Compound | Residual Activity | Km | Vmax | Vmax/Km | Isoform | ||
---|---|---|---|---|---|---|---|
HLMs | UGT1A1 | ||||||
% | μM | nmol/min/mg | μl/min/mg | ||||
Group A | |||||||
Acetaminophen | 92 ± 4 | 94 ± 4 | 4100a | 1.5a | 0.4 | 1A6a | |
Furosemide | 82 ± 6 | 76 ± 5 | 950b | 0.1b | 0.1b | 1A9, 2B7c | |
Ibuprofen | 79 ± 2 | 78 ± 4 | 188d | 0.7d | 3.5d | 2B7e | |
Imipramine | 92 ± 2 | 88 ± 4 | 1000b | 0.4b | 0.4b | 1A4c | |
Ketoprofen | 86 ± 4 | 80 ± 8 | 1600b | 0.4b | 0.2b | 1A9, 2B7c | |
Mycophenolic acid | 84 ± 2 | 82 ± 3 | 180f | 5.2f | 28.7f | 1A9, 2B7f | |
Serotonin | 90 ± 6 | 96 ± 5 | 8800g | 43.4g | 4.9 | 1A6g | |
Valproic acid | 95 ± 3 | 96 ± 2 | 4475b | 0.9b | 0.2b | 1A6, 1A9, 2B7h | |
Group B | |||||||
Ethynylestradiol | 24 ± 7 | 20 ± 3 | 205b | 0.1b | 0.7b | 1A1c | |
Propofol | 23 ± 9 | 18 ± 9 | 235i | 3.8i | 16 | 1A9c | |
Tranilast | 27 ± 7 | 17 ± 8 | 52j | 0.01j | 0.2 | 1A1j | |
Group C | |||||||
4-Methylumbelliferone | 52 ± 7* | 64 ± 1 | 143k | 72.1k | 504 | 1A6k | |
1-Naphthol | 56 ± 7* | 84 ± 2 | 42i | 17.5i | 417 | 1A6l | |
2-Naphthol | 57 ± 7* | 76 ± 2 | 12m | 31.2m | 2600m | 1A6n | |
4-Nitrophenol | 79 ± 6* | 97 ± 2 | 308k | 69.2k | 225 | 1A6k |