1.1.1.62: 17beta-estradiol 17-dehydrogenase

This is an abbreviated version, for detailed information about 17beta-estradiol 17-dehydrogenase, go to the full flat file.

Reaction

17beta-estradiol
+
NAD(P)+
=
estrone
+
NAD(P)H
+
H+

Synonyms

(17beta-HSD) type 1, (17beta-HSD) type 2, 17-beta-HSD 2, 17-beta-hydroxysteroid dehydrogenase type 12, 17-beta-hydroxysteroid dehydrogenase type 2, 17-HOR, 17-HSD, 17beta HSD1, 17beta,20alpha-hydroxysteroid dehydrogenase, 17beta-estradiol dehydrogenase, 17beta-HSD, 17beta-HSD I, 17beta-HSD type 1, 17beta-HSD type 12, 17beta-HSD type 2, 17beta-HSD type 4, 17beta-HSD type 5, 17beta-HSD type 7, 17beta-HSD type 8, 17beta-HSD1, 17beta-HSD12, 17beta-HSD2, 17beta-HSD4, 17beta-HSD5, 17beta-HSD7 2, 17beta-HSDcl, 17beta-hydroxysteroid dehydrogenase, 17beta-hydroxysteroid dehydrogenase 4, 17beta-hydroxysteroid dehydrogenase type 1, 17beta-hydroxysteroid dehydrogenase type 12, 17beta-hydroxysteroid dehydrogenase type 2, 17beta-hydroxysteroid dehydrogenase type 4, 17beta-hydroxysteroid dehydrogenase type 5, 17beta-hydroxysteroid dehydrogenase type 6, 17beta-hydroxysteroid dehydrogenase type 7, 17beta-hydroxysteroid dehydrogenase type 8, 17beta-hydroxysteroid dehydrogenase type I, 17beta-hydroxysteroid dehydrogenase types 1, 17beta-hydroxysteroid dehydrogenases type 1, 17betaHSD, 17betaHSD1, 17betaHSD14, 17betaHSD6, 17HSD1, 20 alpha-hydroxysteroid dehydrogenase, 20-alpha-HSD, 20alpha-hydroxysteroid dehydrogenase, 3beta-HSD, 3beta-hydroxysteroid dehydrogenase, 3betaHSD, 7beta-HSD type 1, AKR1C1, AKR1C2, AKR1C3, AKR1C4, dehydrogenase, estradiol 17beta-, E2DH, EDH, estradiol 17beta-dehydrogenase, estradiol dehydrogenase, estrogen 17-oxidoreductase, estrogenic 17beta-hydroxysteroid dehydrogenase, form 2 type 7 17beta-hydroxysteroid dehydrogenase, HSD17B1, HSD17B12, HSD17B2, HSD17B4, hydroxysteroid (17-beta) dehydrogenase 1, Ke6 protein, mf17beta-HSD12, microsomal 17-beta-hydroxysteroid dehydrogenase, More, oestradiol-17beta hydroxysteroid dehydrogenase, placental 17-beta-hydroxysteroid dehydrogenase, PRAP, PRL receptor associated protein, testicular 17-beta-hydroxysteroid dehydrogenase, type 1 17beta-HSD, type 1 17beta-hydroxysteroid dehydrogenase, type 12 17beta-HSD, type 12 17beta-hydroxysteroid dehydrogenase, type 7 17beta-hydroxysteroid dehydrogenase, type 8 17beta-HSD, type 8 17beta-hydroxysteroid dehydrogenase

ECTree

     1 Oxidoreductases
         1.1 Acting on the CH-OH group of donors
             1.1.1 With NAD+ or NADP+ as acceptor
                1.1.1.62 17beta-estradiol 17-dehydrogenase

Inhibitors

Inhibitors on EC 1.1.1.62 - 17beta-estradiol 17-dehydrogenase

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INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(10R,13S,17R)-10,13-dimethyl-1,2,7,8,9,10,11,12,13,14,15,16-dodecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5',6(4'H)-trione
-
0.003 mM, 45% inhibition, substrate: 4-androstene-3,17-dione
(10R,13S,17R)-10,13-dimethyl-1,6,7,8,9,10,11,12,13,14,15,16-dodecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H,4'H)-dione
-
0.003 mM, 61% inhibition, substrate: 4-androstene-3,17-dione; 0.003 mM, 63% inhibition, substrate: 4-androstene-3,17-dione
(13S,17R)-13-methyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'-diol
-
0.003 mM, 61% inhibition, substrate: 4-androstene-3,17-dione
(13S,17R)-3-hydroxy-13-methyl-3',4',6,7,8,9,11,12,13,14,15,16-dodecahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-5'-one
-
0.003 mM, 79% inhibition, substrate: 4-androstene-3,17-dione
(13S,17R)-3-hydroxy-13-methyl-5'-propyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 83% inhibition, substrate: 4-androstene-3,17-dione
(13S,17R)-3-hydroxy-5',13-dimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 94% inhibition, substrate: 4-androstene-3,17-dione
(13S,17R)-5',13-dimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 94% inhibition, substrate: 4-androstene-3,17-dione
(13S,17R)-5',5',13-trimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 95% inhibition, substrate: 4-androstene-3,17-dione
(13S,17S)-13-methyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 95% inhibition, substrate: 4-androstene-3,17-dione
(13S,17S)-3-hydroxy-13-methyl-3',4',6,7,8,9,11,12,13,14,15,16-dodecahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-5'-one
-
0.003 mM, 45% inhibition, substrate: 4-androstene-3,17-dione
(13S,17S)-3-hydroxy-13-methyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 95% inhibition, substrate: 4-androstene-3,17-dione
(13S,17S)-3-hydroxy-13-methyl-6,7,8,9,11,12,13,14,15,16-decahydro-7'H-spiro[cyclopenta[a]phenanthrene-17,2'-oxepan]-7'-one
-
0.003 mM, 93% inhibition, substrate: 4-androstene-3,17-dione
(15alpha)-3-hydroxy-N-(5-methyl-1,3-thiazol-2-yl)-17-oxoestra-1(10),2,4-triene-15-carboxamide
-
-
(15beta)-15-(4-morpholin-4-yl-4-oxobutyl)-17-oxoestra-1(10),2,4-trien-3-yl sulfamate
-
0.0001 mM, 10% inhibition
(15beta)-3-hydroxy-15-(3-hydroxypropyl)estra-1(10),2,4-trien-17-one
-
-
(15beta)-3-hydroxy-15-(5-hydroxypentyl)estra-1(10),2,4-trien-17-one
-
-
(16alpa,17beta)-16-(3-bromopropyl)estra-1(10),2,4-triene-3,17-diol
-
EM-251
(16alpha)-2-chloro-16-fluoro-3-hydroxyestra-1(10),2,4-trien-17-one
-
-
(16alpha)-3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carbonitrile
-
-
(16beta)-16-(ethoxymethyl)-3-hydroxyestra-1(10),2,4-trien-17-one
-
-
(16beta)-2-chloro-16-fluoro-3-hydroxyestra-1(10),2,4-trien-17-one
-
-
(16beta)-3-hydroxy-16-methyl-17-oxoestra-1(10),2,4-triene-16-carbonitrile
