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Literature summary extracted from

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.51 11-[3-hydroxy-17-beta-hydroxyestr-5(10)-en-17alpha-yl-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-7-yl]-undecanoic acid butyl-methyl-amide selective inhibition of type 2 17beta-HSD Homo sapiens
1.1.1.51 13-cis-retinoic acid
-
Rattus norvegicus
1.1.1.51 17-hydroxy-7alpha-thioethyl-3-oxo-4-androstene-17alpha-propionic acid, gamma-lactone IC50 for reduction of androst-4-en-3,17-dione: 0.0009 mM Homo sapiens
1.1.1.51 17alpha-ethynyl-estradiol 0.01 mM, 54% inhibition, reaction with 0.002 mM estradiol; inhibits oxidation of testosterone Homo sapiens
1.1.1.51 17beta-dihydroequilin 0.01 mM, 88% inhibition, reaction with 0.002 mM estradiol Homo sapiens
1.1.1.51 2-hydroxy-estradiol 0.01 mM, 67% inhibition, reaction with 0.002 mM estradiol Homo sapiens
1.1.1.51 20alpha-dihydroprogesterone 0.01 mM, 71% inhibition, reaction with 0.002 mM estradiol, inhibits oxidation of testosterone Homo sapiens
1.1.1.51 3,4-dihydrobenzoic acid 0.001 mM, 40% inhibition, reduction of androst-4-en-3,17-dione Homo sapiens
1.1.1.51 3-hydroxy-1,3,5(10)-estratriene-17beta-O,17alpha-butanolactone selective for type 2 17beta-HSD versus types 1, 3, and 7 but not versus type 5 17beta-HSD Homo sapiens
1.1.1.51 3-oxo-17alpha-pregna-4-ene-7alpha-(benzylthia)-21,17-carbolactone IC50 for reduction of androst-4-en-3,17-dione: 0.00042 mM,IC50 for oxidation of testosterone: 0.001 mM Homo sapiens
1.1.1.51 3-oxo-17alpha-pregna-4-ene-7alpha-(phenylthia)-21,17-carbolactone IC50 for reduction of androst-4-en-3,17-dione: 0.001 mM Homo sapiens
1.1.1.51 3-oxo-17alpha-pregna-4-ene-7alpha-(propylthia)-21,17-carbolactone IC50 for reduction of androst-4-en-3,17-dione: 0.0011 mM; IC50 for reduction of androst-4-en-3,17-dione: 0.0014 mM Homo sapiens
1.1.1.51 3-oxo-17alpha-pregna-4-ene-7alpha-[4-[2-(1-piperidinyl)-ethoxy]benzylthia]-21,17-carbolactone IC50 for oxidation of testosterone: 0.0007 mM, no inhibition of type 1, 3 and 5 17beta-HSD, nor against P450 aromatase Homo sapiens
1.1.1.51 5alpha-androstane-3alpha,17beta-diol 0.01 mM, 87% inhibition, reaction with 0.002 mM estradiol Homo sapiens
1.1.1.51 5alpha-dihydrotestosterone inhibits oxidation of testosterone Homo sapiens
1.1.1.51 5beta-androstane-3alpha,17beta-diol 0.01 mM, 83% inhibition, reaction with 0.002 mM estradiol Homo sapiens
1.1.1.51 5beta-dihydrotestosterone inhibits oxidation of testosterone Homo sapiens
1.1.1.51 9-cis-retinoic acid weak Homo sapiens
1.1.1.51 9-cis-retinoic acid
-
Rattus norvegicus
1.1.1.51 danazol inhibits oxidation of testosterone, 0.01 mM, 83% inhibition Homo sapiens
1.1.1.51 estradiol inhibits oxidation of testosterone Homo sapiens
1.1.1.51 gallic acid 0.001 mM, 50% inhibition, reduction of androst-4-en-3,17-dione Homo sapiens
