Table 1:

Comparison of PrOF NMR and SPR K_d with AlphaScreen IC₅₀ values for the BPTF bromodomain

Ligand	1, Bromosporine	2, TP-238	3, GSK4027
aReported BPTF Kd	1.8 μM35	120 nM†	130 nM36
5FW-BPTF PrOF NMR Kd	37 μM	*	*
5FW-BPTF SPR Kd	19 ± 3 μM	250 ± 20 nM	2.3 ± 0.2 μM
aBPTF SPR Kd	9 ± 1 μM	200 ± 10 nM	1.7 ± 0.1 μM
aBPTF AlphaScreen IC50	10 μM	430 nM	1.5 ± 0.2 μM

AlphaScreen and SPR values were an average of duplicate measurements, except for TP-238 (2) where the SPR value was an average of triplicate measurements and the AlphaScreen value for 3 which is an average of six experimental replicates.

^aIndicates the unlabeled BPTF protein was used, otherwise the 5FW-labeled protein was used.

^*Indicates molecules entered intermediate/slow exchange and K_d values could not be determined.

^†Value reported on thesgc.org.