta-cyclohexylethyl-3alpha-hydroxy-5alpha-androstan-17-one 0.003 mM, 93% inhibition, IC50: 60 nM Homo sapiens
3beta-cyclohexylmethyl-3alpha-hydroxy-5alpha-androstan-17-one 0.003 mM, 95% inhibition, IC50: 87 nM Homo sapiens
3beta-dodecyl-3alpha-hydroxy-5alpha-androstan-17-one 0.003 mM, 77% inhibition Homo sapiens
3beta-hydroxy-3alpha-(3'-hydroxypropyl)-5alpha-androstan-17-one 0.003 mM, 17% inhibition Homo sapiens
3beta-hydroxy-3alpha-(prop-2'-enyl)-5alpha-androstan-17-one 0.003 mM, 36% inhibition Homo sapiens
3beta-hydroxy-3alpha-methyl-5alpha-androstan-17-one 0.003 mM, 16% inhibition Homo sapiens
3beta-hydroxy-3alpha-phenyl-5alpha-androstan-17-one 0.003 mM, 39% inhibition Homo sapiens
3beta-hydroxy-3alpha-phenylmethyl-5alpha-androstan-17-one 0.003 mM, 39% inhibition Homo sapiens
3beta-hydroxy-3alpha-propyl-5alpha-androstan-17-one 0.003 mM, 33% inhibition Homo sapiens
3beta-n-butyl-3alpha-hydroxy-5alpha-androstan-17-one 0.003 mM, 92% inhibition, IC50: 116 nM Homo sapiens
3beta-n-hexyl-3alpha-hydroxy-5alpha-androstan-17-one 0.003 mM, 95% inhibition, IC50: 100 nM Homo sapiens
3beta-s-butyl-3alpha-hydroxy-5alpha-androstan-17-one 0.003 mM, 90% inhibition, IC50: 73 nM Homo sapiens
3beta-tert-butyl-3alpha-hydroxy-5alpha-androstan-17-one 0.003 mM, 93% inhibition, IC50: 142 nM Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
androstenedione + NADPH + H+ Homo sapiens the enzyme is involved in biosynthesis of testosterone testosterone + NADP+
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
androstenedione + NADPH + H+
-
 Homo sapiens testosterone + NADP+
-
 ?
androstenedione + NADPH + H+ the enzyme is involved in biosynthesis of testosterone Homo sapiens testosterone + NADP+
-
 ?

Synonyms

Synonyms Comment Organism
type 3 17beta-hydroxysteroid dehydrogenase
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000057
-
 0.003 mM, 94% inhibition, IC50: 57 nM Homo sapiens 3alpha-hydroxy-3beta-phenylmethyl-5alpha-androstan-17-one
0.00006
-
 0.003 mM, 93% inhibition, IC50: 60 nM Homo sapiens 3beta-cyclohexylethyl-3alpha-hydroxy-5alpha-androstan-17-one
0.000067
-
 0.003 mM, 94% inhibition, IC50: 67 nM Homo sapiens 3alpha-hydroxy-3beta-propyl-5alpha-androstan-17-one
0.000073
-
 0.003 mM, 90% inhibition, IC50: 73 nM Homo sapiens 3beta-s-butyl-3alpha-hydroxy-5alpha-androstan-17-one
0.000073
-
 0.003 mM, 95% inhibition, IC50: 73 nM Homo sapiens 3alpha-methoxy-3beta-(2'-phenylethyl)-5alpha-androstan-17-one
0.000081
-
 0.003 mM, 95% inhibition, IC50: 81 nM Homo sapiens 3alpha-hydroxy-3'-phenyl-5alpha-androstan-17-one
0.000087
-
 0.003 mM, 95% inhibition, IC50: 87 nM Homo sapiens 3beta-cyclohexylmethyl-3alpha-hydroxy-5alpha-androstan-17-one
0.000097
-
 0.003 mM, 95% inhibition, IC50: 97 nM Homo sapiens 3beta-cyclohexyl-3alpha-hydroxy-5alpha-androstan-17-one
0.000099
-
 0.003 mM, 93% inhibition, IC50: 99 nM Homo sapiens 3alpha-hydroxy-3beta-phenylethyl-5alpha-androstan-17-one
0.0001
-
 0.003 mM, 95% inhibition, IC50: 100 nM Homo sapiens 3beta-n-hexyl-3alpha-hydroxy-5alpha-androstan-17-one
0.000116
-
 0.003 mM, 92% inhibition, IC50: 116 nM Homo sapiens 3beta-n-butyl-3alpha-hydroxy-5alpha-androstan-17-one
0.000142
-
 0.003 mM, 93% inhibition, IC50: 142 nM Homo sapiens 3beta-tert-butyl-3alpha-hydroxy-5alpha-androstan-17-one
0.000147
-
 0.003 mM, 92% inhibition, IC50: 147 nM Homo sapiens 3alpha-hydroxy-3beta-octyl-5alpha-androstan-17-one
0.000154
-
 0.003 mM, 93% inhibition, IC50: 154 nM Homo sapiens 3alpha-methoxy-3beta-(phenylmethyl)-5alpha-androstan-17-one
0.000352
-
 0.003 mM, 92% inhibition, IC50: 352 nM Homo sapiens 3alpha-ethoxy-3beta-(phenylmethyl)-5alpha-androstan-17-one
0.000354
-
 0.003 mM, 88% inhibition, IC50: 354 nM Homo sapiens 3beta-(2'-cyclohexylethyl)-3alpha-methoxy-5alpha-androstan-17-one