1.1.1.51 oleuropein glycoside 0.001 mM, 40% inhibition, reduction of androst-4-en-3,17-dione Homo sapiens
1.1.1.51 spiro-gamma-lactone-estradiol inhibits the reduction of androst-4-en-3,17-dione, reversible, IC50: 0.00025 mM Homo sapiens
1.1.1.51 spironolactone IC50 for oxidation of testosterone: 0.0011 mM Homo sapiens
1.1.1.51 testosterone 0.01 mM, 70% inhibition, reaction with 0.002 mM estradiol Homo sapiens
1.1.1.62 (S)-2-Methoxy-6a-methyl-5,6,6a,10,10a,10b,11,12-octahydro-4bH-7-oxa-8-aza-pentaleno[2,1-a]phenanthrene
-
Homo sapiens
1.1.1.62 (S)-6a-Methyl-5,6,6a,10,10a,10b,11,12-octahydro-4bH-7-oxa-8-aza-pentaleno[2,1-a]phenanthren-2-ol
-
Homo sapiens
1.1.1.62 1'(2')H-estra-1,3,5(10)-trieno[17,16-c]pyrazol-3-ol IC50: 0.0041 mM Homo sapiens
1.1.1.62 1,2-Cyclohexanedione 40 mM, pH 8.5, t1/2: 4.4 h Homo sapiens
1.1.1.62 1,3,5(10),16-estratetraen-3-ol
-
Homo sapiens
1.1.1.62 1,3,5(10)-estratrien-3,16beta,17beta-triol
-
Homo sapiens
1.1.1.62 1,3,5(10)-estratrien-3,16beta-diol
-
Homo sapiens
1.1.1.62 1,3,5(10)-estratrien-3,17alpha-diol
-
Homo sapiens
1.1.1.62 1,3,5(10)-estratrien-3-ol
-
Homo sapiens
1.1.1.62 1,4-dibromo-2,3-butanedione 40 mM, pH 8.5, t1/2: 0.02 h Homo sapiens
1.1.1.62 1,9-decanediol
-
Homo sapiens
1.1.1.62 1-Chloro-4-(2,2-dichloro-1-(5-Chloro-phenyl)-ethyl)-benzene oxidation of estradiol Homo sapiens
1.1.1.62 1-Chloro-4-(2,2-dichloro-1-(6-Chloro-phenyl)-ethyl)-benzene oxidation of estradiol Homo sapiens
1.1.1.62 1-phenyl-1,2-propanedione 40 mM, pH 8.5, t1/2: 0.19 h Homo sapiens
1.1.1.62 1-[2-[4-(6-Methoxy-2-phenyl-3,4-dihydro-naphthalen-1-yl)-phenoxy]-ethyl]-pyrrolidine oxidation of estradiol Homo sapiens
1.1.1.62 10-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-decanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester IC50: 140 nM Homo sapiens
1.1.1.62 11-((13S,17R)-17-Ethynyl-3,17-dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-7-yl)-undecanoic acid butyl-methyl-amide
-
Homo sapiens
1.1.1.62 16-difluoro-estradiol oxidation of estradiol Homo sapiens
1.1.1.62 16-methylen-estra-1,3,5(10)-triene-3,17beta-diol suicide inhibitor Homo sapiens
1.1.1.62 16-oxo-estrone 40 mM, pH 8.5, t1/2: 0.8-1 h, at pH 7.2 inhibition is competitive against estradiol and non-competitive against NAD+ Homo sapiens
1.1.1.62 16alpha-bromobutyl-estradiol
-
Homo sapiens
1.1.1.62 16alpha-bromopropyl-estradiol IC50: 0.00046 mM, reduction of estrone, the inhibitor is totally inactive against type 2 17beta-HSD and type type 1 17beta-HSD Homo sapiens
1.1.1.62 16beta-bromobutyl-estradiol
-
Homo sapiens
1.1.1.62 17(R,S)-14,15-secoestra-1,3,5(10)-trien-15-yne-3,17-diol suicide inhibitor Homo sapiens
1.1.1.62 17-(1-hydroxy-prop-2-ynyl)-10,13-dimethyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-cyclopenta[a]phenanthren-3-one suicide inhibitor Homo sapiens
1.1.1.62 17-deoxy-estradiol oxidation of estradiol Homo sapiens
