Target Validation Information
Target ID T79232
Target Name Vasopressin V1a receptor
Target Type
Successful
Drug Potency against Target Ac-Phe-[Orn-Pro-cha-Trp-Arg] Drug Info IC50 = 740 nM [528343]
L-371257 Drug Info Ki = 3.7 nM [530975]
HO-LVA Drug Info Ki = 0.21 nM [529036]
D[Cha4,Dab8]VP Drug Info Ki = 4400 nM [528674]
SR-149415 Drug Info Ki = 22 nM [530420]
D[Orn4,Orn8]VP Drug Info Ki = 1300 nM [528674]
D[Leu4,Orn8]VP Drug Info Ki = 1400 nM [528674]
D[Cha4]AVP Drug Info Ki = 2300 nM [528674]
D[Arg4]AVP Drug Info Ki = 12.9 nM [528674]
D[Leu4]AVP Drug Info Ki = 1252 nM [528674]
D[Orn4,Lys8]VP Drug Info Ki = 2800 nM [528674]
D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT Drug Info Ki = 3.9 nM [526347]
D[Val4]AVP Drug Info Ki = 60 nM [528674]
D[Cha4,Orn8]VP Drug Info Ki = 2900 nM [528674]
D[Cha4,Dap8]VP Drug Info Ki = 1800 nM [528674]
DesGly-NH2,d(CH2)5[D-Tyr2,Thr4,Orn8(5/6C-Flu)]VT Drug Info Ki = 656 nM [526347]
D[Thr4,Orn8(5/6C-Flu)]VT Drug Info Ki = 30 nM [526347]
D[Orn8(5/6C-Flu)]VT Drug Info Ki = 107 nM [526347]
1'-tosylspiro[indene-1,4'-piperidine] Drug Info Ki = 9800 nM [530975]
[HO1][Orn8(5/6C-Rhm)]VT Drug Info Ki = 7.6 nM [526347]
Mozavaptan Drug Info IC50 = 5000 nM [533576]
D[Leu4,Lys8]VP Drug Info Ki = 3800 nM [528674]
D[Arg4,Dab8]VP Drug Info Ki = 25 nM [528674]
D[Arg4,Orn8]VP Drug Info Ki = 67 nM [528674]
D[Leu4,Dap8]VP Drug Info Ki = 3300 nM [528674]
DVDAVP Drug Info Ki = 316 nM [528674]
[HO1][Lys8(5/6C-Flu)]VT Drug Info Ki = 13.7 nM [526347]
D[Thr4,Lys8(5/6C-Flu)]VT Drug Info Ki = 25.5 nM [526347]
D[Lys8(5/6-Flu)]VT Drug Info Ki = 57 nM [526347]
A-987306 Drug Info Ki = 2.4 nM [529789]
Conivaptan Drug Info Ki = 0.48 nM [537564]
[Lys8(Alexa 546) ]PVA Drug Info Ki = 2.1 nM [529036]
L-372662 Drug Info Ki = 0.76 nM [530975]
PF-3274167 Drug Info Ki = 1120 nM [530975]
D[Arg4,Lys8]VP Drug Info Ki = 130 nM [528674]
D[Cha4,Lys8]VP Drug Info Ki = 9100 nM [528674]
D[D-3-Pal2]AVP Drug Info Ki = 450 nM [528674]
D[Orn4]AVP Drug Info Ki = 900 nM [528674]
ARGENINE VASOPRESSIN Drug Info Ki = 1.54 nM [528674]
D(CH2)5[Tyr(Me)2,Thr4,Orn8(5/6C-Flu),Tyr-NH29]VT Drug Info Ki = 217 nM [526347]
D[Leu4,Dab8]VP Drug Info Ki = 1000 nM [528674]
Relcovaptan Drug Info Ki = 0.52 nM [529036]
[HO1][Thr4,Lys8(5/6C-Flu)]VT Drug Info Ki = 17.3 nM [526347]
[HO1][Orn8(5/6C-Flu)]VT Drug Info Ki = 12.2 nM [526347]
Hoo-Phe-Orn-Pro-hle-Pff-Phe-NH2 Drug Info IC50 = 740 nM [528343]
[HO1][Thr4,Orn8(5/6C-Flu)]VT Drug Info Ki = 11.8 nM [526347]
ATOSIBAN Drug Info Ki = 0.15 nM [529164]
References
Ref 528343Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92. Epub 2006 Jul 28.Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivoactivity.
Ref 530975J Med Chem. 2010 Sep 23;53(18):6525-38.Oral oxytocin antagonists.
Ref 529036J Med Chem. 2007 Oct 4;50(20):4976-85. Epub 2007 Sep 12.Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 530420Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. Epub 2009 Sep 17.Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 530975J Med Chem. 2010 Sep 23;53(18):6525-38.Oral oxytocin antagonists.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 533576J Med Chem. 1981 May;24(5):496-9.New analgesic drugs derived from phencyclidine.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 529789J Med Chem. 2008 Nov 27;51(22):7094-8.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 responses against carrageenan-induced hyperalgesia.
Ref 537564Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
Ref 529036J Med Chem. 2007 Oct 4;50(20):4976-85. Epub 2007 Sep 12.Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands.
Ref 530975J Med Chem. 2010 Sep 23;53(18):6525-38.Oral oxytocin antagonists.
Ref 530975J Med Chem. 2010 Sep 23;53(18):6525-38.Oral oxytocin antagonists.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 528674J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Ref 529036J Med Chem. 2007 Oct 4;50(20):4976-85. Epub 2007 Sep 12.Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 528343Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92. Epub 2006 Jul 28.Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivoactivity.
Ref 526347J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.
Ref 529164Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4. Epub 2007 Nov 6.The discovery of GSK221149A: a potent and selective oxytocin antagonist.

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