Literature summary for 1.1.1.62 extracted from

Laplante, Y.; Cadot, C.; Fournier, M.A.; Poirier, D.
Estradiol and estrone C-16 derivatives as inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: blocking of ER+ breast cancer cell proliferation induced by estrone (2008), Bioorg. Med. Chem., 16, 1849-1860.

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Inhibitors

Inhibitors	Comment	Organism	Structure
3-(17beta-hydroxy-3-methoxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide	0.01 mM, 90% inhibition, substrate: estrone	Homo sapiens
3-(17beta-hydroxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide	0.01 mM, 79% inhibition, substrate: estrone	Homo sapiens
3-(3,17beta-dihydroxy-2-methoxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide	0.01 mM, 81% inhibition, substrate: estrone	Homo sapiens
3-(3,17beta-dihydroxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide	0.001 mM, 94% inhibition, substrate: estrone	Homo sapiens
3-(3-hydroxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide	0.001 mM, 88% inhibition, substrate: estrone	Homo sapiens
3-(3-methoxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide	0.01 mM, 76% inhibition, substrate: estrone	Homo sapiens
4-(17beta-hydroxy-3-methoxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide	0.01 mM, 38% inhibition, substrate: estrone	Homo sapiens
4-(3,17beta-dihydroxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide	0.01 mM, 74% inhibition, substrate: estrone	Homo sapiens
4-(3-Hydroxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide	0.01 mM, 76% inhibition, substrate: estrone	Homo sapiens
4-(3-methoxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide	0.01 mM, 56% inhibition, substrate: estrone	Homo sapiens
estrone	0.001 mM, 85% inhibition	Homo sapiens
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	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P14061	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
T-47D cell	-	Homo sapiens	-

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000044	-	-	Homo sapiens	3-(3,17beta-dihydroxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.000171	-	-	Homo sapiens	3-(3-hydroxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.000218	-	-	Homo sapiens	estrone

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Release 2023.1 (January 2023)