5-fluorouracil [Ligand Id: 4789] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL185 (5-Fluorouracil, 5-fluoruracil, 5.f.u., 5 FU, 5-FU, Accusite, Actikerall, Adrucil, Carac, Efudex, Efudix, Fluoroplex, Fluorouracil, Fluorouracilo, Fluoro-uracil roche, Fluorouracilum, Fluorouricil, Fluracil, NSC-19893, Phthoruracil, Queroplex, RO 2-9757, RO-2-9757, RO-29757, Tolak)
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  • thymidylate synthetase/Thymidylate synthase in Mouse [ChEMBL: CHEMBL3160] [GtoPdb: 2642] [UniProtKB: P07607]
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  • Uracil phosphoribosyltransferase in Escherichia coli [ChEMBL: CHEMBL2233621] [UniProtKB: P0A8F0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511]
ChEMBL Inhibition of human recombinant aromatase expressed in baculovirus insect cell using 7-methoxy-trifluoromethyl coumarin (MFC) as substrate preincubated for 10 mins followed by substrate addition and measured for 30 mins by fluorescence based assay B 6.2 pIC50 630 nM IC50 Eur J Med Chem (2021) 221: 113511-113511 [PMID:34000484]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
thymidylate synthetase/Thymidylate synthase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3160] [GtoPdb: 2642] [UniProtKB: P07607]
ChEMBL Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxycytidine after preincubation for 15 mins by liquid scintillation counting B 5 pIC50 >=10000 nM IC50 Eur J Med Chem (2011) 46: 993-1005 [PMID:21330014]
ChEMBL Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxyuridine after preincubation for 15 mins by liquid scintillation counting B 5.15 pIC50 7000 nM IC50 Eur J Med Chem (2011) 46: 993-1005 [PMID:21330014]
ChEMBL Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxycytidine after preincubation for 4 hrs by liquid scintillation counting B 6.22 pIC50 600 nM IC50 Eur J Med Chem (2011) 46: 993-1005 [PMID:21330014]
ChEMBL Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxyuridine after preincubation for 4 hrs by liquid scintillation counting B 6.66 pIC50 220 nM IC50 Eur J Med Chem (2011) 46: 993-1005 [PMID:21330014]
ChEMBL Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxycytidine after preincubation for 24 hrs by liquid scintillation counting B 7.22 pIC50 60 nM IC50 Eur J Med Chem (2011) 46: 993-1005 [PMID:21330014]
ChEMBL Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxyuridine after preincubation for 24 hrs by liquid scintillation counting B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2011) 46: 993-1005 [PMID:21330014]
Uracil phosphoribosyltransferase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2233621] [UniProtKB: P0A8F0]
ChEMBL Inhibition of Escherichia coli K-12 MTCC 1302 UPRT activity by spectrophotometry B 4.89 pKi 13000 nM Ki Med Chem Res (2012) 21: 1149-1155

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]