Compound | Human | Cynomolgus Monkey | Rat | |||||||
---|---|---|---|---|---|---|---|---|---|---|

t_{1/2}^{a} | [O] Metabolite^{a} | AO Substrate | t_{1/2}^{a} | [O] Metabolite^{a} | AO Substrate | t_{1/2}^{a} | [O] Metabolite^{a} | AO Substrate | ||

min | % Estimate | min | % Estimate | min | % Estimate | |||||

Unknowns | A-77-01 | 2 ± 0.01 | 54 ± 0.4 | Y | 1 ± 0.02 | 46 ± 3 | Y | 2 ± 0.1 | 54 ± 7 | Y |

AMG 900 | 281 ± 21 | 4 ± 1 | Y | >500 | 1 ± 0.2 | N | >500 | 2 ± 0.3 | N | |

AT-9283 | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

Bafetinib | 2 ± 0.3 | 0 | Y^{b} | 2 ± 0.4 | 0 | Yb | 11 ± 0.05 | 0 | Y^{b} | |

Bosutinib | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

Cabozantinib | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

Ceritinib | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

CHIR99021 | >500 | 2 ± 0.01 | N | 211 ± 6 | 31 ± 2 | Y | >500 | 2 ± 0.006 | N | |

CL-387785 | 13 ± 3 | 29 ± 1 | Y | 4 ± 0.3 | 25 ± 0.7 | Y | 4 ± 1 | 0 | Y^{b} | |

Dasatinib | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

Duvelisib | 449 ± 19 | 12 ± 0.7 | Y | >500 | 0 | N | >500 | 1 ± 0.2 | N | |

Erlotinib | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

GDC-0068 | >500 | 0 | N | >500 | 10 ± 0.6 | Y | >500 | 1 ± 0.03 | N | |

Gefitinib | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

Imatinib | >500 | 6 ± 0.3 | Y | 58 ± 1 | 61 ± 0.6 | Y | >500 | 5 ± 0.2 | Y | |

INCB 28060 | 268 ± 6 | 17 ± 0.1 | Y | 44 ± 5 | 43 ± 1 | Y | 85 ± 0.5 | 41 ± 0.6 | Y | |

KIRA6 | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

Lapatinib | 167 ± 23 | 7 ± 0.8 | Y | 241 ± 16 | 5 ± 1 | Y | >500 | 0 | N | |

Lapatinib_M1 | 19 ± 3 | 13 ± 1 | Y | 3 ± 0.2 | 25 ± 2 | Y | 423^{c} | 21 ± 5 | Y | |

LDN-193189 | 2 ± 0.02 | 58 ± 0.5 | Y | 2 ± 0.06 | 54 ± 6 | Y | 38 ± 1 | 110 ± 28 | Y | |

LDN-211904 | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

Linsitinib | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

ML-347 | 6 ± 1 | 16 ± 0.2 | Y | 6 ± 0.4 | 3 ± 0.3 | Y | 25 ± 4 | 4 ± 0.5 | Y | |

Neratinib | 117 ± 1 | 0 | N | >500 | 0 | N | 142 ± 19 | 1 ± 0.1 | N | |

Oclacitinib | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

OSI-027 | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

OXA-01 | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

Ruxolitinib | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

SB-525334 | 31 ± 1 | 55 ± 0.5 | Y | 9 ± 0.5 | 73 ± 0.7 | Y | >500 | 4 ± 0.1 | Y | |

SGI-1776 | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

Sorafenib | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

THZ1 | 256 ± 2 | 0 | N | 235 ± 7 | 0 | N | 231 ± 31 | 0 | N | |

Vatalanib | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

Venetoclax | >500 | 0 | N | >500 | 0 | N | >500 | 0 | N | |

Positive controls | Carbazeran | 2 ± 0.1 | 34 ± 0.1 | Y | 2 ± 0.03 | 28 ± 0.8 | Y | 7 ± 0.5 | 24 ± 0.1 | Y |

O^{6}-Benzylguanine | 48 ± 3 | 43 ± 1 | Y | 52 ± 0.5 | 33 ± 0.4 | Y | >500 | 3 ± 0.05 | N | |

VX-509 | 372 ± 32 | 26 ± 0.5 | Y | 105 ± 10 | 65 ± 6 | Y | 394 ± 50 | 39 ± 2 | Y | |

XK469 | >500 | 1 ± 0.003 | N | 121 ± 12 | 19 ± 0.4 | Y | 428 ± 29 | 2 ± 0.1 | Y | |

Zoniporide | 44 ± 0.7 | 127 ± 3 | Y | 24 ± 1 | 129 ± 5 | Y | 9 ± 0.7 | 185 ± 37 | Y | |

Negative controls | 4-Aminobiphenyl | 106 ± 35 | 0 | N | — | — | — | — | — | — |

Dapsone | >500 | 0 | N | — | — | — | — | — | — | |

Clopidogrel | 21 ± 1 | 0 | N | — | — | — | — | — | — | |

Oseltamivir | 107 ± 1 | 0 | N | — | — | — | — | — | — | |

Enalapril | 340 ± 122 | 0 | N | — | — | — | — | — | — | |

Fenofibrate | 8 ± 1 | 0 | N | — | — | — | — | — | — |