α-Naphthoflavone | CYP1A2 | 0.02 | 0.1 | 91 | Suitably selective; stimulation of CYP2C9 activity observed at high concentrations | 0.0001 – 0.1 | 0.0005 – 0.5 |
Tienilic Acid* | CYP2C9 | 3 | 3 | 96 | Suitably selective | 0.001 – 10 | 0.001 – 10 |
Quinidine | CYP2D6 | 1 | 1 | 96 | Suitably selective | 0.0001 – 1 | 0.0001 – 1 |
Sulfaphenazole | CYP2C9 | 5 | 5b | 96 | Suitably selective | 0.001 – 10 | 0.001 – 10b |
Furafylline* | CYP1A2 | 5 | 5b | 96 | Suitably selective | 0.001 – 10 | 0.001 – 10b |
N-Benzylnirvanol | CYP2C19 | 2 | 2 | 93 | Suitably selective | 0.001 – 10 | 0.001 – 10 |
Gemfibrozil glucuronide* | CYP2C8 | 10 | 12 | 85 | | 0.001 – 100 | 0.001 – 110 |
CYP3cide* | CYP3A4 | 0.2 | 0.2 | 89 | Unable to achieve complete (>95%) inhibition of CYP3A | 0.0001 – 1 | 0.0001 – 1 |
Montelukast | CYP2C8 | 0.0008 | 0.4 | 88 | High nonspecific binding | 0.000001 – 0.01 | 0.0005 – 5 |
PPP* | CYP2B6 | 5 | 5 | 84 | | 0.01 – 100 | 0.01 – 100 |
Ketoconazole | CYP3A4 | 0.03 | 0.1 | 88 | | 0.0001 – 1 | 0.0003 – 3 |
Troleandomycin* | CYP3A4 | 50 | 50b | 88 | Solubility limitations preclude testing of concentrations >100 µM | 0.01 – 100 | 0.01 – 100b |
Dasotraline* | CYP2B6 | 0.007 | 0.1 | 77 | Best used as a CYP2A6-selective or pan-CYP inhibitor | 0.0001 – 1 | 0.0002 – 20 |
Paroxetine* | CYP2D6 | 0.06 | 0.1 | 77 | Currently not recommended for use in HLMs | 0.001 – 1 | 0.002 – 2 |
Ticlopidine* | CYP2CB6 | 0.07 | 0.09 | 75 | Currently not recommended for use in HLMs | 0.001 – 10 | 0.001 – 15 |
Esomeprazole* | CYP2C19 | 5 | 5 | 74 | Currently not recommended for use in HLMs | 0.01 – 100 | 0.01 – 100 |