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Potent equilibrative nucleoside transporter 1 (ENT1) inhibitor (IC50 = 0.43 nM). Inhibits hENT1 and hENT2 uptake of [H3]uridine in K562 cells and K15NTD cells respectively.

Lin et al (2011) Design, synthesis, and evaluation of 2-diethanolamino-4,8-diheptamethyleneimino-2-(N-aminoethyl-N-ethanolamino)-6-(N,N-diethanolamino)pyrimido[5,4-d]pyrimidine-fluorescein conjugate (8MDP-fluor), as a novel equilibrativ Bioconjug.Chem. 22 1221 PMID:21539390 |Lin et al (2007) Synthesis, flow cytometric evaluation, and identification of highly potent dipyrid. analogues as equilibrative nucleoside transporter 1 inhibitors. J.Med.Chem. 50 3906 PMID:17636949

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