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. 2020 Feb;16(1):17–30. doi: 10.2174/1573409915666190708102459

Table 1. The structures and experimental activities of GSK3β inhibitors. (Positions other than para substitution of R3 are indicated explicitly in the table by ortho or meta, Where the R3 group of the Cpd8 is in the meta position of R2, the R3 group of Cpd9 is in the ortho position of R2).

graphic file with name CCADD-16-17-tbl1.jpg
No. R1 R2 R3 IC50/(nm) PIC50
5 H H H 41 7.387
8 H H graphic file with name CCADD-16-17-tbl1-t1.jpg 74 7.131
9 H H graphic file with name CCADD-16-17-tbl1-t2.jpg 300 6.523
10 F H graphic file with name CCADD-16-17-tbl1-t3.jpg 1.3 9.114
11 CH3 H graphic file with name CCADD-16-17-tbl1-t4.jpg 0.46 9.337
12 CF3 H graphic file with name CCADD-16-17-tbl1-t5.jpg 1.1 8.959
13 CH3 CH3 graphic file with name CCADD-16-17-tbl1-t6.jpg 1.5 8.824
14 H F graphic file with name CCADD-16-17-tbl1-t7.jpg 9 8.046
15 H CH3 graphic file with name CCADD-16-17-tbl1-t8.jpg 6.3 8.201
16 H H graphic file with name CCADD-16-17-tbl1-t9.jpg 2 8.699
*17 H H graphic file with name CCADD-16-17-tbl1-t10.jpg 18 7.745
*18 H H graphic file with name CCADD-16-17-tbl1-t11.jpg 4.9 8.31
No. R1 R2 R3 IC50/(nm) PIC50
*19 H H graphic file with name CCADD-16-17-tbl1-t12.jpg 4.4 8.357
20 H H graphic file with name CCADD-16-17-tbl1-t13.jpg 0.4 9.398
21 H H graphic file with name CCADD-16-17-tbl1-t14.jpg 12 7.921
22 H H graphic file with name CCADD-16-17-tbl1-t15.jpg 0.67 9.174
*23 H H graphic file with name CCADD-16-17-tbl1-t16.jpg 20 7.699
*24 H H graphic file with name CCADD-16-17-tbl1-t17.jpg 8.4 8.076
37 H H graphic file with name CCADD-16-17-tbl1-t18.jpg 3.1 8.509
38 H H graphic file with name CCADD-16-17-tbl1-t19.jpg 16 7.796
graphic file with name CCADD-16-17-tbl1-t20.jpg
No. R X Y IC50/(nm) PIC50
27 NH2 C C 120 6.921
28 NH2 N C 64 7.194
41 H N N 370 6.432
graphic file with name CCADD-16-17-tbl1-t21.jpg
No. R3 R5 IC50/(nm) PIC50
25 graphic file with name CCADD-16-17-tbl1-t22.jpg graphic file with name CCADD-16-17-tbl1-t22-1.jpg 0.22 9.658
26 graphic file with name CCADD-16-17-tbl1-t23.jpg graphic file with name CCADD-16-17-tbl1-t23-1.jpg 0.48 9.319
44 graphic file with name CCADD-16-17-tbl1-t24.jpg graphic file with name CCADD-16-17-tbl1-t24-1.jpg 12 7.921
45 graphic file with name CCADD-16-17-tbl1-t25.jpg graphic file with name CCADD-16-17-tbl1-t25-1.jpg 690 6.161
46 graphic file with name CCADD-16-17-tbl1-t26.jpg graphic file with name CCADD-16-17-tbl1-t26-1.jpg 0.99 9.004
49 graphic file with name CCADD-16-17-tbl1-t27.jpg graphic file with name CCADD-16-17-tbl1-t27-1.jpg 74 7.131
*50 graphic file with name CCADD-16-17-tbl1-t28.jpg graphic file with name CCADD-16-17-tbl1-t28-1.jpg 90 7.046
*51 graphic file with name CCADD-16-17-tbl1-t29.jpg graphic file with name CCADD-16-17-tbl1-t29-1.jpg 22 7.658

* The test set molecules.