clofarabine [Ligand Id: 6802] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1750 (Clofarabine, Clolar, Evoltra, NSC-759857)
  • phosphodiesterase 2A/Phosphodiesterase 2A in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
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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
phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
ChEMBL Inhibition of recombinant human PDE2A catalytic domain (580 to 919 residues) expressed in Escherichia coli BL21 (Codonplus) using [3H]cGMP as substrate after 15 mins by liquid scintillation counting method B 5.51 pIC50 3120 nM IC50 Bioorg Med Chem (2018) 26: 119-133 [PMID:29174506]
ribonucleotide reductase catalytic subunit M1 in Human [GtoPdb: 2630] [UniProtKB: P23921]
GtoPdb Inhibition of K562 cell growth - 8.3 pIC50 5 nM IC50 Cancer Res (1991) 51: 2386-94 [PMID:1707752]
ribonucleotide reductase regulatory subunit M2 in Human [GtoPdb: 2631] [UniProtKB: P31350]
GtoPdb Inhibition of growth of K562 cells - 8.3 pIC50 5 nM IC50 Cancer Res (1991) 51: 2386-94 [PMID:1707752]

ChEMBL data shown on this page come from version 32:

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]