Target Validation Information
TTD ID	T66237
Target Name	Vasopressin V2 receptor (V2R)
Type of Target	Successful
Drug Potency against Target	Conivaptan	Drug Info	Ki = 3.04	[9]
	ARGENINE VASOPRESSIN	Drug Info	Ki = 0.45 nM	[2]
	ATOSIBAN	Drug Info	Ki = 330 nM	[3]
	D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT	Drug Info	Ki = 930 nM	[1]
	DVDAVP	Drug Info	Ki = 0.26 nM	[2]
	D[Arg4,Dab8]VP	Drug Info	Ki = 1.8 nM	[2]
	D[Arg4,Lys8]VP	Drug Info	Ki = 3.8 nM	[2]
	D[Arg4,Orn8]VP	Drug Info	Ki = 3.1 nM	[2]
	D[Arg4]AVP	Drug Info	Ki = 0.2 nM	[2]
	D[Cha4,Dab8]VP	Drug Info	Ki = 450 nM	[2]
	D[Cha4,Dap8]VP	Drug Info	Ki = 1050 nM	[2]
	D[Cha4,Lys8]VP	Drug Info	Ki = 600 nM	[2]
	D[Cha4,Orn8]VP	Drug Info	Ki = 450 nM	[2]
	D[Cha4]AVP	Drug Info	Ki = 12.7 nM	[2]
	D[D-3-Pal2]AVP	Drug Info	Ki = 69 nM	[2]
	D[Leu4,Dab8]VP	Drug Info	Ki = 210 nM	[2]
	D[Leu4,Dap8]VP	Drug Info	Ki = 240 nM	[2]
	D[Leu4,Lys8]VP	Drug Info	Ki = 100 nM	[2]
	D[Leu4,Orn8]VP	Drug Info	Ki = 425 nM	[2]
	D[Leu4]AVP	Drug Info	Ki = 3.1 nM	[2]
	D[Orn4,Lys8]VP	Drug Info	Ki = 51 nM	[2]
	D[Orn4,Orn8]VP	Drug Info	Ki = 76 nM	[2]
	D[Orn4]AVP	Drug Info	Ki = 3.4 nM	[2]
	D[Val4]AVP	Drug Info	Ki = 0.3 nM	[2]
	L-372662	Drug Info	Ki = 9700 nM	[7]
	Mozavaptan	Drug Info	IC50 = 300 nM	[8]
	Retosiban	Drug Info	Ki = 950 nM	[3]
	SSR149415	Drug Info	Ki = 325 nM	[6]
	VA-106483	Drug Info	Ki = 2000 nM	[5]
	YM-35278	Drug Info	Ki = 0.4 nM	[4]
References
REF 1	Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors. J Med Chem. 2002 Jun 6;45(12):2579-88.
REF 2	Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasop... J Med Chem. 2007 Feb 22;50(4):835-47.
REF 3	The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4.
REF 4	Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists. Bioorg Med Chem. 2008 Nov 1;16(21):9524-35.
REF 5	New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists. J Med Chem. 2008 Dec 25;51(24):8124-34.
REF 6	Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22.
REF 7	Oral oxytocin antagonists. J Med Chem. 2010 Sep 23;53(18):6525-38.
REF 8	New analgesic drugs derived from phencyclidine. J Med Chem. 1981 May;24(5):496-9.
REF 9	Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.

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