General Information of the Protein
Protein ID
PT04007
Protein Name
Melanocortin receptor 4
Gene Name
MC4R
Sequence
MNSTHHHGMYTSLHLWNRSSHGLHGNASESLGKGHSDGGCYEQLFVSPEVFVTLGVISLLENILVIVAIAKNKNLHSPMYFFICSLAVADMLVSVSNGSETIVITLLNSTDTDAQSFTVNIDNVIDSVICSSLLASICSLLSIAVDRYFTIFYALQYHNIMTVRRVGIIISCIWAACTVSGVLFIIYSDSSAVIICLITMFFTMLVLMASLYVHMFLMARLHIKRIAVLPGTGTIRQGANMKGAITLTILIGVFVVCWAPFFLHLLFYISCPQNPYCVCFMSHFNLYLILIMCNAVIDPLIYALRSQELRKTFKEIICFYPLGGICELPGRY
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Organism
Rattus norvegicus, Rat
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).
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Uniprot ID
P70596
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
CP0083436
 Compound Info 
N-[(1S)-1-[2-[1-[(3S,4R)-4-(4-bromo-2-fluorophenyl)-1-tert-butylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
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C31H40BrClFN3O2
  1
1
EC50 = 0.5 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0202447
 Compound Info 
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-(4-chloro-2-fluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
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C31H40Cl2FN3O2
  1
1
EC50 = 0.9 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
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
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C33H38ClF2N3O3
  1
1
EC50 = 1.1 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0162604
 Compound Info 
N-[(1S)-1-[2-[1-[(3R,4S)-4-(4-bromo-2-fluorophenyl)-1-tert-butylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
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C31H40BrClFN3O2
  1
1
EC50 = 10.3 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0149367
 Compound Info 
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-amide
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C33H41ClN6O2
  1
1
IC50 = 0.6 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
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C34H51FN4O3
  1
1
IC50 = 3000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0162604
 Compound Info 
N-[(1S)-1-[2-[1-[(3R,4S)-4-(4-bromo-2-fluorophenyl)-1-tert-butylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
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C31H40BrClFN3O2
  1
1 IC50 = 1.5 nM
CP0083436
 Compound Info 
N-[(1S)-1-[2-[1-[(3S,4R)-4-(4-bromo-2-fluorophenyl)-1-tert-butylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
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C31H40BrClFN3O2
  1
1 IC50 = 1.7 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01431 Melanocortin receptor 4 Mus musculus, Mouse
 Protein Info