AO Status | Compound | Mean Hepatocyte t1/2 ± S.E.a | ||
---|---|---|---|---|
–Hydralazinea | +Hydralazine | fm,AO | ||
min | mina | % | ||
Substrate | A77-01 | 10 ± 0.1 | 25 ± 2 | 60 |
Bafetinib | 22 ± 2 | 53 ± 0.4 | 58 | |
Carbazeran | 9 ± 0.1 | 81 ± 3 | 89 | |
CL-387785 | 16 ± 4 | 30 ± 7 | 47 | |
Duvalisib | 185 ± 7 | 294 ± 25 | 37 | |
Imatinib | 208 ± 16 | 246 ± 3 | BQL (15)b | |
INCB28060 | 115 ± 0.8 | 154 ± 4 | BQL (25)b | |
Lapatinib | 130 ± 11 | 132 ± 7 | BQL (2)b | |
Lapatinib M1 | 50 ± 1 | 68 ± 0.5 | BQL (26)b | |
LDN-193189 | 27 ± 2 | 119 ± 9 | 77 | |
ML-347 | 36 ± 0.07 | 57 ± 2 | 37 | |
SB-525344 | 42 ± 0.07 | >700 | >94 | |
VX-509 | 132 ± 14 | 127 ± 2 | BQL (-4)b | |
Zoniporide | 58 ± 0.9 | >700 | >92 | |
Nonsubstrate | Ceritinib | 362 ± 5 | 268 ± 12 | BQL (–35)b |
GDC-0068 | 103 ± 3 | 115 ± 1 | BQL (11)b | |
KIRA6 | 51 ± 10 | 49 ± 1 | BQL (–4)b | |
Linsitinib | 54 ± 4 | 74 ± 2 | BQL (28)b | |
Midazolam | 39 ± 1 | 42 ± 0.3 | BQL (7)b | |
Neratinib | 51 ± 0.2 | 58 ± 8 | BQL (13)b | |
Oclacitinib | 416 ± 13 | 414 ± 16 | BQL (0)b | |
OSI-027 | 810 ± 208 | 1098 ± 322 | BQL (26)b | |
OXA-01 | 613 ± 30 | 887 ± 33 | BQL (31)b | |
SGI-1776 | 139 ± 0.02 | 156 ± 7 | BQL (11)b | |
THZ1 | 85 ± 11 | 93 ± 8 | BQL (8)b | |
Vatalanib | 48 ± 0.8 | 49 ± 0.2 | BQL (3)b |