Table 3.
Comparison of virtual screening results (number of compounds in hit list and hit rates) for the AfroCancer and NPACT datasets of the pharmacophore models generated
PDB code | AfroCancer
|
NPACT
|
||
---|---|---|---|---|
Number of hits | Hit rate (%) | Number of hits | Hit rate (%) | |
1IEP | 12 | 3.07* | 11 | 0.70 |
2JDO | 107 | 27.37* | 338 | 21.47 |
2XMY | 69 | 17.65* | 223 | 14.17 |
3E37a | 189 | 48.34 | 882 | 56.04 |
3E37b | 228 | 58.31* | 907 | 57.62 |
3E37c | 95 | 24.30 | 440 | 27.95 |
3PE1d | 37 | 9.46 | 149 | 9.47 |
3PE1e | 3 | 0.77* | 3 | 0.19 |
3PE2 | 106 | 27.11* | 367 | 23.32 |
4ACM | 35 | 8.95* | 110 | 6.99 |
4BBGf | 26 | 6.65a | 93 | 5.91 |
4BBGg | 0 | 0.00 | 0 | 0.00 |
4BBGh | 1 | 0.26* | 3 | 0.19 |
4PK5i | 94 | 24.04* | 301 | 19.12 |
4PK5j | 102 | 26.09* | 308 | 19.57 |
Notes:
Hit rate for AfroCancer supersedes that of NPACT;
3E37-I model is a four-point pharmacophore centered on two HBAs and two hydrophobic centers;
3E37-II model is a three-point pharmacophore centered on two HBAs and one hydrophobic center;
3E37-III model is a three-point pharmacophore centered on two HBAs and one hydrophobic center;
3PE1-I model is a six-point pharmacophore centered on one HBD, three HBAs, and two hydrophobic centers;
3PE1-II model is a four-point pharmacophore centered on one HBD, one HBA, and two hydrophobic centers;
4BBG-I model is a four-point pharmacophore centered on one positive ionizable group;
4BBG-II model is a four-point pharmacophore similar to the 4BBG-I model, except that an HBD replaces the positive ionizable group in the former model;
4BBG-III model is almost identical to 4BBG-I, but separated by exclusion volumes;
4PK5-I model is a three-point pharmacophore centered on one HBD and two hydrophobic centers; and
4PK5-II model is an almost identical model to 4PK5-I, but separated by exclusion volumes.
Abbreviations: NPACT, Naturally Occurring Plant-based Anticancer Compound-Activity-Target; PDB, Protein Data Bank; HBA, H-bond acceptor; HBD, H-bond donor.