Literature summary for 1.1.1.64 extracted from

Harada, K.; Kubo, H.; Abe, J.; Haneta, M.; Conception, A.; Inoue, S.; Okada, S.; Nishioka, K.
Discovery of potent and orally bioavailable 17beta-hydroxysteroid dehydrogenase type 3 inhibitors (2012), Bioorg. Med. Chem., 20, 3242-3254.

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Cloned(Commentary)

Cloned (Comment)	Organism
expression in HeLa cell	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
5-(3-bromo-4-hydroxybenzylidene)-3-(4-fluorophenyl)-2-thioxo-1,3-oxazolidin-4-one	strong inhibitory activity on isoform 3beta-HSD3	Homo sapiens
5-(3-bromo-4-hydroxybenzylidene)-3-(4-methylphenyl)-2-thioxo-1,3-oxazolidin-4-one	strong inhibitory activity on isoform 3beta-HSD3	Homo sapiens
5-(3-chloro-5-fluoro-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-thioxo-1,3-oxazolidin-4-one	strong inhibitory activity on isoform 3beta-HSD3	Homo sapiens
5-(3-fluoro-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-tioxo-1,3-oxazolidin-4-one	strong inhibitory activity on isoform 3beta-HSD3	Homo sapiens
5-[3,5-dichloro-4-(phosphonoxy)benzylidene]-3-(4-methoxyphenyl)-2-thioxo-1,3-oxazolidin-4-one	strong inhibitory activity on isoform 3beta-HSD3	Homo sapiens
5-[3,5-dichloro-4-(phosphonoxy)benzylidene]-3-(4-methoxyphenyl)-2-thioxo-1,3-oxazolidin-4-one	strong inhibitory activity on isoform 3beta-HSD3. When administered orally at a high dose of 100 mg/kg, compound shows approximately two times more potent testosterone-lowering effect against a positive control in the luteinizing hormone-releasing hormone-induced T production assay. The T-lowering effect continues at ca 10% level of control over 4 h after administration	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P37058	-	-
Rattus norvegicus	-	-	-

Synonyms

Synonyms	Comment	Organism
17beta-HSD3	-	Rattus norvegicus
17beta-HSD3	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000001	-	cell-based assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	5-[3,5-dichloro-4-(phosphonoxy)benzylidene]-3-(4-methoxyphenyl)-2-thioxo-1,3-oxazolidin-4-one
0.000002	-	cell-based assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	5-(3-bromo-4-hydroxybenzylidene)-3-(4-fluorophenyl)-2-thioxo-1,3-oxazolidin-4-one
0.000002	-	cell-based assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	5-(3-bromo-4-hydroxybenzylidene)-3-(4-methylphenyl)-2-thioxo-1,3-oxazolidin-4-one
0.000002	-	cell-based assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	5-(3-fluoro-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-tioxo-1,3-oxazolidin-4-one
0.000002	-	cell-based assay, pH not specified in the publication, temperature not specified in the publication	Homo sapiens	5-(3-chloro-5-fluoro-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-thioxo-1,3-oxazolidin-4-one

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Release 2023.1 (January 2023)