-
-
(16beta)-3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carbonitrile
-
-
(16Z)-3-hydroxy-16-(2,2,2-trifluoro-1-hydroxyethylidene)estra-1(10),2,4-trien-17-one
-
-
(16Z)-3-hydroxy-16-(hydroxymethylidene)estra-1(10),2,4-trien-17-one
-
-
(17beta)-3,17-dihydroxy-N-(pyridin-3-ylmethyl)estra-1(10),2,4-triene-16-carboxamide
-
-
(17E)-3-hydroxyestra-1(10),2,4-trien-17-one oxime
-
-
(17Z)-3-hydroxyestra-1(10),2,4-triene-16,17-dione dioxime
-
-
(1Z)-N'-[[(3,5-dimethylisoxazol-4-yl)carbonyl]oxy]-2-[4-(1,2,3-thiadiazol-4-yl)phenyl]ethanimidamide
-
-
(2'R,13S)-3-hydroxy-13-methyl-6,7,8,9,11,12,13,14,15,16-decahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 92% inhibition, substrate: 4-androstene-3,17-dione
(2'R,13S)-3-hydroxy-4',13-dimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 94% inhibition, substrate: 4-androstene-3,17-dione
(2'R,13S)-3-hydroxy-5',5',13-trimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 94% inhibition, substrate: 4-androstene-3,17-dione
(2'R,13S)-5'-cyclopropyl-3-hydroxy-13-methyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 91% inhibition, substrate: 4-androstene-3,17-dione
(2'R,13S)-methyl 3-hydroxy-13-methyl-6'-oxo-3',4',5',6,6',7,8,9,11,12,13,14,15,16-tetradecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-5'-carboxylate
-
0.003 mM, 92% inhibition, substrate: 4-androstene-3,17-dione
(2,4-dihydroxyphenyl)-phenylmethanone
-
-
(2E)-3-[2-hydroxy-6-(3-hydroxyphenyl)-1-naphthyl]-N-methylacrylamide
-
58% inhibition at 0.001 mM
(2E)-3-[2-hydroxy-6-(3-hydroxyphenyl)-1-naphthyl]-N-phenylacrylamide
-
60% inhibition at 0.001 mM
(2R,4aS,4bR,10bS,12aS)-9-chloro-2-fluoro-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
-
(2S,4aS,4bR,10bS,12aS)-9-chloro-2-fluoro-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
-
(2Z,2'E)-N,N'-1H-1,5-benzodiazepine-2,4-diylbis(3-phenylprop-2-enamide)
-
30% inhibition at 0.006 mM
(3-amino-5-[13-[(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]tridecyl]phenyl)acetic acid
-
-
(3-[(4-aminophenyl)carbonyl]-5-[13-[(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]tridecyl]phenyl)acetic acid
-
-
(3-[13-[(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]tridecyl]phenyl)acetic acid
-
-
(3alpha,7alpha,17beta)-17-ethynyl-7-methylestr-5(10)-ene-3,17-diol
-
-
(3beta,7alpha,17beta)-17-ethynyl-7-methylestr-5(10)-ene-3,17-diol
-
-
(4aS,4bR,10bS,12aS)-8-hydroxy-12a-methyl-9-(2-phenylethyl)-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
-
(4aS,4bR,10bS,12aS)-8-hydroxy-12a-methyl-9-prop-2-en-1-yl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
-
(4aS,4bR,10bS,12aS)-8-hydroxy-9-iodo-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
-
(4aS,4bR,10bS,12aS)-8-hydroxy-9-methoxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
-
(4aS,4bR,10bS,12aS)-9-bromo-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
-
(4aS,4bR,10bS,12aS)-9-chloro-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
-
(6-hydroxy-1,3-benzothiazol-2-yl)(3-hydroxyphenyl)methanone
-
modeling of binding to crystal structure shows five hydrogen bond interactions and a cation-pi-interaction
(6aS)-2-(benzyloxy)-6a-methyl-9-[(2E)-4-morpholin-4-yl-4-oxobut-2-en-1-yl]-5,6,6a,10,10a,10b,11,12-octahydro-4bH-naphtho[2',1':4,5]indeno[2,1-d]isoxazole
-
0.0001 mM, 21% inhibition
(6aS)-2-hydroxy-6a,8-dimethyl-5,6,6a,7,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-9(4bH)-one
-
0.01 mM, 32% inhibition
(6aS)-2-hydroxy-6a-methyl-5,6,6a,7,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-9(4bH)-one
-
0.01 mM, 86% inhibition
(6aS)-2-hydroxy-6a-methyl-N-(2-pyridin-3-ylethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-2-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-3-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
(6aS)-2-hydroxy-6a-methyl-N-[(1-methyl-1H-pyrrol-2-yl)methyl]-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
-
0.01 mM, 90% inhibition, IC50: 0.0023 mM
(6aS)-2-hydroxy-6a-methyl-N-[(5-methylpyrazin-2-yl)methyl]-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
-
0.01 mM, 80% inhibition
(6aS)-3-ethyl-2-hydroxy-6a-methyl-N-(2-pyridin-3-ylethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
-
-
(6aS)-6a-methyl-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-2-ol
-
-
(6aS)-6a-methyl-9-(4-morpholin-4-yl-4-oxobutyl)-4b,5,6,6a,7,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-2-ol
-
0.0001 mM, 53% inhibition
(6aS)-6a-methyl-9-(trifluoromethyl)-4b,6,6a,7,9a,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-2,6b(5H)-diol
-
-
(6aS)-8-(2-methoxyethyl)-6a-methyl-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-2-ol
-
-
(6aS)-9-(hydroxymethyl)-6a-methyl-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-2-ol
-
-
(6aS,6bR,10aR)-2-hydroxy-6a-methyl-5,6,6a,6b,9,10,10a,11,11a,11b,12,13-dodecahydronaphtho[2',1':4,5]indeno[1,2-b]pyran-8(4bH)-one
-
0.003 mM, 52% inhibition, substrate: 4-androstene-3,17-dione
(6aS,6bS,10aS)-2-hydroxy-6a-methyl-5,6,6a,6b,9,10,10a,11,11a,11b,12,13-dodecahydronaphtho[2',1':4,5]indeno[1,2-b]pyran-8(4bH)-one
-
0.003 mM, 85% inhibition, substrate: 4-androstene-3,17-dione
(6aS,6bS,11aS)-2-hydroxy-6a-methyl-4b,5,6,6a,6b,9,10,11,11a,12,12a,12b,13,14-tetradecahydro-8H-naphtho[2',1':4,5]indeno[1,2-b]oxepin-8-one
-
0.003 mM, 91% inhibition, substrate: 4-androstene-3,17-dione
(6aS,6bS,9aR)-2-hydroxy-6a-methyl-4b,5,6,6a,6b,9,9a,10,10a,10b,11,12-dodecahydro-8H-naphtho[2',1':4,5]indeno[1,2-b]furan-8-one
-
0.003 mM, 62% inhibition, substrate: 4-androstene-3,17-dione
