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Literature summary for 1.1.1.64 extracted from

  • Poirier, D.
    Inhibitors of 17beta-hydroxysteroid dehydrogenases (2003), Curr. Med. Chem., 10, 453-477.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3R,10S,13S)-3-(Adamantan-1-ylmethyl-butyl-amino)-3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one IC50: 80 nM Homo sapiens
(3R,10S,13S)-3-[(2-Cyclopentyl-ethyl)-morpholin-4-yl-amino]-3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one IC50: 74 nM Homo sapiens
(RS)-3(2,3,3-triphenyl-prop-2-enoxycarbonyl)-3(prop-2-ynyl)pyrrolidine-2,5-dione IC50: 0.0091 mM, reduction of androstenedione Homo sapiens
2,5-diphenyl-p-benzoquinone IC50: 0.0027 mM, reduction of androstenedione Homo sapiens
3-(4-Bromo-2-methyl-benzyl)-7-hydroxy-chroman-4-one IC50: 0.0083 mM, reduction of androstenedione Homo sapiens
3-(4-Chloro-2-methyl-benzyl)-7-hydroxy-chroman-4-one IC50: 0.0018 mM, reduction of androstenedione Homo sapiens
3-(4-Fluoro-2-methyl-benzyl)-7-hydroxy-chroman-4-one IC50: 0.007 mM, reduction of androstenedione Homo sapiens
3-cyclohexyl-3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
3-cyclohexylmethyl-3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
3-hexyl-3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
3-hydroxy-10,13-dimethyl-3-octyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
3-hydroxy-10,13-dimethyl-3-phenethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
3-hydroxy-10,13-dimethyl-3-phenyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
3b-Methyl-5a-androstan-3a-ol-17-on
-
Homo sapiens
3beta-cyclohexylethyl-androsterone IC50: 60 nM Homo sapiens
3beta-phenylmethyl-androsterone IC50: 57 nM Homo sapiens
3beta-propyl-androsterone IC50: 67 nM Homo sapiens
3beta-sec-butyl-androsterone IC50: 73 nM Homo sapiens
4-estrene-3,17-dione
-
Canis lupus familiaris
4-Methylumbelliferone IC50: 0.0009 mM, reduction of androstenedione Homo sapiens
5-androstene-3,17-dione
-
Canis lupus familiaris
7-hydroxyflavone IC50: 0.009 mM, reduction of androstenedione Homo sapiens
atamestane
-
Homo sapiens
baicalein IC50: 0.0093 mM, reduction of androstenedione Homo sapiens
Biochanin A IC50: 0.0108 mM, reduction of androstenedione Homo sapiens
Cyclopropanecarboxylic acid ((3R,10S,13S)-3-hydroxy-10,13-dimethyl-17-oxo-hexadecahydro-cyclopenta[a]phenanthren-3-yl)-octyl-amide IC50: 57 nM Homo sapiens
Cyclopropanecarboxylic acid cyclohexylmethyl-((3R,10S,13S)-3-hydroxy-10,13-dimethyl-17-oxo-hexadecahydro-cyclopenta[a]phenanthren-3-yl)-amide IC50: 85 nM Homo sapiens
heptanoic acid (1-{1-[(3-hydroxy-10,13-dimethyl-17-oxo-hexadecahydro-cyclopenta[a]phenanthren-3-ylmethyl)-carbamoyl]-2-phenyl-ethylcarbamoyl}-2-phenyl-ethyl)-amide IC50: 227 nM Homo sapiens
N-Adamantan-1-ylmethyl-N-((3R,10S,13S)-3-hydroxy-10,13-dimethyl-17-oxo-hexadecahydro-cyclopenta[a]phenanthren-3-yl)-butyramide IC50: 35-57 nM Homo sapiens
phenyl-p-benzoquinone IC50: 0.0057 mM, reduction of androstenedione Homo sapiens
S-petasin
-
Rattus norvegicus
umbelliferone IC50: 0.0014 mM, reduction of androstenedione Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.001
-
androstenedione
-
Homo sapiens
0.001
-
androstenedione
-
Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-
microsome
-
Canis lupus familiaris
-
-

Organism

Organism UniProt Comment Textmining
Canis lupus familiaris
-
-
-
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
Homo sapiens
-
testis
-
Homo sapiens
-
testis
-
Rattus norvegicus
-
testis
-
Canis lupus familiaris
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
androstenedione + NADPH + H+
-
Homo sapiens testosterone + NADP+
-
?
androstenedione + NADPH + H+
-
Rattus norvegicus testosterone + NADP+
-
?
androstenedione + NADPH + H+
-
Canis lupus familiaris testosterone + NADP+
-
?

