Target Information

Target General Information

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Target ID

T45457 (Former ID: TTDR00057)

Target Name

Melanocortin receptor (MCR)

Synonyms

Melanocortin receptor

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Gene Name

NO-GeName

Target Type

Clinical trial target

[1]

Disease

[+] 1 Target-related Diseases

Ulcerative colitis [ICD-11: DD71]

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Clinical Trial Drug(s)

[+] 1 Clinical Trial Drugs

ASP-3291

Drug Info

Phase 2

Ulcerative colitis

[2]

Mode of Action

[+] 2 Modes of Action

Modulator

[+] 1 Modulator drugs

ASP-3291

Drug Info

[3]

Inhibitor

[+] 39 Inhibitor drugs

Ac-His-DNal(2)-Arg-Trp-NH2

Drug Info

[4]

Ac-His-DPhe(3,4-diCl)-Arg-Trp-NH2

Drug Info

[4]

Ac-His-DPhe(pBr)-Arg-Trp-NH2

Drug Info

[4]

Ac-His-DPhe(pCF3)-Arg-Trp-NH2

Drug Info

[4]

Ac-His-DPhe(pI)-Arg-Trp-NH2

Drug Info

[4]

Ac-Nle-c[Asp-His-DNal(2')-Pro-Trp-Lys]-NH2

Drug Info

[5]

Ac-YRC(Me)*EHdFRWC(Me)NH2

Drug Info

[6]

Ac-YRMEHdFRWG-NH2

Drug Info

[6]

Ac-YRMEHdFRWGSPPKD-NH2

Drug Info

[6]

Ac-YR[CEH(d-2alpha-Nal)RWC]-NH2

Drug Info

[6]

Ac-YR[CEH(pCl-dF)RWC]-NH2

Drug Info

[6]

Ac-YR[CEH(pF-dF)RWC]-NH2

Drug Info

[6]

AEKKDEGPYRMEHFRWGSPPKD

Drug Info

[6]

C[CO-(CH2)2-CO-Nle-D-Nal(2)-Arg-Trp-Lys]-NH2

Drug Info

[7]

C[CO-(CH2)2-CO-Nle-D-Phe-Arg-Trp-Lys]-NH2

Drug Info

[7]

C[CO-(CH2)3-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2

Drug Info

[7]

C[CO-(CH2)3-CO-Pro-D-Phe-Arg-Trp-Lys]-NH2

Drug Info

[7]

C[CO-2,3-pyrazine-CO-D-Nal(2)-Arg-Trp-Lys]-NH2

Drug Info

[7]

C[CO-o-C6H4-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2

Drug Info

[7]

C[Nle-Arg-D-Nal(2')-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Asp-D-Nal(2')-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Gln-D-Nal(2')-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Gln-D-Phe-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Glu-D-Nal(2')-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Glu-D-Phe-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-His-D-Nal(2')-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-His-D-Phe-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Nle-D-Nal(2')-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Nle-D-Phe-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Pro-D-Nal(2')-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Pro-D-Phe-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Val-D-Nal(2')-Arg-Trp-Glu]-NH2

Drug Info

[8]

C[Nle-Val-D-Phe-Arg-Trp-Glu]-NH2

Drug Info

[8]

GPYRMEHFRWGSPPKD-NH2

Drug Info

[6]

MK-10

Drug Info

[9]

MK-11

Drug Info

[9]

MT-II

Drug Info

[5]

NDP-SYSMEHFRWGKPVG

Drug Info

[6]

Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Target Poor or Non Binders

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Target Poor or Non Binders

Target Poor or Non Binders Info

Target-Related Models and Studies

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Target Validation

Target Validation Info

References

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REF 1

Wikipedia: Bremelanotide

REF 2

ClinicalTrials.gov (NCT01612039) Safety, Efficacy, and Tolerability Study of ASP3291 in Patients With Active Ulcerative Colitis. U.S. National Institutes of Health.

REF 3

Clinical pipeline report, company report or official report of Drais Pharmaceuticals.

REF 4

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 5

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.

REF 6

Discovery of a beta-MSH-derived MC-4R selective agonist. J Med Chem. 2005 May 5;48(9):3095-8.

REF 7

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 8

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 9

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.

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