. Author manuscript; available in PMC: 2022 Dec 13.

Published in final edited form as: Angew Chem Int Ed Engl. 2021 Oct 6:10.1002/anie.202108848. doi: 10.1002/anie.202108848

Table 3.

PROTACs: Viabilities of cancer cells

Compound	CRBN warhead	MV4–11 IC₅₀ (nM)^a	HD-MB03 IC₅₀ (nM)^a
2a	PG	>7,000	>7,000
3a	IMiD	0.222 ± 0.075	710.45 ± 90.16
3b	IMiD	0.208 ± 0.031	105.00 ± 10.40
3c	PG	0.199 ± 0.002	334.55 ± 72.76
3d	PG	0.133 ± 0.058	102.78 ± 59.83
4a (dBET1)	IMiD	6.100 ± 1.559	1,237.80 ± 261.25
4b	PG	0.060 ± 0.021	13.22 ± 3.42
4c (SJ995973)	PG	0.003 ± 0.001	1.83 ± 0.35
4d	PG	20.076 ± 7.252	379.65 ± 61.02
4e	PG	1.147 ± 0.413	64.85 ± 1.54
4f	Inact-PG	1,282.160 ± 456.725	>10 μM
JQ1	-	82.960 ± 10.315	265.20 ± 62.59

Antiproliferative effects of compounds assessed after 3 days of incubation, using the CellTiter-Glo assay kit (Promega). Data represent the average of ≥ 2 independent determinations. ± Deviation represents standard error of the mean.