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 |