Table 1.

Results of 4-anilinoquinazolines 2, 7, 15–17 & 20 in the TNNi3K binding assay.

Compound	R1	R2	R3	R4	R5	TNNi3K (Kd) a (nM)
7 (GSK114)	OMe	OMe	N-SO2NHMe	NMe2	H	25 b
15	OMe	OMe	N-SO2NHMe	NMe2	Me	0% Inh. at 1 µM
16	OMe	H	N-SO2NHMe	NMe2	H	90
17	H	OMe	N-SO2NHMe	NMe2	H	11
2	OMe	OMe	N-SO2NHMe	H	H	120
20	OMe	OMe	H	NMe2	H	6200

^a binding assay (n = 1); ^b previously reported enzyme assay IC₅₀ [10].