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. 2022 Jul 6;17(7):1733–1744. doi: 10.1021/acschembio.2c00076

Table 1. Cell Painting Activity Score (Grit) for Published PROTACs.

    grit score at different concentrations (μM)
compound name target 0.1 1 10
MZ1 BRD4 1.60 3.84 dead cells
ZXH 3–26 BRD4 0.92 2.19 4.31
AT1 BRD4 1.22 2.15 4.20
dBET1 BRD4 –0.47 1.27 2.34
BSJ-03-123 CDK6 0.81 2.78 2.17
BSJ-03-204 CDK4/6 1.17 2.39 1.69
BSJ-04-132 CDK4 0.91 1.20 1.82
CM11 VHL 0.92 0.15 1.95
CRBN-6-5-5-VHL CRBN 1.03 2.04 2.63
THAL-SNS-032 CDK9 –0.69 2.59 5.42
TL 13-12 ALK 2.08 1.50 5.46
lenalidomide IKZF1, IKZF3 0.56 0.32 –0.18
pomalidomide IKZF1, IKZF3 0.46 0.45 –0.02