Table 3.

Kinase inhibitory activity of 7-(2-anilinopyrimidin-4-yl)-1-benzazepin-2-ones 2a–2n against Aurora A, Aurora B, VEGF-R2 and VEGF-R3, represented by either IC₅₀ value (µM) or residual activity at 10 µM (%) ^a.

Compound	R	Aurora A	Aurora B	VEGF-R2	VEGF-R3
2a	H	2.4 µM	26 µM	2.8 µM	5.9 µM
2b	4-CH3	2.4 µM	16 µM	1.8 µM	4.3 µM
2c	4-OCH3	1.8 µM	18 µM	1.3 µM	2.5 µM
2d	4-OC2H5	1.5 µM	20 µM	2.0 µM	3.0 µM
2e	4-OH	0.99 µM	3.5 µM	1.1 µM	1.5 µM
2f	4-Cl	9.4 µM	40 µM	11 µM	19 µM
2g	4-Br	3.5 µM	18 µM	5.4 µM	4.1 µM
2h	4-I	3.5 µM	52 µM	17 µM	6.2 µM
2i	4-NO2	>100 µM	>100 µM	11 µM	35 µM
2j	2-OH	>100 µM	>100 µM	8.4 µM	19 µM
2k	2-Cl	74%	87%	74%	72%
2l	2-Br	73%	116%	78%	64%
2m	3-OH	1.7 µM	6.7 µM	0.78 µM	0.54 µM
2n	3-OH, 4-OCH3	1.4 µM	4.5 µM	0.63 µM	0.55 µM

^a As a measure of assay quality, the Z’-factor [26,27] was used. The Z’ factor did not drop below 0.4 and was above 0.6 in most cases, indicating a very good to excellent assay quality.