Target Validation Information
Target ID T13491
Target Name Equilibrative nucleoside transporter 1
Target Type
Successful
Drug Potency against Target 6-(4-Nitro-benzylsulfanyl)-9-phenethyl-9H-purine Drug Info Ki = 2200 nM [527247]
9-Benzyl-6-(4-nitro-benzylsulfanyl)-9H-purine Drug Info Ki = 135 nM [527247]
S6-nitrobenzyl mercaptopurine riboside Drug Info Ki = 0.7 nM [529877]
LIDOFLAZINE Drug Info Ki = 279.9 nM [528952]
N6-CYCLOPENTYLADENOSINE Drug Info Ki = 1100 nM [527371]
References
Ref 527247J Med Chem. 2004 Oct 21;47(22):5441-50.Inhibition of nucleoside transport by new analogues of 4-nitrobenzylthioinosine: replacement of the ribose moiety by substituted benzyl groups.
Ref 527247J Med Chem. 2004 Oct 21;47(22):5441-50.Inhibition of nucleoside transport by new analogues of 4-nitrobenzylthioinosine: replacement of the ribose moiety by substituted benzyl groups.
Ref 529877Bioorg Med Chem Lett. 2009 Feb 1;19(3):917-21. Epub 2008 Dec 6.Synthesis and biological evaluation of phloridzin analogs as human concentrative nucleoside transporter 3 (hCNT3) inhibitors.
Ref 528952J Med Chem. 2007 Aug 9;50(16):3906-20. Epub 2007 Jul 18.Synthesis, flow cytometric evaluation, and identification of highly potent dipyridamole analogues as equilibrative nucleoside transporter 1 inhibitors.
Ref 527371J Med Chem. 2005 Jan 13;48(1):321-9.Inhibition of nucleoside transport proteins by C8-alkylamine-substituted purines.

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