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Literature summary for 1.1.1.62 extracted from

  • Marchais-Oberwinkler, S.; Kruchten, P.; Frotscher, M.; Ziegler, E.; Neugebauer, A.; Bhoga, U.; Bey, E.; Mueller-Vieira, U.; Messinger, J.; Thole, H.; Hartmann, R.W.
    Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics (2008), J. Med. Chem., 51, 4685-4698.
    View publication on PubMed
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Cloned(Commentary)

Cloned (Comment) Organism
expressed in Sf9 insect cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2E)-3-[2-hydroxy-6-(3-hydroxyphenyl)-1-naphthyl]-N-methylacrylamide 58% inhibition at 0.001 mM Homo sapiens
(2E)-3-[2-hydroxy-6-(3-hydroxyphenyl)-1-naphthyl]-N-phenylacrylamide 60% inhibition at 0.001 mM Homo sapiens
1-bromo-6-(3-hydroxyphenyl)-2-naphthol 88% inhibition at 0.001 mM Homo sapiens
2-hydroxy-6-(3-hydroxyphenyl)-N-(5-methyl-1,3,4-thiadiazol-2-yl)-1-naphthamide 73% inhibition at 0.001 mM Homo sapiens
2-hydroxy-6-(3-hydroxyphenyl)-N-methyl-1-naphthamide 76% inhibition at 0.001 mM Homo sapiens
2-hydroxy-6-(3-hydroxyphenyl)-N-phenyl-1-naphthamide 80% inhibition at 0.001 mM Homo sapiens
2-hydroxy-N,6-bis(3-hydroxyphenyl)-1-naphthamide 70% inhibition at 0.001 mM Homo sapiens
3-hydroxy-7-(3-hydroxyphenyl)-1-naphthonitrile 99% inhibition at 0.001 mM Homo sapiens
3-hydroxy-7-(3-hydroxyphenyl)-N-methyl-2-naphthamide 18% inhibition at 0.001 mM Homo sapiens
3-hydroxy-7-(3-hydroxyphenyl)-N-phenyl-2-naphthamide 62% inhibition at 0.001 mM Homo sapiens
3-[2-hydroxy-6-(3-hydroxyphenyl)-1-naphthyl]-N-methylpropanamide 80% inhibition at 0.001 mM Homo sapiens
6-(3-hydroxyphenyl)-1-((4-methylphenyl)sulfonyl)-2-naphthol 75% inhibition at 0.001 mM Homo sapiens
6-(3-hydroxyphenyl)-1-(morpholin-4-ylcarbonyl)-2-naphthol 62% inhibition at 0.001 mM Homo sapiens
6-(3-hydroxyphenyl)-1-(phenylsulfonyl)-2-naphthol 33% inhibition at 0.001 mM Homo sapiens
6-(3-hydroxyphenyl)-1-(piperazin-1-ylcarbonyl)-2-naphthol 45% inhibition at 0.001 mM Homo sapiens
6-(3-hydroxyphenyl)-1-(piperidin-1-ylcarbonyl)-2-naphthol 73% inhibition at 0.001 mM Homo sapiens
6-(3-hydroxyphenyl)-1-phenyl-2-naphthol 89% inhibition at 0.001 mM Homo sapiens
6-(3-hydroxyphenyl)-2-naphthol 94% inhibition at 0.001 mM Homo sapiens
7-hydroxy-3-(3-hydroxyphenyl)-1-naphthonitrile 53% inhibition at 0.001 mM Homo sapiens
additional information not inhibited by 2-hydroxy-6-(3-hydroxyphenyl)-N-pyridin-2-yl-1-naphthamide and 2-hydroxy-6-(3-hydroxyphenyl)-N-(pyrimidin-2-yl)-1-naphthamide Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P14061
-
-

Source Tissue

Source Tissue Comment Organism Textmining
placenta
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
estradiol-17beta + NAD+
-
 Homo sapiens estrone + NADH + H+
-
 ?
estradiol-17beta + NADP+
-
 Homo sapiens estrone + NADPH + H+
-
 ?

Synonyms

Synonyms Comment Organism
17beta-HSD1
-
 Homo sapiens
17beta-hydroxysteroid dehydrogenase type 1
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NAD+
-
 Homo sapiens
NADP+
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00002
-
 in 20 mM KH2PO4, pH 7.4, at 25°C Homo sapiens 6-(3-hydroxyphenyl)-1-phenyl-2-naphthol
0.00004
-
 in 20 mM KH2PO4, pH 7.4, at 25°C Homo sapiens 1-bromo-6-(3-hydroxyphenyl)-2-naphthol
0.000116
-
 in 20 mM KH2PO4, pH 7.4, at 25°C Homo sapiens 6-(3-hydroxyphenyl)-2-naphthol