xanthine dehydrogenase | 1.-.-.- Oxidoreductases | IUPHAR/BPS Guide to PHARMACOLOGY

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xanthine dehydrogenase

Target not currently curated in GtoImmuPdb

Target id: 2646

Nomenclature: xanthine dehydrogenase

Abbreviated Name: XDH

Family: 1.-.-.- Oxidoreductases, Nucleoside synthesis and metabolism

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1333 2p23.1 XDH xanthine dehydrogenase
Mouse - 1335 17 E2 Xdh xanthine dehydrogenase
Rat - 1331 6q13 Xdh xanthine dehydrogenase
Previous and Unofficial Names
xanthine dehydrogenase/oxidase | xanthine oxidase | XO | XOR
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
febuxostat Bt Inhibition 9.9 pKi 5
pKi 9.9 (Ki 1.2x10-10 M) [5]
Description: In vitro assay using purified bovine enzyme
allopurinol Hs Inhibition 5.2 pKi 1
pKi 5.2 (Ki 7x10-6 M) [1]
febuxostat Hs Inhibition 8.9 pIC50 2
pIC50 8.9 (IC50 1.26x10-9 M) [2]
Description: Inhibition of baculovirus expressed C-terminally FLAG-tagged human xanthine oxidase (aa 1-1333).
febuxostat Bt Inhibition 7.5 pIC50 4
pIC50 7.5 (IC50 3x10-8 M) [4]
Description: In vitro assay using purified bovine enzyme
allopurinol Hs Inhibition 5.4 pIC50 1
pIC50 5.4 (IC50 4.2x10-6 M) [1]
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology
Disease:  Xanthinuria type I
OMIM: 278300
Orphanet: ORPHA93601
Click column headers to sort
Type Species Amino acid change Nucleotide change Description Reference
Nonsense Human R228X 682C>T This nucleotide transition causes a Arg to Ter (termination) nonsense substitution at codon 228 resulting in a truncated protein. 3


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1. Biagi G, Costantini A, Costantino L, Giorgi I, Livi O, Pecorari P, Rinaldi M, Scartoni V. (1996) Synthesis and biological evaluation of new imidazole, pyrimidine, and purine derivatives and analogs as inhibitors of xanthine oxidase. J. Med. Chem., 39 (13): 2529-35. [PMID:8691450]

2. Evenäs J, Edfeldt F, Lepistö M, Svitacheva N, Synnergren A, Lundquist B, Gränse M, Rönnholm A, Varga M, Wright J et al.. (2014) HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase. Bioorg. Med. Chem. Lett., 24 (5): 1315-21. [PMID:24508129]

3. Ichida K, Amaya Y, Kamatani N, Nishino T, Hosoya T, Sakai O. (1997) Identification of two mutations in human xanthine dehydrogenase gene responsible for classical type I xanthinuria. J. Clin. Invest., 99 (10): 2391-7. [PMID:9153281]

4. Khanna S, Burudkar S, Bajaj K, Shah P, Keche A, Ghosh U, Desai A, Srivastava A, Kulkarni-Almeida A, Deshmukh NJ et al.. (2012) Isocytosine-based inhibitors of xanthine oxidase: design, synthesis, SAR, PK and in vivo efficacy in rat model of hyperuricemia. Bioorg. Med. Chem. Lett., 22 (24): 7543-6. [PMID:23122864]

5. Okamoto K, Eger BT, Nishino T, Kondo S, Pai EF, Nishino T. (2003) An extremely potent inhibitor of xanthine oxidoreductase. Crystal structure of the enzyme-inhibitor complex and mechanism of inhibition. J. Biol. Chem., 278 (3): 1848-55. [PMID:12421831]

How to cite this page

1.-.-.- Oxidoreductases: xanthine dehydrogenase. Last modified on 28/11/2018. Accessed on 18/09/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2646.