Target Validation Information
TTD ID	T29683
Target Name	Neuromedin-K receptor (TACR3)
Type of Target	Successful
Drug Potency against Target	CS-003	Drug Info	Ki = 0.74 nM	[4]
	Talnetant	Drug Info	Ki = 1 nM	[3]
	2-phenyl-N-(1-phenylethyl)quinoline-4-carboxamide	Drug Info	IC50 = 2200 nM	[2]
	3-methoxy-N',2-diphenylquinoline-4-carbohydrazide	Drug Info	IC50 = 32 nM	[1]
	NEUROKININ B	Drug Info	IC50 = 10 nM
	PD-157672	Drug Info	IC50 = 16 nM
	PD-160946	Drug Info	IC50 = 16 nM
	PD-161182	Drug Info	IC50 = 7.3 nM
Action against Disease Model	Talnetant	Drug Info	Two NK3 antagonists, osanetant (SR-142801) and talnetant (SB-223412), have been tested in clinical trials. Both agents are small-molecule, nonpeptide antagonists that inhibit [125I]-MePhe7-NKB binding to the h uMan NK3R (hNK3R) expressed in CHO cell membranes with Kis of 1 nM.In HEK-293 cells expressing the hNK3R, talnetant inhibited the Ca2+ responses induced by IC50 of 6.1nM.	[2]
References
REF 1	N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5748-51.
REF 2	Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor. J Med Chem. 2010 Nov 25;53(22):8080-8.
REF 3	Development and potential utility of dual and triple NK receptor antagonists. Curr Top Med Chem. 2003;3(12):1410-22.
REF 4	Novel triple neurokinin receptor antagonist CS-003 strongly inhibits neurokinin related responses. Eur J Pharmacol. 2008 May 31;586(1-3):306-12.

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