Table 3.

Structure-activity relationships for substituted N²,N⁴-diphenyl-2,4-pyrimidinediamine inhibition of TSSK2

Compound	R1	X	Y	R2	R3	R4	R5	R6	R7	TSSK2 IC50, nM[a]
17	Me	N	N	H	OMe	Br		H	H	31 ± 7
18	Me	N	N	H	OMe	Cl		H	H	37 ± 5
19	Me	N	CH	H	OMe	Cl		H	H	66 ± 8
20	-	O	N	H	OMe	Cl		H	H	750 ± 110
21	-	O	N	H	OMe	F		H	H	13,000 ± 2000
22		CH	N	H	OMe	Cl		H	H	80 ± 13
23	H	N	CH	Me	OiPr	Cl		H	H	610 ± 30
24	N(CH3)2	CH	N	H	OMe	Cl		H	H	230 ± 30
25		CH	N	H	OMe	Cl		H	H	510 ± 80
26	H	N	N	H	H	Cl		H	H	963 ± 7
27	-	O	N	H	OMe	Cl		H	H	7600 ± 800
28	-	O	N	H	H	Cl		H	H	> 100,000
29	H	CH	N	H	H	H	COOH	H	H	> 100,000
30	Me	N	N	H	H	Me	H		H	6200 ± 900
31		N	N	H	OMe	CF3	H		H	15,000 ± 1000
32		N	N	H	OMe	Cl	OMe	H		62,000 ± 4000
33	-	O	N	H	H	F	H	H		> 100,000

^[a]Mean ± SEM of at least 3 independent experiments.