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. 2012 Jan 23;3(3):248–251. doi: 10.1021/ml200293c

Table 1. Inhibition of the NorA-Mediated Efflux of EtBr in SA-1199B Cells and of the Pgp-Mediated Cell Efflux of R123 in Mouse T Lymphoma L5178 MDR1 Cells.

Cpd IDa common name % inhibition of EtBr efflux % inhibition of R123 efflux
1b reserpine 84.8c N.A.
2 amlodipine 60.6 52.8d
3 astemizole 80.6 12.8d
4 dipyridamole 42.3 4.7e
5 loperamide 77.7 4.5d
6 quinidine 31.5 21.1e
7 aripiprazole 92.3 99e,f
8 ebastine 88.3 99e,f
9 sertindole 81.8 74e,f
10 ziprasidone 86.6 19e,f
11 aprindine 51.6 16e,f
12 repaglinide 14.0 35e,f
13g cyclosporine A N.A. 92e,f
14h alprenolol N.A. 5.0e,f
15   22.8i 44.1e
16   23.6i 64.7e
17   33.9j 1.9e
18   1.7j 2.6d
19   4.4j 3.2e
20   91.2k 40.6e
21   19.7f 16.8e
22   88.2c 4.3e
23   88.4c 1.6e
24   0c 2.3e
25   30.6c 21.7e
26   86.6c 7.8d
27   0c 2.2e
28   2.8c 2.1e
29   71.7c 0.6d
30   41.8c 2.6e
31   41.3c 20.4e
32   81.0c 0.7d
33   15.5c 2.6e
34   74.7c 1.7d
35   0c 11.3e
a

Structures for compounds 135, IUPAC names for compounds 1535, and SMILES are given as Supporting Information.

b

Reserpine was used as a positive control for EtBr efflux inhibition.

c

From ref (16).

d

Tested at 10–5 M concentration.

e

Tested at 10–4 M concentration.

f

From ref (18).

g

Cyclosporine A was used as a positive control for R123 efflux inhibition.

h

Alprenolol was used as a negative control for R123 efflux inhibition.

i

From ref (21).

j

From ref (22).

k

From ref (17).