Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDS00056
Target NameXanthine dehydrogenase/oxidase    
Type of TargetSuccessful target    
Drug Potency against TargetFebuxostatIC50 = 20 nM/L[1]
FebuxostatIC50 = 3 nM[2]
AllopurinolIC50 = 776 nM[3]
AllopurinolKi = 7000 nM[4]
LIQUIRTIGENINIC50 = 11300 nM[5]
SCUTELLAREINIC50 = 12600 nM[5]
3,4'-(1H-1,2,4-triazole-3,5-diyl)dipyridineIC50 = 130 nM[6]
CHRYSOERIOLIC50 = 14000 nM[5]
ACACETINIC50 = 14100 nM[5]
3,5-di(pyridin-4-yl)-1H-1,2,4-triazoleIC50 = 170 nM[6]
3,5-bis(2-methylpyridin-4-yl)-1H-1,2,4-triazoleIC50 = 310 nM[6]
pentagalloyl glucoseIC50 = 3200 nM[7]
1-(3-Cyano-phenyl)-1H-pyrazole-4-carboxylic acidIC50 = 3300 nM[8]
BAICALEINIC50 = 3300 nM[5]
ROBINETINIC50 = 4300 nM[5]
Ref 1Rheumatology (Oxford). 2009 May;48 Suppl 2:ii15-ii19.Febuxostat: a new treatment for hyperuricaemia in gout. To Reference
Ref 2Eur J Med Chem. 2010 Jun;45(6):2663-70. Epub 2010 Feb 10.Synthesis of some 5-phenylisoxazole-3-carboxylic acid derivatives as potent xanthine oxidase inhibitors. To Reference
Ref 3Biochemistry (Mosc). 2006;71 Suppl 1:S49-54.Biochemical characterization of some pyrazolopyrimidine-based inhibitors of xanthine oxidase. To Reference
Ref 4J Med Chem. 1996 Jun 21;39(13):2529-35.Synthesis and biological evaluation of new imidazole, pyrimidine, and purine derivatives and analogs as inhibitors of xanthine oxidase. To Reference
Ref 5J. Nat. Prod. 51(2):345-348 (1988) To Reference
Ref 6Bioorg 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]. To Reference
Ref 7J. Nat. Prod. 52(1):210-211 (1989) To Reference
Ref 8Bioorg Med Chem Lett. 2001 Apr 9;11(7):879-82.Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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