Summary of enzyme kinetic estimates using the ODA and the MDCM
Values displayed as means with CV% within parentheses.
| Compound | CLint | Vmax | Km | |||
|---|---|---|---|---|---|---|
| MDCM | ODA | MDCM | ODA | MDCM | ODA | |
| μl/min/mg protein | pmol/min/mg protein | μM | ||||
| Amodiaquine* | 829 (5.1) | 224 (6.7) | 2770 (9.5) | 1180 (25) | 3.33 (9.6) | 5.17 (28) |
| Bufuralol | 31.0 (26) | 32.3 (30) | 340 (99) | 405 (110) | 11.7 (113) | 12.8 (127) |
| Dextromethorphan | 84.1 (18) | 54.2 (12) | 590 (46) | 309 (37) | 7.16 (58) | 6.32 (46) |
| Diclofenac | 143 (4.2) | 135 (11) | 1680 (16) | 1100 (35) | 11.6 (18) | 8.55 (40) |
| Diltiazem* | 47.6 (13) | 75.4 (14) | 495 (46) | 730 (45) | 10.0 (54) | 9.8 (51) |
| Imipramine* | 39.6 (16) | 51.1 (27) | 585 (42) | 654 (53) | 14.2 (47) | 14.3 (70) |
| Midazolam * | 717 (6.4) | 220 (8.2) | 880 (11) | 657 (35) | 1.26 (12) | 3.04 (39) |
| Phenacetin | 39.5 (14) | 50.4 (21) | 794 (60) | 1100 (63) | 22.6 (69) | 22.6 (73) |
| AZ01 | 63.3 (12) | 79.7 (6.2) | 497 (39) | 845 (21) | 7.85 (48) | 10.6 (24) |
| AZ02 | 42.4 (21) | 53.7 (16) | 210 (68) | 431 (60) | 4.94 (83) | 8.03 (68) |
| AZ03 | 104 (9.1) | 118 (6.4) | 455 (30) | 1020 (22) | 4.39 (36) | 8.66 (25) |
| AZ04 | 71.2 (8.4) | 108 (6.8) | 1800 (35) | 1530 (22) | 25.3 (40) | 14.2 (26) |
| AZ05 | 123 (5.7) | 138 (12) | 147 (36) | 492 (48) | 1.19 (9.2) | 3.56 (54) |
| AZ06 | 71.8 (20) | 106 (14) | 242 (72) | 366 (55) | 3.38 (81) | 3.44 (63) |
| AZ07 | 85.8 (12) | 131 (9.2) | 512 (33) | 931 (32) | 5.97 (42) | 7.11 (36) |
| AZ08 | 135 (5.0) | 161 (8.1) | 377 (15) | 560 (34) | 2.79 (19) | 3.47 (39) |
| AZ09 | 272 (11) | 162 (5.6) | 1460 (20) | 1280 (19) | 5.39 (29) | 7.93 (22) |
| AZ10 | 242 (7.5) | 161 (4.1) | 1730 (13) | 1750 (12) | 7.18 (19) | 10.9 (14) |
| AZ11 | 58.3 (24) | 79.5 (14) | 308 (64) | 574 (59) | 5.29 (79) | 7.22 (66) |
| AZ12 | 53.4 (22) | 29.8 (23) | 370 (64) | 388 (92) | 6.93 (77) | 13.1 (103) |
| AZ13 | 239 (9.1) | 193 (6.5) | 2420 (17) | 2190 (19) | 10.1 (22) | 11.4 (22) |
| AZ14 | 49.1 (12) | 26.3 (27) | 812 (51) | 455 (88) | 16.5 (58) | 17.3 (100) |
| AZ15 | 492 (12) | 255 (5.5) | 2300 (21) | 1520 (18) | 4.68 (31) | 5.98 (20) |
| AZ16 | 156 (7.3) | 172 (5.0) | 632 (19) | 1530 (17) | 4.06 (24) | 8.88 (19) |
| AZ17 | 42.8 (13) | 36.3 (20) | 314 (76) | 385 (53) | 8.99 (61) | 8.65 (86) |
| AZ18 | 188 (3.3) | 187 (3.8) | 784 (8.7) | 1070 (13) | 4.16 (11) | 5.74 (15) |
| AZ19 | 52.8 (13) | 33.8 (8.9) | 855 (45) | 365 (31) | 16.2 (53) | 10.8 (35) |
| AZ20 | 11.1 (18) | 166 (13) | 274 (160) | 49.5 (550) | 24.7 (181) | 2.72 (677) |
| AZ21* | 87.1 (15) | 76.8 (5.2) | 914 (23) | 557 (19) | 10.5 (23) | 7.26 (21) |
| AZ22 | 164 (5.3) | 151 (4.3) | 539 (16) | 1210 (15) | 3.31 (20) | 8.03 (17) |
↵* MDCM analysis performed compensating for enzyme activity loss: amodiaquine (ke = 0.035), imipramine (ke = 0.042), diltiazem (ke = 0.035), midazolam (ke = 0.063), and AZ21 (ke = 0.024).