TABLE 1.
Structure and corresponding activity data of reported PGAM1 inhibitors.
Number | R1 | R2 | R3 | R4 | R5 | R6 | X | IC50 (μM) | pIC50 |
---|---|---|---|---|---|---|---|---|---|
1 |
![]() |
H | OH | H | H | H | O | 10.10 | 5.00 |
2 |
![]() |
H | OH | H | H | H | O | 13.20 | 4.88 |
3 a |
![]() |
H | OH | H | H | H | O | 6.40 | 5.19 |
4 |
![]() |
H | OH | H | H | H | O | 10.2 | 4.99 |
5 |
![]() |
H | OH | H | H | H | O | 8.40 | 5.08 |
6 |
![]() |
H | OH | H | H | H | O | 5.90 | 5.23 |
7 |
![]() |
H | OH | H | H | H | O | 5.50 | 5.26 |
8 |
![]() |
H | OH | H | H | H | O | 6.00 | 5.22 |
9 a |
![]() |
H | H | H | H | H | O | 14.3 | 4.84 |
10 |
![]() |
H | H | H | H | -OCH3 | O | 6.50 | 5.19 |
11 a |
![]() |
H | H | H | H | -CH3 | O | 8.60 | 5.07 |
12 |
![]() |
H | H | -OCH3 | H | H | O | 4.60 | 5.34 |
13 |
![]() |
H | H | -CH3 | H | H | O | 8.00 | 5.10 |
14 |
![]() |
H | H | Cl | H | H | O | 3.50 | 5.46 |
15 |
![]() |
H | H | F | H | H | O | 13.7 | 4.86 |
16 |
![]() |
H | H | -NO2 | H | H | O | 2.10 | 5.68 |
17 |
![]() |
H | H | OH | H | H | O | 6.40 | 5.19 |
18 |
![]() |
H | H | −COOCH3 | H | H | O | 2.70 | 5.57 |
19 | -CH3 | OH | H | H | H | H | -C=O | 5.37 | 5.27 |
20 |
![]() |
OH | H | H | H | H | -C=O | 2.05 | 5.69 |
21 |
![]() |
OH | H | H | H | H | -C=O | 1.75 | 5.76 |
22 |
![]() |
OH | H | H | H | H | -C=O | 1.50 | 5.82 |
23 a |
![]() |
OH | H | H | H | H | -C=O | 0.36 | 6.44 |
24 |
![]() |
OH | H | H | H | H | -C=O | 0.84 | 6.08 |
25 |
![]() |
OH | H | H | H | H | -C=O | 0.55 | 6.26 |
26 |
![]() |
OH | H | H | H | H | -C=O | 0.48 | 6.32 |
27 |
![]() |
OH | H | H | H | H | -C=O | 2.81 | 5.55 |
28 |
![]() |
OH | H | H | H | H | -C=O | 2.86 | 5.54 |
29 |
![]() |
OH | H | H | H | H | -C=O | 0.63 | 6.20 |
30 |
![]() |
OH | H | H | H | H | -C=O | 0.55 | 6.26 |
31 |
![]() |
OH | H | H | H | H | -C=O | 0.49 | 6.31 |
32 a |
![]() |
OH | H | H | H | H | -C=O | 0.19 | 6.72 |
33 a |
![]() |
OH | H | H | H | H | -C=O | 1.29 | 5.89 |
34 |
![]() |
OH | H | H | H | H | -C=O | 2.05 | 5.69 |
35 |
![]() |
OH | H | H | H | H | -C=O | 0.097 | 7.01 |
36 |
![]() |
OH | H | H | H | H | -C=O | 0.25 | 6.60 |
37 a |
![]() |
OH | H | H | H | H | -C=O | 0.26 | 6.59 |
38 |
![]() |
OH | H | H | H | H | -C=O | 0.14 | 6.85 |
39 |
![]() |
OH | H | H | H | H | -C=O | 0.33 | 6.48 |
40 |
![]() |
OH | H | H | H | H | -C=O | 2.60 | 5.59 |
41 |
![]() |
OH | H | H | H | H | -C=O | 0.54 | 6.27 |
42 |
![]() |
OH | H | H | H | H | -C=O | 0.90 | 6.05 |
43 |
![]() |
OH | H | H | H | H | -C=O | 0.47 | 6.33 |
44 |
![]() |
OH | H | H | H | H | -C=O | 2.20 | 5.66 |
45 a |
![]() |
OH | H | H | H | H | -C=O | 0.61 | 6.21 |
46 |
![]() |
OH | H | H | H | H | -C=O | 0.54 | 6.27 |
47 |
![]() |
OH | H | H | H | H | -C=O | 0.79 | 6.10 |
48 a |
![]() |
OH | H | H | H | H | -C=O | 0.89 | 6.05 |
49 |
![]() |
OH | H | H | H | H | -C=O | 0.27 | 6.57 |
50 |
![]() |
OH | H | H | H | H | -C=O | 0.28 | 6.55 |
51 |
![]() |
OH | H | H | H | H | -C=O | 0.89 | 6.05 |
52 |
![]() |
OH | H | H | H | H | -C=O | 0.90 | 6.05 |
53 |
![]() |
OH | H | H | H | H | -C=O | 0.26 | 6.59 |
54 |
![]() |
OH | H | H | H | H | -C=O | 0.20 | 6.70 |
55 |
![]() |
OH | H | H | H | H | -C=O | 0.35 | 6.46 |
56 |
![]() |
OH | H | H | H | H | -C=O | 0.47 | 6.33 |
57 |
![]() |
OH | H | H | H | H | -C=O | 0.26 | 6.59 |
58 |
![]() |
-OCH3 | H | H | H | H | -C=O | 2.92 | 5.53 |
59 |
![]() |
![]() |
H | H | H | H | -C=O | 2.00 | 5.70 |
60 |
![]() |
OH | OH | H | H | H | O | 2.80 | 5.55 |
61 |
![]() |
OH | OH | H | H | H | O | 7.20 | 5.14 |
62 |
![]() |
OH | OH | H | H | H | O | 1.90 | 5.72 |
63 |
![]() |
OH | OH | H | H | H | O | 3.50 | 5.46 |
64 |
![]() |
OH | OH | H | H | H | O | 6.30 | 5.20 |
65 a |
![]() |
OH | OH | H | H | H | O | 5.80 | 5.24 |
66 |
![]() |
OH | OH | H | H | H | O | 5.50 | 5.26 |
67 |
![]() |
OH | OH | H | H | H | O | 3.60 | 5.44 |
68 a |
![]() |
OH | OH | H | H | H | O | 2.90 | 5.54 |
69 a |
![]() |
OH | OH | H | H | H | O | 1.90 | 5.72 |
70 a |
![]() |
OH | OH | H | H | H | O | 4.20 | 5.38 |
71 a |
![]() |
OH | OH | H | H | H | O | 2.10 | 5.68 |
72 |
![]() |
OH | OH | H | H | H | O | 1.70 | 5.77 |
73 |
![]() |
OH | OH | H | H | H | O | 1.60 | 5.80 |
74 |
![]() |
OH | OH | H | H | H | O | 1.20 | 5.92 |
75 |
![]() |
OH | OH | H | H | H | O | 2.60 | 5.59 |
76 a |
![]() |
OH | OH | H | H | H | O | 0.50 | 6.30 |
77 a |
![]() |
OH | OH | H | H | H | O | 2.70 | 5.57 |
78 |
![]() |
OH | OH | H | H | H | O | 1.00 | 6.00 |
Test set for the validation of the 3D-QSAR model.