Table 1.

IC₅₀ values and affinity to ClpP for each TR compound.

	IC50 (nM), MDA-MB-231			IC50 (nM), HEK293 T-REx			Casein-FITC degradation
Compound	WT	CLPP −/−	CLPX −/−	WT	CLPP −/−	CLPX −/−	Kd, app (nM)	h (at 2.5 μM ClpP)
TR-27	90.7 ± 1.7	> 1000	98.9 ± 1.7	46.1 ± 1.3	> 1000	57.7 ± 3.4	23.7 ± 10.0	8.1 ± 1.2
TR-57	19.3 ± 0.2	> 1000	19.9 ± 0.3	8.9 ± 0.2	> 1000	11.8 ± 0.4	15.5 ± 12.0	9.4 ± 7.8
TR-65	9.4 ± 0.2	> 1000	9.4 ± 0.2	9.8 ± 0.3	> 1000	11.0 ± 0.2	23.3 ± 9.1	10.9 ± 2.5
TR-107	29.4 ± 0.2	> 1000	27.4 ± 0.8	22.8 ± 0.7	> 1000	27.0 ± 2.0	32.2 ± 6.3	5.5 ± 0.7
TR-133	27.8 ± 0.4	> 1000	29.5 ± 0.7	20.7 ± 0.7	> 1000	26.0 ± 2.0	29.1 ± 7.8	6.2 ± 1.3
ONC201	1720 ± 10	> 10000	1530 ± 20	750 ± 10	> 10000	790 ± 10	3556 ± 130	2.1 ± 0.2

Errors represent standard deviations from three experiments.