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. Author manuscript; available in PMC: 2016 Sep 15.
Published in final edited form as: Bioorg Med Chem Lett. 2015 Jul 17;25(18):3956–3960. doi: 10.1016/j.bmcl.2015.07.031

Table 1.

SAR of N-phenylpicolinamide derivatives.

graphic file with name nihms711916u2.jpg
Compd R1 R2 MW CLogP tPSA Affinity IC50 (nM) Log(IC50 ± SE)
2 H graphic file with name nihms711916t1.jpg 262.69 2.80 50.69 5.1 −8.29 ± 0.09
3 H graphic file with name nihms711916t2.jpg 264.23 2.67 50.69 4.6 −8.34 ± 0.08
10 H graphic file with name nihms711916t3.jpg 246.24 2.26 50.69 31.6 −7.50 ± 0.09
11 H graphic file with name nihms711916t4.jpg 307.15 2.95 50.69 322 −6.49 ± 0.08
12 H graphic file with name nihms711916t5.jpg 354.15 3.16 50.69 146 −6.84 ± 0.10
13 H graphic file with name nihms711916t6.jpg 228.25 2.22 50.69 13.7 −7.86 ± 0.10
14 H graphic file with name nihms711916t7.jpg 244.31 2.81 41.46 4.9 −8.31 ± 0.07
15 F graphic file with name nihms711916t8.jpg 280.68 2.96 50.69 7.3 −8.13 ± 0.11
16 F graphic file with name nihms711916t9.jpg 282.22 2.85 50.69 6.7 −8.18 ± 0.10
17 F graphic file with name nihms711916t10.jpg 264.23 2.42 50.69 89.2 −7.05 ± 0.10
18 H graphic file with name nihms711916t11.jpg 223.23 1.89 65.25 10.4 −7.98 ± 0.05
19 H graphic file with name nihms711916t12.jpg 241.23 2.06 65.25 7.4 −8.13 ± 0.04
20 H graphic file with name nihms711916t13.jpg 257.68 2.50 65.25 5.3 −8.28 ± 0.04
21 H graphic file with name nihms711916t14.jpg 302.13 2.78 65.25 47 −7.33 ± 0.08
22 H graphic file with name nihms711916t15.jpg 349.13 3.04 65.25 172 −6.77 ± 0.08
23 H graphic file with name nihms711916t16.jpg 280.68 2.97 50.69 3.2 −8.49 ± 0.07
24 H graphic file with name nihms711916t17.jpg 282.70 2.97 50.69 3.2 −8.49 ± 0.11
25 H graphic file with name nihms711916t18.jpg 248.25 2.39 50.69 3.7 −8.43 ± 0.03