Figure 3. Small Molecule Library Used to Probe the pVHL:HIF-1α Interaction.
(A) Micromolar small molecule inhibitors 1–3 used for the biophysical and structural characterization of the pVHL:ligand interactions and fragments used to probe individual subsites.
(B) Fragments designed to probe more than one subsite, including reference molecules used to calculate group efficiencies and group lipophilicity efficiencies.
(C) Library of compounds placing a t-butyl, phenyl, pyridyl, or Me-(is)oxazole group at the left-hand site (LHS), right-hand site 1 (RHS1), or 2 (RHS2). ClogP values are not defined for groups and depend on the context of the whole molecule. The values listed were calculated for parent molecules containing a methyl attached to each group.
See also Figure S2.