(6beta,17beta)-6-(hexylsulfanyl)estra-1(10),2,4-triene-3,17-diol
-
-
(6Z,17E)-3-hydroxyestra-1(10),2,4-triene-6,17-dione dioxime
-
-
(7alpha,17beta)-17-ethynyl-17-hydroxy-7-methylestr-4-en-3-one
-
-
(S)-2-Methoxy-6a-methyl-5,6,6a,10,10a,10b,11,12-octahydro-4bH-7-oxa-8-aza-pentaleno[2,1-a]phenanthrene
-
-
(S)-6a-Methyl-5,6,6a,10,10a,10b,11,12-octahydro-4bH-7-oxa-8-aza-pentaleno[2,1-a]phenanthren-2-ol
-
-
1'(2')H-estra-1,3,5(10)-trieno[17,16-c]pyrazol-3-ol
-
IC50: 0.0041 mM
1,1':4',1''-terphenyl-3,3''-diol
-
-
1,2-Cyclohexanedione
-
40 mM, pH 8.5, t1/2: 4.4 h
1,3,5(10),16-estratetraen-3-ol
-
-
1,3,5(10)-estratrien-3,16beta,17beta-triol
-
-
1,3,5(10)-estratrien-3,16beta-diol
-
-
1,3,5(10)-estratrien-3,17alpha-diol
-
-
1,3,5(10)-estratrien-3-ol
-
-
1,4-dibromo-2,3-butanedione
-
40 mM, pH 8.5, t1/2: 0.02 h
1,9-decanediol
-
-
1-(3'-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
1-(3-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
1-(4'-hydroxy-2'-methyl-biphenyl-4-yl)-ethanone
-
89% inhibition at 0.001 mM
1-(4'-hydroxy-2'_methyl-biphenyl-4-yl)-ethanone
-
37C, 0.01 mM, 89% inhibition, substrate: estrone, 7beta-HSD type 1
1-(4'-hydroxy-biphenyl-4-yl)-ethanone
-
37C, 01 mM, 97% inhibition, substrate: estrone, 7beta-HSD type 1; 97% inhibition at 0.001 mM
1-(4-fluorophenyl)-3-[4-(1,2,3-thiadiazol-4-yl)benzyl]urea
-
-
1-(4-hydroxy-phenyl)-butan-1-one
-
weak inhibitor with 35.1% inhibition at 0.1 mM
1-(4-hydroxy-phenyl)-decan-1-one
-
weak inhibitor with 28.2% inhibition at 0.1 mM
1-(4-hydroxy-phenyl)-dodecan-1-one
-
weak inhibitor with 42.5% inhibition at 0.1 mM
1-(4-hydroxy-phenyl)-ethanone
-
weak inhibitor with 20.8% inhibition at 0.1 mM
1-(4-hydroxy-phenyl)-heptan-1-one
-
weak inhibitor with 47.6% inhibition at 0.1 mM
1-(4-hydroxy-phenyl)-hexan-1-one
-
weak inhibitor with 45.7% inhibition at 0.1 mM
1-(4-hydroxy-phenyl)-octan-1-one
-
weak inhibitor with 36.9% inhibition at 0.1 mM
1-(4-hydroxy-phenyl)-pentan-1-one
-
weak inhibitor with 39.8% inhibition at 0.1 mM
1-(4-hydroxy-phenyl)-propan-1-one
-
weak inhibitor with 17.5% inhibition at 0.1 mM
1-(4-hydroxy-phenyl)-undecan-1-one
-
weak inhibitor with 30.6% inhibition at 0.1 mM
1-(4-hydroxyphenyl)-nonan-1-one
-
weak inhibitor with 36.3% inhibition at 0.1 mM
1-(6-hydroxy-9H-fluoren-2-yl)-ethanone
-
37C, 0.01 mM, 86% inhibition, substrate: estrone, 7beta-HSD type 1; 86% inhibition at 0.001 mM
1-bromo-6-(3-hydroxyphenyl)-2-naphthol
-
88% inhibition at 0.001 mM
1-Chloro-4-(2,2-dichloro-1-(5-Chloro-phenyl)-ethyl)-benzene
-
oxidation of estradiol
1-Chloro-4-(2,2-dichloro-1-(6-Chloro-phenyl)-ethyl)-benzene
-
oxidation of estradiol
1-phenyl-1,2-propanedione
-
40 mM, pH 8.5, t1/2: 0.19 h
1-[(3-hydroxyphenyl)sulfanyl]-5-oxo-4,5,7,8,9,10,11,13-octahydro-3H-indeno[2',1':4,5]pyrimido[1,2-a]azepine-2-carbaldehyde
-
-
1-[2-[4-(6-Methoxy-2-phenyl-3,4-dihydro-naphthalen-1-yl)-phenoxy]-ethyl]-pyrrolidine
-
oxidation of estradiol
1-[5-(3'-hydroxybiphenyl-3-yl)-2-thienyl]ethanone
-
0.001 mM, 10 min, 22% inhibition; 0.001 mM, 10 min, 23% inhibition
1-[5-(3'-Hydroxybiphenyl-4-yl)-2-thienyl]ethanone
-
0.001 mM, 10 min, 10% inhibition; 0.001 mM, 10 min, 38% inhibition
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
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
-
-
13-oxo-4-(phenylsulfanyl)-1,2,7,8,9,10,11,13-octahydro[1]benzothieno[2',3':4,5]pyrimido[1,2-a]azepine-3-carbaldehyde
-
0.001 mM, 80% inhibition
13-oxo-4-(propylsulfanyl)-1,2,7,8,9,10,11,13-octahydro[1]benzothieno[2',3':4,5]pyrimido[1,2-a]azepine-3-carbaldehyde
-
0.001 mM, 74% inhibition
16-cyano-17-oxoestra-1(10),2,4-trien-3-yl sulfamate
-
-
16-cyano-2-methoxy-17-oxoestra-1(10),2,4-trien-3-yl sulfamate
-
-
16-difluoro-estradiol
-
oxidation of estradiol
16-methylen-estra-1,3,5(10)-triene-3,17beta-diol
-
suicide inhibitor
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+
16alpha-Bromoacetoxyprogesterone
-
-
16alpha-bromobutyl-estradiol
-
-
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
16beta-bromobutyl-estradiol
-
-
16beta-m-pyridylmethylamidomethyl-2-methoxyoestrone
-
IC50: 0.00029 mM
17(R,S)-14,15-secoestra-1,3,5(10)-trien-15-yne-3,17-diol
-
suicide inhibitor
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
17-deoxy-estradiol
-
oxidation of estradiol
2',4',4-trihydroxy-4'-chalcone
-
IC50: 0.0338 mM
2',4'-dihydroxy-chalcone
-
IC50: 0.0346 mM
2',5'-ADP
-
-
2'-AMP
-
competitive with respect to NAD(H) or NADP(H) and noncompetitive with respect to the steroid
2,2',4,4'-tetrahydroxybenzophenone
-
-
2,2'-diimino-7,7'-dimethyl-5,5'-bis(1-methylethyl)-2H,2'H-8,8'-binaphtho[1,8-bc]furan-3,3',4,4'-tetrol
-
-
2,3-Butanedione
-
40 mM, pH 8.5, t1/2: 2 h
2,3-Pentanedione
-
40 mM, pH 8.5, t1/2: 5.3 h
2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
44% inhibition at 0.006 mM
2-(3-hydroxyphenyl)quinolin-6-ol
-
0.001 mM, 63% inhibition, substrate: estrone
2-chloro-3-hydroxyestra-1(10),2,4-trien-17-one
-
-
2-ethyl-17-oxo-16-[2-oxo-2-[(pyridin-3-ylmethyl)amino]ethyl]estra-1(10),2,4-trien-3-yl sulfamate
-
-
2-ethyl-3-sulfamoyloxy-17-oxo-estra-1,3,5(10)-trien-16-methylcarboxylic acid-S-alpha-methylbenzyl amide
-
50% inhibition at 0.001 mM
2-ethyl-3-sulfamoyloxy-17-oxo-estra-1,3,5(10)-trien-16alpha/beta-methylcarboxylic acid-(5-methylpyrimidinyl-2-ylmethyl)amide
-
37% inhibition at 0.001 mM
2-ethyl-3-sulfamoyloxy-17-oxo-estra-1,3,5(10)-trien-16alpha/beta-methylcarboxylic acid-(pyridine-3-ylmethyl)amide
-
64% inhibition at 0.01 mM
2-hydroxy-6-(3-hydroxyphenyl)-N-(5-methyl-1,3,4-thiadiazol-2-yl)-1-naphthamide
