Inhibitor | Structure | Observed CYP51 IC50a | Estimated CYP51 IC50a | |
---|---|---|---|---|
μM | ||||
Clotrimazole | 0.13 | 1.3 | ||
Ketoconazole | 0.19 | 0.082 | ||
Miconazole | 0.2 | 1.7 | ||
Analog A | 0.3 | 1.2 | ||
Analog B | 0.8 | 2.2 | ||
Analog C | 0.91 | 2 | ||
Analog D | 1.3 | 6.9 | ||
Analog E | 2.5 | 2.9 | ||
Analog F | 3.1 | 1.5 | ||
CP-320626 | 4.0 | 2.8 | ||
Analog G | 4.5 | 3.2 | ||
Analog H | 9.7 | 3.5 | ||
Analog I | 26 | 3.3 | ||
Rifampicin | 30 | 130 | ||
Griseofulvin | 50 | 120 | ||
Tolnaftate | 50 | 25 | ||
Testosterone | 50 | 160 | ||
Analog J | 75 | 44 | ||
Analog K | 100 | 60 | ||
μM | ||||
Analog L | 100 | 14 | ||
Benzimidazole | >200 | 150 | ||
Metronidazole | >200 | 64 | ||
Methimazole | >200 | 130 | ||
Analog M | >200 | 110 | ||
Analog N | >200 | 130 | ||
Analog O |
| >200 | 89 |
↵ a Experimental data are the average of triplicate determinations.