Table 1. Biological evaluations of the tool compounds ^a .

Compounds	Bioassay IC50 (μM)	Anti-proliferative IC50 (μM)
		A375	HCT116
SCH772984	0.0013 (2)	0.037 (>10)	0.05 (>10)
TCO-SCH	0.022 (2)	—	—
SCH-TCO	0.0053 (2)	0.060 (2)	0.10 (2)
Biotin clicked SCH-TCO	45% @ 0.003 μM (2)	—	—
GDC-0994	0.0037 (2)	0.13 (9)	1.00 (8)
TCO-GDC-1	0.028 (2)	—	—
TCO-GDC-2	0.008 (3)	0.93 (2)	1.00 (2)
Biotin-clicked TCO-GDC-2	0.009 (2)	—	—
Biotin-PEG4-Tz	8.1 (2)	—	—
LY3214996	62% @ 0.003 μM (2)	0.35 (9)	0.48 (3)

^aGeometric means.