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Literature summary for 1.1.1.62 extracted from

  • Poirier, D.; Chang, H.J.; Azzi, A.; Boivin, R.P.; Lin, S.X.
    Estrone and estradiol C-16 derivatives as inhibitors of type 1 17beta-hydroxysteroid dehydrogenase (2006), Mol. Cell. Endocrinol., 248, 236-238.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
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 Homo sapiens
3-benzyl-2-(2-bromo-3,4,5-trimethoxyphenyl)-8-hydroxy[1]benzothieno[2,3-d]pyrimidin-4(3H)-one 87% inhibition at 100 nM, 95% inhibition at 0.001 mM. IC50: 5 nM Homo sapiens
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 Homo sapiens
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 Homo sapiens
3-benzyl-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. IC50: 5 nM Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P14061
-
-

Substrates and Products (Substrate)

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000005
-
87% inhibition at 100 nM, 95% inhibition at 0.001 mM. IC50: 5 nM Homo sapiens 3-benzyl-2-(2-bromo-3,4,5-trimethoxyphenyl)-8-hydroxy[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
0.000005
-
94% inhibition at 100 nM, 99% inhibition at 0.001 mM. IC50: 5 nM Homo sapiens 3-benzyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one