Table 1. Inhibitory Potencies of 5-Hydroxybenzoheterocyclic Inhibitors^a.

					IC50 [μM]/% inhibition @ 5 μM
compd	X	R1	R2	R3	Dyrk1A	Dyrk1B	Dyrk2	Clk1	Ck2α
10	s	OH	H	H	0.4	0.2	49%	0.1	12%
11	0	OH	H	H	3.1	6.1	34%	1.9	21%
12	NH	OH	H	H	15	41%	24%	2	22%
13	NMe	OH	H	H	3.4	2.7	25%	2.1	31%
14	S	H	OH	H	3.4	0.8	25%	0.3	33%
15	O	H	OH	H	9.7	1.3	38%	1–5	17%
16	S	OH	Me	H	0.2	0.2	50%	0.05	10%
17	S	Me	OH	H	11	7	8%	25%
18	S	OH	H	F	2	0.4	30%	0.05	20%
19	S	OH	F	H	1.2	0.4	27%	0.3	15%
20	S	CN	H	H	6	2.3	6%	0.4	10%
21	S	H	H	H	2	1	37%	0.2	13%
22	S				42	6%	15%		24%
23	S				0.2	0.1	46%	0.06	9%
24	S				10%	40%	–7%	47%
25	S				0.9	1.6	41%	0.1
TG003					0.83			0.17

^a[ATP] = 100 μM.