Table 1.

Biochemical activities (IC₅₀, Mean ± SD, nM) of ROS1 inhibitors and SAF-189s.

Kinase	SAF-189s	Crizotinib	Ceritinib	Lorlatinib
ROS1	0.5 ± 0.1	1.5 ± 0.2	2.7 ± 0.8	0.3 ± 0.2
ROS1G2032R	12.4 ± 5.4	222.5 ± 55.2	271.4 ± 82.8	17.3 ± 3.7
ROS1L2026M	0.2 ± 0.2	9.8 ± 1.3	2.6 ± 0.2	2.4 ± 0.1
ROS1S1986F	0.7 ± 0.4	3.1 ± 0.9	3.7 ± 1.1	0.4 ± 0.2
ROS1S1986Y	0.3 ± 0.3	2.9 ± 0.7	5.7 ± 1.4	0.4 ± 0.3
ROS1D2033N	2.9 ± 0.9	20.2 ± 3.3	24.0 ± 2.5	2.2 ± 0.3