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. 2020 Mar 12;11(4):491–496. doi: 10.1021/acsmedchemlett.9b00612

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