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. Author manuscript; available in PMC: 2014 May 28.
Published in final edited form as: J Med Chem. 2013 Mar 27;56(7):2804–2812. doi: 10.1021/jm301538e

Table 2.

SAR of 4-Substituted Adamantan-1-yl-benzyl-aminesa

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R1= -H Amt graphic file with name nihms574764t1.jpg graphic file with name nihms574764t2.jpg graphic file with name nihms574764t3.jpg graphic file with name nihms574764t4.jpg graphic file with name nihms574764t5.jpg graphic file with name nihms574764t6.jpg graphic file with name nihms574764t7.jpg graphic file with name nihms574764t8.jpg graphic file with name nihms574764t9.jpg graphic file with name nihms574764t10.jpg
/ ID # 1 5 6 7 8 9 10 11 12 13 14
S31N
% inh/ 35 ± 2/ 1 ± 1 10 ± 1 20 ± 2 32 ± 2 3 ± 1 8 ± 1 26 ± 3 25 ± 2 8 ± 1 15 ± 1
IC50 199.9 μM
WT
% inh/ 91 ± 3/ 77 ± 1 31 ± 2 13 ± 2 3 ± 2 7 ± 2 3 ± 2 4 ± 3 4 ± 2 6 ± 1 6 ± 1
IC50 16.1 μM
R1= graphic file with name nihms574764t11.jpg graphic file with name nihms574764t12.jpg graphic file with name nihms574764t13.jpg graphic file with name nihms574764t14.jpg graphic file with name nihms574764t15.jpg graphic file with name nihms574764t16.jpg graphic file with name nihms574764t17.jpg graphic file with name nihms574764t18.jpg graphic file with name nihms574764t19.jpg graphic file with name nihms574764t20.jpg graphic file with name nihms574764t21.jpg
/ ID # 15 16 17 18 19 20 21 22 23 24 25
S31N
% inh/ 12 ± 1 21 ± 2 14 ± 1 8 ± 2 8 ± 2 42 ± 2/ 31 ± 2 17 ± 2 31 ± 2 19 ± 2 8 ± 2
IC50 166 μM
WT
% inh/ 2 ± 2 45 ± 2 49 ± 2 36 ± 2 77 ± 1 67 ± 2 43 ± 1 26 ± 2 2 ± 2 16 ± 1 73 ± 2
IC50
a

The activity of the inhibitors was measured using the TEVC technique with full length AM2 protein in the Xenopus oocytes membrane; the average of three measurements was reported (see Experimental Section in the Supporting Information).