Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDS00430
Target NameEquilibrative nucleoside transporter 1    
Type of TargetSuccessful target    
Drug Potency against TargetS6-nitrobenzyl mercaptopurine ribosideKi = 0.7 nM[1]
N6-CYCLOPENTYLADENOSINEKi = 1100 nM[2]
9-Benzyl-6-(4-nitro-benzylsulfanyl)-9H-purineKi = 135 nM[3]
6-(4-Nitro-benzylsulfanyl)-9-phenethyl-9H-purineKi = 2200 nM[3]
LIDOFLAZINEKi = 279.9 nM[4]
Ref 1Bioorg 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. To Reference
Ref 2J Med Chem. 2005 Jan 13;48(1):321-9.Inhibition of nucleoside transport proteins by C8-alkylamine-substituted purines. To Reference
Ref 3J 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. To Reference
Ref 4J 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. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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