Table 1.
Compound | Structure of R1 |
PRMT5 IC50 (μM) FP40min |
PBS Solubility (μM) |
Plasma Stability (%Remaining) | GSH T½ (min) |
|
---|---|---|---|---|---|---|
Human | Mouse | |||||
1 | 12.4 | 1.2 | 92 | 0 | 46 | |
2 | 5.4 | 98 | 84 | 0 | ND | |
3 | 12.7 | 0.8 | ND | ND | ND | |
4 | 10.1 | 89 | 72 | 0 | ND | |
5 | 14.1 | 56 | 89 | 0 | 25 | |
6 | 2.2 | 47 | 82 | 14 | 31 | |
7 | 4.6 | 88 | 100 | 21 | ND | |
8 | 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 |