Target Validation Information
TTD ID	T79232
Target Name	Vasopressin V1a receptor (V1AR)
Type of Target	Successful
Drug Potency against Target	Conivaptan	Drug Info	Ki = 0.48 nM	[10]
	1'-tosylspiro[indene-1,4'-piperidine]	Drug Info	Ki = 9800 nM	[8]
	A-987306	Drug Info	Ki = 2.4 nM	[6]
	ARGENINE VASOPRESSIN	Drug Info	Ki = 1.54 nM	[3]
	ATOSIBAN	Drug Info	Ki = 0.15 nM	[5]
	D(CH2)5[Tyr(Me)2,Thr4,Orn8(5/6C-Flu),Tyr-NH29]VT	Drug Info	Ki = 217 nM	[1]
	D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT	Drug Info	Ki = 3.9 nM	[1]
	DesGly-NH2,d(CH2)5[D-Tyr2,Thr4,Orn8(5/6C-Flu)]VT	Drug Info	Ki = 656 nM	[1]
	DVDAVP	Drug Info	Ki = 316 nM	[3]
	D[Arg4,Dab8]VP	Drug Info	Ki = 25 nM	[3]
	D[Arg4,Lys8]VP	Drug Info	Ki = 130 nM	[3]
	D[Arg4,Orn8]VP	Drug Info	Ki = 67 nM	[3]
	D[Arg4]AVP	Drug Info	Ki = 12.9 nM	[3]
	D[Cha4,Dab8]VP	Drug Info	Ki = 4400 nM	[3]
	D[Cha4,Dap8]VP	Drug Info	Ki = 1800 nM	[3]
	D[Cha4,Lys8]VP	Drug Info	Ki = 9100 nM	[3]
	D[Cha4,Orn8]VP	Drug Info	Ki = 2900 nM	[3]
	D[Cha4]AVP	Drug Info	Ki = 2300 nM	[3]
	D[D-3-Pal2]AVP	Drug Info	Ki = 450 nM	[3]
	D[Leu4,Dab8]VP	Drug Info	Ki = 1000 nM	[3]
	D[Leu4,Dap8]VP	Drug Info	Ki = 3300 nM	[3]
	D[Leu4,Lys8]VP	Drug Info	Ki = 3800 nM	[3]
	D[Leu4,Orn8]VP	Drug Info	Ki = 1400 nM	[3]
	D[Leu4]AVP	Drug Info	Ki = 1252 nM	[3]
	D[Lys8(5/6-Flu)]VT	Drug Info	Ki = 57 nM	[1]
	D[Orn4,Lys8]VP	Drug Info	Ki = 2800 nM	[3]
	D[Orn4,Orn8]VP	Drug Info	Ki = 1300 nM	[3]
	D[Orn4]AVP	Drug Info	Ki = 900 nM	[3]
	D[Orn8(5/6C-Flu)]VT	Drug Info	Ki = 107 nM	[1]
	D[Thr4,Lys8(5/6C-Flu)]VT	Drug Info	Ki = 25.5 nM	[1]
	D[Thr4,Orn8(5/6C-Flu)]VT	Drug Info	Ki = 30 nM	[1]
	D[Val4]AVP	Drug Info	Ki = 60 nM	[3]
	HO-LVA	Drug Info	Ki = 0.21 nM	[4]
	Hoo-Phe-Orn-Pro-hle-Pff-Phe-NH2	Drug Info	IC50 = 740 nM	[2]
	L-371257	Drug Info	Ki = 3.7 nM	[8]
	L-372662	Drug Info	Ki = 0.76 nM	[8]
	Mozavaptan	Drug Info	IC50 = 5000 nM	[9]
	PF-3274167	Drug Info	Ki = 1120 nM	[8]
	PMX-53	Drug Info	IC50 = 740 nM	[2]
	Relcovaptan	Drug Info	Ki = 0.52 nM	[4]
	SSR149415	Drug Info	Ki = 22 nM	[7]
	[HO1][Lys8(5/6C-Flu)]VT	Drug Info	Ki = 13.7 nM	[1]
	[HO1][Orn8(5/6C-Flu)]VT	Drug Info	Ki = 12.2 nM	[1]
	[HO1][Orn8(5/6C-Rhm)]VT	Drug Info	Ki = 7.6 nM	[1]
	[HO1][Thr4,Lys8(5/6C-Flu)]VT	Drug Info	Ki = 17.3 nM	[1]
	[HO1][Thr4,Orn8(5/6C-Flu)]VT	Drug Info	Ki = 11.8 nM	[1]
	[Lys8(Alexa 546) ]PVA	Drug Info	Ki = 2.1 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	Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92.
REF 3	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 4	Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands. J Med Chem. 2007 Oct 4;50(20):4976-85.
REF 5	The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4.
REF 6	cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
REF 7	Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22.
REF 8	Oral oxytocin antagonists. J Med Chem. 2010 Sep 23;53(18):6525-38.
REF 9	New analgesic drugs derived from phencyclidine. J Med Chem. 1981 May;24(5):496-9.
REF 10	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.

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