Table 1.
No. | Target | E3 | Potency (DC50) | Disordered region (>40 a.a) | DOI |
---|---|---|---|---|---|
1 | ABL1 | CRBN,VHL | 100 nM | O | 10.1002/anie.201507634 |
2 | AKT | VHL | 100–300 nM | X | 10.1002/psc.2858 |
3 | ALK | CRBN | 10 nM | O | 10.1016/j.ejmech.2018.03.071 |
4 | AR | VHL | 5 nM | O | 10.1038/s42003-018-0105-8 |
5 | BCL6 | CRBN | <1 μM | O | 10.1021/acschembio.8b00698 |
6 | BCR/ABL | CRBN | 0.5–1 μM | O | 10.1002/anie.201507634 |
7 | BRD4 | CRBN | <10 nM | O | 10.1016/j.chembiol.2015.05.009 |
8 | BRD9 | CRBN | 5–50 nM | O | 10.1002/anie.201611281 |
9 | BTK | CRBN | 25 nM | O | 10.1021/acs.biochem.8b00391 |
10 | CDK4 | CRBN | 10–100 nM | X | 10.1039/c9cc00163h |
11 | CDK6 | CRBN | 10–100 nM | X | 10.1039/c9cc00163h |
12 | CDK8 | CRBN | ~100 nM | O | 10.1021/acsmedchemlett.8b00011 |
13 | c-MET | VHL | 50 nM | X | 10.1016/j.chembiol.2017.09.009 |
14 | CRABP2 | cIAP1 | ~1 μM | X | 10.1016/j.febslet.2011.03.019 |
15 | DHODH | VHL | 0.1–1 μM | X | 10.1002/chem.201702999 |
16 | EGFR | VHL | 22.3 nM | O | 10.1016/j.chembiol.2017.09.009 |
17 | ER | VHL | 1 nM | O | 10.1021/acs.jmedchem.8b01572 |
18 | ERK2 | CRBN | ~1 μM | X | 10.1021/acscentsci.6b00280 |
19 | ERRa | VHL | 100 nM | O | 10.1038/nchembio.1858 |
20 | FAK1 | VHL | 10 nM | O | 10.1021/jacs.8b08008 |
21 | FKBP12 | CRBN | <100 nM | X | 10.1126/science.aab1433 |
22 | FLT3 | VHL | 2 nM | X | 10.1021/jacs.8b10320 |
23 | GCN5 | CRBN | 3 nM | O | 10.1021/acschembio.8b00705 |
24 | HDAC6 | CRBN | 100–300 nM | O | 10.1016/j.bmcl.2018.05.057 |
25 | HER2 | VHL | 25–100 nM | O | 10.1016/j.chembiol.2017.09.009 |
26 | PCAF | CRBN | 1.5 nM | O | 10.1021/acschembio.8b00705 |
27 | RIPK2 | VHL | 1 nM | O | 10.1038/nchembio.1858 |
28 | Sirt2 | CRBN | ~0.5 μM | O | 10.1021/acs.jmedchem.6b01872 |
29 | TBK1 | VHL | 3 nM | X | 10.1021/acs.jmedchem.7b00635 |
30 | VHL | VHL | ~10 nM | O | 10.1038/s41467-017-00954-1 |
Based on a literature search, PROTACs with high potency (DC50 < 1 μM) were selected, and then analyzed them for a disordered region using the IUPred2A.