Table 1.

Structure-activity relationships for substituted 4-anilino-2-(2-methoxyanilino)-7H-pyrrolo[2,3-d]pyrimidine inhibition of TSSK2 activity

Compound	R1	R2	R3	R4	R5	R6	TSSK2 IC50, nM[a]
1		H	H	F	H	NH2	72 ± 10
2		H	H	F	F	NH2	150 ± 30
3		H	H	F	H		1200 ± 200
4		H	H	H	F	OH	2000 ± 200
5		H	F	H	H	NH2	107 [b]
6		H	F	H	H	NH2	250 ± 50
7	CH3		H	H	F	NH2	280 ± 60
8	CH3		H	H	F	NH2	14,000 ± 2000
9	Cl		H	H	F	NH2	1300 ± 200

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

^[b]N = 2 due to limited sample availability.