| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T40954 | ||||
| Target Name | Xanthine dehydrogenase/oxidase | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | LIQUIRTIGENIN | Drug Info | IC50 = 11300 nM | ||
| ROBINETIN | Drug Info | IC50 = 4300 nM | |||
| Febuxostat | Drug Info | IC50 = 3 nM | [1] | ||
| 1,2,3,4,6-penta-O-galloyl-beta-D-glucose | Drug Info | IC50 = 3200 nM | |||
| BAICALEIN | Drug Info | IC50 = 3300 nM | |||
| SCUTELLAREIN | Drug Info | IC50 = 12600 nM | |||
| 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] | ||
| 1-(3-Cyano-phenyl)-1H-pyrazole-4-carboxylic acid | Drug Info | IC50 = 3300 nM | [3] | ||
| ACACETIN | Drug Info | IC50 = 14100 nM | |||
| CHRYSOERIOL | Drug Info | IC50 = 14000 nM | |||
| Allopurinol | Drug Info | IC50 = 776 nM | [4] | ||
| References | |||||
| REF 1 | Synthesis of some 5-phenylisoxazole-3-carboxylic acid derivatives as potent xanthine oxidase inhibitors. Eur J Med Chem. 2010 Jun;45(6):2663-70. doi: 10.1016/j.ejmech.2010.02.013. Epub 2010 Feb 10. | ||||
| REF 2 | Bioorg Med Chem Lett. 2009 Nov 1;19(21):6225-9. Epub 2009 Sep 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 [corrected]. | ||||
| REF 3 | Bioorg Med Chem Lett. 2001 Apr 9;11(7):879-82.Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors. | ||||
| REF 4 | Biochemical characterization of some pyrazolopyrimidine-based inhibitors of xanthine oxidase. Biochemistry (Mosc). 2006;71 Suppl 1:S49-54. | ||||
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