Target Validation Information
Target ID T76846
Target Name Melanocortin-3 receptor
Target Type
Research
Drug Potency against Target C[CO-2,3-pyrazine-CO-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info IC50 = 23 nM [529226]
Tic-D-Phe-Arg-2-Nal-NHCH3 Drug Info Ki = 1632 nM [527941]
Ac-His-D-Phe-Arg-2-Nal-NHCH3 Drug Info Ki = 1195 nM [528247]
C[Nle-Arg-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 2.6 nM [528082]
Melanotetan II Drug Info IC50 = 0.57 nM [553146]
afamelanotide Drug Info IC50 = 19 nM [527610]
GPYRMEHFRWGSPPKD-NH2 Drug Info Ki = 9.23 nM [527529]
AEKKDEGPYRMEHFRWGSPPKD Drug Info Ki = 10.64 nM [527529]
Ac-YR[CEH(pF-dF)RWC]-NH2 Drug Info Ki = 15.87 nM [527529]
Ac-YRMEHdFRWG-NH2 Drug Info Ki = 1.44 nM [527529]
Ac-[CEHdFRWC]-NH2 Drug Info Ki = 399.7 nM [527529]
Ac-R[CEHdFRWC]-NH2 Drug Info Ki = 33.76 nM [527529]
Ac-YR[CEHdFRWC]SPPKD-NH2 Drug Info Ki = 7.91 nM [527529]
Ac-Tyr-D-Phe-Arg-2-Nal-NHCH3 Drug Info Ki = 1727 nM [528247]
C[Nle-Glu-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 1200 nM [528082]
C[Nle-Gln-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 1.4 nM [528082]
C[Nle-Pro-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 2700 nM [528082]
C[Nle-Nle-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 250 nM [528082]
C[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 140 nM [528082]
C[CO-(CH2)2-CO-Nle-D-Phe-Arg-Trp-Lys]-NH2 Drug Info IC50 = 84 nM [529226]
C[CO-(CH2)3-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info IC50 = 11 nM [529226]
Ac-dR[CEHdFRWC]-NH2 Drug Info Ki = 56.79 nM [527529]
Ac-YRMEHdFRWGSPPKD-NH2 Drug Info Ki = 0.11 nM [527529]
Ac-YK[CEHdFRWC]-NH2 Drug Info Ki = 97.97 nM [527529]
C[Nle-Val-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 600 nM [528082]
C[Nle-Val-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 1.7 nM [528082]
C[Nle-Pro-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 13 nM [528082]
C[Nle-Gln-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 270 nM [528082]
Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 Drug Info IC50 = 1.3 nM [530169]
C[CO-(CH2)3-CO-Pro-D-Phe-Arg-Trp-Lys]-NH2 Drug Info IC50 = 385 nM [529226]
C[CO-o-C6H4-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info IC50 = 32 nM [529226]
MK-11 Drug Info Ki = 140 nM [526348]
NDP-SYSMEHFRWGKPVG Drug Info Ki = 0.23 nM [527529]
MK-10 Drug Info Ki = 390 nM [526348]
Ac-YR[CEH(d-2alpha-Nal)RWC]-NH2 Drug Info Ki = 6.84 nM [527529]
Ac-YR[CEHdFRWC]-NH2 Drug Info Ki = 55.02 nM [527529]
C[Nle-His-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 560 nM [528082]
C[Nle-Asp-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 820 nM [528082]
C[Nle-Glu-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 140 nM [528082]
Ac-Nle-c[Asp-His-DNal(2')-Pro-Trp-Lys]-NH2 Drug Info IC50 = 2.3 nM [530169]
C[CO-2,3-pyrazine-CO-D-Phe-Arg-Trp-Lys]-NH2 Drug Info IC50 = 1100 nM [529226]
C[CO-(CH2)2-CO-Nle-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info IC50 = 12 nM [529226]
Ac-YR[CEH(pCl-dF)RWC]-NH2 Drug Info Ki = 3.12 nM [527529]
Ac-YCit[CEHdFRWC]-NH2 Drug Info Ki = 313.48 nM [527529]
Ac-YRC(Me)*EHdFRWC(Me)NH2 Drug Info Ki = 166.41 nM [527529]
C[Nle-His-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 12 nM [528082]
C[Nle-Nle-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 6 nM [528082]
MK-9 Drug Info Ki = 5.9 nM [529226]
References
Ref 529226J Med Chem. 2008 Jan 24;51(2):187-95. Epub 2007 Dec 19.Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
Ref 527941Bioorg Med Chem Lett. 2006 Mar 15;16(6):1721-5. Epub 2005 Dec 20.Synthesis of Tic-D-Phe Psi[CH2-CH2] isostere and its use in the development of melanocortin receptor agonists.
Ref 528247Bioorg Med Chem Lett. 2006 Sep 1;16(17):4668-73.Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 553146Metabolic fate of endogenously synthesized prostaglandin D2 in a human female with mastocytosis. Prostaglandins. 1985 Sep;30(3):383-400.
Ref 527610Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5.Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 528247Bioorg Med Chem Lett. 2006 Sep 1;16(17):4668-73.Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 529226J Med Chem. 2008 Jan 24;51(2):187-95. Epub 2007 Dec 19.Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
Ref 529226J Med Chem. 2008 Jan 24;51(2):187-95. Epub 2007 Dec 19.Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 530169J Med Chem. 2009 Jun 25;52(12):3627-35.Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
Ref 529226J Med Chem. 2008 Jan 24;51(2):187-95. Epub 2007 Dec 19.Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
Ref 529226J Med Chem. 2008 Jan 24;51(2):187-95. Epub 2007 Dec 19.Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
Ref 526348J Med Chem. 2002 Jun 6;45(12):2644-50.Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 526348J Med Chem. 2002 Jun 6;45(12):2644-50.Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 530169J Med Chem. 2009 Jun 25;52(12):3627-35.Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
Ref 529226J Med Chem. 2008 Jan 24;51(2):187-95. Epub 2007 Dec 19.Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
Ref 529226J Med Chem. 2008 Jan 24;51(2):187-95. Epub 2007 Dec 19.Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 529226J Med Chem. 2008 Jan 24;51(2):187-95. Epub 2007 Dec 19.Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.

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