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Literature summary for 1.1.1.62 extracted from

  • Brozic, P.; Lanisnik Risner, T.; Gobec, S.
    Inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (2008), Curr. Med. Chem., 15, 137-150.
    View publication on PubMed
Search for more literature for 1.1.1.62

Inhibitors

Inhibitors Comment Organism Structure
(15beta)-15-(4-morpholin-4-yl-4-oxobutyl)-17-oxoestra-1(10),2,4-trien-3-yl sulfamate 0.0001 mM, 10% inhibition Homo sapiens
(16alpha)-2-chloro-16-fluoro-3-hydroxyestra-1(10),2,4-trien-17-one
-
 Homo sapiens
(16alpha)-3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carbonitrile
-
 Homo sapiens
(16beta)-16-(ethoxymethyl)-3-hydroxyestra-1(10),2,4-trien-17-one
-
 Homo sapiens
(16beta)-2-chloro-16-fluoro-3-hydroxyestra-1(10),2,4-trien-17-one
-
 Homo sapiens
(16beta)-3-hydroxy-16-methyl-17-oxoestra-1(10),2,4-triene-16-carbonitrile
-
 Homo sapiens
(16beta)-3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carbonitrile
-
 Homo sapiens
(16Z)-3-hydroxy-16-(2,2,2-trifluoro-1-hydroxyethylidene)estra-1(10),2,4-trien-17-one
-
 Homo sapiens
(16Z)-3-hydroxy-16-(hydroxymethylidene)estra-1(10),2,4-trien-17-one
-
 Homo sapiens
(17beta)-3,17-dihydroxy-N-(pyridin-3-ylmethyl)estra-1(10),2,4-triene-16-carboxamide
-
 Homo sapiens
(17E)-3-hydroxyestra-1(10),2,4-trien-17-one oxime
-
 Homo sapiens
(17Z)-3-hydroxyestra-1(10),2,4-triene-16,17-dione dioxime
-
 Homo sapiens
(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
-
 Homo sapiens
(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
-
 Homo sapiens
(3alpha,7alpha,17beta)-17-ethynyl-7-methylestr-5(10)-ene-3,17-diol
-
 Homo sapiens
(3beta,7alpha,17beta)-17-ethynyl-7-methylestr-5(10)-ene-3,17-diol
-
 Homo sapiens
(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
-
 Homo sapiens
(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
-
 Homo sapiens
(4aS,4bR,10bS,12aS)-8-hydroxy-9-iodo-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
 Homo sapiens
(4aS,4bR,10bS,12aS)-8-hydroxy-9-methoxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
 Homo sapiens
(4aS,4bR,10bS,12aS)-9-bromo-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
 Homo sapiens
(4aS,4bR,10bS,12aS)-9-chloro-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
 Homo sapiens
(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 Homo sapiens
(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 Homo sapiens
(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 Homo sapiens
(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
-
 Homo sapiens
(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
-
 Homo sapiens
(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
-
 Homo sapiens
(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
-
 Homo sapiens
(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
-
 Homo sapiens
(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 Homo sapiens
(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
-
 Homo sapiens
(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
-
 Homo sapiens
(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
-
 Homo sapiens
(6beta,17beta)-6-(hexylsulfanyl)estra-1(10),2,4-triene-3,17-diol
-
 Homo sapiens
(6Z,17E)-3-hydroxyestra-1(10),2,4-triene-6,17-dione dioxime
-
 Homo sapiens
(7alpha,17beta)-17-ethynyl-17-hydroxy-7-methylestr-4-en-3-one
-
 Homo sapiens
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 Homo sapiens
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 Homo sapiens
16-cyano-17-oxoestra-1(10),2,4-trien-3-yl sulfamate
-
 Homo sapiens
16-cyano-2-methoxy-17-oxoestra-1(10),2,4-trien-3-yl sulfamate
-
 Homo sapiens
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
-
 Homo sapiens
2-chloro-3-hydroxyestra-1(10),2,4-trien-17-one
-
 Homo sapiens
2-ethyl-17-oxo-16-[2-oxo-2-[(pyridin-3-ylmethyl)amino]ethyl]estra-1(10),2,4-trien-3-yl sulfamate
-
 Homo sapiens
2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-2-ylmethyl)acetamide
-
 Homo sapiens
2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
-
 Homo sapiens
2-[3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(2-pyridin-2-ylethyl)acetamide 0.01 mM, 58% inhibition Homo sapiens
2-[3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-2-ylmethyl)acetamide 0.01 mM, 82% inhibition Homo sapiens
2-[3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
-
 Homo sapiens
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
-
 Homo sapiens
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 Homo sapiens
3-benzyl-2-(2-bromo-3,4,5-trimethoxyphenyl)-8-hydroxy[1]benzothieno[2,3-d]pyrimidin-4(3H)-one 0.001 mM, 95% inhibition Homo sapiens
3-benzyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one 0.001 mM, 99% inhibition Homo sapiens
3-butyl-8-hydroxy-2-(3,4,5-trimethoxybenzyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one 0.001 mM,k 95% inhibition Homo sapiens
3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carboxylic acid
-
 Homo sapiens
3-hydroxy-17-oxoestra-1(10),2,4-triene-2-carbonitrile
-
 Homo sapiens
3-hydroxy-2-methoxy-17-oxoestra-1(10),2,4-triene-16-carbonitrile 0.01 mM, 35% inhibition Homo sapiens
3-hydroxyestra-1(10),2,4-triene-16,17-dione 16-oxime
-
 Homo sapiens
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 Homo sapiens
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
-
 Homo sapiens
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 Homo sapiens
5'-O-[9-[(16b,17b)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]nonanoyl]adenosine
-
 Homo sapiens
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 Homo sapiens
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 Homo sapiens
ethyl (2Z)-hydroxy[(16Z)-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-ylidene]ethanoate
-
 Homo sapiens
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
-
 Homo sapiens
methyl 3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carboxylate 0.01 mM, 69% inhibition Homo sapiens
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
-
 Homo sapiens
N-butyl-6-[[(6beta,17beta)-17-hydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
-
 Homo sapiens
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
-
 Homo sapiens
N-butyl-7-[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]-N-methylheptanamide
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
 Homo sapiens 5829
-