1.1.1.62 2',4',4-trihydroxy-4'-chalcone IC50: 0.0338 mM Homo sapiens
1.1.1.62 2',4'-dihydroxy-chalcone IC50: 0.0346 mM Homo sapiens
1.1.1.62 2,3-Butanedione 40 mM, pH 8.5, t1/2: 2 h Homo sapiens
1.1.1.62 2,3-Pentanedione 40 mM, pH 8.5, t1/2: 5.3 h Homo sapiens
1.1.1.62 3',4',5,7-tetrahydroxy-flavone IC50: 0.0006 mM Homo sapiens
1.1.1.62 3',4',7-trihydroxy-isoflavone IC50: 0.0052 mM Homo sapiens
1.1.1.62 3,3',4',7-tetrahydroxy-flavone
-
Homo sapiens
1.1.1.62 3,5,7-trihydroxy-4'-methoxy-flavone IC50: 15 mM Homo sapiens
1.1.1.62 3,5,7-trihydroxy-flavone
-
Homo sapiens
1.1.1.62 3-hydroxyestra-1,3,5(10),7-tetraen-17-one IC50: 0.0019 mM, oxidation of estradiol Homo sapiens
1.1.1.62 3-methoxy-1'(2')H-estra-1,3,5(10)-trieno[17,16-c]pyrazole
-
Homo sapiens
1.1.1.62 3beta-hydroxy-5,16-androstadiene
-
Homo sapiens
1.1.1.62 3beta-hydroxy-5-androsten-16-one
-
Homo sapiens
1.1.1.62 4',5,7-trihydroxy-flavanone
-
Homo sapiens
1.1.1.62 4',5,7-trihydroxy-flavone IC50: 0.0003 mM Homo sapiens
1.1.1.62 4',5,7-trihydroxy-isoflavone IC50: 0.001 mM Homo sapiens
1.1.1.62 4',7-dihydroxy-isoflavone IC50: 0.01 mM Homo sapiens
1.1.1.62 4-hydroxychalcone IC50: 0.016 mM Homo sapiens
1.1.1.62 5,7-dihydroxy-4'-methoxy-flavone
-
Homo sapiens
1.1.1.62 5-androsten-3beta-ol
-
Homo sapiens
1.1.1.62 5-androstene-3beta,16beta-diol
-
Homo sapiens
1.1.1.62 7-hydroxy-flavanone IC50: 0.028 mM Homo sapiens
1.1.1.62 7-hydroxy-flavone IC50: 0.0009 mM Homo sapiens
1.1.1.62 8-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-octanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester IC50: 93 nM Homo sapiens
1.1.1.62 9-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-nonanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester IC50: 52 nM Homo sapiens
1.1.1.62 arachidonic acid 0.018 mM, complete inhibition, oxidation of estradiol Homo sapiens
1.1.1.62 Benzoic acid (13S,17R)-7-[10-(butyl-methyl-carbamoyl)-decyl]-17-ethynyl-17-hydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl ester
-
Homo sapiens
1.1.1.62 benzyl alcohol
-
Homo sapiens
1.1.1.62 coumestrol IC50: 0.0002 mM Homo sapiens
1.1.1.62 Cyclohexanol
-
Homo sapiens
1.1.1.62 Cyclopentanol
-
Homo sapiens
1.1.1.62 diethylstilbestrol oxidation of estradiol Homo sapiens
1.1.1.62 estrone oxidation of estradiol Homo sapiens
1.1.1.62 Glyoxal 40 mM, pH 8.5, t1/2: 29 h Homo sapiens
1.1.1.62 linoleic acid 0.018 mM, 58% inhibition, oxidation of estradiol Homo sapiens
1.1.1.62 linolenic acid 0.018 mM, 34% inhibition, oxidation of estradiol Homo sapiens
1.1.1.62 medrogestone although the inhibitor is not selective for the type 1 17beta-HSD, it is weakly active and has a mechanism that appears to be complex, it offers new possibilities in treatment of estrogen-dependent diseases Homo sapiens
1.1.1.62 N-n-butyl-N-methyl-11-(16'a-bromo-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
