Table 1. GSK2606414 and GSK2656157 are potent RIPK1 inhibitors.

				IC50 (μM)
System	Stimulus	Biological process	Parameter/methodology	GSK'414	GSK'157	NEC-1	NEC-1s	GSK'963	AMG'44
MEFs	TNF + TAK1-inh	Apoptosis	SYTOX Green+	0.0063	0.0029	3.29	0.65	0.0018	NI
MEFs	TNF + TAK1-inh	Caspase-3 activity	C3 DEVD-AMC	0.0068	0.0040	3.35	1.34	ND	ND
MEFs	TNF + zVAD	Necroptosis	SYTOX Green+	0.0073	0.0019	2.07	0.74	ND	NI
L929s	TNF	Necroptosis	SYTOX Green+	0.0004	0.0001	0.47	0.23	ND	ND
MEFs	Tm	PERK- phosphorylation	Electrophoretic mobility shift	ND	0.1977	ND	ND	NI	0.2178
MEFs	Tm	ATF4 induction	WB	ND	0.2079	ND	ND	N.D	0.7392
GST-hRIPK	–	Kinase activity	ADP-Glo assay	0.0182	0.0691	ND	0.8655	0.0178	NI
GST-hPERK	–	Kinase activity	ADP-Glo assay	0.0038	0.0097	ND	NI	NI	0.1812

ND, not determined; NI, no inhibition until 10 μM.