Table 1. Optimization of 7-Azaindoles.

compd	R1	R2	cLogP	HPK1 Ki (nM)a	LLEb	Abl selectivityc	LCK selectivityd
1	2-MeOPh	H	3.1	0.4	6.3	<1×	55×
2	Et	H	2.1	2.1	6.6	10×	237×
3	H	H	1.5	130	5.4		66×
4	Et	Me	2.4	0.4	7.0	58×	808×
5	Et	Et	2.8	0.2	6.9		2556×
6	Et	Cl	2.6	0.5	6.7		501×

^aAll apparent K_i values represent arithmetic means of at least two determinations using the HPK1 Lantha binding biochemical assay.

^bLLE, lipophilic ligand efficiency based on HPK1 K_i.

^cSelectivity expressed as the ratio of Abl K_i over HPK1 K_i.

^dSelectivity expressed as the ratio of LCK K_i over HPK1 K_i.