Table 6. Summary Profiles of 5f, 5g, and 6.
| parameter | 5f | 5g | 6 |
|---|---|---|---|
| CDK2/E (nM)a | 1.2 | 0.3 | 2.0 |
| selectivity(1/7/9)b | 490/NR/2800 | 1200/17000/8200 | 660/1100/2500 |
| selectivity(4/6)b | 240/95 | 770/230 | 110/35 |
| off-targetsc | 5/54 | 5/54 | 0/54 |
| hWB (nM) | 746 | 642 | 316 |
| hERG (% Inh)d | 16 | 9.7 | 7.2 |
| CYPe | >25 μM | >25 μM | >25 μM |
| CYP TDIf | none | none | none |
| solubility (μg/mL) | >400g | N/A | >400 |
a
Measured at 1 mM [ATP].
b
Fold selectivity over the corresponding CDK isoform as measured by enzyme IC50.
c
# kinases <1 μM in a 54 membered kinase panel
d
At 10 μM concentration
e
CYP isomforms tested: CYP3A4, CYP1A2, CYP2C8, CYP2C19, CYP2B6, CYP2D6, CYP2C9.
f
CYP isoforms tested: CYP3A4, CYP2D6, CYP2C9, CYP2C19
g
Solubility determined for 4f; NR = not recorded.