Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T45457 | ||||
Target Name | Melanocortin receptor | ||||
Target Type | Clinical Trial |
||||
Drug Potency against Target | Ac-His-DPhe(3,4-diCl)-Arg-Trp-NH2 | Drug Info | Ki = 260 nM | [529699] | |
Ac-His-DPhe(pCF3)-Arg-Trp-NH2 | Drug Info | Ki = 6170 nM | [529699] | ||
Ac-His-DPhe(pBr)-Arg-Trp-NH2 | Drug Info | Ki = 350 nM | [529699] | ||
MK-10 | Drug Info | Ki = 990 nM | [526348] | ||
AEKKDEGPYRMEHFRWGSPPKD | Drug Info | Ki = 76.9 nM | [527529] | ||
GPYRMEHFRWGSPPKD-NH2 | Drug Info | Ki = 24.8 nM | [527529] | ||
C[Nle-Val-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 2.2 nM | [528082] | ||
C[Nle-His-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 100 nM | [528082] | ||
C[Nle-Asp-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 220 nM | [528082] | ||
C[Nle-Pro-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 10 nM | [528082] | ||
C[Nle-Nle-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 70 nM | [528082] | ||
C[CO-o-C6H4-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 | Drug Info | IC50 = 210 nM | [529226] | ||
Ac-Nle-c[Asp-His-DNal(2')-Pro-Trp-Lys]-NH2 | Drug Info | IC50 = 0.9 nM | [530169] | ||
C[CO-(CH2)3-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 | Drug Info | IC50 = 27 nM | [529226] | ||
afamelanotide | Drug Info | IC50 = 118 nM | [527610] | ||
Ac-His-DNal(2)-Arg-Trp-NH2 | Drug Info | Ki = 19 nM | [529699] | ||
C[Nle-His-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 2.3 nM | [528082] | ||
Ac-His-DPhe(pI)-Arg-Trp-NH2 | Drug Info | Ki = 260 nM | [529699] | ||
C[Nle-Glu-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 3060 nM | [528082] | ||
C[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 68 nM | [528082] | ||
C[CO-2,3-pyrazine-CO-D-Nal(2)-Arg-Trp-Lys]-NH2 | Drug Info | IC50 = 230 nM | [529226] | ||
MK-11 | Drug Info | Ki = 880 nM | [526348] | ||
Ac-YRMEHdFRWGSPPKD-NH2 | Drug Info | Ki = 0.26 nM | [527529] | ||
Ac-YRMEHdFRWG-NH2 | Drug Info | Ki = 0.84 nM | [527529] | ||
Ac-YR[CEH(pF-dF)RWC]-NH2 | Drug Info | Ki = 239.3 nM | [527529] | ||
C[Nle-Gln-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 500 nM | [528082] | ||
C[Nle-Arg-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 2.3 nM | [528082] | ||
C[Nle-Val-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 110 nM | [528082] | ||
C[CO-(CH2)3-CO-Pro-D-Phe-Arg-Trp-Lys]-NH2 | Drug Info | IC50 = 870 nM | [529226] | ||
C[Nle-Glu-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 44 nM | [528082] | ||
C[CO-(CH2)2-CO-Nle-D-Phe-Arg-Trp-Lys]-NH2 | Drug Info | IC50 = 520 nM | [529226] | ||
C[CO-(CH2)2-CO-Nle-D-Nal(2)-Arg-Trp-Lys]-NH2 | Drug Info | IC50 = 17 nM | [529226] | ||
Ac-YRC(Me)*EHdFRWC(Me)NH2 | Drug Info | Ki = 62.11 nM | [527529] | ||
Ac-YR[CEH(pCl-dF)RWC]-NH2 | Drug Info | Ki = 42.19 nM | [527529] | ||
NDP-SYSMEHFRWGKPVG | Drug Info | Ki = 0.17 nM | [527529] | ||
Ac-YR[CEH(d-2alpha-Nal)RWC]-NH2 | Drug Info | Ki = 37.8 nM | [527529] | ||
C[Nle-Gln-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 1.4 nM | [528082] | ||
C[Nle-Nle-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 3.8 nM | [528082] | ||
C[Nle-Pro-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | IC50 = 400 nM | [528082] | ||
Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 | Drug Info | IC50 = 7.5 nM | [530169] | ||
References | |||||
Ref 529699 | J Med Chem. 2008 Sep 25;51(18):5585-93.Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. | ||||
Ref 529699 | J Med Chem. 2008 Sep 25;51(18):5585-93.Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. | ||||
Ref 529699 | J Med Chem. 2008 Sep 25;51(18):5585-93.Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. | ||||
Ref 526348 | J 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 527529 | J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. | ||||
Ref 527529 | J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. | ||||
Ref 528082 | J 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 528082 | J 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 528082 | J 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 528082 | J 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 528082 | J 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 529226 | J 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 530169 | J 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 529226 | J 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 527610 | Bioorg 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 529699 | J Med Chem. 2008 Sep 25;51(18):5585-93.Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. | ||||
Ref 528082 | J 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 529699 | J Med Chem. 2008 Sep 25;51(18):5585-93.Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. | ||||
Ref 528082 | J 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 528082 | J 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 529226 | J 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 526348 | J 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 527529 | J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. | ||||
Ref 527529 | J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. | ||||
Ref 527529 | J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. | ||||
Ref 528082 | J 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 528082 | J 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 528082 | J 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 529226 | J 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 528082 | J 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 529226 | J 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 529226 | J 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 527529 | J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. | ||||
Ref 527529 | J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. | ||||
Ref 527529 | J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. | ||||
Ref 527529 | J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. | ||||
Ref 528082 | J 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 528082 | J 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 528082 | J 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 530169 | J 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. |
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