-
73% inhibition at 0.001 mM
2-hydroxy-6-(3-hydroxyphenyl)-N-methyl-1-naphthamide
-
76% inhibition at 0.001 mM
2-hydroxy-6-(3-hydroxyphenyl)-N-phenyl-1-naphthamide
-
80% inhibition at 0.001 mM
2-hydroxy-N,6-bis(3-hydroxyphenyl)-1-naphthamide
-
70% inhibition at 0.001 mM
2-methoxyoestrone
-
IC50: 0.0024 mM
2-methylcinnamic acid
-
IC50: 0.0064 mM
2-nitrophenyl (2E)-3-phenylprop-2-enoate
-
45% inhibition at 0.006 mM
2-phenylethyl (2E)-3-phenylprop-2-enoate
-
-
2-[(16beta)-2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
-
-
2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-2-ylmethyl)acetamide
-
-
2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
-
-
2-[3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(2-pyridin-2-ylethyl)acetamide
-
0.01 mM, 58% inhibition
2-[3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-2-ylmethyl)acetamide
-
0.01 mM, 82% inhibition
2-[3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
-
-
2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-pyridin-3-ylmethyl-acetamide
-
37C, 0.001 mM, 39% inhibition, substrate: estrone, 7beta-HSD type 1; 39% inhibition at 0.001 mM
3',4',5,7-tetrahydroxy-flavone
-
IC50: 0.0006 mM
3',4',7-trihydroxy-isoflavone
-
IC50: 0.0052 mM
3',5'-ADP
-
-
3'-(1-benzothien-2-yl)biphenyl-3-ol
-
0.001 mM, 10 min, 39% inhibition; 0.001 mM, 10 min, 49% inhibition
3'-(2-thienyl)biphenyl-3-ol
-
0.001 mM, 10 min, 40% inhibition; 0.001 mM, 10 min, 48% inhibition
3'-(5-chloro-2-thienyl)biphenyl-3-ol
-
0.001 mM, 10 min, 31% inhibition; 0.001 mM, 10 min, 71% inhibition
3'-(5-methyl-2-thienyl)biphenyl-3-ol
-
0.001 mM, 10 min, 32% inhibition; 0.001 mM, 10 min, 36% inhibition
3,3',4',7-tetrahydroxy-flavone
-
-
3,3',4,4'-tetrahydroxy-7,7'-dimethyl-5,5'-bis(1-methylethyl)-2H,2'H-8,8'-binaphtho[1,8-bc]furan-2,2'-dione
-
-
3,3'-(1-methyl-1H-1,2,4-triazole-3,5-diyl)diphenol
-
-
3,3'-(1-phenyl-1H-1,2,4-triazole-3,5-diyl)diphenol
-
-
3,3'-(1H-1,2,3-triazole-1,4-diyl)diphenol
-
; 17% inhibition at 0.001 mM
3,3'-pyridine-2,5-diyldiphenol
-
-
3,4,5-trimethoxycinnamic acid
3,5,7,4'-tetrahydroxyflavone
-
IC50 between 0.001 and 0.005 mM, reduction of estra-4-en-3,17-dione
3,5,7-trihydroxy-4'-methoxy-flavone
-
IC50: 15 mM
3,5,7-trihydroxy-flavone
-
-
3,5-dibromosalicylic acid
-
-
3,7-dihydroxyflavone
-
IC50 below 0.001 mM, oxidation of 17beta-hydroxyestra-4-en-3-one
3-(17beta-hydroxy-3-methoxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
-
0.01 mM, 90% inhibition, substrate: estrone
3-(17beta-hydroxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
-
0.01 mM, 79% inhibition, substrate: estrone
3-(2-furylmethyl)-8-hydroxy-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
33% inhibition at 100 nM, 78% inhibition at 0.001 mM
3-(2-naphthyl)phenol
-
0.001 mM, 61% inhibition, substrate: estrone
3-(3,17beta-dihydroxy-2-methoxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
-
0.01 mM, 81% inhibition, substrate: estrone
3-(3,17beta-dihydroxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
-
0.001 mM, 94% inhibition, substrate: estrone
3-(3-hydroxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
-
0.001 mM, 88% inhibition, substrate: estrone
3-(3-hydroxyphenyl)quinolin-7-ol
-
0.001 mM, 57% inhibition, substrate: estrone
3-(3-methoxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
-
0.01 mM, 76% inhibition, substrate: estrone
3-(6-hydroxy-2-naphthyl)benzoic acid
-
0.001 mM, 76% inhibition, substrate: estrone
3-(hydroxymethyl)-4-(phenylsulfanyl)-2,7,8,9,10,11-hexahydro[1]benzothieno[2',3':4,5]pyrimido[1,2-a]azepin-13(1H)-one
-
0.001 mM, 52% inhibition
3-(quinolin-3-yl)phenol
-
0.001 mM, 18% inhibition, substrate: estrone
3-(trifluoromethyl)-cinnamic acid
-
-
3-([(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]methyl)benzamide
-
-
-
3-acetyl-2-oxo-2H-chromen-7-yl trifluoromethanesulfonate
-
IC50 value of 360 nM against recombinant enzyme in bacterial homogenate
3-acetyl-7-(4-hydroxyphenyl)-2H-chromen-2-one
-
IC50 value of 270 nM against recombinant enzyme in bacterial homogenate, and high selectivity for isoform 17beta-HSD1 over 17beta-HSD2 and against the alpha and beta estrogen receptors
3-benzyl-2-(2-bromo-3,4,5-trimethoxyphenyl)-8-hydroxy[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
3-benzyl-8-hydroxy-2-(2-methylprop-1-en-1-yl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
82% inhibition at 100 nM, 97% inhibition at 0.001 mM
3-benzyl-8-hydroxy-2-(2-thienyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
83% inhibition at 100 nM, 89% inhibition at 0.001 mM
3-benzyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
3-benzyl-8-hydroxy-2-(3-methoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
89% inhibition at 100 nM, 95% inhibition at 0.001 mM
3-benzylidene camphor
-
-
3-bromo-5-phenylsalicylic acid
-
-
3-butyl-8-hydroxy-2-(3,4,5-trimethoxybenzyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
0.001 mM,k 95% inhibition
3-butyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
86% inhibition at 100 nM, 95% inhibition at 0.001 mM
3-coumaric acid
-
34% inhibition at 0.05 mM
3-cyclohexylpropanoic acid
-
weak inhibition, IC50: 0.1 mM, above
3-hydroxy-1,3,5(10)-triene-[17,16-c]-(5'-carboxylic acid)-pyrazole
-
0.01 mM: 32% inhibition
3-hydroxy-1,3,5(10)-triene-[17,16-c]-(5'-hydroxymethyl)-pyrazole
-
0.01 mM: 94% inhibition, IC50: 0.00095 mM
3-hydroxy-1,3,5(10)-triene-[17,16-c]-[5'-(carboxylic acid ethyl ester)]-pyrazole
-
0.01 mM: 94% inhibition, IC50: 0.00185 mM
