Table 1.

IC₅₀ values (nM) for in vitro competition assays performed with HT-1 and ATP-competitive inhibitors 2–10 against SRC and HCK variants.

Compound	Activated SRC*	SRCSH2eng	Activated HCK*	HCKSH2eng	HCKSH3eng
Dasatinib	< 25	< 25	< 25	< 20	< 1
2	42 ± 15	70 ± 9	440 ± 120	54 ± 7	39 ± 1
3	270 ± 50	1900 ± 300	2100 ± 700	3100 ± 300	400 ± 100
4	14 ± 2	26 ± 1	81 ± 8	37 ± 11	33 ± 11
5	> 10000	> 10000	> 10000	> 10000	1300 ± 300
6	64 ± 13	390 ± 20	450 ± 40	550 ± 60	310 ± 50
7	110 ± 10	74 ± 10	87 ± 14	46 ± 10	110 ± 80
8	270 ± 70	35 ± 4	1100 ± 100	< 20	13 ± 3
9	800 ± 160	180 ± 70	2700 ± 40	63 ± 9	27 ± 10
10	1100 ± 500	< 25	490 ± 170	27 ± 4	< 1

^*Activated SRC and Activated HCK were obtained via autophosphorylation of the activation loop of SRC^Y527F and HCK^Y527F.

All IC₅₀ values were determined using the competition assay protocol described in the Methods section. All experiments were performed in triplicate, and data represent mean values ± SEM.