Table 1. In Vitro JARID1A, JMJD2C, JMJD1A, and JHDM1F Inhibitory Activities of Compounds 1–4 and 6^a.

		structure			IC50 (μM)
entry	compd	R1	R2	n	JARID1A	JMJD2C	JMJD1A	JHDM1F
1	1				250	430	569	640
2	3b				13	2.2	NDc	19
3	4b				55	83	NDc	1.2
4	6a	n-Bu	Me	4	4.3 ± 0.9	55 ± 11	>100	>100
5	6b	n-Bu	Me	2	53 ± 8.5	>100	NDc	NDc
6	6c	n-Bu	Me	3	6.3 ± 1.8	63 ± 6.4	NDc	NDc
7	6d	n-Bu	Me	5	4.0 ± 0.6	61 ± 1.6	NDc	58 ± 16
8	6e	n-Bu	Me	6	1.8 ± 0.1	6.5 ± 0.3	NDc	NDc
9	6f	Me	Me	4	18 ± 2.0	51 ± 6.3	NDc	NDc
10	6g	Et	Me	4	7.8 ± 1.0	62 ± 11	NDc	NDc
11	6h	n-Pr	Me	4	8.9 ± 3.0	76 ± 4.7	NDc	NDc
12	6i	n-pentyl	Me	4	2.3 ± 0.9	37 ± 26	>100	>100
13	6j	n-hexyl	Me	4	3.3 ± 1.3	43 ± 11	>100	73 ± 9
14	6k	n-Bu	Et	4	14 ± 5.0	65 ± 13	NDc	NDc
15	6l	n-Bu	n-Bu	4	19 ± 6.2	>100	NDc	NDc
16	6m	n-Bu	n-hexyl	4	4.5 ± 0.9	>100	>100	29 ± 13
17	6n	n-Bu	n-octyl	4	3.1 ± 0.3	83 ± 17	>100	24 ± 8
18	7i				63 ± 16	NDc	NDc	NDc
19	7j				21 ± 3.7	NDc	NDc	NDc

^aValue are means of at least three experiments.

^bTaken from the literature (ref (22)).

^cND = no data available.