Homo sapiens
1.1.1.62 N-n-butyl-N-methyl-11-(16'a-chloro-3',17'a-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
Homo sapiens
1.1.1.62 N-n-butyl-N-methyl-11-(16'a-chloro-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
Homo sapiens
1.1.1.62 N-n-butyl-N-methyl-11-(16'a-fluoro-3',17'a-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
Homo sapiens
1.1.1.62 N-n-butyl-N-methyl-11-(16'a-fluoro-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
Homo sapiens
1.1.1.62 N-n-butyl-N-methyl-11-(16'a-iodo-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
Homo sapiens
1.1.1.62 N-n-Butyl-N-methyl-11-(3,17b-dihydroxyestra-1,3,5(10)-trien-7a-yl)undecanamide
-
Homo sapiens
1.1.1.62 nomegestrol acetate although the inhibitor is not selective for the type 1 17beta-HSD, it is weakly active and has a mechanism that appears to be complex, it offers new possibilities in treatment of estrogen-dependent diseases Homo sapiens
1.1.1.62 oleic acid 0.018 mM, complete inhibition, oxidation of estradiol Homo sapiens
1.1.1.62 phenol noncompetitive Homo sapiens
1.1.1.62 Phenylglyoxal 40 mM, pH 8.5, t1/2: 0.33 h Homo sapiens
1.1.1.62 testosterone weak Homo sapiens
1.1.1.62 tibolone although the inhibitor is not selective for the type 1 17beta-HSD, it is weakly active and has a mechanism that appears to be complex, it offers new possibilities in treatment of estrogen-dependent diseases Homo sapiens
1.1.1.64 (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
1.1.1.64 (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
1.1.1.64 (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
1.1.1.64 2,5-diphenyl-p-benzoquinone IC50: 0.0027 mM, reduction of androstenedione Homo sapiens
1.1.1.64 3-(4-Bromo-2-methyl-benzyl)-7-hydroxy-chroman-4-one IC50: 0.0083 mM, reduction of androstenedione Homo sapiens
1.1.1.64 3-(4-Chloro-2-methyl-benzyl)-7-hydroxy-chroman-4-one IC50: 0.0018 mM, reduction of androstenedione Homo sapiens
1.1.1.64 3-(4-Fluoro-2-methyl-benzyl)-7-hydroxy-chroman-4-one IC50: 0.007 mM, reduction of androstenedione Homo sapiens
1.1.1.64 3-cyclohexyl-3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
1.1.1.64 3-cyclohexylmethyl-3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
1.1.1.64 3-hexyl-3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
1.1.1.64 3-hydroxy-10,13-dimethyl-3-octyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
1.1.1.64 3-hydroxy-10,13-dimethyl-3-phenethyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
1.1.1.64 3-hydroxy-10,13-dimethyl-3-phenyl-hexadecahydro-cyclopenta[a]phenanthren-17-one
-
Homo sapiens
1.1.1.64 3b-Methyl-5a-androstan-3a-ol-17-on
-
Homo sapiens
1.1.1.64 3beta-cyclohexylethyl-androsterone IC50: 60 nM Homo sapiens
1.1.1.64 3beta-phenylmethyl-androsterone IC50: 57 nM Homo sapiens
1.1.1.64 3beta-propyl-androsterone IC50: 67 nM Homo sapiens
