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Literature summary for 1.1.1.62 extracted from

  • Oster, A.; Klein, T.; Werth, R.; Kruchten, P.; Bey, E.; Negri, M.; Marchais-Oberwinkler, S.; Frotscher, M.; Hartmann, R.W.
    Novel estrone mimetics with high 17beta-HSD1 inhibitory activity (2010), Bioorg. Med. Chem., 18, 3494-3505.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-[5-(3'-hydroxybiphenyl-3-yl)-2-thienyl]ethanone 0.001 mM, 10 min, 22% inhibition; 0.001 mM, 10 min, 23% inhibition Homo sapiens
1-[5-(3'-Hydroxybiphenyl-4-yl)-2-thienyl]ethanone 0.001 mM, 10 min, 10% inhibition; 0.001 mM, 10 min, 38% inhibition Homo sapiens
3'-(1-benzothien-2-yl)biphenyl-3-ol 0.001 mM, 10 min, 39% inhibition; 0.001 mM, 10 min, 49% inhibition Homo sapiens
3'-(2-thienyl)biphenyl-3-ol 0.001 mM, 10 min, 40% inhibition; 0.001 mM, 10 min, 48% inhibition Homo sapiens
3'-(5-chloro-2-thienyl)biphenyl-3-ol 0.001 mM, 10 min, 31% inhibition; 0.001 mM, 10 min, 71% inhibition Homo sapiens
3'-(5-methyl-2-thienyl)biphenyl-3-ol 0.001 mM, 10 min, 32% inhibition; 0.001 mM, 10 min, 36% inhibition Homo sapiens
3-[2-(2-thienyl)pyridin-4-yl]phenol 0.001 mM, 10 min, 33% inhibition; 0.001 mM, 10 min, 62% inhibition Homo sapiens
3-[2-(5-chloro-2-thienyl)pyridin-4-yl]phenol 0.001 mM, 10 min, 39% inhibition; 0.001 mM, 10 min, 63% inhibition Homo sapiens
3-[4-(5-chloro-2-thienyl)pyridin-2-yl]phenol 0.001 mM, 10 min, 25% inhibition; 0.001 mM, 10 min, 61% inhibition Homo sapiens
3-[5-(5-chloro-2-thienyl)pyridin-3-yl]phenol 0.001 mM, 10 min, 40% inhibition; 0.001 mM, 10 min, 46% inhibition Homo sapiens
3-[6-(5-chloro-2-thienyl)pyridin-2-yl]phenol 0.001 mM, 10 min, 21% inhibition; 0.001 mM, 10 min, 40% inhibition Homo sapiens
4'-(2-thienyl)biphenyl-3-ol 0.001 mM, 10 min, 22% inhibition; 0.001 mM, 10 min, 36% inhibition Homo sapiens
4'-(3-furyl)biphenyl-3-ol 0.001 mM, 10 min, 17% inhibition Homo sapiens
4'-(3-thienyl)biphenyl-3-ol 0.001 mM, 10 min, 36% inhibition; 0.001 mM, 10 min, 41% inhibition Homo sapiens
4'-(5-chloro-2-thienyl)biphenyl-3-ol 0.001 mM, 10 min, 48% inhibition Homo sapiens
4'-(6-methoxypyridin-3-yl)biphenyl-3-ol 0.001 mM, 10 min, 35% inhibition; 0.001 mM, 10 min, 58% inhibition Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P14061
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
17beta-HSD1
-
Homo sapiens
17beta-HSD2
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00047
-
37°C, pH not specified in the publication Homo sapiens 3-[2-(5-chloro-2-thienyl)pyridin-4-yl]phenol
0.00056
-
37°C, pH not specified in the publication Homo sapiens 3'-(5-chloro-2-thienyl)biphenyl-3-ol
0.00069
-
37°C, pH not specified in the publication Homo sapiens 4'-(6-methoxypyridin-3-yl)biphenyl-3-ol
0.00085
-
37°C, pH not specified in the publication Homo sapiens 3-[4-(5-chloro-2-thienyl)pyridin-2-yl]phenol
0.00102
-
37°C, pH not specified in the publication Homo sapiens 4'-(5-chloro-2-thienyl)biphenyl-3-ol
0.00137
-
37°C, pH not specified in the publication Homo sapiens 3'-(1-benzothien-2-yl)biphenyl-3-ol
0.00139
-
37°C, pH not specified in the publication Homo sapiens 3-[6-(5-chloro-2-thienyl)pyridin-2-yl]phenol
0.00194
-
37°C, pH not specified in the publication Homo sapiens 3'-(1-benzothien-2-yl)biphenyl-3-ol
0.00237
-
37°C, pH not specified in the publication Homo sapiens 3'-(5-chloro-2-thienyl)biphenyl-3-ol
0.00238
-
37°C, pH not specified in the publication Homo sapiens 3-[2-(5-chloro-2-thienyl)pyridin-4-yl]phenol
0.00297
-
37°C, pH not specified in the publication Homo sapiens 4'-(6-methoxypyridin-3-yl)biphenyl-3-ol
0.00364
-
37°C, pH not specified in the publication Homo sapiens 3-[4-(5-chloro-2-thienyl)pyridin-2-yl]phenol
0.00711
-
37°C, pH not specified in the publication Homo sapiens 3-[6-(5-chloro-2-thienyl)pyridin-2-yl]phenol
0.01
-
value higher than 0.01, 37°C, pH not specified in the publication Homo sapiens 4'-(5-chloro-2-thienyl)biphenyl-3-ol