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. Author manuscript; available in PMC: 2022 Aug 12.
Published in final edited form as: J Med Chem. 2021 Aug 3;64(15):11148–11168. doi: 10.1021/acs.jmedchem.1c00507

Table 1.

R1 modifications

graphic file with name nihms-1786730-t0012.jpg
Compound Structure
of R1
PRMT5
IC50 (μM)
FP40min
PBS
Solubility
(μM)
Plasma Stability (%Remaining) GSH T½
(min)
Human Mouse
1 graphic file with name nihms-1786730-t0013.jpg 12.4 1.2 92 0 46
2 graphic file with name nihms-1786730-t0014.jpg 5.4 98 84 0 ND
3 graphic file with name nihms-1786730-t0015.jpg 12.7 0.8 ND ND ND
4 graphic file with name nihms-1786730-t0016.jpg 10.1 89 72 0 ND
5 graphic file with name nihms-1786730-t0017.jpg 14.1 56 89 0 25
6 graphic file with name nihms-1786730-t0018.jpg 2.2 47 82 14 31
7 graphic file with name nihms-1786730-t0019.jpg 4.6 88 100 21 ND
8 graphic file with name nihms-1786730-t0020.jpg 2.5 93 92 2 ND
EPZ015666 >100 101 ND ND ND
JNJ-64619178 >100 7 ND ND ND
MTA >100 110 ND ND ND