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