Target Validation Information
TTD ID T45457
Target Name Melanocortin receptor (MCR)
Type of Target
Clinical trial
Drug Potency against Target Ac-His-DNal(2)-Arg-Trp-NH2 Drug Info Ki = 19 nM [6]
Ac-His-DPhe(3,4-diCl)-Arg-Trp-NH2 Drug Info Ki = 260 nM [6]
Ac-His-DPhe(pBr)-Arg-Trp-NH2 Drug Info Ki = 350 nM [6]
Ac-His-DPhe(pCF3)-Arg-Trp-NH2 Drug Info Ki = 6170 nM [6]
Ac-His-DPhe(pI)-Arg-Trp-NH2 Drug Info Ki = 260 nM [6]
Ac-Nle-c[Asp-His-DNal(2')-Pro-Trp-Lys]-NH2 Drug Info IC50 = 0.9 nM [7]
Ac-YRC(Me)*EHdFRWC(Me)NH2 Drug Info Ki = 62.11 nM [2]
Ac-YRMEHdFRWG-NH2 Drug Info Ki = 0.84 nM [2]
Ac-YRMEHdFRWGSPPKD-NH2 Drug Info Ki = 0.26 nM [2]
Ac-YR[CEH(d-2alpha-Nal)RWC]-NH2 Drug Info Ki = 37.8 nM [2]
Ac-YR[CEH(pCl-dF)RWC]-NH2 Drug Info Ki = 42.19 nM [2]
Ac-YR[CEH(pF-dF)RWC]-NH2 Drug Info Ki = 239.3 nM [2]
AEKKDEGPYRMEHFRWGSPPKD Drug Info Ki = 76.9 nM [2]
Afamelanotide Drug Info IC50 = 118 nM [3]
C[CO-(CH2)2-CO-Nle-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info IC50 = 17 nM [5]
C[CO-(CH2)2-CO-Nle-D-Phe-Arg-Trp-Lys]-NH2 Drug Info IC50 = 520 nM [5]
C[CO-(CH2)3-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info IC50 = 27 nM [5]
C[CO-(CH2)3-CO-Pro-D-Phe-Arg-Trp-Lys]-NH2 Drug Info IC50 = 870 nM [5]
C[CO-2,3-pyrazine-CO-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info IC50 = 230 nM [5]
C[CO-o-C6H4-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info IC50 = 210 nM [5]
C[Nle-Arg-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 2.3 nM [4]
C[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 68 nM [4]
C[Nle-Asp-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 220 nM [4]
C[Nle-Gln-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 1.4 nM [4]
C[Nle-Gln-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 500 nM [4]
C[Nle-Glu-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 44 nM [4]
C[Nle-Glu-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 3060 nM [4]
C[Nle-His-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 2.3 nM [4]
C[Nle-His-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 100 nM [4]
C[Nle-Nle-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 3.8 nM [4]
C[Nle-Nle-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 70 nM [4]
C[Nle-Pro-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 10 nM [4]
C[Nle-Pro-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 400 nM [4]
C[Nle-Val-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info IC50 = 2.2 nM [4]
C[Nle-Val-D-Phe-Arg-Trp-Glu]-NH2 Drug Info IC50 = 110 nM [4]
GPYRMEHFRWGSPPKD-NH2 Drug Info Ki = 24.8 nM [2]
MK-10 Drug Info Ki = 990 nM [1]
MK-11 Drug Info Ki = 880 nM [1]
MT-II Drug Info IC50 = 7.5 nM [7]
NDP-SYSMEHFRWGKPVG Drug Info Ki = 0.17 nM [2]
References
REF 1 Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors. J Med Chem. 2002 Jun 6;45(12):2644-50.
REF 2 Discovery of a beta-MSH-derived MC-4R selective agonist. J Med Chem. 2005 May 5;48(9):3095-8.
REF 3 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-oxo... Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5.
REF 4 Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. J Med Chem. 2006 Mar 23;49(6):1946-52.
REF 5 Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 ... J Med Chem. 2008 Jan 24;51(2):187-95.
REF 6 Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-... J Med Chem. 2008 Sep 25;51(18):5585-93.
REF 7 Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 rece... J Med Chem. 2009 Jun 25;52(12):3627-35.

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