Protein Information

General Information of the Protein

Protein ID	PT01431
Protein Name	Melanocortin receptor 4
Gene Name	MC4R
Sequence	MNSTHHHGMYTSLHLWNRSSYGLHGNASESLGKGHPDGGCYEQLFVSPEVFVTLGVISLLENILVIVAIAKNKNLHSPMYFFICSLAVADMLVSVSNGSETIVITLLNSTDTDAQSFTVNIDNVIDSVICSSLLASICSLLSIAVDRYFTIFYALQYHNIMTVRRVGIIISCIWAACTVSGVLFIIYSDSSAVIICLISMFFTMLVLMASLYVHMFLMARLHIKRIAVLPGTGTIRQGTNMKGAITLTILIGVFVVCWAPFFLHLLFYISCPQNPYCVCFMSHFNLYLILIMCNAVIDPLIYALRSQELRKTFKEIICFYPLGGICELSSRY Show/Hide
Organism	Mus musculus, Mouse
Protein Classification	Membrane receptor > Family A G protein-coupled receptor > Peptide receptor (family A GPCR) > Short peptide receptor (family A GPCR) > Melanocortin receptor
Function	Receptor specific to the heptapeptide core common to adrenocorticotropic hormone and alpha-, beta-, and gamma-MSH. Plays a central role in energy homeostasis and somatic growth. This receptor is mediated by G proteins that stimulate adenylate cyclase (cAMP). Show/Hide
Uniprot ID	Primary ID: P56450 Secondarily ID: Q49NR4 Q9EQM7 Show/Hide
Ensembl ID	ENSG00000166603
Subcellular Location	Cell membrane

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000011 , CHO

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0283823 Compound Info	2-((S)-6-chloro-1'-((3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidine-3-carbonyl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile Show/Hide	C33H38ClF2N3O3	1
1	EC50 = 3.4 nM Bioactivity Info	TI LI LO TS
CP0377912 Compound Info	(1R,4S,6R)-2-Methyl-2-aza-bicyclo[2.2.2]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide Show/Hide	C34H51FN4O3	1
1	IC50 = 3000 nM Bioactivity Info	TI LI LO TS

Cell Line Info

Cell Line Info

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0091326 Compound Info	(3S,6S,9R,12S,15S,23S)-15-((S)-2-acetylamino-hexanoylamino)-9-benzyl-6-(3-guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid amide Show/Hide	C50H69N15O9	1
1	EC50 = 0.053 nM
CP0041451 Compound Info	CAS_75921-69-6 Show/Hide	C78H111N21O19	3
1	EC50 = 0.16 nM
2	EC50 = 0.21 nM
3	IC50 = 4.22 nM
CP0045108 Compound Info	(4S)-4-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(2S)-6-amino-1-[(2S)-2-{[(1S)-1-carbamoyl-2-methylpropyl]carbamoyl}pyrrolidin-1-yl]-1-oxohexan-2-yl]carbamoyl}methyl)carbamoyl]-2-(1H-indol-3-yl)ethyl]carbamoyl}-4-carbamimidamidobutyl]carbamoyl}-2-phenylethyl]carbamoyl}-2-(1H-imidazol-5-yl)ethyl]carbamoyl}-4-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-acetamido-3-hydroxypropanamido]-3-(4-hydroxyphenyl)propanamido]-3-hydroxypropanamido]-4-(methylsulfanyl)butanamido]butanoic acid Show/Hide	C77H109N21O19S	2
1	EC50 = 1.93 nM
2	EC50 = 5.37 nM
CP0045745 Compound Info	(S)-2-{(R)-2-[(S)-2-Acetylamino-3-(1H-imidazol-4-yl)-propionylamino]-3-phenyl-propionylamino}-5-guanidino-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide Show/Hide	C34H43N11O5	1
1	EC50 = 17.2 nM
CP0298526 Compound Info	3-{2-[1-[1-[1-acetyl-(5S)-dihydro-1H-5-pyrrolylcarboxamido]-2-phenyl-(1R)-ethylcarboxamido]-4-amino(imino)methylamino-(1S)-butylcarboxamido]-2-carbamoylethyl}-1H-indole Show/Hide	C33H43N9O5	1
1	EC50 = 1500 nM

Similar Protein(s) and Bioactivity Statistics

90% Identity

Protein ID	Protein Name	Protein Organism
PT04007	Melanocortin receptor 4	Rattus norvegicus, Rat	Protein Info