Table 2. Mdm2 Binding Properties of Oxopiperazine-Dipeptide analogues.
mimetic | R1 | R2 | R3 | R4 | Kd (μM)a |
---|---|---|---|---|---|
9 | Phe | Trp | Ser | Leu | >400 |
10 | Phe | Trp | Asp | Leu | 125 ± 73 |
11 | Phe | Trp | Leu | Leu | 94 ± 16 |
12 | Phe | Trp | Phe | Leu | 49 ± 10 |
Binding affinity for Mdm2 as determined by a competitive fluorescence polarization assay.