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 | (65, 66) | ||
| 15 | 29 | 41 nM | SJSA-1; 1 μM | (65, 66) | ||
| 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) |
Binding affinity was measured as Kd;
Binding affinity was measured as Ki
Average of three cell lines SJSA-1, HCT116, and RKO