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. 2022 Dec 30;66(1):657–676. doi: 10.1021/acs.jmedchem.2c01612

Table 4. Inhibitory Potencies of Selected Indole Derivatives against the ABC Transporters ABCB1, ABCC1, and ABCG2 Obtained in Calcein AM (ABCB1),2,5259 Daunorubicin (ABCB152,60 and ABCC152,5860), and Pheophorbide A (ABCG2)2,5260 Assays Using ABCB1-Expressing A2780/ADR (A), ABCC1-Expressing H69AR (B), and ABCG2-Expressing MDCK II BCRP (C) Cells, Respectivelya.

no. ABCB1 calcein AMIC50 ± SEM [μM] ABCB1 daunorubicinIC50 ± SEM [μM] ABCC1 daunorubicinIC50 ± SEM [μM] ABCG2 pheophorbide AIC50 ± SEM [μM]
22 24.3 ± 6.4b n.t. 17.3 ± 2.2i 99.5 ± 24.5j
23 5.32 ± 1.67b n.t. 19.1 ± 3.4i 43.5 ± 7.5j
24 0.983 ± 0.135c 1.49 ± 0.05f n.t. n.t.
30 1.51 ± 0.08d 2.77 ± 0.02g n.t. n.t.
31 1.40 ± 0.11e 1.19 ± 0.12h n.t. n.t.
34 0.960 ± 0.018 0.851 ± 0.003    
35     0.215 ± 0.033  
36       0.161 ± 0.011
a

Mean ± SEM values of at least three independent experiments are shown.

b

Constrained to the reference ABCB1 inhibitor 34.

c

Imax = 66.8 ± 3.3%.

d

Imax = 61.1 ± 2.1%

e

Imax = 47.9 ± 4.9%.

f

Imax = 84.0 ± 2.5%.

g

Imax = 93.3 ± 2.6%.

h

Imax = 39.0 ± 2.8%.

i

Constrained to the reference ABCC1 inhibitor 35.58,61

j

Constrained to the reference ABCG2 inhibitor 36; n.t., not tested due to lack of inhibitory activity in the initial screening.