Table 2.

Antiproliferative effects of c-MET degraders D9–D15 with modification of the linker types and sites tethered to thalidomide.

Cpd.	Site	Linker	IC50 (μmol/L)a
			c-MET-sensitive		c-MET-insensitive
			EBC-1	Hs746T	A549	HepG2
D9	5′		0.00398 ± 0.00068	0.00721 ± 0.00230	0.977 ± 0.220	2.47 ± 0.67
D10	5′		0.00334 ± 0.00048	0.00589 ± 0.00150	0.511 ± 0.247	1.54 ± 0.50
D11	5′		0.00555 ± 0.00060	0.00619 ± 0.00185	1.15 ± 0.24	7.47 ± 1.42
D12	5′		0.00461 ± 0.00044	0.00772 ± 0.00216	0.433 ± 0.096	0.672 ± 0.141
D13	4′		0.00585 ± 0.00095	0.0247 ± 0.0113	3.29 ± 0.99	10.74 ± 2.28
D14	5′		0.00244 ± 0.00033	0.00388 ± 0.00060	0.665 ± 0.103	1.95 ± 0.83
D15	5′		0.00211 ± 0.00031	0.00350 ± 0.00056	0.377 ± 0.058	0.543 ± 0.107
Tepotinib	–	–	0.00132 ± 0.00039	0.00263 ± 0.00072	0.277 ± 0.059	0.476 ± 0.045

^aThe data are averages of three independent determinations.