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 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]