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