Figure 3

Hit validation in 19F Ligand-Observed NMR. The TFA-WVIP-NH2 tetrapeptide was used as a reporter in a 19F-LO-NMR peptide displacement assay. (A) The SMRT peptide and compound 21 (bright green and purple traces), but not the negative control 4-chlorobenzoic acid (ClBA, blue trace), were able to displace the BCL6-bound TFA-WVIP-NH2 peptide, as indicated by the recovery of the peptide fluorine signal. (B) The LO-NMR data correlated well with biochemical FP potency, with the 11 strongest FP hits yielding a peptide displacement greater than 50% in LO-NMR.