Target Validation Information
TTD ID T40954
Target Name Xanthine dehydrogenase/oxidase (XDH)
Type of Target
Successful
Drug Potency against Target Allopurinol Drug Info IC50 = 776 nM [3]
Febuxostat Drug Info IC50 = 3 nM [4]
1,2,3,4,6-penta-O-galloyl-beta-D-glucose Drug Info IC50 = 3200 nM
1-(3-Cyano-phenyl)-1H-pyrazole-4-carboxylic acid Drug Info IC50 = 3300 nM [1]
3,4'-(1H-1,2,4-triazole-3,5-diyl)dipyridine Drug Info IC50 = 130 nM [2]
3,5-bis(2-methylpyridin-4-yl)-1H-1,2,4-triazole Drug Info IC50 = 310 nM [2]
3,5-di(pyridin-4-yl)-1H-1,2,4-triazole Drug Info IC50 = 170 nM [2]
ACACETIN Drug Info IC50 = 14100 nM
BAICALEIN Drug Info IC50 = 3300 nM
CHRYSOERIOL Drug Info IC50 = 14000 nM
LIQUIRTIGENIN Drug Info IC50 = 11300 nM
ROBINETIN Drug Info IC50 = 4300 nM
SCUTELLAREIN Drug Info IC50 = 12600 nM
References
REF 1 Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors. Bioorg Med Chem Lett. 2001 Apr 9;11(7):879-82.
REF 2 Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia [... Bioorg Med Chem Lett. 2009 Nov 1;19(21):6225-9.
REF 3 Biochemical characterization of some pyrazolopyrimidine-based inhibitors of xanthine oxidase. Biochemistry (Mosc). 2006;71 Suppl 1:S49-54.
REF 4 Synthesis of some 5-phenylisoxazole-3-carboxylic acid derivatives as potent xanthine oxidase inhibitors. Eur J Med Chem. 2010 Jun;45(6):2663-70.

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