3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carboxylic acid
-
-
3-hydroxy-17-oxoestra-1(10),2,4-triene-2-carbonitrile
-
-
3-hydroxy-2-methoxy-17-oxoestra-1(10),2,4-triene-16-carbonitrile
-
0.01 mM, 35% inhibition
3-hydroxy-7-(3-hydroxyphenyl)-1-naphthonitrile
-
99% inhibition at 0.001 mM
3-hydroxy-7-(3-hydroxyphenyl)-N-methyl-2-naphthamide
-
18% inhibition at 0.001 mM
3-hydroxy-7-(3-hydroxyphenyl)-N-phenyl-2-naphthamide
-
62% inhibition at 0.001 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-isobutyl)-pyrazole
-
0.01 mM: 77% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methoxyethyl)-pyrazole
-
0.01 mM: 95% inhibition, IC50: 0.00053 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methyl acetate)-pyrazole
-
0.01 mM: 95% inhibition, IC50: 0.00092 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methyl)-pyrazole
-
0.01 mM: 94% inhibition, IC50: 0.00275 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-propionitrile)-pyrazole
-
0.01 mM: 95% inhibition, IC50: 0.00073 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-isobutyl)-pyrazole
-
0.01 mM: 70% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-methoxy-ethyl)-pyrazole
-
0.01 mM: 83% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-methyl acetate)-pyrazole
-
0.01 mM: 79% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-methyl)-pyrazole
-
0.01 mM: 43% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-ethylme-thylcarbamoyl)-pyrazole
-
0.01 mM: 88% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-isopropylcarbamoyl)-pyrazole
-
0.01 mM: 57% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-methyl)-pyrazole
-
0.01 mM: 75% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-methyl-carbamoyl)-pyrazole
-
0.01 mM: 62% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(1''-methylpiperazin-4''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 50% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(1'-methylpyrrol-2''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 89% inhibition, IC50: 0.0023 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(5''-methylpyrazin-2''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 80% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-2''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 93% inhibition, IC50: 0.00088 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-3''-ylethyl)carbamoyl]-pyrazole
-
0.01 mM: 99% inhibition, IC50: 0.0003 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-3''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 92% inhibition, IC50: 0.00078 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(tetrahydrofuran-2''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 87% inhibition
3-hydroxy-N-(6-hydroxy-1,3-benzothiazol-2-yl)benzamide
-
modeling of binding to crystal structure shows five hydrogen bond interactions and a cation-pi-interaction
3-hydroxyestra-1(10),2,4-triene-16,17-dione 16-oxime
-
-
3-hydroxyestra-1,3,5(10),7-tetraen-17-one
-
IC50: 0.0019 mM, oxidation of estradiol
3-hydroxyflavone
-
IC50 below 0.001 mM, oxidation of 17beta-hydroxyestra-4-en-3-one; IC50 between 0.001 and 0.005 mM, reduction of estra-4-en-3,17-dione
3-methoxy-1'(2')H-estra-1,3,5(10)-trieno[17,16-c]pyrazole
-
-
3-phenoxybenzyl (2E)-3-(1,3-benzodioxol-5-yl)prop-2-enoate
-
14% inhibition at 0.006 mM
3-phenoxybenzyl (2E)-3-phenylprop-2-enoate
-
13% inhibition at 0.006 mM
3-phenyl-5-bromosalicylic acid
-
-
3-trifluoromethylcinnamic acid
-
IC50: 0.043 mM
3-[(15beta)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-(4-methyl-1,3-thiazol-2-yl)propanamide
-
-
3-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-(5-methyl-1,3-thiazol-2-yl)propanamide
-
-
3-[(4-chlorophenyl)sulfanyl]-6-(2,4-dimethyl-1H-pyrrol-1-yl)pyridazine
-
-
3-[(5-bromofuran-2-yl)methyl]-8-hydroxy-2-(3,4,5-trimethoxybenzyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
0.001 mM, 95% inhibition
3-[(5-bromofuran-2-yl)methyl]-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
94% inhibition at 100 nM, 99% inhibition at 0.001 mM
3-[(6aS)-2-hydroxy-6a-methyl-4b,6,6a,10,10a,10b,11,12-octahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-8(5H)-yl]propanenitrile
-
-
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]-phenol
-
17beta-HSD1; substrate: estradiol-17beta, 17beta-HSD2
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]phenol
-
-
3-[2-(2-thienyl)pyridin-4-yl]phenol
-
0.001 mM, 10 min, 33% inhibition; 0.001 mM, 10 min, 62% inhibition
3-[2-(5-chloro-2-thienyl)pyridin-4-yl]phenol
-
0.001 mM, 10 min, 39% inhibition; 0.001 mM, 10 min, 63% inhibition
3-[2-hydroxy-6-(3-hydroxyphenyl)-1-naphthyl]-N-methylpropanamide
-
80% inhibition at 0.001 mM
3-[3-(4-hydroxyphenyl)-1-methyl-1H-1,2,4-triazol-5-yl]phenol
-
-
3-[3-(4-hydroxyphenyl)-1-phenyl-1H-1,2,4-triazol-5-yl]phenol
-
-
3-[3-(4-hydroxyphenyl)isoxazol-5-yl]-phenol
-
17beta-HSD1; substrate: estradiol-17beta, 17beta-HSD2
3-[4-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
-
17beta-HSD1
3-[4-(4-hydroxyphenyl)-1,3-oxazol-2-yl]phenol
-
substrate: estradiol-17beta, 17beta-HSD2
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]-phenol
-
17beta-HSD1; substrate: estradiol-17beta, 17beta-HSD2
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]phenol
-
-
3-[4-(4-hydroxyphenyl)thiophen-2-yl]phenol
-
-
3-[4-(5-chloro-2-thienyl)pyridin-2-yl]phenol
-
0.001 mM, 10 min, 25% inhibition; 0.001 mM, 10 min, 61% inhibition
3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
-
