Table 4.

Reported cell data (IC₅₀) and in vivo/ex vivo data for selected ADAM17 inhibitors.

Compound	Effect	Cell Line	IC50	In Vivo/Ex Vivo Assay
1	Inhibition of TNFα release	Human Keratinocytes (NHEK)	1.3 µM	-
2	Inhibition of TNFα release	NHEK	3 nM	Strong activity in a mouse model of oxazolone- induced chronic skin inflammation
3 (KP475)	Inhibition of GPIbα shedding	human iPSC platelets	≈ 100 nM	Positive results in a thrombus formation model using immunodeficient mice
5	Inhibition of TNFα production	human whole blood (hWBA):	287 nM	-
6	Inhibition of TNFα production	human whole blood (hWBA):	281 nM	Good PK properties in rats and monkeys
7 (JTP-96193)	Inhibition of TNFα release	rat whole blood (rWBA)	170 nM	In mouse models of obesity, it reduced the TNF-α release from the fat tissue and prevented development of diabetes; in mouse models of diabetes, it improved insulin resistance
8	Inhibition of TNFα release	PMA-differentiated THP-1 cells	11.24 µM	-
9	Inhibition of TNFα release	Rat serum	68.48% inhibition at 20 mg/kg dose	Good anti- inflammatory activity in carrageenan-induced rat paw edema model
10	Inhibition of TNF-α cleavage	THP-1 cells	100 µM	-
	Inhibition of Heregulin cleavage
		A549 cells	100% inhibition at 40 µM
11 (ZLDI-8)	Inhibition of Notch signaling pathway	LoVo cells	5.57 μM	11 enhanced the effect of Sorafenib on inhibiting tumor growth in a nude HCC-bearing mice model [194]
		SW480 cells	7.42 μM
		MHCC97-H cells	5.32 μM

“-”: Not tested or unknown from the corresponding original reference.