tipiracil [Ligand Id: 8696] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL235668 (MA-1, Tipiracil, TPI (freebase))
  • Thymidine phosphorylase in Human [ChEMBL: CHEMBL3106] [UniProtKB: P19971]
  • Thymidine phosphorylase in Escherichia coli [ChEMBL: CHEMBL3726] [UniProtKB: P07650]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Thymidine phosphorylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3106] [UniProtKB: P19971]
ChEMBL Competitive inhibition of thymidine phosphorylase (unknown origin) B 7.7 pKi 20 nM Ki J Med Chem (2019) 62: 1231-1245 [PMID:30615449]
ChEMBL Inhibitory activity against human thymidine phosphorylase B 7.77 pKi 17 nM Ki Bioorg Med Chem Lett (2003) 13: 3705-3709 [PMID:14552762]
ChEMBL Binding affinity towards recombinant thymidine phosphorylase TP B 8.3 pKi 5 nM Ki Bioorg Med Chem Lett (2003) 13: 107-110 [PMID:12467627]
ChEMBL Inhibition of human placental thymidine phosphorylase B 8.68 pKi 2.1 nM Ki J Med Chem (2007) 50: 6016-6023 [PMID:17963370]
ChEMBL Inhibition of human recombinant thymidine phosphorylase expressed in V79 cells B 8.89 pKi 1.3 nM Ki J Med Chem (2007) 50: 6016-6023 [PMID:17963370]
ChEMBL Inhibitory concentration against human thymidine phosphorylase TP B 7.46 pIC50 35 nM IC50 Bioorg Med Chem Lett (2003) 13: 107-110 [PMID:12467627]
ChEMBL Inhibition of thymidine phosphorylase (unknown origin) B 7.46 pIC50 35 nM IC50 J Med Chem (2019) 62: 1231-1245 [PMID:30615449]
ChEMBL Inhibitory activity against Escherichia coli thymidine phosphorylase B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2003) 13: 3705-3709 [PMID:14552762]
Thymidine phosphorylase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3726] [UniProtKB: P07650]
ChEMBL Inhibition of Escherichia coli thymidine phosphorylase B 7.46 pKi 35 nM Ki Bioorg Med Chem Lett (2010) 20: 1648-1651 [PMID:20138520]

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]