substrate: estradiol-17beta, 17beta-HSD2, very good selectivity, high cell permeability and medium CaCo-2 permeability; very good selectivity, high cell permeability and medium CaCo-2 permeability, 17beta-HSD1
3-[5-(4-hydroxyphenyl)-1-methyl-1H-1,2,4-triazol-3-yl]phenol
-
-
3-[5-(4-hydroxyphenyl)-1-phenyl-1H-1,2,4-triazol-3-yl]phenol
-
-
3-[5-(4-hydroxyphenyl)thiophen-2-yl]phenol
-
-
3-[5-(4-hydroxyphenyl)thiophen-3-yl]phenol
-
-
3-[5-(5-chloro-2-thienyl)pyridin-3-yl]phenol
-
0.001 mM, 10 min, 40% inhibition; 0.001 mM, 10 min, 46% inhibition
3-[6-(5-chloro-2-thienyl)pyridin-2-yl]phenol
-
0.001 mM, 10 min, 21% inhibition; 0.001 mM, 10 min, 40% inhibition
3beta-hydroxy-5,16-androstadiene
-
-
3beta-hydroxy-5-androsten-16-one
-
-
4',5,7-trihydroxy-flavanone
-
-
4',5,7-trihydroxy-flavone
-
IC50: 0.0003 mM
4',5,7-trihydroxy-isoflavone
-
IC50: 0.001 mM
4',7-dihydroxy-isoflavone
-
IC50: 0.01 mM
4'-(2-thienyl)biphenyl-3-ol
-
0.001 mM, 10 min, 22% inhibition; 0.001 mM, 10 min, 36% inhibition
4'-(3-furyl)biphenyl-3-ol
-
0.001 mM, 10 min, 17% inhibition
4'-(3-thienyl)biphenyl-3-ol
-
0.001 mM, 10 min, 36% inhibition; 0.001 mM, 10 min, 41% inhibition
4'-(5-chloro-2-thienyl)biphenyl-3-ol
-
; 0.001 mM, 10 min, 48% inhibition
4'-(6-methoxypyridin-3-yl)biphenyl-3-ol
-
0.001 mM, 10 min, 35% inhibition; 0.001 mM, 10 min, 58% inhibition
4'-cyanophenyl 3,4-methylenedioxycinnamate
-
-
4-(17beta-hydroxy-3-methoxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
-
0.01 mM, 38% inhibition, substrate: estrone
4-(3'-ethyl-4'-hydroxy-3-methyl-biphenyl)-4-oxo-N-pyridin-3-ylethyl-butyramide
-
15% inhibition at 0.001 mM
4-(3'-ethyl-4'-hydroxy-3-methyl-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide
-
21% inhibition at 0.001 mM; 37C, 0.001 mM, 21% inhibition, substrate: estrone,7beta-HSD type 1
4-(3'-ethyl-4'-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylethyl-butyramide
-
15% inhibition at 0.001 mM; 37C, 0.001 mM, 15% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3'-ethyl-4'-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide
-
38% inhibition at 0.001 mM
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-(2-hydroxyethyl)-butyramide
-
23% inhibition at 0.001 mM; 37C, 0.001 mM, 23% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylethyl-butyramide
-
17% inhibition at 0.001 mM; 37C, 0.001 mM, 17% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide
-
24% inhibition at 0.001 mM; 37C, 0.001 mM, 24% inhibition, substrate: estrone, 7beta-HSD type 1; 37C, 0.01 mM, 12% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2
4-(3'-ethyl-4'-methoxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide
-
17% inhibition at 0.001 mM; 37C, 0.001 mM, 17% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3,17beta-dihydroxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
-
0.01 mM, 74% inhibition, substrate: estrone
4-(3-ethyl-4-hydroxy-3-methyl-biphenyl)-4-oxo-N-pyridin-3-ylethyl-butyramide
-
37C, 0.001 mM, 15% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3-ethyl-4-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide
-
37C, 0.001 mM, 38% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3-Hydroxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
-
0.01 mM, 76% inhibition, substrate: estrone
4-(3-methoxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
-
0.01 mM, 56% inhibition, substrate: estrone
4-(octanoylamino)phenyl (2E)-3-phenylprop-2-enoate
-
15% inhibition at 0.006 mM
4-cyanophenyl (2E)-3-(1,3-benzodioxol-5-yl)prop-2-enoate
-
76% inhibition at 0.006 mM
4-hydroxychalcone
-
IC50: 0.016 mM
4-methyl-3-(trifluoromethyl)-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole
-
-
4-methyl-5-[6-(2,2,2-trifluoroethoxy)pyridin-3-yl]-4H-1,2,4-triazole-3-thiol
-
-
4-methyl-N-[4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]benzenesulfonamide
-
-
4-methylbenzylidene camphor
-
-
4-[(15beta)-3-hydroxy-17-oxo-2-propylestra-1(10),2,4-trien-15-yl]-N-[2-(7-methyl-1H-indol-2-yl)ethyl]butanamide
-
0.0001 mM, 69% inhibition
4-[(15beta)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-[2-(7-methyl-1H-indol-3-yl)ethyl]butanamide
-
-
4-[5-(3-hydroxyphenyl)thiophen-2-yl]-2-methylphenol
-
-
5'-ADP
-
-
5'-ADP-ribose
-
-
5'-AMP
-
-
5'-ATP
-
-
5'-O-(10-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-decanoyl)adenosine
-
IC50: 140 nM
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-undecanoyl) adenosine
-
IC50: 310 nM
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha/beta-yl]-undecanoyl)adenosine
-
IC50: 90 nM
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'beta-yl]-undecanoyl)adenosine
-
IC50: 120 nM
5'-O-(12-[3',17'beta-(dihydroxy)-1',3',5'(10')-estratrien-16'alpha-yl]-dodecanoyl)adenosine
-
IC50: 1000 nM
5'-O-(6-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha/beta-yl]-hexanoyl)adenosine
-
IC50: 6900 nM
5'-O-(7-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-heptanoyl)adenosine
-
IC50: 430 nM
5'-O-(8-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-octanoyl)adenosine
-
IC50: 93 nM
5'-O-(9-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-nonanoyl)adenosine
-
IC50: 52 nM
5'-O-[9-[(16b,17b)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]nonanoyl]adenosine
-
-
5'-O-[9-[(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]nonanoyl]adenosine
-
EM-1745, bisubstrate inhibitor of 17beta-HSD1
5,6,7-trihydroxy-2-phenyl-4H-chromen-4-one
-
-
5,7-dihydroxy-4'-methoxy-flavone
-
-
5,7-dihydroxyflavone
-
IC50 below 0.001 mM, oxidation of 17beta-hydroxyestra-4-en-3-one
