Target Validation Information
TTD ID	T49072
Target Name	Urotensin II receptor (UTS2R)
Type of Target	Clinical trial
Drug Potency against Target	Ac-FWKY-NH2	Drug Info	Ki < 10000 nM	[4]
	Ac-SFWKYS-NH2	Drug Info	Ki < 10000 nM	[4]
	Ac-WKY-NH2	Drug Info	Ki < 10000 nM	[4]
	Ac-[CFWKFC]-NH2	Drug Info	Ki = 17 nM	[4]
	AGTAD[CFWKYC]V	Drug Info	Ki = 0.19 nM	[4]
	ICI-199441	Drug Info	Ki = 4000 nM	[1]
	JNJ-28318706	Drug Info	IC50 = 84 nM	[3]
	PALOSURAN	Drug Info	IC50 = 17 nM	[4]
	SB-328872	Drug Info	Ki = 110 nM	[2]
	SB-436811	Drug Info	Ki = 3.2 nM	[4]
References
REF 1	Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3716-9.
REF 2	Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3950-4.
REF 3	Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits. J Med Chem. 2009 Dec 10;52(23):7432-45.
REF 4	Urotensin-II receptor modulators as potential drugs. J Med Chem. 2010 Apr 8;53(7):2695-708.

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