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. 2013 May 24;4(7):660–665. doi: 10.1021/ml400062c

Table 1. Structures, Molecular Weights, and MDM2 Binding Activity for RG7112 and Its Fragments.

graphic file with name ml-2013-00062c_0005.jpg

compd 1 2 3 4 5 6 7 8 9 10 11
MW 727.78 70.09 112.56 246.35 305.2 236.31 356.89 478.65 495.48 565.56 554.75
NMR binding? yes no no no yes no yes no yes yes yes
SPR binding? (Kd, μM) 0.22 no no no 26 no no no 20 14 1000
ligand efficiency 0.18       0.31       0.19 0.18 0.10