Literature summary for 1.1.1.146 extracted from

Wang, H.; Robl, J.A.; Hamann, L.G.; Simpkins, L.; Golla, R.; Li, Y.X.; Seethala, R.; Zvyaga, T.; Gordon, D.A.; Li, J.J.
Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD-1) (2011), Bioorg. Med. Chem. Lett., 21, 4146-4149.

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Inhibitors

Inhibitors	Comment	Organism	Structure
5-(3-chloro-2-methylphenoxy)-3-(4-hydroxybicyclo[2.2.2]oct-1-yl)-[1,2,4]triazolo[4,3-a]pyridine	potent and metabolically stable inhibitor with about 200fold selectivity for isoform 11beta-HSD-1 versus isoform 11beta-HSD-2	Homo sapiens
5-(3-chloro-2-methylphenoxy)-3-(4-hydroxybicyclo[2.2.2]oct-1-yl)-[1,2,4]triazolo[4,3-a]pyridine	potent and metabolically stable inhibitor with about 200fold selectivity for isoform 11beta-HSD-1 versus isoform 11beta-HSD-2	Mus musculus

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P28845	-	-
Mus musculus	P50172	-	-

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000012	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	5-(3-chloro-2-methylphenoxy)-3-(4-hydroxybicyclo[2.2.2]oct-1-yl)-[1,2,4]triazolo[4,3-a]pyridine
0.00103	-	pH not specified in the publication, temperature not specified in the publication	Mus musculus	5-(3-chloro-2-methylphenoxy)-3-(4-hydroxybicyclo[2.2.2]oct-1-yl)-[1,2,4]triazolo[4,3-a]pyridine

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Release 2023.1 (January 2023)