Table 3. Activities of the IAP-addressing CDK4/6 degrader.

Cmpd	Linker	X	Y	elog D7.4 a	D CDK4 b	D CDK6 b
					0.1 μM	0.1 μM	1 μM
5	—	—	—	n.d. c	n.d.	n.d.	n.d.
8 (BSJ)	—	—	—	2.5	27	5.5	2.1
35		Me	H	4.3	77	75	18
36		H	Me	4.5	>95	>95	n.d.

^aExperimental distribution coefficient at pH 7.4.

^bCDK4 or CDK6 degradation indicated as remaining CDK4 or CDK6 levels after 16 h treatment of each compound at the indicated concentration. Percentage values are normalized to DMSO-treated MM.1S cells and the respective loading controls (100%). All of the data were the average of at least three independent experiments.

^cNot determined.