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. Author manuscript; available in PMC: 2022 Jun 24.
Published in final edited form as: J Med Chem. 2021 May 17;64(12):8510–8522. doi: 10.1021/acs.jmedchem.1c00430

Table 2.

Binding of Peptidomimetic Ligands with Non-Natural Kme Mimetics to PHF1 Tudor

ITC
graphic file with name nihms-1705801-t0005.jpg R1 R2 Kd (μM)a Compound ID
graphic file with name nihms-1705801-t0006.jpg graphic file with name nihms-1705801-t0007.jpg 10.1 ± 1.2 UNC7643
graphic file with name nihms-1705801-t0008.jpg graphic file with name nihms-1705801-t0009.jpg 17.9 ± 4.6 UNC6640
graphic file with name nihms-1705801-t0010.jpg graphic file with name nihms-1705801-t0011.jpg 0.96 ± 0.03 UNC6641
TR-FRET
R1 R2 IC50 (μM)b Compound ID
graphic file with name nihms-1705801-t0012.jpg graphic file with name nihms-1705801-t0013.jpg 1.6 ± 0.5 UNC6641
graphic file with name nihms-1705801-t0014.jpg graphic file with name nihms-1705801-t0015.jpg 8 ± 3 UNC7259
graphic file with name nihms-1705801-t0016.jpg graphic file with name nihms-1705801-t0017.jpg 19 ± 4 UNC7253
graphic file with name nihms-1705801-t0018.jpg graphic file with name nihms-1705801-t0019.jpg 21 ± 1 UNC7258
a

Kd values were determined by two independent ITC experiments (mean ± SD).

b

IC50 values were determined by three technical replicates (mean ± SD).