Synonyms

Synonyms Comment Organism
type 3 17beta-HSD
-
Homo sapiens
type 3 17beta-HSD
-
Rattus norvegicus
type 3 17beta-HSD
-
Canis lupus familiaris

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Homo sapiens
NADP+
-
Rattus norvegicus
NADP+
-
Canis lupus familiaris
NADPH
-
Homo sapiens
NADPH
-
Rattus norvegicus
NADPH
-
Canis lupus familiaris

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0024
-
4-estrene-3,17-dione
-
Canis lupus familiaris
0.0068
-
5-androstene-3,17-dione
-
Canis lupus familiaris

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000035 0.000057 IC50: 35-57 nM Homo sapiens N-Adamantan-1-ylmethyl-N-((3R,10S,13S)-3-hydroxy-10,13-dimethyl-17-oxo-hexadecahydro-cyclopenta[a]phenanthren-3-yl)-butyramide
0.000057
-
IC50: 57 nM Homo sapiens 3beta-phenylmethyl-androsterone
0.000057
-
IC50: 57 nM Homo sapiens Cyclopropanecarboxylic acid ((3R,10S,13S)-3-hydroxy-10,13-dimethyl-17-oxo-hexadecahydro-cyclopenta[a]phenanthren-3-yl)-octyl-amide
0.00006
-
IC50: 60 nM Homo sapiens 3beta-cyclohexylethyl-androsterone
0.000067
-
IC50: 67 nM Homo sapiens 3beta-propyl-androsterone
0.000073
-
IC50: 73 nM Homo sapiens 3beta-sec-butyl-androsterone
0.000074
-
IC50: 74 nM Homo sapiens (3R,10S,13S)-3-[(2-Cyclopentyl-ethyl)-morpholin-4-yl-amino]-3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
0.00008
-
IC50: 80 nM Homo sapiens (3R,10S,13S)-3-(Adamantan-1-ylmethyl-butyl-amino)-3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
0.000085
-
IC50: 85 nM Homo sapiens Cyclopropanecarboxylic acid cyclohexylmethyl-((3R,10S,13S)-3-hydroxy-10,13-dimethyl-17-oxo-hexadecahydro-cyclopenta[a]phenanthren-3-yl)-amide
0.000227
-
IC50: 227 nM Homo sapiens heptanoic acid (1-{1-[(3-hydroxy-10,13-dimethyl-17-oxo-hexadecahydro-cyclopenta[a]phenanthren-3-ylmethyl)-carbamoyl]-2-phenyl-ethylcarbamoyl}-2-phenyl-ethyl)-amide
0.0009
-
IC50: 0.0009 mM, reduction of androstenedione Homo sapiens 4-Methylumbelliferone
0.0014
-
IC50: 0.0014 mM, reduction of androstenedione Homo sapiens umbelliferone
0.0018
-
IC50: 0.0018 mM, reduction of androstenedione Homo sapiens 3-(4-Chloro-2-methyl-benzyl)-7-hydroxy-chroman-4-one
0.0027
-
IC50: 0.0027 mM, reduction of androstenedione Homo sapiens 2,5-diphenyl-p-benzoquinone
0.0057
-
IC50: 0.0057 mM, reduction of androstenedione Homo sapiens phenyl-p-benzoquinone
0.007
-
IC50: 0.007 mM, reduction of androstenedione Homo sapiens 3-(4-Fluoro-2-methyl-benzyl)-7-hydroxy-chroman-4-one
0.0083
-
IC50: 0.0083 mM, reduction of androstenedione Homo sapiens 3-(4-Bromo-2-methyl-benzyl)-7-hydroxy-chroman-4-one
0.009
-
IC50: 0.009 mM, reduction of androstenedione Homo sapiens 7-hydroxyflavone
0.0091
-
IC50: 0.0091 mM, reduction of androstenedione Homo sapiens (RS)-3(2,3,3-triphenyl-prop-2-enoxycarbonyl)-3(prop-2-ynyl)pyrrolidine-2,5-dione
0.0093
-
IC50: 0.0093 mM, reduction of androstenedione Homo sapiens baicalein
0.0108
-
IC50: 0.0108 mM, reduction of androstenedione Homo sapiens Biochanin A