1.1.1.64 3beta-sec-butyl-androsterone IC50: 73 nM Homo sapiens
1.1.1.64 4-estrene-3,17-dione
-
Canis lupus familiaris
1.1.1.64 4-Methylumbelliferone IC50: 0.0009 mM, reduction of androstenedione Homo sapiens
1.1.1.64 5-androstene-3,17-dione
-
Canis lupus familiaris
1.1.1.64 7-hydroxyflavone IC50: 0.009 mM, reduction of androstenedione Homo sapiens
1.1.1.64 atamestane
-
Homo sapiens
1.1.1.64 baicalein IC50: 0.0093 mM, reduction of androstenedione Homo sapiens
1.1.1.64 Biochanin A IC50: 0.0108 mM, reduction of androstenedione Homo sapiens
1.1.1.64 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
1.1.1.64 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
1.1.1.64 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
1.1.1.64 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
1.1.1.64 phenyl-p-benzoquinone IC50: 0.0057 mM, reduction of androstenedione Homo sapiens
1.1.1.64 S-petasin
-
Rattus norvegicus
1.1.1.64 umbelliferone IC50: 0.0014 mM, reduction of androstenedione Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.62 0.0022
-
3-methyl-O-estradiol
-
Homo sapiens
1.1.1.62 0.004
-
estradiol
-
Homo sapiens
1.1.1.64 0.001
-
androstenedione
-
Homo sapiens
1.1.1.64 0.001
-
androstenedione
-
Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.1.1.51 microsome
-
Homo sapiens
-
-
1.1.1.62 cytosol
-
Homo sapiens 5829
-
1.1.1.62 microsome
-
Homo sapiens
-
-
1.1.1.64 microsome
-
Homo sapiens
-
-
1.1.1.64 microsome
-
Canis lupus familiaris
-
-

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.51 Homo sapiens
-
-
-
1.1.1.51 Rattus norvegicus
-
-
-
1.1.1.62 Homo sapiens
-
-
-
1.1.1.64 Canis lupus familiaris
-
-
-
1.1.1.64 Homo sapiens
-
-
-
1.1.1.64 Rattus norvegicus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.51 A-431 cell derived from an epidermoid carcinoma of the vulva Homo sapiens
-
1.1.1.51 HEK-293 cell
-
Homo sapiens
-
1.1.1.51 liver
-
Homo sapiens
-
1.1.1.51 liver
-
Rattus norvegicus
-
1.1.1.51 placenta
-
Homo sapiens
-
1.1.1.62 placenta
-
Homo sapiens
-
1.1.1.62 T-47D cell
-
Homo sapiens
-
1.1.1.64 HEK-293 cell
-
Homo sapiens
-
1.1.1.64 testis
-
Homo sapiens
-
1.1.1.64 testis
-
Rattus norvegicus
-
1.1.1.64 testis
-
Canis lupus familiaris
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.51 estradiol + NAD(P)+
-
Homo sapiens estrone + NAD(P)H
-
?
1.1.1.51 estradiol + NAD(P)+
-
Rattus norvegicus estrone + NAD(P)H
-
?
1.1.1.51 testosterone + NAD(P)+
-
Homo sapiens androst-4-en-3,17-dione + NAD(P)H + H+
-
r
1.1.1.51 testosterone + NAD(P)+
-
Rattus norvegicus androst-4-en-3,17-dione + NAD(P)H + H+
-
r
1.1.1.62 3-methyl-O-estradiol + NAD(P)+
-
Homo sapiens 3-methyl-O-estrone + NAD(P)H
-
?
1.1.1.62 estradiol + NAD(P)+
-
Homo sapiens estrone + NAD(P)H
-
?
1.1.1.64 androstenedione + NADPH + H+
-
Homo sapiens testosterone + NADP+
-
?
1.1.1.64 androstenedione + NADPH + H+
-
Rattus norvegicus testosterone + NADP+
-
?
