fludarabine [Ligand Id: 4802] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1568 (2-Fluoro-Ara-A, Fludarabine)
  • Ecto-5'-Nucleotidase/5`-nucleotidase in Human [ChEMBL: CHEMBL5957] [GtoPdb: 1232] [UniProtKB: P21589]
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  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
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  • ribonucleotide reductase catalytic subunit M1 in Human [GtoPdb: 2630] [UniProtKB: P23921]
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  • ribonucleotide reductase regulatory subunit M2 in Human [GtoPdb: 2631] [UniProtKB: P31350]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Ecto-5'-Nucleotidase/5`-nucleotidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5957] [GtoPdb: 1232] [UniProtKB: P21589]
ChEMBL Non-competitive type of inhibition of human 5'-nucleotidase using IMP as substrate assessed as inhibitor constant for enzyme substrate complex by Lineweaver-Burk plot analysis B 3.05 pKi 900000 nM Ki Eur J Med Chem (2019) 168: 28-44 [PMID:30798051]
ChEMBL Competitive type of inhibition of human 5'-nucleotidase using IMP as substrate assessed as inhibitor constant for free enzyme by Lineweaver-Burk plot analysis B 3.3 pKi 500000 nM Ki Eur J Med Chem (2019) 168: 28-44 [PMID:30798051]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand. B 8.23 pKi 5.9 nM Ki J Med Chem (1995) 38: 1174-1188 [PMID:7707320]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Binding affinity to adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand B 7.55 pKi 28 nM Ki J Med Chem (1995) 38: 1174-1188 [PMID:7707320]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat adenosine A3 receptor B 4.98 pKi 10400 nM Ki J Med Chem (1995) 38: 1174-1188 [PMID:7707320]
ribonucleotide reductase catalytic subunit M1 in Human [GtoPdb: 2630] [UniProtKB: P23921]
GtoPdb Inhibition of ADP reduction by ribonucleotide reductase from HeLa cells - 6 pIC50 1000 nM IC50 Mol Pharmacol (1982) 21: 474-7 [PMID:7048062]
ribonucleotide reductase regulatory subunit M2 in Human [GtoPdb: 2631] [UniProtKB: P31350]
GtoPdb Inhibition of ADP reduction by ribonucleotide reductase from HeLa cells - 6 pIC50 1000 nM IC50 Mol Pharmacol (1982) 21: 474-7 [PMID:7048062]

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]