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. Author manuscript; available in PMC: 2015 Aug 15.
Published in final edited form as: Bioorg Med Chem Lett. 2014 Jun 19;24(16):3968–3973. doi: 10.1016/j.bmcl.2014.06.032

Table 2.

TASK thallium flux assay data for 1,3-bis-amides bearing phenyl group replacements

entry analog structure thallium flux (TF) assay dataa,b selectivity
graphic file with name nihms613776u2.jpg TASK-1 channel TASK-3 channel TASK-3 IC50/TASK-1 IC50
R2 %c IC50 (μM) IC50 (μM)
1 31 2-CH3-phenyl 95.5 0.091 0.96 11
2 32 3-CH3-phenyl c 95.6 0.030 0.15 5.0
3 33 2-i-propyl-phenyl 94.5 0.33 1.7 5.2
4 34 4-t-butyl-phenyl 96.6 0.19 >30 >160
5 35 2-OCH3-phenyl 96.6 0.004 0.39 100
6 36 3-OCH3-phenyl 92.0 0.031 2.2 69
7 37 4-OCH3-phenyl 69.3 1.3 >30 >23
8 38 2,5-di-OCH3-phenyl 93.2 0.15 2.3 15
9 39 2-OCH2CH3-phenyld 100 0.009 0.41 46
10 40 2-OCF3-phenyl 93.4 0.029 0.75 26
11 41 2-isopropoxyphenyl 100 0.21 2.7 13
12 42 2-Cl-phenyl 92.0 0.023 1.34 58
13 43 3-Cl-phenyl 92.2 0.003 0.48 160
14 44 4-Cl-phenyl 77.9 0.15 >30 >200
15 45 3-F-phenyl 93.7 0.025 0.60 24
16 46 2-CF3-phenyl 91.9 0.014 1.4 100
17 47 3-CF3-phenyl 79.3 0.010 5.5 550
18 48 4-CF3-phenyl 20.2 >3 >30 NA
19 49 4-N(CH3)2-phenyl 100 0.15 >30 >200
20 50 2-furyl 92.8 0.14 2.7 19
21 51 2-thiophene 94.1 0.005 0.33 66
22 52 4-pyridyl 96.0 0.095 > 30 > 310
a

Data was averaged from n ≥ 2 experiments.

b

Percent inhibition of TASK-1 at 3μM.

c

hERG IC50 = 12.4 μM.

NA = not applicable.