Identification and Preclinical Pharmacology of the -Secretase Modulator BMS-869780

Table 1

A𝛽 and Notch IC₅₀ values.

Assay (cell line)	BMS-869780 (GSM)			BMS-299897 (GSI )			BMS-433796 (GSI)
	IC50 (nM)	sd	𝑛	IC50 (nM)	sd	𝑛	IC50 (nM)	sd	𝑛
A𝛽1-42 (H4-APPsw)	5.1	2.2	13	0.47	0.61	322	0.16	0.08	256
A𝛽1-40 (H4-APPsw)	24.1	7.7	7	1.3	1.2	93	0.19	0.14	20
A𝛽1-42 (MEF PS1wt)	7.7	2.3	2
A𝛽1-40 (MEF PS1wt)	11	4	2
A𝛽1-42 (MEF M146V)	22	1.4	2
A𝛽1-40 (MEF M146V)	34	9	2
mNotch1ΔE (luciferase)	>10000		3	340	108	147	2.1	1.0	256
mNotch1ΔE/A𝛽1-42	>1785x			723x			13x