Target Validation Information
Target ID T84486
Target Name Oxytocin receptor
Target Type
Successful
Drug Potency against Target PF-3274167 Drug Info Ki = 9.5 nM [1]
[Lys8(Alexa 546) ]PVA Drug Info Ki = 1.95 nM [2]
[Mpa1, D-Tic2, Aib7]OT Drug Info IC50 = 8500 nM [3]
[Mpa1, L-Tic7]OT Drug Info IC50 = 103 nM [3]
[Mpa1, D-Tyr(Et)2, Aib7, D-Tic9]OT Drug Info IC50 = 55 nM [3]
L-371257 Drug Info Ki = 19 nM [1]
L-372662 Drug Info Ki = 14 nM [1]
D[Leu4,Dap8]VP Drug Info Ki = 134 nM [4]
D[Orn4,Orn8]VP Drug Info Ki = 37 nM [4]
D[Orn4]AVP Drug Info Ki = 997 nM [4]
D[Cha4]AVP Drug Info Ki = 1430 nM [4]
D[Leu4,Dab8]VP Drug Info Ki = 41 nM [4]
D[Leu4,Lys8]VP Drug Info Ki = 64 nM [4]
D[Thr4,Orn8(5/6C-Flu)]VT Drug Info Ki = 0.4 nM [5]
DesGly-NH2,d(CH2)5[D-Tyr2,Thr4,Orn8(5/6C-Flu)]VT Drug Info Ki = 126 nM [5]
[HO1][Orn8(5/6C-Flu)]VT Drug Info Ki = 0.18 nM [5]
Carbetocin Drug Info Affinity = 7.24+/-0.29 nM [6]
[Mpa1, D-Tyr(Et)2, D-Tic7, Aib9]OT Drug Info IC50 = 80 nM [3]
1'-tosylspiro[indene-1,4'-piperidine] Drug Info Ki = 1600 nM [1]
[D-Tic7]OT Drug Info IC50 = 730 nM [3]
D[Cha4,Dap8]VP Drug Info Ki = 1200 nM [4]
[Mpa1, D-Tyr(Et)2, L-Tic7]OT Drug Info IC50 = 176 nM [3]
[Mpa1, D-Tyr(Et)2, D-Tic7, D-Tic9]OT Drug Info IC50 = 25 nM [3]
D[Arg4,Orn8]VP Drug Info Ki = 130 nM [4]
D[Arg4,Dab8]VP Drug Info Ki = 195 nM [4]
D[Leu4]AVP Drug Info Ki = 481 nM [4]
D[Arg4,Lys8]VP Drug Info Ki = 125 nM [4]
[Mpa1, D-Tyr(Et)2, D-Tic7]OT Drug Info IC50 = 51 nM [3]
[L-Tic7]OT Drug Info IC50 = 130 nM [3]
D[Lys8(5/6-Flu)]VT Drug Info Ki = 0.29 nM [5]
[Pip7]OT Drug Info IC50 = 7 nM [3]
[Mpa1, D-Tyr(Et)2, Gly(But)7]OT Drug Info IC50 = 1002 nM [3]
[Mpa1, D-Tyr(Et)2, Gly(But)3, Gly(But)7]OT Drug Info IC50 = 7850 nM [3]
[Gly(But)7]OT Drug Info IC50 = 1380 nM [3]
[Aib7]OT Drug Info IC50 = 75 nM [3]
[Mpa1, D-Tic7]OT Drug Info IC50 = 380 nM [3]
[Mpa1, D-Tyr(Et)2, Aib7]OT Drug Info IC50 = 485 nM [3]
[Mpa1, D-Tyr(Et)2, Pip7]OT Drug Info IC50 = 40 nM [3]
[HO1][Thr4,Lys8(5/6C-Flu)]VT Drug Info Ki = 0.32 nM [5]
SR-149415 Drug Info Ki = 19 nM [7]
D[Cha4,Orn8]VP Drug Info Ki = 550 nM [4]
D[Arg4]AVP Drug Info Ki = 3550 nM [4]
D[Leu4,Orn8]VP Drug Info Ki = 55 nM [4]
ARGENINE VASOPRESSIN Drug Info Ki = 1.17 nM [4]
D[Orn4,Lys8]VP Drug Info Ki = 22 nM [4]
D[Cha4,Lys8]VP Drug Info Ki = 590 nM [4]
[HO1][Lys8(5/6C-Flu)]VT Drug Info Ki = 0.34 nM [5]
D(CH2)5[Tyr(Me)2,Thr4,Orn8(5/6C-Flu),Tyr-NH29]VT Drug Info Ki = 6.24 nM [5]
D[Orn8(5/6C-Flu)]VT Drug Info Ki = 0.25 nM [5]
ATOSIBAN Drug Info IC50 = 12 nM [8]
Retosiban Drug Info Ki = 0.65 nM [9]
[Lys8(Alexa 488) ]PVA Drug Info Ki = 1.04 nM [2]
D[Cha4,Dab8]VP Drug Info Ki = 430 nM [4]
D[Val4]AVP Drug Info Ki = 826 nM [4]
[HO1][Thr4,Orn8(5/6C-Flu)]VT Drug Info Ki = 0.17 nM [5]
D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT Drug Info Ki = 0.21 nM [5]
D[Thr4,Lys8(5/6C-Flu)]VT Drug Info Ki = 1.8 nM [5]
References
REF 1J Med Chem. 2010 Sep 23;53(18):6525-38.Oral oxytocin antagonists.
REF 2J 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 3Eur J Med Chem. 2007 Jun;42(6):799-806. Epub 2007 Jan 10.Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7.
REF 4J 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 5J 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 6[International therapeutic trial comparing the value of radical mastectomy(Halsted) and extended mastectomy (Halsted plus internal mammary node dissection in the treatment of breast cancer. 5-year results].
REF 7Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. Epub 2009 Sep 17.Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.
REF 8Bioorg Med Chem Lett. 2006 Feb 15;16(4):954-9. Epub 2005 Nov 15.Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.
REF 9Bioorg 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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