5-(3-ethyl-4-hydroxyphenyl)-indan-1-one
-
37C, 0.01 mM, 48% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2; 37C, 0.01 mM, 86% inhibition, substrate: estrone, 7beta-HSD type 1; 86% inhibition at 0.001 mM
5-(3-fluoro-4-hydroxyphenyl)-indan-1-one
-
37C, 0.01 mM, 24% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2; 37C, 0.01 mM, 75% inhibition, substrate: estrone, 7beta-HSD type 1; 75% inhibition at 0.001 mM
5-(3-fluoro-4-methoxyphenyl)-indan-1-one
-
37C, 0.01 mM, 56% inhibition, substrate: estrone, 7beta-HSD type 1; 56% inhibition at 0.001 mM
5-(4-hydroxyphenyl)-indan-1-one
-
37C, 0.01 mM, 17% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2; 37C, 0.01 mM, 81% inhibition, substrate: estrone, 7beta-HSD type 1; 81% inhibition at 0.001 mM
5-(6-hydroxy-2-naphthyl)pyridin-3-ol
-
0.001 mM, 58% inhibition, substrate: estrone
5-androsten-3beta-ol
-
-
5-androstene-3beta,16beta-diol
-
-
5-benzyl-3-(furan-2-ylmethyl)-8-hydroxy-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
5% inhibition at 100 nM, 26% inhibition at 0.001 mM
5-bromo-3-(2-methylpropyl)-2-(3,4,5-trimethoxyphenyl)-6,7-dihydro[1]benzothieno[2,3-d]pyrimidine-4,8(3H,5H)-dione
-
0.001 mM, 54% inhibition
5-butyl-3-(furan-2-ylmethyl)-8-hydroxy-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
9% inhibition at 100 nM, 27% inhibition at 0.001 mM
5-hydroxyflavone
-
IC50 below 0.001 mM, oxidation of 17beta-hydroxyestra-4-en-3-one
5-methoxyflavone
-
IC50 between 0.001 and 0.005 mM, reduction of estra-4-en-3,17-dione
5-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-(2-thiophen-2-ylethyl)pentanamide
-
-
6-(3-ethyl-4-hydroxyphenyl)-3,4-dihydro-2H-naphthalen-1-one
-
37C, 0.01 mM, 51% inhibition, substrate: estrone, 7beta-HSD type 1; 51% inhibition at 0.001 mM
6-(3-ethyl-4-methoxyphenyl)-3,4-dihydro-2H-naphthalen-1-one
-
37C, 0.01 mM, 71% inhibition, substrate: estrone, 7beta-HSD type 1; 71% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-1-((4-methylphenyl)sulfonyl)-2-naphthol
-
75% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-1-(morpholin-4-ylcarbonyl)-2-naphthol
-
62% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-1-(phenylsulfonyl)-2-naphthol
-
33% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-1-(piperazin-1-ylcarbonyl)-2-naphthol
-
45% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-1-(piperidin-1-ylcarbonyl)-2-naphthol
-
73% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-1-naphthol
-
0.001 mM, 23% inhibition, substrate: estrone
6-(3-hydroxyphenyl)-1-phenyl-2-naphthol
-
89% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-2-naphthol
6-(3-hydroxyphenyl)-3,4-dihydronaphthalen-1(2H)-one
-
0.001 mM, 23% inhibition, substrate: estrone
6-(4-hydroxy-phenyl)-3,4-dihydro-2H-naphthalen-1-one
-
37C, 0.01 mM, 89% inhibition, substrate: estrone, 7beta-HSD type 1; 89% inhibition at 0.001 mM
6-(4-hydroxyphenyl)-1-naphthol
-
0.001 mM, 55% inhibition, substrate: estrone
6-(hexylsulfanyl)estra-1(10),2,4-triene-3,17beta-diol
-
30% inhibition at 0.001 mM, reduction of estrone with NADH as cofactor
6-butyl-3-(furan-2-ylmethyl)-8-hydroxy-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
52% inhibition at 100 nM, 81% inhibition at 0.001 mM
6-hydroxyflavone
-
53.3% inhibition at 0.006 mM
6-pyridin-3-yl-2-naphthol
-
0.001 mM, 32% inhibition, substrate: estrone
6-[(1,3-benzothiazol-2-ylsulfanyl)methyl]-4-butoxy-2-(trifluoromethyl)quinoline
-
-
6-[4-(hydroxymethyl)phenyl]-2-naphthol
-
0.001 mM, 13% inhibition, substrate: estrone
6-[4-(trifluoromethyl)phenoxy]pyridin-3-amine
-
-
7,4'-Dihydroxyflavone
-
more than 90% inhibition at 0.006 mM
7-(3-hydroxyphenyl)-2-naphthol
-
0.001 mM, 62% inhibition, substrate: estrone
7-hydroxy-2-phenyl-4H-chromen-4-one
-
-
7-hydroxy-3-(3-hydroxyphenyl)-1-naphthonitrile
-
53% inhibition at 0.001 mM
7-hydroxy-flavanone
-
IC50: 0.028 mM
7-hydroxy-flavone
-
IC50: 0.0009 mM
7-hydroxyflavone
-
weak inhibitor with 14.2% inhibition at 0.1 mM
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
8-hydroxy-3-(2-methylbutyl)-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
91% inhibition at 100 nM, 94% inhibition at 0.001 mM
8-hydroxy-3-(2-methylprop-1-en-1-yl)-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
0.001 mM, 97% inhibition
8-hydroxy-3-(2-methylpropyl)-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
93% inhibition at 100 nM, 98% inhibition at 0.001 mM
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
9-(5-O-(9-[(16alpha,17alpha)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]nonanoyl)-alpha-L-arabinofuranosyl)-9H-purin-6-amine
-
shows key interactions with two different enzyme-binding sites, namely the substrate- and the cofactor-binding sites
-
androstenedione
-
-
androsterone
-
-
arachidonic acid
-
0.018 mM, complete inhibition, oxidation of estradiol
baicalein
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
-
-
benzyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
60% inhibition at 0.006 mM
benzyl (2E)-3-phenylprop-2-enoate
-
35% inhibition at 0.006 mM
benzyl alcohol
-
-
caffeic acid
-
18% inhibition at 0.05 mM
chrysin
-
0.02 mM, about 65% inhibition
chrysoeriol
-
i.e. 4',5,7-trihydroxy-3'-methoxyflavone, 82% inhibition at 0.006 mM
Cinnamic acid
coumarin-3-carboxylic acid
coumestrol
cyclobutyl-(4-hydroxyphenyl)-methanone
-
weak inhibitor with 43.9% inhibition at 0.1 mM
cycloheptyl-(4-hydroxyphenyl)-methanone
-
weak inhibitor with 47.2% inhibition at 0.1 mM
Cyclohexanol
-
-
cyclohexyl (2E)-3-phenylprop-2-enoate
-
