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. Author manuscript; available in PMC: 2012 Mar 24.
Published in final edited form as: J Med Chem. 2011 Feb 24;54(6):1555–1564. doi: 10.1021/jm101323b

Table 1.

D2, D3 and D4 Affinities (Ki ± SD, nM) of the benzamide analogs.

D2 D3 D4 D2/D3 Ratio Log Pa
1 34.4 ± 4.7 0.8 ± 0.1 896 ± 272 43 3.09
2 54.5 ± 4.4 2.4 ± 0.4 804 ± 46 23 2.94
18a 27.1 ± 3.5 1.1 ± 0.1 1,400 ± 320 25 3.48
18b 20.9 ± 3.7 6.2 ± 0.9 ND 3.4 3.08
18c 52.0 ± 6.6 4.2 ± 0.2 2,100 ± 380 12.2 2.72
19a 131 ± 13 24.9 ± 3.3 ND 5.2 3.43
19b 55.3 ± 6.0 6.2 ± 0.3 ND 8.9 3.55
19c 59.2 ± 5.8 18.2 ± 2.3 ND 3.3 3.16
19d 17.8 ± 0.8 18.5 ± 2.4 ND 1 3.66
19e 13.4 ± 2.3 13.6 ± 2.0 ND 1 4.49
19f 13.2 ± 0.8 10.9 ± 1.5 ND 1.2 4.73
19g 57.6 ± 3.7 13.8 ± 1.2 ND 4.2 4.15
20a 15.1 ± 1.7 0.65 ± 0.2 890 ± 100 23 3.75
20b 21.4 ± 2.9 6.9 ± 1.0 ND 3.1 3.68
20c 15.1 ± 2.7 0.52 ± 0.03 990 ± 200 29 3.73
20d 14.2 ± 1.9 2.5 ± 0.3 ND 5.7 3.34
20e 27.7 ± 5.4 0.17 ± 0.01 246 ± 13 163 4.67
20f 31.7 ± 2.1 5.2 ± 0.3 ND 6.1 2.98
21a 35.2 ± 2.5 3.6 ± 0.6 ND 9.8 3.83
21b 17.7 ± 2.7 1.1 ± 0.2 890 ± 380 16.1 3.61
21c 37.9 ± 5.0 8.4 ± 1.3 ND 4.5 3.81
21d 64.8 ± 8.4 19.6 ± 3.2 ND 3.3 3.41
21e 70.5 ± 9.6 1.1 ± 0.2 182 ± 5 64 4.74
21f 25.9 ± 2.4 11.2 ± 2.2 ND 2.3 3.26
21g 10.9 ± 0.4 6.7 ± 1.1 ND 1.6 3.72
21h 12.0 ± 0.6 3.1 ± 0.3 ND 3.9 4.36
a

Calculated using ACD log D software, Advanced Chemistry Development, Toronto, Canada.