From: Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease
Compound | gamma:APP IC50 (nM) | gamma:Notch IC50 (nM) | enzyme selectivity (APP/Notch) | SNC Aβ EC50 (nM) | SNC Notch Signaling EC50 (nM) | Cellular Selectivity (APP/Notch) |
---|---|---|---|---|---|---|
L-685,458 | 0.63 (1) | nd | NA | 13.2 ± 4.5 (4) | 184 ± 145 (3) | 14 |
LY411575 | 0.035 (1) | 0.082 ± 0.008 (3) | 2.4 | 0.116 ± 0.011 (3) | 1.8 ± 1.35 (3) | 16 |
ELN158162 | 650 | 14,000 | 21.5 | nd | nd | NA |
ELN318463 | 37.2 ± 18 (51) | 1,889 ± 722 (3) | 51 | 23.4 ± 8.6 (10) | 2,818 ± 670 (10) | 120 |
ELN475516 | 2.06 ± 0.35 (16) | 29.81 ± 2.59 (4) | 14.5 | 8.73 ± 3.96 (298) | 719 ± 224.6 (298) | 82 |