Extended Data Fig. 4: EOS301984 is a potent and selective human ENT1 antagonist.
From: Inhibition of ENT1 relieves intracellular adenosine-mediated T cell suppression in cancer
a, Percent inhibition of ENT2 in a transporter assay by dose ranges of EOS301984 or dilazep. b-e, Inhibition profile of EOS301984 against ENT4, CNT1, CNT2 and CNT3, respectively. f, Saturation binding of [3H]NBMPR against JAR cell membrane preparations in the presence (non-specific binding) and absence (total binding) of an excess (10 µM) of unlabeled NBMPR. g, Derivation of kon for [3H]NBMPR against JAR cell membrane preparations. h, Derivation of koff for [3H]NBMPR against JAR cell membrane preparations. i, Competition binding experiments between [3H]NBMPR and EOS301984 to generate the IC50 of EOS301984. j, Derivation of KD value for EOS301984 on human ENT1 from kinetic binding experiments in competition with [3H]NBMPR. k, Saturation binding of [3H]NBMPR against MCA205-ENT2KO cell membrane preparations in the presence (non-specific binding) and absence (total binding) of a 200-fold excess of unlabeled NBMPR. l, Derivation of kon for [3H]NBMPR against MCA205-ENT2KO cell membrane preparations. m, Derivation of koff for [3H]NBMPR against MCA205-ENT2KO cell membrane preparations. n, Competition binding experiments between [3H]NBMPR and EOS301984 to generate the IC50 of EOS301984. o, Derivation of KD value for EOS301984 on mouse ENT1 from kinetic binding experiments in competition with [3H]NBMPR. Mean values displayed from technical duplicates (a-e, g-j, l-o) and mean values ± s.d. displayed from technical triplicates (f, k).