1.1.1.64 androstenedione + NADPH + H+
-
Canis lupus familiaris testosterone + NADP+
-
?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.51 type 2 17beta-HSD
-
Homo sapiens
1.1.1.51 type 2 17beta-HSD
-
Rattus norvegicus
1.1.1.62 type 1 17beta-HSD
-
Homo sapiens
1.1.1.64 type 3 17beta-HSD
-
Homo sapiens
1.1.1.64 type 3 17beta-HSD
-
Rattus norvegicus
1.1.1.64 type 3 17beta-HSD
-
Canis lupus familiaris

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.51 NAD+
-
Homo sapiens
1.1.1.51 NAD+
-
Rattus norvegicus
1.1.1.51 NADH
-
Homo sapiens
1.1.1.51 NADH
-
Rattus norvegicus
1.1.1.51 NADP+
-
Homo sapiens
1.1.1.51 NADP+
-
Rattus norvegicus
1.1.1.51 NADPH
-
Homo sapiens
1.1.1.51 NADPH
-
Rattus norvegicus
1.1.1.62 NAD(P)+
-
Homo sapiens
1.1.1.62 NAD(P)H
-
Homo sapiens
1.1.1.64 NADP+
-
Homo sapiens
1.1.1.64 NADP+
-
Rattus norvegicus
1.1.1.64 NADP+
-
Canis lupus familiaris
1.1.1.64 NADPH
-
Homo sapiens
1.1.1.64 NADPH
-
Rattus norvegicus
1.1.1.64 NADPH
-
Canis lupus familiaris

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.51 0.0003
-
17alpha-ethynyl-estradiol
-
Homo sapiens
1.1.1.51 0.0006
-
danazol
-
Homo sapiens
1.1.1.51 0.0008
-
estradiol
-
Homo sapiens
1.1.1.51 0.0024
-
13-cis-retinoic acid
-
Rattus norvegicus
1.1.1.51 0.0041
-
9-cis-retinoic acid
-
Rattus norvegicus
1.1.1.62 0.00004
-
1,3,5(10)-estratrien-3-ol
-
Homo sapiens
1.1.1.62 0.00017
-
1,3,5(10),16-estratetraen-3-ol
-
Homo sapiens
1.1.1.62 0.00019
-
17-deoxy-estradiol
-
Homo sapiens
1.1.1.62 0.00022
-
1-Chloro-4-(2,2-dichloro-1-(6-Chloro-phenyl)-ethyl)-benzene
-
Homo sapiens
1.1.1.62 0.0004
-
estrone
-
Homo sapiens
1.1.1.62 0.00061
-
1-[2-[4-(6-Methoxy-2-phenyl-3,4-dihydro-naphthalen-1-yl)-phenoxy]-ethyl]-pyrrolidine
-
Homo sapiens
1.1.1.62 0.0008
-
diethylstilbestrol
-
Homo sapiens
1.1.1.62 0.0008
-
1,3,5(10)-estratrien-3,16beta-diol
-
Homo sapiens
1.1.1.62 0.0011
-
1,3,5(10)-estratrien-3,16beta,17beta-triol
-
Homo sapiens
1.1.1.62 0.0018
-
3beta-hydroxy-5,16-androstadiene
-
Homo sapiens
1.1.1.62 0.0022
-
1,3,5(10)-estratrien-3,17alpha-diol
-
Homo sapiens
1.1.1.62 0.0025
-
16-difluoro-estradiol
-
Homo sapiens
1.1.1.62 0.0028
-
1-Chloro-4-(2,2-dichloro-1-(5-Chloro-phenyl)-ethyl)-benzene
-
Homo sapiens
1.1.1.62 0.0033
-
diethylstilbestrol
-
Homo sapiens
1.1.1.62 0.0037
-
estrone
-
Homo sapiens
1.1.1.62 0.006
-
5-androsten-3beta-ol
-
Homo sapiens
1.1.1.62 0.0095
-
1'(2')H-estra-1,3,5(10)-trieno[17,16-c]pyrazol-3-ol
-
Homo sapiens
1.1.1.62 0.0128
-
3-methoxy-1'(2')H-estra-1,3,5(10)-trieno[17,16-c]pyrazole
-
Homo sapiens
1.1.1.62 0.0255
-
5-androstene-3beta,16beta-diol
-
Homo sapiens
1.1.1.62 0.0368
-
3beta-hydroxy-5-androsten-16-one
-
Homo sapiens
1.1.1.62 0.0694
-
