TABLE 2

Screening of 4, 5, and 6 position-substituted benzothiazoles on KCa2.3 and KCa3.1

The reported numbers are the ratios of slope conductance at −80 mV measured in the presence and absence of drug with 250 nM [Ca2+]i.

Compound
KCa2.3
KCa3.1
1 μM
10 μM
100 μM
1 μM
10 μM
100 μM
1 Riluzole Embedded Image 1.1 ± 0.3 11.5 ± 4 30 ± 3 6 ± 0.9 30 ± 1.5 30 ± 2
8 SKA-1 Embedded Image N.E. 1.9 ± 0.3 N.D. 1.3 ± 0.2 3.1 ± 0.3 35 ± 4
9 SKA-36 Embedded Image N.E. 1.2 ± 0.2 15.5 ± 2 N.E. 1.2 ± 0.2 17 ± 1
10 SKA-4 Embedded Image N.E. 1.2 ± 0.3 N.D. N.E. 1.2 ± 0.1 1.3 ± 0.1
11 SKA-16 Embedded Image N.E. N.E. N.E. N.E. 1.5 ± 0.3 1.1 ± 0.3
12 SKA-24 Embedded Image N.E. N.E. N.E. N.E. 4.0 ± 0.5 13 ± 2
13 SKA-2 Embedded Image N.E. 2.0 ± 0.3 N.D. N.E. 1.1 ± 0.1 5.1 ± 0.4
14 SKA-17 Embedded Image N.E. 1.4 ± 0.2 2.1 ± 1.0 1.4 ± 0.3 1.3 ± 0.4 2.2 ± 0.3
15 SKA-13 Embedded Image 1.8 ± 0.2 3.3 ± 0.5 36 ± 4 1.3 ± 0.3 5.0 ± 1.0 29 ± 5
16 SKA-7 Embedded Image N.E. N.E. N.E. N.E. 1.5 ± 0.3 14 ± 2
17 SKA-32 Embedded Image N.E. N.E. N.E. N.E. N.E. N.E.
18 SKA-22 Embedded Image N.E. 1.4 ± 0.2 Insoluble N.E. 1.2 ± 0.3 Insoluble
19 SKA-48 Embedded Image 1.9 ± 0.1 12 ± 4 39 ± 8 4.3 ± 0.8 40 ± 7 35 ± 8
20 SKA-18 Embedded Image 1.8 ± 0.2 6.5 ± 0.5 42 ± 5 3.0 ± 0.5 32 ± 5 39 ± 5
21 SKA-42 Embedded Image 1.5 ± 0.1 3.5 ± 1.5 35 ± 5 1.3 ± 0.5 2.8 ± 6 14 ± 2
22 SKA-3 Embedded Image 2.2 ± 0.4 14 ± 3 32 ± 3 2.0 ± 0.5 38 ± 3 41 ± 3
23 SKA-8 Embedded Image 1.1 ± 0.2 7.4 ± 0.5 32 ± 3 6.0 ± 0.7 38 ± 5 34 ± 6
24 SKA-35 Embedded Image 1.6 ± 0.5 3.5 ± 1.0 24 ± 3 1.2 ± 0.5 5 ± 3 26 ± 4
25
SKA-51
Embedded Image
2.2 ± 0.9
18 ± 3
N.D.
1.6 ± 0.5
35 ± 7
N.D.
26 SKA-34 Embedded Image 1.4 ± 0.3 2.5 ± 0.5 33 ± 5 2.5 ± 0.5 13 ± 6 32 ± 2
27 SKA-19 Embedded Image 1.5 ± 0.3 10 ± 1 30 ± 3 1.2 ± 0.2 12 ± 4 29 ± 4
28 SKA-11 Embedded Image 2.3 ± 0.9 22 ± 4 30 ± 5 3.0 ± 2 10 ± 3 19 ± 5
29
SKA-53
Embedded Image
N.E.
Insoluble
Insoluble
N.E.
Insoluble
Insoluble

  • N.E., no effect; N.D., not determined.