. Author manuscript; available in PMC: 2012 May 15.

Published in final edited form as: Bioorg Med Chem Lett. 2011 Mar 4;21(10):3152–3158. doi: 10.1016/j.bmcl.2011.02.114

Table 1.

IC₅₀ (nM) values of selected active quinazolines (4, 15–33)^a


Compound	R¹	R²	R³	Clk4	Dyrk1A	Compound	R¹	R²	R³	Clk4	Dyrk1A
4		H	H	39	62	24		H	H	3981	>10000
15^b		OMe	CH₃	>10000	>10000	25		H	H	7943	>10000
16		H	H	249	1262	26		H	H	128	164
17		H	H	1090	3480	27		H	H	>10000	4517
18		H	H	1051	5697	28		H	H	1642	>10000
19		H	H	331	3152	29		H	H	126	180
20		H	H	3675	>10000	30		H	H	88	1437
21		H	H	>10000	>10000	31		H	H	199	>10000
22		H	H	7943	9012	32		H	H	241	4657
23		H	H	>10000	>10000	33	H		H	>10000	>10000

IC₅₀ values determined by Reaction Biology (www.reactionbiology.com). Compounds were tested in 10-dose IC₅₀ mode with 3-fold serial dilution starting at 50 μM. Reactions were carried out at 10 μM ATP.

IC₅₀ values determined using KinaseGlo (Promega) assay.