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. Author manuscript; available in PMC: 2023 Mar 5.
Published in final edited form as: Eur J Med Chem. 2022 Jan 10;231:114103. doi: 10.1016/j.ejmech.2022.114103

Table 5.

EC50 and IC50 values for ABCG2 ATPase activity and inhibitory effect on mitoxantrone efflux by A3 adenosine receptor ligands

Compounds ATPase activity Inhibition of mitoxantrone efflux
EC50 or IC50 (nM) % of pcDNA control cells a, at 10 μM of compounds IC50 (μM)b
5 EC50 = 80.0 ± 10.0 99.2 ± 12.0 NCc
13 EC50 = 16.0 ± 3.0 100.0 ± 6.3 NC
14 EC50 = 13.0 ± 3.0 97.4 ± 12.1 NC
15 EC50 = 14.0 ± 5.0 97.2 ± 11.9 NC
16 IC50 = 2590 ± 40 101.7 ± 17.0 NC
17 IC50 = 2570 ± 30 92.5 ± 13.5 NC
20 IC50 = 4010 ± 20 105.3 ± 3.0 NC
35 EC50 = 50.0 ± 10.0 81.4 ± 11.5 NC
37c EC50 = 13.2 ± 1.7 110.4 ± 15.8 4.98 ± 1.69
60 EC50 = 13.2 ± 2.2 92.6 ± 9.2 0.44 ± 0.06
64 EC50 = 24.3 ± 4.9 109.1 ± 16.4 0.60 ± 0.08
a

Fluorescence intensity of pcDNA control cells was taken as a 100% inhibition, and percentage of mitoxantrone efflux inhibition in R-5 cells by 10 μM of A3 adenosine receptor ligands was calculated compared to pcDNA control cells.

b

Compound concentration that produces 50% inhibition of mitoxantrone efflux in R-5 cells is given as IC50 value.

c

NC, Not calculated.