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. 2014 May 23;136(22):7877–7888. doi: 10.1021/ja502310r

Table 2. Mdm2 Binding Properties of Oxopiperazine-Dipeptide analogues.

graphic file with name ja-2014-02310r_0016.jpg

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
a

Binding affinity for Mdm2 as determined by a competitive fluorescence polarization assay.