nitisinone [Ligand Id: 6834] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1337 (Nitisinone, Orfadin, SC-0735, Nityr)
  • 4-hydroxyphenylpyruvate dioxygenase in Human [ChEMBL: CHEMBL1861] [GtoPdb: 2621] [UniProtKB: P32754]
  • 4-hydroxyphenylpyruvate dioxygenase in Pig [ChEMBL: CHEMBL3203] [UniProtKB: Q02110]
  • 4-hydroxyphenylpyruvate dioxygenase in Rat [ChEMBL: CHEMBL5863] [GtoPdb: 2621] [UniProtKB: P32755]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
4-hydroxyphenylpyruvate dioxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1861] [GtoPdb: 2621] [UniProtKB: P32754]
ChEMBL Inhibition of purified His6-tagged recombinant human HPPD assessed as inhibition of maleylacetoacetate formation after 30 mins by UV/visible spectrophotometry B 7.43 pKi 37 nM Ki Bioorg. Med. Chem. (2014) 22: 5194-5211 [PMID:25182962]
4-hydroxyphenylpyruvate dioxygenase in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3203] [UniProtKB: Q02110]
ChEMBL Inhibition of 4-hydroxyphenylpyruvate dioxygenase of purified pig liver by enol-borate method B 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 843-845 [PMID:10853644]
4-hydroxyphenylpyruvate dioxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5863] [GtoPdb: 2621] [UniProtKB: P32755]
ChEMBL Inhibition of Wistar rat liver HPPD using 4-Hydroxyphenylpyruvate as substrate assessed as reduction in oxygen consumption preincubated for 3 mins followed by substrate addition B 7.4 pIC50 40 nM IC50 J Med Chem (2017) 60: 4101-4125 [PMID:28128559]
ChEMBL Inhibition of Wistar rat liver cytosol HPPD using HPP as substrate assessed as reduction in O2 consumption B 7.4 pIC50 40 nM IC50 J Med Chem (2017) 60: 4101-4125 [PMID:28128559]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]