. Author manuscript; available in PMC: 2013 Nov 8.

Published in final edited form as: J Med Chem. 2012 Sep 6;55(21):9195–9207. doi: 10.1021/jm3008823

Table 1.

BACE 1 inhibitory and cellular activity of inhibitors 4–9.

Entry	K_i (nM)	IC₅₀ (nM)^a
1	27.12	9.5
2	0.017	1
3.	98.8	>1000
4.	>1000	---
5.	25	---
6.	>1000	---

IC₅₀ was determined in neuroblastoma cells. GRL-8234 exhibited K_i = 1.8 nM, IC₅₀ = 2.5 nM in this assay.