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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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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]