Comparison of rank order between fluorogenic and conventional probes for P450s 2D6 and 3A4
Compound | IC50 | Rank Order | ||||
|---|---|---|---|---|---|---|
|
Conventional
|
Fluorogenic
|
Conventional
|
Fluorogenic
| |||
| μM | ||||||
| CYP2D6 | ||||||
| CP−1 | >10 | 14 | C | C | ||
| CP−2 | >10 | 14 | C | C | ||
| CP−3 | 10 | 6 | B | B | ||
| CP−4 | 9 | 24 | B | C | ||
| CP−5 | 8 | 11 | B | C | ||
| CP−6 | 7 | 22 | B | C | ||
| CP−7 | 5 | 13 | B | C | ||
| CP−8 | 3 | 19 | A | C | ||
| CP−9 | 3 | 17 | A | C | ||
| CP−10 | 2 | 11 | A | B | ||
| CP−11 | 2 | 19 | A | C | ||
| Quinidine | 0.1 | 0.05 | A | A | ||
| CYP3A4 | ||||||
| CP−21 | >10 | >30 | C | C | ||
| CP−22 | 1.2 | 0.6 | A | A | ||
| CP−23 | 1 | 0.6 | A | A | ||
| CP−24 | 0.8 | 0.4 | A | A | ||
| CP−25 | 0.6 | 0.2 | A | A | ||
| CP−26 | >10 | 21.2 | C | C | ||
| CP−27 | 0.4 | 0.2 | A | A | ||
| CP−28 | 0.5 | 0.2 | A | A | ||
| CP−29 | 0.3 | 0.1 | A | A | ||
| CP−30 | 0.3 | 0.1 | A | A | ||
| CP−31 | 0.7 | 0.4 | A | A | ||
|
Ketoconazole
|
0.05
|
0.09
|
A
|
A
| ||