. 2021 Feb 26;4(2):941–952. doi: 10.1021/acsptsci.1c00032

Table 3. IC₅₀ Values of (+)-JQ1, HJB97, Thalidomide, and Lenalidomide in Previous Reports and the TR-FRET PROTAC Ternary Complex Formation Assay.

	BRD2(BD1) IC₅₀ (nM)		CRBN IC₅₀ (nM)
compound	previously reported FP assay⁸	TR-FRET PROTAC assay^a	previously reported TR-FRET assay¹⁵	TR-FRET PROTAC assay^a
(+)-JQ1	36.1	239.8	NA^b	NA
HJB97	3.1	27.1	NA	NA
thalidomide	NA	NA	22.4	34.7
lenalidomide	NA	NA	8.9	13.2

IC₅₀ value measured with our TR-FRET ternary complex assay [Tb-anti-GST (2 nM), GST-BRD2(BD1) (2 nM), PROTAC BET Degrader-1 (4.1 nM), His-CRBN(DDB1) (8 nM), and AF488-anti-His (4 nM) with a 180 min incubation.

Notation: NA = not applicable.

Table 3. IC50 Values of (+)-JQ1, HJB97, Thalidomide, and Lenalidomide in Previous Reports and the TR-FRET PROTAC Ternary Complex Formation Assay.

Table 3. IC₅₀ Values of (+)-JQ1, HJB97, Thalidomide, and Lenalidomide in Previous Reports and the TR-FRET PROTAC Ternary Complex Formation Assay.