Compound | HLM | rUGT | pKa | clogP | ||
---|---|---|---|---|---|---|
Km | Ki | Km | Ki | |||
Triazoles | μM | |||||
Alprazolam | 158 | N.A. | 261 | N.A. | 2.37 | 1.92 |
Fluconazole | 2691 | N.A. | UGT2B7 substrate | UGT2B7 substrate | 2.44 | 0.45 |
Itraconazole | 8.4 | 421 | No data | No data | 2.94 | 4.99 |
Posaconazole | 27.9a | N.A. | 15.9a | N.A. | 2.75 | 4.67 |
Voriconazole | 550 | N.A. | 1130 | N.A. | 2.72 | 1.21 |
Imidazoles | ||||||
Midazolam | 46b | 58b | 64b | 79b | 6.03 | 3.8 |
Tioconazole | 14.8 | 170 | 124 | 245 | 6.66 | 4.28 |
Ketoconazole | 23.3 | 326 | 7 (n = 2) | 941 (n = 2) | 6.88 | 4.04 |
Econazole | 30 | 286 | 115 | 192 | 6.68 | 4.48 |
Miconazole | 33 | 517 | 58.7 | 475 | 6.64 | 4.97 |
Bifonazole | 84 | 72 | 28 | 47 | 6.55 | 4.69 |
Sulconazole | 144 | 371 | 35 | 290 | 6.55 | 4.36 |