25% inhibition at 0.006 mM
cyclohexyl-(4-hydroxyphenyl)-methanone
-
weak inhibitor with 47.2% inhibition at 0.1 mM
Cyclopentanol
-
-
cyclopentyl-(4-hydroxyphenyl)-methanone
-
weak inhibitor with 49.5% inhibition at 0.1 mM
daidzein
-
0.02 mM, about 75% inhibition
diethylstilbestrol
diosmetin
-
i.e. 3',5,7-trihydroxy-4'-methoxyflavone, more than 90% inhibition at 0.006 mM
EM-139
EM-1745
enterodiol
-
-
enterolactone
-
0.05 mM, 84% inhibition
equilin
estrone
ethyl (2Z)-hydroxy[(16Z)-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-ylidene]ethanoate
-
-
ethyl 4-[([4-[(15alpha)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]butyl]carbamoyl)amino]benzoate
-
-
ethyl [(6aS)-2-hydroxy-6a-methyl-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-9-yl]acetate
-
-
eupatorin
-
37% inhibition at 0.006 mM
fisetin
-
72% inhibition at 0.006 mM
genistein
genkwanin
-
3',5-dihydroxy-7-methoxyflavone, 81% inhibition at 0.006 mM
Glyoxal
-
40 mM, pH 8.5, t1/2: 29 h
gossypol
-
and derivatives of gossypol, competitive with respect to NAD+ in reverse reaction
iodoacetamide
-
1 mM, 78% inhibition
linoleic acid
-
0.018 mM, 58% inhibition, oxidation of estradiol
linolenic acid
-
0.018 mM, 34% inhibition, oxidation of estradiol
luteolin
-
0.02 mM, about 40% inhibition
m-coumaric acid
-
-
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
methyl 3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carboxylate
-
0.01 mM, 69% inhibition
methyl [(6aS)-2-hydroxy-6a-methyl-4b,6,6a,10,10a,10b,11,12-octahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-8(5H)-yl]acetate
-
-
myricetin
-
i.e. 3,3',4',5',5,7-hexahydroxyflavone, 52% inhibition at 0.006 mM
N'-[(2,4-difluorophenyl)sulfonyl]-2-pyridin-3-yl-4,5-dihydro-1,3-thiazole-4-carbohydrazide
-
-
N-(1,3-benzodioxol-5-ylmethyl)-5-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]pentanamide
-
-
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-methyl-1,2,3-thiadiazole-5-carboxamide
-
-
N-(2,4-difluorobenzyl)-4-[(15beta)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]butanamide
-
-
N-benzyl-2-oxo-2H-chromene-3-carboxamide
-
-
N-benzyl-4-[(15alpha)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]butanamide
-
-
N-benzyl-4-[(15beta)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]butanamide
-
-
N-benzyl-4-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-methylbutanamide
-
-
N-butyl-6-[[(6beta,17beta)-17-hydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]oxy]-N-methylhexanamide
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
N-butyl-7-[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]-N-methylheptanamide
-
-
N-butyl-N-methyl-11-[16beta-(3-carbamoylbenzyl)-3,17-dihydroxy-estra-1,3,5(10)-trien-7alpha-yl]-undecanamide
-
0.01 mM, 61% inhibition, substrate: estrone
N-cyclohexyl-3-[(15beta)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]propanimidamide
-
-
N-cyclohexyl-3-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-methylpropanamide
-
-
N-cyclohexyl-3-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]propanamide
-
-
N-cyclooctyl-3-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]propanamide
-
-
N-n-butyl-N-methyl-11-(16'a-bromo-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-butyl-N-methyl-11-(16'a-chloro-3',17'a-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-butyl-N-methyl-11-(16'a-chloro-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-butyl-N-methyl-11-(16'a-fluoro-3',17'a-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-butyl-N-methyl-11-(16'a-fluoro-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-butyl-N-methyl-11-(16'a-iodo-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-Butyl-N-methyl-11-(3,17b-dihydroxyestra-1,3,5(10)-trien-7a-yl)undecanamide
-
-
N-[2-(4-hydroxyphenyl)ethyl]-3-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]propanamide
-
-
N-[3-(6-hydroxy-2-naphthyl)phenyl]acetamide
-
0.001 mM, 19% inhibition, substrate: estrone
N-[[(15alpha)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]methyl]-N-methylthiophene-2-sulfonamide
-
-
N-[[(15alpha)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]methyl]benzenesulfonamide
-
-
N-[[(15alpha)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]methyl]thiophene-2-sulfonamide
-
-
NADP+
-
strong inhibitor of NAD+-linked activity
naphthalen-2-yl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
56% inhibition at 0.006 mM
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
oleic acid
-
0.018 mM, complete inhibition, oxidation of estradiol
p-aminocinnamic acid
-
-
p-carboxycinnamic acid
-
-
p-nitro-cinnamic acid
-
-
palm oil carotenoids
-
0.0001 mM, significant inhibition of the conversion of estradiol to estrone in the MCF-7 cell line
-
phenol
-
noncompetitive
phenyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
35% inhibition at 0.006 mM
Phenylglyoxal
-
40 mM, pH 8.5, t1/2: 0.33 h
progesterone
-
-
S-(4-fluorophenyl) 2-methyl-4-(trifluoromethyl)benzenecarbothioate
-
-
S-[(7R,10R,13S,17R)-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,9,10,11,12,13,14,15,16-hexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-yl] ethanethioate
-
0.003 mM, 57% inhibition, substrate: 4-androstene-3,17-dione
scutellarein
-
i.e. 4',5,6,7-tetrahydroxyflavone, 88% inhibition at 0.006 mM
STX1040
-
-
testosterone
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
vitamin D3
-
inhibits reductive activity in HCT8 and LoVo cells
[4-[4-(2-methoxyphenyl)piperidin-1-yl]-3-nitrophenyl]methanol
-
-
additional information
-