Table 1.

Evaluation of TPX-0131 in biochemical assays of WT and mutant ALK variants.

Kinase	IC50 (nmol/L)	Kinase	IC50 (nmol/L)	Kinase	IC50 (nmol/L)
WT	1.4	S1206R	0.5	T1151-L1152insT	1.2
C1156Y	0.2	G1202R/L1198F	0.6	V1180L	1.6
E1210K/S1206C	0.2	F1174L	0.7	G1269A	1.6
L1198F/C1156Y	0.2	F1245C	0.7	F1174C	1.8
L1196M/L1198F	0.2	R1275Q	0.8	I1171N	2.3
E1210K	0.3	G1202R	0.9	L1152P	2.9
L1196M	0.3	L1198F	1.0	D1203N	4.4
T1151M	0.4	L1152R	1.1	D1203N/E1210K	6.3
Deleted G1202	0.5	F1174S	1.2	G1269S	6.6

Note: The biochemical kinase assays were performed in the presence of 10 μmol/L ATP following previously described procedures (15).