Table 2.
Reported optical substrates for human CYPs.
| Target enzyme | No. | Substrate | Metabolite | Km or S50 (μmol/L) | Vmax or Kcat | λex (nm)/λem (nm) | Ref. |
|---|---|---|---|---|---|---|---|
| CYP1A1 | CYP1A1-F1 |  |
 |
0.84 | 18.99a | 450/562 | 32 |
| CYP1A1-F2 |  |
 |
0.29 | 5.54a | 470/525 | 35 | |
| CYP1A1-F3 |  |
 |
11.99 | 17.44a | 450/564 | 153 | |
| CYP1A1-F4 |  |
 |
N.A. | N.A. | 458/552 | 177 | |
| CYP1A1-F5 |  |
 |
N.A. | N.A. | 446/550 | 178 | |
| CYP1A1-F6 |  |
 |
N.A. | N.A. | 555/673 | 179 | |
| CYP1A1-F7 |  |
 |
2.80 | 18.2a | 530/590 | 180 | |
| CYP1A1-F8 |  |
 |
0.278 | 9.17a | 540/590 | 33 | |
| CYP1A1-F9 |  |
 |
1.2 | 24.2a | 409/460 | 34 | |
| CYP1A2 | CYP1A2-F1 |  |
 |
9.8 | 32.06a | 450/564 | 153 |
| CYP1A2-F2 |  |
 |
N.A. | N.A. | 458/552 | 177 | |
| CYP1A2-F3 |  |
 |
3.0 | 0.23a | 530/590 | 180 | |
| CYP1A2-F4 |  |
 |
1.14 | 7.13a | 409/460 | 34 | |
| CYP1A2-F5 |  |
 |
11 | 21.0c | 415/460 | 181 | |
| CYP1A2-F6 |  |
 |
4.1 | 11.1a | 410/510 | 182 | |
| CYP1B1 | CYP1B1-F1 |  |
 |
1.0 | 1.33a | 530/590 | 180 |
| CYP2A6 | CYP2A6-F1 |  |
 |
2.1 | 0.79b | 390/460 | 34 |
| CYP2B6 | CYP2B6-F1 |  |
 |
8.5 | 14.0a | 409/530 | 38 |
| CYP2B6-F2 |  |
 |
6.79 | 6.48a | 409/530 | 34 | |
| CYP2B6-F3 |  |
 |
52 | 66.0c | 415/460 | 181 | |
| CYP2B6-F4 |  |
 |
0.73 | 0.80c | 550/590 | 181 | |
| CYP2C8 | CYP2C8-F1 |  |
 |
3.6 | 2.10 c | 490/520 | 181 |
| CYP2C9 | CYP2C9-F1 |  |
 |
43 | 2.10c | 425/460 | 181 |
| CYP2C9-F2 |  |
 |
4.5 | 4.50c | 490/520 | 181 | |
| CYP2C9-F3 |  |
 |
54.7 | 0.56a | 409/530 | 34 | |
| CYP2C19 | CYP2C19-F1 |  |
 |
9.11 | 0.84a | 409/460 | 34 |
| CYP2C19-F2 |  |
 |
16.6 | 5.70c | 415/460 | 181 | |
| CYP2C19-F3 |  |
 |
1.14 | 0.01b | 485/530 | 31 | |
| CYP2D6 | CYP2D6-F1 |  |
 |
11.5 | 2.81c | 390/460 | 183 |
| CYP2D6-F2 |  |
 |
4.81 | 6.19a | 390/460 | 34 | |
| CYP2D6-F3 |  |
 |
5.0 | 0.60c | 405/490 | 181 | |
| CYP2E1 | CYP2E1-F1 |  |
 |
22 | 2.10a | 415/460 | 184 |
| CYP2J2 | CYP2J2-F1 |  |
 |
4.2 | 0.44d | 656/718 | 185 |
| CYP2J2-F2 |  |
 |
N.A. | N.A. | 555/673 | 186 | |
| CYP3A | CYP3A-F1 |  |
 |
89 for 3A4 N.A. for 3A5 |
10.0c for 3A4 N.A. for 3A5 |
415/460 | 187 |
| CYP3A-F2 |  |
 |
7.8b for 3A4 N.A. for 3A5 |
16.0c for 3A4 N.A. for 3A5 |
490/520 | 187 | |
| CYP3A-F3 |  |
 |
1.03 for 3A4 2.17 for 3A5 |
0.55 for 3A4 1.28 for 3A5 |
490/520 | 34 | |
| CYP3A4 | CYP3A4-F1 |  |
 |
59.8 | 2.18a | 450/558 | 36 |
| CYP3A4-F2 |  |
 |
70 | 3.39b | 420/530 | 37 | |
| CYP3A4-F3 |  |
 |
26 | 61.2c | 410/510 | 182 | |
| CYP3A4-F4 |  |
 |
7.8 | 1.6 | 490/520 | 187 | |
| CYP3A4-F5 |  |
 |
1.4 | 1.1 | 550/590 | 181 | |
| CYP3A4-F6 |  |
 |
4.6 | 0.02b | 410/510 | 37 | |
| CYP1A1 | Luciferin-1A1 |  |
 |
3.0 | N.A. | 560 | 188 |
| CYP1A2 | Luciferin-1A2 |  |
 |
6.0 | N.A. | 560 | 188 |
| CYP2B6 | Luciferin-2B6 |  |
 |
3.0 | N.A. | 560 | 189 |
| CYP2C9 | Luciferin-H |  |
 |
100 | N.A. | 560 | 188 |
| CYP2C19 | Luciferin-H EGE |  |
 |
10 | N.A. | 560 | 189 |
| CYP2D6 | Luciferin-ME EGE |  |
 |
30 | N.A. | 560 | 189 |
| CYP2J2 | Luciferin-2J2/4F12 |  |
 |
1.0 | N.A. | 560 | 188 |
| CYP3A4 | Luciferin-IPA |  |
 |
3.0 | N.A. | 560 | 188 |
| CYP3A7 | Luciferin-3A7 |  |
 |
33b | N.A. | 560 | 188 |
| CYP4A11 | Luciferin-4A |  |
 |
80 | N.A. | 560 | 188 |
| CYP4F3B | Luciferin-4F2/3 |  |
 |
∼10b | N.A. | 560 | 188 |
| CYP4F12 | Luciferin-4F12 |  |
 |
10 | N.A. | 560 | 188 |
NA.: not available or not assayed.
a
Vmax values were in nmol/min/nmol P450 for CYP enzymes.
b
Vmax values were in nmol/min/mg human liver microsome.
c
kcat or Vmax values were in min‒1.
d
Vmax values were in nmol/min/mg CYP2J2; λex: excitation wavelength; λem: emission wavelength.