nitisinone [Ligand Id: 6834] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1337 (Nitisinona, Nitisinone, Nityr, Orfadin, SC-0735) |
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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
