Target Validation Information
Target ID T66237
Target Name Vasopressin V2 receptor
Target Type
Successful
Drug Potency against Target Retosiban Drug Info Ki = 950 nM [529164]
Conivaptan Drug Info Ki = 3.04 [552263]
Mozavaptan Drug Info IC50 = 300 nM [533576]
D[Orn4,Orn8]VP Drug Info Ki = 76 nM [528674]
SR-149415 Drug Info Ki = 325 nM [530420]
DVDAVP Drug Info Ki = 0.26 nM [528674]
D[Arg4,Dab8]VP Drug Info Ki = 1.8 nM [528674]
D[Orn4,Lys8]VP Drug Info Ki = 51 nM [528674]
D[D-3-Pal2]AVP Drug Info Ki = 69 nM [528674]
D[Leu4,Lys8]VP Drug Info Ki = 100 nM [528674]
L-372662 Drug Info Ki = 9700 nM [530975]
D[Leu4]AVP Drug Info Ki = 3.1 nM [528674]
D[Orn4]AVP Drug Info Ki = 3.4 nM [528674]
D[Cha4,Dab8]VP Drug Info Ki = 450 nM [528674]
D[Leu4,Dab8]VP Drug Info Ki = 210 nM [528674]
D[Leu4,Orn8]VP Drug Info Ki = 425 nM [528674]
D[Cha4,Lys8]VP Drug Info Ki = 600 nM [528674]
YM-35278 Drug Info Ki = 0.4 nM [529738]
VA-106483 Drug Info Ki = 2000 nM [529841]
D[Cha4,Orn8]VP Drug Info Ki = 450 nM [528674]
D[Leu4,Dap8]VP Drug Info Ki = 240 nM [528674]
D[Cha4]AVP Drug Info Ki = 12.7 nM [528674]
D[Val4]AVP Drug Info Ki = 0.3 nM [528674]
D[Cha4,Dap8]VP Drug Info Ki = 1050 nM [528674]
D[Arg4,Lys8]VP Drug Info Ki = 3.8 nM [528674]
D[Arg4,Orn8]VP Drug Info Ki = 3.1 nM [528674]
ARGENINE VASOPRESSIN Drug Info Ki = 0.45 nM [528674]
D[Arg4]AVP Drug Info Ki = 0.2 nM [528674]
D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT Drug Info Ki = 930 nM [526347]
ATOSIBAN Drug Info Ki = 330 nM [529164]
References
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.
Ref 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
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 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 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 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 529738Bioorg Med Chem. 2008 Nov 1;16(21):9524-35. Epub 2008 Sep 17.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.
Ref 529841J Med Chem. 2008 Dec 25;51(24):8124-34.New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists.
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 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 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.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.