As the final step in this investigation, we experimentally evaluated the performance of these three self-assembled dendrimers in binding heparin in the presence of human serum. Although, as expected, this more competitive condition had an adverse effect on the micelle/polyanion interaction, the order in affinity was preserved, the corresponding CE50 values being 133 ± 10, 182 ± 15, and 166 ± 2 for C18,1G0, C18,2G0, and C18,3G0, respectively. Importantly, these values are still substantially lower than those pertaining to our “lead” self-assembled dendrimer C22G1.