Table 5.

Inhibitory effect of azetidine, pyrrolidine and 3-piperidine derivatives in seven JmjC KDMs

Compound			pIC50a KDM
28	n	R	2A	3A	4A	4C	4E	5C	6B
28a	0	Me	<4.0 (2)	4.3 ± 0.17 (2)	5.6 ± 0.29 (2)	5.8 ± 0.19 (2)	5.3 ± 0.07 (2)	6.2 ± 0.07 (2)	<4.0 (2)
28b		Et	4.1 ± 0.15 (2)	<4.0 (2)	5.3 ± 0.22 (2)	4.9 ± 0.31 (2)	<4.0 (2)	5.6 ± 0.04 (2)	4.3 ± 0.87 (2)
28c		nPr	4.3 ± 0.13 (2)	<4.0 (2)	5.3 ± 0.26 (2)	5.1 ± 0.19 (2)	4.1 ± 0.24 (2)	5.2 ± 0.06 (2)	4.2 ± 0.83 (2)
28d		Ph	5.3 ± 0.21 (2)	4.5 ± 0.07 (2)	<4.0 (4)	4.7 ± 0.14 (2)	4.3 ± 0.07 (2)	5.4 ± 0.03 (2)	4.0 ± 0.03 (2)
28e		Bn	5.2 ± 0.20 (2)	4.0 ± 0.07 (2)	ND	4.4 ± 0.13 (4)	<4.0 (2)	5.2 ± 0.10 (2)	<4.0 (2)
28f			5.0 ± 0.20 (2)	<4.0 (2)	5.2 ± 0.25 (2)	5.1 ± 0.12 (4)	4.6 ± 0.11 (2)	5.9 ± 0.05 (2)	<4.0 (2)
28g	1	nPr	4.9 ± 0.10 (2)	<4.0 (4)	ND	4.7 ± 0.15 (6)	<4.0 (4)	5.5 ± 0.13 (4)	<4.0 (4)
28h		Ph	6.4 ± 0.10 (2)	ND	ND	ND	ND	ND	ND
28i		Bn	6.0 ± 0.09 (2)	4.2 ± 0.19 (2)	ND	4.5 ± 0.18 (2)	<4.0 (2)	5.2 ± 0.06 (2)	4.3 ± 0.63 (2)
28j			ND	4.0 ± 0.10 (2)	ND	4.4 ± 0.16 (2)	<4.0 (2)	5.7 ± 0.07 (2)	4.1 ± 0.03 (2)
28k	2	Me	4.9 ± 0.15 (2)	4.4 ± 0.27 (2)	4.4 ± 1.65 (2)	4.8 ± 0.21 (2)	<4.0 (2)	5.6 ± 0.06 (2)	4.0 ± 0.17 (2)
28l		Et	5.1 ± 0.17 (2)	4.2 ± 0.17 (2)	ND	4.8 ± 0.38 (2)	4.0 ± 0.13 (2)	5.4 ± 0.05 (2)	4.3 ± 0.16 (2)
28m		nPr	5.3 ± 0.09 (2)	4.5 ± 0.22 (2)	ND	4.7 ± 0.29 (2)	4.0 ± 0.15 (2)	5.3 ± 0.06 (2)	4.1 ± 0.10 (2)
28n		Ph	6.9 ± 0.13 (6)	4.3 ± 0.10 (2)	4.2 ± 1.13 (2)	4.7 ± 0.14 (14)	<4.0 (10)	5.0 ± 0.11 (2)	4.7 ± 0.13 (8)
28o		Bn	5.7 ± 0.08 (2)	4.6 ± 0.14 (2)	ND	4.7 ± 0.42 (2)	<4.0 (2)	5.1 ± 0.27 (2)	4.9 ± 0.19 (2)
28p			6.2 ± 0.08 (2)	4.3 ± 0.17 (2)	ND	4.6 ± 0.78 (4)	<4.0 (2)	5.3 ± 0.07 (2)	4.9 ± 0.13 (2)

^aMean pIC₅₀ ± standard error of the mean (number of determinations) as determined by AlphaScreen.