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ChEMBL ligand: CHEMBL1568 (2-Fluoro-Ara-A, Fludarabine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]