Target Information
| Target General Information | Top | |||||
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| Target ID |
T45457
(Former ID: TTDR00057)
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| Target Name |
Melanocortin receptor (MCR)
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| Synonyms |
Melanocortin receptor
Click to Show/Hide
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| Gene Name |
NO-GeName
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Ulcerative colitis [ICD-11: DD71] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | ASP-3291 | Drug Info | Phase 2 | Ulcerative colitis | [2] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | ASP-3291 | Drug Info | [3] | |||
| Inhibitor | [+] 31 Inhibitor drugs | + | ||||
| 1 | Ac-His-DNal(2)-Arg-Trp-NH2 | Drug Info | [4] | |||
| 2 | Ac-His-DPhe(3,4-diCl)-Arg-Trp-NH2 | Drug Info | [4] | |||
| 3 | Ac-His-DPhe(pBr)-Arg-Trp-NH2 | Drug Info | [4] | |||
| 4 | Ac-His-DPhe(pCF3)-Arg-Trp-NH2 | Drug Info | [4] | |||
| 5 | Ac-Nle-c[Asp-His-DNal(2')-Pro-Trp-Lys]-NH2 | Drug Info | [5] | |||
| 6 | Ac-YRMEHdFRWG-NH2 | Drug Info | [6] | |||
| 7 | Ac-YRMEHdFRWGSPPKD-NH2 | Drug Info | [6] | |||
| 8 | Ac-YR[CEH(d-2alpha-Nal)RWC]-NH2 | Drug Info | [6] | |||
| 9 | Ac-YR[CEH(pCl-dF)RWC]-NH2 | Drug Info | [6] | |||
| 10 | AEKKDEGPYRMEHFRWGSPPKD | Drug Info | [6] | |||
| 11 | C[CO-(CH2)2-CO-Nle-D-Phe-Arg-Trp-Lys]-NH2 | Drug Info | [7] | |||
| 12 | C[CO-(CH2)3-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 | Drug Info | [7] | |||
| 13 | C[CO-(CH2)3-CO-Pro-D-Phe-Arg-Trp-Lys]-NH2 | Drug Info | [7] | |||
| 14 | C[CO-o-C6H4-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 | Drug Info | [7] | |||
| 15 | C[Nle-Arg-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 16 | C[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 17 | C[Nle-Asp-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 18 | C[Nle-Gln-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 19 | C[Nle-Glu-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 20 | C[Nle-Glu-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 21 | C[Nle-His-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 22 | C[Nle-His-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 23 | C[Nle-Nle-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 24 | C[Nle-Nle-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 25 | C[Nle-Pro-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 26 | C[Nle-Val-D-Nal(2')-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 27 | C[Nle-Val-D-Phe-Arg-Trp-Glu]-NH2 | Drug Info | [8] | |||
| 28 | GPYRMEHFRWGSPPKD-NH2 | Drug Info | [6] | |||
| 29 | MK-10 | Drug Info | [9] | |||
| 30 | MK-11 | Drug Info | [9] | |||
| 31 | NDP-SYSMEHFRWGKPVG | Drug Info | [6] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "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 | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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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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