TABLE 2.

Kinetic parameters of aumolertinib catalyzing by CYP3A4.

Variants	Vmax (pmol/min/pmol P450)	Km (μM)	CLint (Vmax/Km) (μl/min/pmol P450)
*1	1.866 ± 0.036	3.204 ± 0.202	0.583 ± 0.026
*3	2.020 ± 0.032	3.631 ± 0.149	0.557 ± 0.017
*4	1.153 ± 0.018**	3.952 ± 0.389	0.293 ± 0.027**
*5	1.882 ± 0.038	10.144 ± 0.833*	0.186 ± 0.012**
*7	0.377 ± 0.016***	4.937 ± 0.649	0.077 ± 0.006**
*8	0.717 ± 0.016***	3.158 ± 0.077	0.227 ± 0.010**
*9	1.280 ± 0.031**	4.080 ± 0.370	0.315 ± 0.023**
*10	1.045 ± 0.010**	2.314 ± 0.065	0.452 ± 0.009
*12	0.318 ± 0.031***	19.773 ± 4.091	0.016 ± 0.002**
*13	0.405 ± 0.007**	6.015 ± 0.384*	0.067 ± 0.003**
*14	0.996 ± 0.063**	3.445 ± 0.109	0.289 ± 0.012**
*15	2.260 ± 0.024**	3.540 ± 0.181	0.640 ± 0.039
*16	1.382 ± 0.024**	3.013 ± 0.205	0.460 ± 0.024
*17	0.321 ± 0.058***	58.283 ± 13.120	0.006 ± 0.000**
*18	0.759 ± 0.008**	5.859 ± 0.286**	0.130 ± 0.005**
*19	1.160 ± 0.015**	3.625 ± 0.237	0.321 ± 0.017**
*20	N.D	N.D	N.D
*23	1.163 ± 0.025***	4.085 ± 0.391	0.286 ± 0.021**
*24	1.012 ± 0.074**	3.732 ± 0.252	0.271 ± 0.014**
*28 (*L22V)	1.287 ± 0.005*	2.519 ± 0.054	0.511 ± 0.010
*29 (*F113I)	3.053 ± 0.121*	4.031 ± 0.319	0.759 ± 0.043
*31 (*H324Q)	1.129 ± 0.016**	3.213 ± 0.502	0.356 ± 0.050
*32 (*I335T)	1.759 ± 0.066	2.963 ± 0.092	0.594 ± 0.021
*33 (*A370S)	1.345 ± 0.079*	3.520 ± 0.403	0.384 ± 0.024*
*34 (*I427V)	0.730 ± 0.028***	5.817 ± 0.439	0.126 ± 0.007**

Note. compared to wild type, *p < 0.05; **p < 0.01; ***p < 0.001. ND, not determined.