Table 3.

Inhibitory effect of N-substituted 1,2,3-triazole isonicotinic acids in seven JmjC KDMs

Compound		pIC50a KDM
14	R	2A	3A	4A	4C	4E	5C	6B
14a	H	5.3 ± 0.20 (8)	4.7 ± 0.15 (2)	5.5 ± 0.33 (2)	5.2 ± 0.14 (4)	4.8 ± 0.15 (4)	4.9 ± 0.22 (4)	<4.0 (6)
14b	Me	4.9 ± 0.18 (8)	4.6 ± 0.24 (2)	4.7 ± 0.19 (4)	5.0 ± 0.23 (4)	4.1 ± 0.10 (4)	5.2 ± 0.13 (4)	<4.0 (6)
14c	Et	4.5 ± 0.13 (8)	5.1 ± 0.21 (2)	ND	5.2 ± 0.19 (4)	4.1 ± 0.10 (2)	5.0 ± 0.10 (4)	<4.0 (4)
14d		5.2 ± 0.16 (8)	5.1 ± 0.28 (2)	ND	5.3 ± 0.20 (4)	4.3 ± 0.21 (2)	5.3 ± 0.09 (4)	4.3 ± 0.17 (6)
14e	Bn	5.0 ± 0.14 (2)	4.9 ± 0.25 (2)	4.1 ± 0.11 (4)	4.4 ± 0.12 (2)	<4.0 (4)	5.1 ± 0.13 (2)	<4.0 (4)
14f		5.1 ± 0.12 (2)	5.5 ± 0.13 (2)	4.2 ± 0.12 (4)	4.4 ± 0.08 (2)	4.0 ± 0.20 (2)	5.1 ± 0.16 (2)	4.1 ± 0.17 (4)
14g		5.2 ± 0.10 (2)	5.0 ± 0.19 (2)	<4.0 (2)	<4.0 (2)	<4.0 (2)	5.0 ± 0.09 (2)	4.1 ± 0.12 (4)
14h		5.1 ± 0.17 (2)	4.7 ± 0.28 (2)	<4.0 (2)	<4.0 (2)	<4.0 (2)	5.4 ± 0.09 (2)	<4.0 (4)

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