nitisinone [Ligand Id: 6834] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1337 (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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
