Table 1.

Common GSIs at various stages of (pre‐)clinical development. IC₅₀ values of each compound for different Notch receptors as well as those for APP (inhibition of amyloid beta production) are provided

GSI	Names	IC50 (nM)					Clinical status	Reference
		Notch1	Notch2	Notch3	Notch4	APP
BMS‐906024	AL101	0.29–1.6	0.14–0.7	0.32–3.4	0.71–2.9		II	Gavai, 2015 [35]; Ran, 2017 [33]; Lessard, 2019 [36]
BMS‐708163	Avagacestat	20.6–58				0.30–0.79	II	Mitani, 2012 [38]; Gillman, 2010 [37]
BMS‐986115							I
DAPT	GSI‐IX	4.9	85.22	552.4–623.5	51.5	29	preclinical	Ran, 2017 [33]; Lessard, 2019 [36]; Martone, 2009 [39]
MK‐0752		55–87.44	46.62	146.3–370	191	5	II	Ran, 2017 [33]; Deangelo, 2006 [41]; Lessard, 2019 [36]; Cook, 2010 [40]
PF‐03084014	Nirogacestat	0.6–13.3	0.002–0.01	1.21–15.07	0.81–10.77	1.2–6.2	III	Wei, 2010 [43]; Ran 2017 [33]; Lessard, 2019 [36]; Lanz, 2010 [42]
RO4929097		0.46–4	2.24	19.8–28.31	3.4	14	II	Ran, 2017 [33]; Luistro, 2009 [47]; Lessard, 2019 [36]; Gu, 2017 [44]
GSI‐953	Begacestat					8	I	Martone, 2009 [39]
LY‐450139	Semagacestat	7.02–14.1	38.7	390.9–523.3	45.98	10.9–38	III	Ran, 2017 [33]; Mitani, 2012 [38]; Lessard, 2019 [36]; Martone, 2009 [39]
LY‐411,575		0.129				0.119	preclinical	Lewis, 2003 [45]
LY‐900009		0.27					I	Pant, 2012 [109]

Abbreviations: APP, amyloid precursor protein; GSI, gamma secretase inhibitor; IC50, half‐maximal inhibitory concentration.