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

Table 3. Computationally Predicted Oxopiperazine p53 Mimics and Their Potential to Target Mdm2.

graphic file with name ja-2014-02310r_0017.jpg

mimetic R1 R2 R3 R4 Kd (μM)a
13 Phe Trp Phe Nle 2.5 ± 0.5
14 Phe Trp Tyr Leu 3.1 ± 0.2
15 Nap Trp Phe Leu 0.9 ± 0.1
16 Tyr Trp Phe Leu 0.4 ± 0.05
17 Tyr(O-Me) Trp Phe Leu 0.3 ± 0.01
18 Phe(3-Cl) Trp Phe Leu 0.3 ± 0.04
19 Phe(3-Me) Trp Phe Leu 2.6 ± 0.04
20 Phe(4-Cl) Trp Phe Leu 1.3 ± 0.1
a

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