(S)-6a-Methyl-5,6,6a,10,10a,10b,11,12-octahydro-4bH-7-oxa-8-aza-pentaleno[2,1-a]phenanthren-2-ol
-
Homo sapiens
1.1.1.62 0.4245
-
(S)-2-Methoxy-6a-methyl-5,6,6a,10,10a,10b,11,12-octahydro-4bH-7-oxa-8-aza-pentaleno[2,1-a]phenanthrene
-
Homo sapiens
1.1.1.62 0.7
-
phenol
-
Homo sapiens
1.1.1.62 2
-
1,9-decanediol
-
Homo sapiens
1.1.1.62 9
-
Cyclohexanol
-
Homo sapiens
1.1.1.62 10
-
benzyl alcohol
-
Homo sapiens
1.1.1.62 37
-
Cyclopentanol
-
Homo sapiens
1.1.1.64 0.0024
-
4-estrene-3,17-dione
-
Canis lupus familiaris
1.1.1.64 0.0068
-
5-androstene-3,17-dione
-
Canis lupus familiaris

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.51 0.00025
-
inhibits the reduction of androst-4-en-3,17-dione, reversible, IC50: 0.00025 mM Homo sapiens spiro-gamma-lactone-estradiol
1.1.1.51 0.0007
-
IC50 for oxidation of testosterone: 0.0007 mM, no inhibition of type 1, 3 and 5 17beta-HSD, nor against P450 aromatase Homo sapiens 3-oxo-17alpha-pregna-4-ene-7alpha-[4-[2-(1-piperidinyl)-ethoxy]benzylthia]-21,17-carbolactone
1.1.1.51 0.0009
-
IC50 for reduction of androst-4-en-3,17-dione: 0.0009 mM Homo sapiens 17-hydroxy-7alpha-thioethyl-3-oxo-4-androstene-17alpha-propionic acid, gamma-lactone
1.1.1.51 0.001
-
IC50 for reduction of androst-4-en-3,17-dione: 0.00042 mM,IC50 for oxidation of testosterone: 0.001 mM Homo sapiens 3-oxo-17alpha-pregna-4-ene-7alpha-(benzylthia)-21,17-carbolactone
1.1.1.51 0.001
-
IC50 for reduction of androst-4-en-3,17-dione: 0.001 mM Homo sapiens 3-oxo-17alpha-pregna-4-ene-7alpha-(phenylthia)-21,17-carbolactone
1.1.1.51 0.0011
-
IC50 for oxidation of testosterone: 0.0011 mM Homo sapiens spironolactone
1.1.1.51 0.0011
-
IC50 for reduction of androst-4-en-3,17-dione: 0.0011 mM Homo sapiens 3-oxo-17alpha-pregna-4-ene-7alpha-(propylthia)-21,17-carbolactone
1.1.1.51 0.0014
-
IC50 for reduction of androst-4-en-3,17-dione: 0.0014 mM Homo sapiens 3-oxo-17alpha-pregna-4-ene-7alpha-(propylthia)-21,17-carbolactone
1.1.1.62 0.000052
-
IC50: 52 nM Homo sapiens 9-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-nonanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester
1.1.1.62 0.000093
-
IC50: 93 nM Homo sapiens 8-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-octanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester
1.1.1.62 0.00014
-
IC50: 140 nM Homo sapiens 10-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-decanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester
1.1.1.62 0.0002
-
IC50: 0.0002 mM Homo sapiens coumestrol
1.1.1.62 0.0003
-
IC50: 0.0003 mM Homo sapiens 4',5,7-trihydroxy-flavone
1.1.1.62 0.00046
-
IC50: 0.00046 mM, reduction of estrone, the inhibitor is totally inactive against type 2 17beta-HSD and type type 1 17beta-HSD Homo sapiens 16alpha-bromopropyl-estradiol
