Table 1. cAbl, hERG, and CYP3A4 Activities as Well as Metabolic Stability and CC50 Values for Target Compounds.
cAbl IC50 (nM) | hERG IC50 (μM) | CYP3A4 IC50 (μM) | Mouse Liver Microsomes t1/2 (min) | Human Liver Microsomes t1/2 (min) | THLE-3 CC50 (μM) | HEK293 CC50 (μM) | |
---|---|---|---|---|---|---|---|
1 | 0.30 | 0.34 | 11.7 | ||||
2 | 0.39 | 0.10 | 13.4 | ||||
3 | 0.65 | 0.08 | 13.5 | ||||
4 | 9.96 | 5.02 | 5.58 | 10.95 | 26.87 | 17.0 | 14.5 |
5 | 8.31 | 12.1 | 7.28 | 16.78 | 39.84 | >50.0 | >50.0 |
6 | >30 | 0.78 | 4.61 | 26.45 | 157.53 | ||
Nilotinib | 5.56 | 0.45 | 0.58 | 7.89 | 7.89 | ||
Ponatinib | 0.31 | 0.77 | 11.4 | 31.94 | 182.4 |