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

Table 1. pIC₅₀ of Representative Compounds As Measured by AlphaScreen and ΔT_m As Measured by DSF.

	6		7		8		15
target	ΔT_m °C^a^,^b	pIC₅₀	ΔT_m °C^a^,^b	pIC₅₀	ΔT_m °C^a^,^b	pIC₅₀	ΔT_m °C^a^,^b	pIC₅₀
BRD4(1)	1.4 ± 0.40 (3)	4.7 (4.6–4.8)^c	2.2 ± 0.15 (3)	5.7 (5.6–5.8)^c	1.7 ± 0.08 (3)	5.9 (5.9–5.9)^c	4.3 ± 0.16 (3)	5.3 ± 0.54 (2)^a
BRD9	2.1 ± 0.56 (3)	ND	3.6 ± 0.31 (3)	5.9 (5.7–6.1)^c	1.8 ± 0.22 (3)	5.8 (5.6–6)^c	5.6 ± 0.30 (3)	6.3 ± 0.12 (2)^a
CECR2	1.5 ± 0.54 (3)	5.3 (5.1–5.5)^c	2.4 ± 0.7 (3)	5.5 (4.9–6.0)^c	3.2 ± 0.87 (3)	6.6 (6.5–6.7)^c	3.3 ± 0.14 (3)	6.3 ± 0.17 (2)^a
CREBBP	1.6 ± 0.10 (3)	5.2 ± 0.48 (2)^a	1.9 ± 0.12 (3)	5.8 (5.5–6.1)^c	0.7 ± 0.1 (3)	5.9 (5.7–6.2)^c	2.8 ± 0.13 (3)	4.8 ± 0.061 (3)^a
BAZ2B	0.03 ± 0.03 (3)	<4^d	0.23 ± 0.09 (3)	<4^d	0.20 ± 0.11 (3)	<4^d	–0.013 ± 0.18 (3)	<4^d
PB1(5)	0.16 ± 0.03 (3)	<4^d	–0.18 ± 0.13 (3)	<4^d	–0.33 ± 0.05 (3)	<4^d	–0.070 ± 0.087 (3)	<4^d
TIF1α	–0.14 ± 0.04 (3)	<4^d	–0.27 ± 0.05 (3)	<4^d	–0.19 ± 0.06 (3)	<4^d	–0.12 ± 0.082 (3)	<4^d
R²^e	0.90		0.90		0.80		0.82

^a

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

^b

Compound concentration 10 μM.

^c

pIC₅₀ (95% CI based on duplicate pIC₅₀ measurements).

^d

<25% inhibition at 100 μM.

^e

Coefficient of determination based on a linear correlation between DSF Tm shift (abscissa) and AlphaScreen pIC₅₀ (ordinate).