1.1.1.62 0.0006
-
IC50: 0.0006 mM Homo sapiens 3',4',5,7-tetrahydroxy-flavone
1.1.1.62 0.0009
-
IC50: 0.0009 mM Homo sapiens 7-hydroxy-flavone
1.1.1.62 0.001
-
IC50: 0.001 mM Homo sapiens 4',5,7-trihydroxy-isoflavone
1.1.1.62 0.0019
-
IC50: 0.0019 mM, oxidation of estradiol Homo sapiens 3-hydroxyestra-1,3,5(10),7-tetraen-17-one
1.1.1.62 0.0041
-
IC50: 0.0041 mM Homo sapiens 1'(2')H-estra-1,3,5(10)-trieno[17,16-c]pyrazol-3-ol
1.1.1.62 0.0052
-
IC50: 0.0052 mM Homo sapiens 3',4',7-trihydroxy-isoflavone
1.1.1.62 0.01
-
IC50: 0.01 mM Homo sapiens 4',7-dihydroxy-isoflavone
1.1.1.62 0.016
-
IC50: 0.016 mM Homo sapiens 4-hydroxychalcone
1.1.1.62 0.028
-
IC50: 0.028 mM Homo sapiens 7-hydroxy-flavanone
1.1.1.62 0.0338
-
IC50: 0.0338 mM Homo sapiens 2',4',4-trihydroxy-4'-chalcone
1.1.1.62 0.0346
-
IC50: 0.0346 mM Homo sapiens 2',4'-dihydroxy-chalcone
1.1.1.62 15
-
IC50: 15 mM Homo sapiens 3,5,7-trihydroxy-4'-methoxy-flavone
1.1.1.64 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
1.1.1.64 0.000057
-
IC50: 57 nM Homo sapiens 3beta-phenylmethyl-androsterone
1.1.1.64 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
1.1.1.64 0.00006
-
IC50: 60 nM Homo sapiens 3beta-cyclohexylethyl-androsterone
1.1.1.64 0.000067
-
IC50: 67 nM Homo sapiens 3beta-propyl-androsterone
1.1.1.64 0.000073
-
IC50: 73 nM Homo sapiens 3beta-sec-butyl-androsterone
1.1.1.64 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
1.1.1.64 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
1.1.1.64 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
1.1.1.64 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
1.1.1.64 0.0009
-
IC50: 0.0009 mM, reduction of androstenedione Homo sapiens 4-Methylumbelliferone
1.1.1.64 0.0014
-
IC50: 0.0014 mM, reduction of androstenedione Homo sapiens umbelliferone
1.1.1.64 0.0018
-
IC50: 0.0018 mM, reduction of androstenedione Homo sapiens 3-(4-Chloro-2-methyl-benzyl)-7-hydroxy-chroman-4-one
1.1.1.64 0.0027
-
IC50: 0.0027 mM, reduction of androstenedione Homo sapiens 2,5-diphenyl-p-benzoquinone
1.1.1.64 0.0057
-
IC50: 0.0057 mM, reduction of androstenedione Homo sapiens phenyl-p-benzoquinone
1.1.1.64 0.007
-
IC50: 0.007 mM, reduction of androstenedione Homo sapiens 3-(4-Fluoro-2-methyl-benzyl)-7-hydroxy-chroman-4-one
1.1.1.64 0.0083
-
IC50: 0.0083 mM, reduction of androstenedione Homo sapiens 3-(4-Bromo-2-methyl-benzyl)-7-hydroxy-chroman-4-one
1.1.1.64 0.009
-
IC50: 0.009 mM, reduction of androstenedione Homo sapiens 7-hydroxyflavone
1.1.1.64 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
1.1.1.64 0.0093
-
IC50: 0.0093 mM, reduction of androstenedione Homo sapiens baicalein
1.1.1.64 0.0108
-
IC50: 0.0108 mM, reduction of androstenedione Homo sapiens Biochanin A