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. 2013 Dec 8;57(2):462–476. doi: 10.1021/jm401568s

Table 2. pIC₅₀ of Representative Compounds As Measured by AlphaScreen and ΔT_m As Measured by DSF.

	50		51		53		55
target	ΔT_m °C^a^,^b^,^c	pIC₅₀^a^,^d	ΔT_m °C^a^,^b^,^c	pIC₅₀^a^,^d	ΔT_m °C^a^,^b^,^c	pIC₅₀^a^,^d	ΔT_m °C^a^,^b^,^c	pIC₅₀^a^,^d
BRD4(1)	2.6 ± 0.099 (6)	6.6 ± 0.49 (2)	4.4 ± 0.81 (11)	6.8 ± 0.12 (2)	4.4 ± 0.38 (9)	6.0 ± 0.16 (2)	2.5 ± 0.38 (8)	5.3 ± 0.014 (2)
BRD9	4.9 ± 0.24 (4)	6.5 ± 0.092 (3)	6.6 ± 0.82 (6)	6.7 ± 0.11 (3)	6.2 ± 0.35 (5)	6.0 ± 0.11 (2)	7.3 ± 0.44 (3)	6.2 ± 0.99 (2)
CECR2	3.7 ± 0.16 (3)	6.8 ± 0.17 (2)	1.62 ± 0.48 (4)	4.6 ± 0.24 (2)	2.0 ± 0.16 (3)	4.7 ± 0.10 (2)	2.0 ± 0.16 (3)	6.0 ± 0.14 (2)
CREBBP	3.9 ± 0.33 (4)	6.2 ± 0.62 (2)	7.6 ± 0.94 (7)	6.7 ± 0.074 (2)	7.9 ± 0.33 (6)	6.2 ± 0.57 (2)	6.7 ± 0.35 (6)	6.1 ± 0.61 (2)

^a

Mean ± standard error of the mean (number of determinations).

^b

Compound concentration 10 μM.

^c

All compounds tested showed ΔT_m < 0.2 °C for TIF1α.

^d

All compounds tested showed <30% inhibition of TIF1α at 50 μM.