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. 2021 Oct;379(1):96–107. doi: 10.1124/jpet.121.000619

TABLE 1.

IC50 values for inhibition of atenolol, metformin, and MPP transport into CHO cells stably transfected with hOCT1, hOCT2, hMATE1, or hMATE2-K. Each value is a mean IC50 (in μM; ±S.D.) of three or more separate experiments.

Inhibitors
IC50
Transporter Substrates Chloroquine Hydroxychloroquine Quinacrine Tilorone Pyronaridine Cetylpyridinium Miramistin
µM
hOCT2 [3H]Atenolol 2.9 ± 0.02 5.4 ± 0.7 0.6 ± 0.16 1.11 ± 0.77 1.7 ± 0.5 22.5 ± 3.1 1.2 ± 0.05
[14C]Metformin 15.7 ± 1.6 15.3 ± 5.03 2.08 ± 0.14 4.4 ± 0.34 5.2 ± 0.7 69.3 ± 18.3 11.5 ± 0.6
[3H]MPP 106.4 ± 19.3 103.7 ± 40.2 30.3 ± 3.9 60.4 ± 11.8 65.1 ± 17.7 161.8 ± 62.1 54.4 ± 4.8
hMATE1 [3H]Atenolol 1.7 ± 0.19 2.3 ± 0.6 16.9 ± 6.4 52.9 ± 21.5 56.1 ± 22.1 20.2 ± 2.8 5.7 ± 0.9
[14C]Metformin 2.4 ± 1.5 2.3 ± 0.3 17.13 ± 3.3 67.9 ± 19.4 84.7 ± 22.6 17.1 ± 6.1 11.98 ± 2.2
[3H]MPP 2.9 ± 1.6 3.6 ± 0.19 22.9 ± 8.2 84.0 ± 35 81.7 ± 32.3 19.0 ± 11.2 12.4 ± 2.3
hMATE2K [3H]Atenolol 3.1 ± 2.5 5.5 ± 3.7 1.8 ± 0.8 N/A N/A 23.4 ± 7.2 21.1 ± 6.8
[14C]Metformin 11.1 ± 18.2 3.4 ± 4.2 7.3 ± 8.3 N/A N/A 7.6 ± 5.4 29.6 ± 27.9
[3H]MPP 4.2 ± 2.4 6.9 ± 0.7 0.6 ± 0.3 N/A N/A 36.3 ± 12.3 12.4 ± 2.8
hOCT1 [3H]Atenolol 18.1 ± 3.7 39.3 ± 13.9 52.6 ± 7.5 8.4 ± 0.4 10.8 ± 1.6 7.5 ± 2.2 16.5 ± 4.2
[3H]MPP 37.1 ± 21.4 46.92 ± 12.3 10.5 ± 1.8 18.3 ± 4.4 35.1 ± 11.2 30.1 ± 8.2 45.9 ± 4.5