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. Author manuscript; available in PMC: 2010 Dec 22.
Published in final edited form as: Biochemistry. 2009 Dec 22;48(50):11872–11882. doi: 10.1021/bi9014488

Table 1.

Inhibition efficiency of the synthesized compounds on A/M2 channels.

graphic file with name nihms161434u1.jpg
Compound R1 R2 AM2 channel activity after 100μM compound inhibition IC50 (μM) Kd (μM)a
Amantadine 6% 15.76±1.24 15.17
BL-1743 25% 45.31±3.92 193.54
8 H NH3+Cl− 11% 12.59±1.11 9.16
9 H NH2+Cl−CH3 8% 15.72±1.89 46.36
10 H graphic file with name nihms161434t1.jpg 8% 14.60±1.70 11.50
11 H graphic file with name nihms161434t2.jpg 25% n.d
12 H NH2+Cl−(CH3)2NH3+Cl− 100% n.d
13 H NH2+Cl−(CH3)3NH3+Cl− 100% n.d >500
14 H graphic file with name nihms161434t3.jpg 91% n.d
15 OH graphic file with name nihms161434t4.jpg 40% n.d
16 H graphic file with name nihms161434t5.jpg 13% 12.54±1.24
17 F graphic file with name nihms161434t6.jpg 31% 57.57±2.24
18 H graphic file with name nihms161434t7.jpg 30% n.d
19 H graphic file with name nihms161434t8.jpg 25% 29.19±1.46
20 5% 0.92±0.11 12.87
a

Kd was obtained by global fitting of Circular Dichroism (CD) data of ligand titration to A/M2TM (22–46) using Igor Pro (wavemetrics). The variation of Kd values is ±25% based on different fitting values obtained from three repeats of amantadine titration and two repeats of compound 20 titration. See supplementary information for details.