Target Validation Information
Target ID T35842
Target Name Melanocyte stimulating hormone receptor
Target Type
Clinical Trial
Drug Potency against Target Ac-Nle-c[Asp-His-DNaI(2')-Pro-Trp-Lys]-NH2 Drug Info IC50 = 600 nM [530169]
Ac-YR[CEH(pF-dF)RWC]-NH2 Drug Info Ki = 9.91 nM [527529]
Ac-[CEHdFRWC]-NH2 Drug Info Ki = 67.09 nM [527529]
Ac-R[CEHdFRWC]-NH2 Drug Info Ki = 10.34 nM [527529]
GPYRMEHFRWGSPPKD-NH2 Drug Info Ki = 0.51 nM [527529]
Ac-YR[CEH(d-2alpha-Nal)RWC]-NH2 Drug Info Ki = 121.3 nM [527529]
C[Nle-Gln-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 1000 nM [528082]
C[Nle-Gln-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 1000 nM [528082]
C[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 1400 nM [528082]
C[CO-(CH2)2-CO-Nle-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info IC50 = 2000 nM [529226]
C[CO-o-C6H4-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info IC50 = 410 nM [529226]
Ac-YK[CEHdFRWC]-NH2 Drug Info Ki = 15.76 nM [527529]
Ac-YR[CEHdFRWC]-NH2 Drug Info Ki = 17.12 nM [527529]
Ac-dR[CEHdFRWC]-NH2 Drug Info Ki = 16.78 nM [527529]
NDP-SYSMEHFRWGKPVG Drug Info Ki = 0.1 nM [527529]
Ac-YR[CEH(pCl-dF)RWC]-NH2 Drug Info Ki = 8.22 nM [527529]
Ac-YCit[CEHdFRWC]-NH2 Drug Info Ki = 49.42 nM [527529]
Ac-His-D-Phe-Arg-2-Nal-NHCH3 Drug Info Ki = 13 nM [528247]
C[Nle-Arg-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 1500 nM [528082]
C[Nle-Val-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 4000 nM [528082]
C[Nle-Nle-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 3000 nM [528082]
C[CO-2,3-pyrazine-CO-D-Phe-Arg-Trp-Lys]-NH2 Drug Info IC50 = 412 nM [529226]
C[CO-2,3-pyrazine-CO-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info IC50 = 707 nM [529226]
Tic-D-Phe-Arg-2-Nal-NHCH3 Drug Info Ki = 2276 nM [527941]
Ac-His-DPhe-Arg-Trp-NH2 Drug Info IC50 = 615 nM [534420]
Ac-YRC(Me)*EHdFRWC(Me)NH2 Drug Info Ki = 2.73 nM [527529]
AEKKDEGPYRMEHFRWGSPPKD Drug Info Ki = 0.89 nM [527529]
Ac-Tyr-D-Phe-Arg-2-Nal-NHCH3 Drug Info Ki = 4520 nM [528247]
Ac-YR[CEHFRWC]-NH2 Drug Info Ki = 147.07 nM [527529]
Ac-YR[CEHdFRWC]SPPKD-NH2 Drug Info Ki = 0.57 nM [527529]
Ac-YRMEHdFRWG-NH2 Drug Info Ki = 0.21 nM [527529]
Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 Drug Info IC50 = 0.2 nM [530169]
Ac-Nle-c[Asp-His-DNal(2')-Pro-Trp-Lys]-NH2 Drug Info IC50 = 1 nM [530169]
References
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 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 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 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 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 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 534420J Med Chem. 1997 Jul 4;40(14):2133-9.Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
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 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 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 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.

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