Skip to main content
. Author manuscript; available in PMC: 2021 Jan 17.
Published in final edited form as: ACS Chem Biol. 2019 Dec 12;15(1):112–131. doi: 10.1021/acschembio.9b00654

Table 2.

Kd values of fluorescein-conjugated ligands to PcG CBX ChDs. Values were determined by direct fluorescence polarization and are displayed as the average of n=4 ± s.d. NB: No binding. ND: Not determined due to an inability to acquire full binding curves due to low affinity or compound aggregation. MST: MicroScale Thermophoresis. TSA: Thermal Shift Assay. *The non-derivatized ligand was used for for Kd determination by TSA. Full binding curves are provided in SI 7 for FP data, SI 8 for MST data, and SI 9 for TSA data.

 graphic file with name nihms-1573719-t0022.jpg
CBX Protein Chromodomain (Kd (µM))
Compound R = CBX2 CBX4 CBX6 CBX7 CBX8
KED97L-FL graphic file with name nihms-1573719-t0023.jpg 1.1 ± 0.4 2.7 ± 0.4 0.3 ± 0.1 4.7 ± 0.9 0.24 ± 0.03
SW2_110A-FL graphic file with name nihms-1573719-t0024.jpg 4.6 ± 0.9 NB NB >16 ± 5 0.8 ± 0.2
(MST: 0.7 ± 0.1)
(TSA*: 0.5 ± 0.3)
SW2_104A-FL graphic file with name nihms-1573719-t0025.jpg 0.05 ± 0.04 0.17 ± 0.04 0.014 ± 0.004 0.8 ± 0.4 0.0029 ± 0.0008
(MST: 0.005 ± 0.001)
SW2_110B-FL graphic file with name nihms-1573719-t0026.jpg ND NB NB NB ND
(MST: 0.8 ± 0.1)
SW2_90L-FL graphic file with name nihms-1573719-t0027.jpg 0.79 ± 0.01 0.17 ± 0.01 0.030 ± 0.001 0.140 ± 0.008 0.110 ± 0.008