Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T72458 Target Info
Target Name Melanocortin receptor 4 (MC4R)
Synonyms
MC4-R
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Target Type Successful Target
Gene Name MC4R
Biochemical Class GPCR rhodopsin
UniProt ID
MC4R_HUMAN
Co-Targets of This Target  Top
Co-Target Name Opioid receptor mu (MOP) Successful Target
UniProt ID OPRM_HUMAN
Gene Name OPRM1
Synonyms
hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
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Representative Drug(s) Methylnaltrexone bromide Drug Info Ki = 5.48 nM [1]
Co-Target Name Opioid receptor delta (OPRD1) Successful Target
UniProt ID OPRD_HUMAN
Gene Name OPRD1
Synonyms
OPRD; Delta-type opioid receptor; Delta opioid receptor; DOR-1; D-OR-1
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Representative Drug(s) Methylnaltrexone bromide Drug Info Ki = 501.19 nM [2]
Co-Target Name Vasopressin V1a receptor (V1AR) Successful Target
UniProt ID V1AR_HUMAN
Gene Name AVPR1A
Synonyms
Vascular/hepatic-type arginine vasopressin receptor; V1aR; V1a vasopressin receptor; Antidiuretic hormone receptor 1a; AVPR1; AVPR V1a
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Representative Drug(s) PMX-53 Drug Info IC50 = 740 nM [3]
Co-Target Name Melanocortin receptor 1 (MC1R) Clinical trial Target
UniProt ID MSHR_HUMAN
Gene Name MC1R
Synonyms
Melanotropin receptor; Melanocyte-stimulating hormone receptor; Melanocortin-1 receptor; MSHR; MSH-R; MC1-R
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Representative Drug(s) Bremelanotide Drug Info EC50 = 0.0955 nM [4]
Co-Target Name C5a anaphylatoxin chemotactic receptor (C5AR1) Successful Target
UniProt ID C5AR1_HUMAN
Gene Name C5AR1
Synonyms
CD88; C5aR; C5a-R; C5a anaphylatoxin chemotactic receptor 1; C5R1
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Representative Drug(s) PMX-53 Drug Info IC50 = 15 nM [5]
Co-Target Name Melanocortin receptor 5 (MC5R) Clinical trial Target
UniProt ID MC5R_HUMAN
Gene Name MC5R
Synonyms
MC5-R; MC2; MC-2
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Representative Drug(s) Bremelanotide Drug Info Ki = 17 nM [6]
Co-Target Name Substance-K receptor (TACR2) Clinical trial Target
UniProt ID NK2R_HUMAN
Gene Name TACR2
Synonyms
Tachykinin receptor 2; Tachykinin neurokinin 2 receptor; TACR2; SKR; Neurokinin A receptor; NK-2R; NK-2 receptor
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Representative Drug(s) PMX-53 Drug Info IC50 = 87 nM [3]
Co-Target Name Melanocortin receptor 3 (MC3R) Literature-reported Target
UniProt ID MC3R_HUMAN
Gene Name MC3R
Synonyms
MC3-R
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Representative Drug(s) Bremelanotide Drug Info EC50 = 2.399 nM [4]
References  Top
REF 1 Discovery of naldemedine: A potent and orally available opioid receptor antagonist for treatment of opioid-induced adverse effects. Bioorg Med Chem Lett. 2019 Jan 1;29(1):73-77.
REF 2 Discovery of Axelopran (TD-1211): A Peripherally Restricted mu-Opioid Receptor Antagonist. ACS Med Chem Lett. 2019 Nov 26;10(12):1641-1647.
REF 3 Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92.
REF 4 Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1. J Med Chem. 2018 Apr 26;61(8):3674-3684.
REF 5 Selective hexapeptide agonists and antagonists for human complement C3a receptor. J Med Chem. 2010 Jul 8;53(13):4938-48.
REF 6 Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective alpha-melanocyte-stimulating hormone (alpha-MSH) analogues. J Med Chem. 2012 Mar 8;55(5):1969-77.

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