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. 2014 Nov 14;58(3):1038–1052. doi: 10.1021/jm501092z

Table 2. Summary of Other MDM2 Inhibitors.

entry compd MDM2 binding IC50 cell line; assay; IC50 PDB code in vivo data ref
1 15 80 nMa MCF7; BrdU; 38 μM 1T4E   (53, 54)
2 16 394 nM MCF7; BrdU; 1.1 μM     (55)
3 17 170 nM SJSA-1; SRB; 5.2 μM     (56)
4 18 350 nM SJSA-1; p21; 12 μM   PK data (57)
5 19 >5 μM MCF-7; MTT; 40 nM     (58)
6 20 9.2 nM   3VZV   (59)
7 21 58 nM MV4;11; luminescent; 220 nM 3W69 PK and efficacy in SCID mice (59)
8 22 30 nM   4DIJ   (60)
9 23 916 nMb   3LBK   (61)
10 24 130 nMb       (62)
11 25 150 nMb A549; MTT; 1.97 μM   efficacy in nude mice (63)
12 26 0.90 μM SJSA-1; SRB; 102.3 μM     (64)
13 27 0.8 μMa       (61)
14 28 169 nM SJSA-1; 4.7 μM     (6566)
15 29 41 nM SJSA-1; 1 μM     (6566)
16 30 0.4 nM SJSA-1; EdU; 25 nM 4OBA PK and efficacy in nude mice (67)
17 31 0.1 nM SJSA-1; EdU; 16 nM 4ODE PK and efficacy in nude mice (68)
18 32 6 nM av of three;c MTT; 15 nM   PK and efficacy in nude mice (69)
19 33 7 nM av of three;c MTT; 7 nM 4LWV PK and efficacy in nude mice (69)
a

Binding affinity was measured as Kd;

b

Binding affinity was measured as Ki

c

Average of three cell lines SJSA-1, HCT116, and RKO