Table 2.
Compd | MWa | logPb | logSwc | tPSAd | Lipinskie | Solubility (mg L−1) | Solubility FIf | VEBERg | EGANh | 4_400i | 3_75j |
---|---|---|---|---|---|---|---|---|---|---|---|
1 | 135.19 | 3.40 | −3.07 | 44.45 | 0 | 6267 | Good | Good | Good | Good | Bad |
2 | 149.21 | 3.69 | −3.28 | 44.45 | 0 | 5587 | Good | Good | Good | Good | Bad |
3 | 165.21 | 3.29 | −3.05 | 53.68 | 0 | 7811 | Good | Good | Good | Good | Bad |
4 | 203.18 | 4.21 | −3.88 | 44.45 | 0 | 4191 | Good | Good | Good | Good | Bad |
5 | 211.28 | 4.95 | −4.51 | 44.45 | 0 | 2332 | Reduced | Good | Good | Good | Bad |
6 | 214.08 | 4.01 | −3.94 | 44.45 | 0 | 4144 | Good | Good | Good | Good | Bad |
7 | 169.63 | 3.95 | −3.63 | 44.45 | 0 | 4492 | Good | Good | Good | Good | Bad |
8 | 160.20 | 3.04 | −2.98 | 68.24 | 0 | 8150 | Good | Good | Good | Good | Bad |
9 | 163.24 | 4.12 | −3.54 | 44.45 | 0 | 4747 | Good | Good | Good | Good | Bad |
10 | 153.18 | 3.42 | −3.20 | 44.45 | 0 | 6272 | Good | Good | Good | Good | Bad |
11 | 261.08 | 3.97 | −4.21 | 44.45 | 0 | 3872 | Good | Good | Good | Good | Bad |
12 | 180.18 | 3.15 | −3.09 | 90.27 | 0 | 8282 | Good | Good | Good | Good | Bad |
13 | 149.21 | 3.72 | −3.30 | 44.45 | 0 | 5482 | Good | Good | Good | Good | Bad |
14 | 165.21 | 3.68 | −3.30 | 53.68 | 0 | 6109 | Good | Good | Good | Good | Bad |
15 | 203.18 | 4.37 | −3.98 | 44.45 | 0 | 3789 | Good | Good | Good | Good | Bad |
16 | 211.28 | 4.99 | −4.53 | 44.45 | 0 | 2274 | Reduced | Good | Good | Good | Bad |
17 | 214.08 | 4.12 | −4.01 | 44.45 | 0 | 3866 | Good | Good | Good | Good | Warning |
18 | 169.63 | 3.36 | −3.26 | 44.45 | 0 | 6514 | Good | Good | Good | Good | Bad |
19 | 160.20 | 3.13 | −3.04 | 68.24 | 0 | 7700 | Good | Good | Good | Good | Bad |
20 | 163.24 | 4.16 | −3.56 | 44.45 | 0 | 4629 | Good | Good | Good | Good | Bad |
21 | 153.18 | 3.53 | −3.26 | 44.45 | 0 | 5852 | Good | Good | Good | Good | Bad |
22 | 261.08 | 4.94 | −4.82 | 44.45 | 0 | 2101 | Reduced | Good | Good | Good | Bad |
23 | 180.18 | 3.26 | −3.16 | 90.27 | 0 | 7672 | Good | Good | Good | Good | Warning |
24 | 179.20 | 2.96 | −2.94 | 84.58 | 0 | 9426 | Good | Good | Good | Good | Good |
25 | 136.17 | 2.25 | −2.38 | 57.34 | 0 | 12,637 | Good | Good | Good | Good | Warning |
26 | 149.21 | 3.92 | −3.43 | 44.45 | 0 | 4833 | Good | Good | Good | Good | Bad |
27 | 165.21 | 3.58 | −3.23 | 53.68 | 0 | 6507 | Good | Good | Good | Good | Bad |
28 | 203.18 | 4.44 | −4.03 | 44.45 | 0 | 3625 | Good | Good | Good | Good | Bad |
29 | 214.08 | 4.03 | −3.96 | 44.45 | 0 | 4092 | Good | Good | Good | Good | Bad |
30 | 169.63 | 3.91 | −3.61 | 44.45 | 0 | 4606 | Good | Good | Good | Good | Bad |
31 | 160.20 | 3.06 | −2.99 | 68.24 | 0 | 8048 | Good | Good | Good | Good | Bad |
32 | 163.24 | 4.35 | −3.68 | 44.45 | 0 | 4107 | Good | Good | Good | Good | Bad |
33 | 153.18 | 3.44 | −3.21 | 44.45 | 0 | 6194 | Good | Good | Good | Good | Bad |
34 | 261.08 | 4.22 | −4.37 | 44.45 | 0 | 3308 | Good | Good | Good | Good | Bad |
35 | 180.18 | 3.62 | −3.38 | 90.27 | 0 | 6115 | Good | Good | Good | Good | Warning |
36 | 149.21 | 3.16 | −2.89 | 44.45 | 0 | 8333 | Good | Good | Good | Good | Bad |
37 | 185.24 | 4.34 | −4.03 | 44.45 | 0 | 3303 | Reduced | Good | Good | Good | Bad |
38 | 185.24 | 4.34 | −4.03 | 44.45 | 0 | 3303 | Reduced | Good | Good | Good | Bad |
39 | 99.15 | 2.41 | −1.84 | 44.45 | 0 | 15,731 | Good | Good | Good | Good | Warning |
40 | 101.17 | 2.37 | −1.89 | 44.45 | 0 | 15,217 | Good | Good | Good | Good | Warning |
41 | 143.25 | 3.98 | −2.91 | 44.45 | 0 | 7838 | Good | Good | Good | Good | Bad |
42 | 99.15 | 2.12 | −1.72 | 47.69 | 0 | 17,678 | Good | Good | Good | Good | Warning |
43 | 127.21 | 2.83 | −2.35 | 44.45 | 0 | 12,185 | Good | Good | Good | Good | Warning |
44 | 141.23 | 3.38 | −2.78 | 44.45 | 0 | 8770 | Good | Good | Good | Good | Bad |
45 | 193.31 | 4.24 | −3.64 | 44.45 | 0 | 5056 | Good | Good | Good | Good | Bad |
MW: molecular weight; blogP: octanol/water partition coefficient calculated by means of XLOGP3 program; clogSw: aqueous solubility; dtPSA: topological polar surface area; eLipinski: number of violations of Lipinski’s rule of five (up to 1 violation is allowed); fSolubility FI: solubility calculated by using the Forecaster Index (FI); gVEBER: oral bioavailability calculated by Veber rules; hEGAN: oral bioavailability calculated by Egan rules; i4_400: safety profile calculated by the GSK 4_400 rules; j3_75: safety profile calculated by the Pfizer 3_75 rules.