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
34500
-
 2 * 34500 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P14061
-
-

Source Tissue

Source Tissue Comment Organism Textmining
bone
-
 Homo sapiens
-
breast
-
 Homo sapiens
-
lymphocyte
-
 Homo sapiens
-
ovary
-
 Homo sapiens
-
placenta
-
 Homo sapiens
-
prostate gland
-
 Homo sapiens
-
uterine endometrium
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dehydroepiandrosterone + NADPH + H+
-
 Homo sapiens 5-androstene-3beta,17beta-diol + NADP+
-
 ?
dihydrotestosterone + NADPH + H+
-
 Homo sapiens 5alpha-androstane-3beta,17beta-diol + NADP+
-
 ?
estrone + NADPH + H+
-
 Homo sapiens estradiol + NADP+
-
 ?

Subunits

Subunits Comment Organism
dimer 2 * 34500 Homo sapiens

Synonyms

Synonyms Comment Organism
17beta-HSD
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0041
-
 (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
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000362
-
-
 Homo sapiens 2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-2-ylmethyl)acetamide
0.000005
-
-
 Homo sapiens 3-benzyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
0.000015
-
-
 Homo sapiens (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
0.000024
-
-
 Homo sapiens (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
0.000027
-
-
 Homo sapiens 2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
0.000035
-
-
 Homo sapiens (16beta)-2-chloro-16-fluoro-3-hydroxyestra-1(10),2,4-trien-17-one
0.000037
-
-
 Homo sapiens 2-[3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
0.000052
-
-
 Homo sapiens (4aS,4bR,10bS,12aS)-8-hydroxy-9-iodo-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
0.000052
-
-
 Homo sapiens (4aS,4bR,10bS,12aS)-9-bromo-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
0.000052
-
-
 Homo sapiens 5'-O-[9-[(16b,17b)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]nonanoyl]adenosine
0.000077
-
-
 Homo sapiens (4aS,4bR,10bS,12aS)-9-chloro-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
0.000085
-
-
 Homo sapiens (4aS,4bR,10bS,12aS)-8-hydroxy-9-methoxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
0.000087
-
-
 Homo sapiens (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
0.000101
-
-
 Homo sapiens (16alpha)-2-chloro-16-fluoro-3-hydroxyestra-1(10),2,4-trien-17-one
0.00011
-
-
 Homo sapiens (16Z)-3-hydroxy-16-(hydroxymethylidene)estra-1(10),2,4-trien-17-one
0.000126
-
-
 Homo sapiens (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
0.00014
-
-
 Homo sapiens 2-chloro-3-hydroxyestra-1(10),2,4-trien-17-one
0.00016
-
-
 Homo sapiens N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
0.000165
-
-
 Homo sapiens 2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-2-ylmethyl)acetamide
0.000168
-
-
 Homo sapiens 3-hydroxy-17-oxoestra-1(10),2,4-triene-2-carbonitrile
0.00032
-
-
 Homo sapiens (16beta)-16-(ethoxymethyl)-3-hydroxyestra-1(10),2,4-trien-17-one
0.00051
-
-
 Homo sapiens (17beta)-3,17-dihydroxy-N-(pyridin-3-ylmethyl)estra-1(10),2,4-triene-16-carboxamide
0.00053
-
-
 Homo sapiens (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
0.0007
-
-
 Homo sapiens (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
0.00073
-
-
 Homo sapiens 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
0.00092
-
-
 Homo sapiens 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
0.00094
-
-
 Homo sapiens 3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carboxylic acid
0.00095
-
-
 Homo sapiens (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
0.0011
-
-
 Homo sapiens 3-hydroxyestra-1(10),2,4-triene-16,17-dione 16-oxime
0.00144
-
-
 Homo sapiens (7alpha,17beta)-17-ethynyl-17-hydroxy-7-methylestr-4-en-3-one
0.00185
-
-
 Homo sapiens 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
0.0019
-
-
 Homo sapiens (6Z,17E)-3-hydroxyestra-1(10),2,4-triene-6,17-dione dioxime
0.00203
-
-
 Homo sapiens (3alpha,7alpha,17beta)-17-ethynyl-7-methylestr-5(10)-ene-3,17-diol
0.0021
-
-
 Homo sapiens 16-cyano-2-methoxy-17-oxoestra-1(10),2,4-trien-3-yl sulfamate
0.0022
-
-
 Homo sapiens 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
0.0043
-
-
 Homo sapiens 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
0.00483
-
-
 Homo sapiens (3beta,7alpha,17beta)-17-ethynyl-7-methylestr-5(10)-ene-3,17-diol
0.0051
-
-
 Homo sapiens 2-ethyl-17-oxo-16-[2-oxo-2-[(pyridin-3-ylmethyl)amino]ethyl]estra-1(10),2,4-trien-3-yl sulfamate
0.01
-
-
 Homo sapiens (16beta)-3-hydroxy-16-methyl-17-oxoestra-1(10),2,4-triene-16-carbonitrile
0.01
-
-
 Homo sapiens 16-cyano-17-oxoestra-1(10),2,4-trien-3-yl sulfamate