Skip to main content
. 2019 Dec 23;9:19654. doi: 10.1038/s41598-019-56177-5

Table 1.

Disordered region prediction of proteins targeted by PROTAC.

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.