General Information of the Protein
Protein ID
PT01804
Protein Name
Melanocortin receptor 5
Secondarily
Protein Name
MC-2
Gene Name
MC5R
Sequence
MNSSFHLHFLDLNLNATEGNLSGPNVKNKSSPCEDMGIAVEVFLTLGVISLLENILVIGAIVKNKNLHSPMYFFVCSLAVADMLVSMSSAWETITIYLLNNKHLVIADAFVRHIDNVFDSMICISVVASMCSLLAIAVDRYVTIFYALRYHHIMTARRSGAIIAGIWAFCTGCGIVFILYSESTYVILCLISMFFAMLFLLVSLYIHMFLLARTHVKRIAALPGASSARQRTSMQGAVTVTMLLGVFTVCWAPFFLHLTLMLSCPQNLYCSRFMSHFNMYLILIMCNSVMDPLIYAFRSQEMRKTFKEIICCRGFRIACSFPRRD
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Organism
Homo sapiens, Human
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 for MSH (alpha, beta and gamma) and ACTH. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. This receptor is a possible mediator of the immunomodulation properties of melanocortins.
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Uniprot ID
Primary ID:
P33032

Secondarily ID:
B0YJ34
Q502V1
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Ensembl ID
ENSG00000176136
HGNC ID
HGNC:6933
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: CL000404 , BHK570
Compound ID Compound Name Compound Formula
CP0299138
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-12-carbamoyl-18-[3-(diaminomethylideneamino)propyl]-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-6-(diaminomethylideneamino)-1-oxohexan-2-yl]-2-[[(2S)-2-[[2-(hexadecanoylamino)acetyl]amino]-3-hydroxypropanoyl]amino]pentanediamide
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C84H134N22O18
 1
1
Ki = 0.47 nM
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CP0041451
CAS_75921-69-6
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C78H111N21O19
 1
1
Ki = 0.48 nM
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CP0304263
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-12-carbamoyl-18-[3-(diaminomethylideneamino)propyl]-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-2-[[(2S)-2-[[2-[4-(hexadecanoylsulfamoyl)butanoylamino]acetyl]amino]-3-hydroxypropanoyl]amino]pentanediamide
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C87H134N22O21S
 1
1
Ki = 1.2 nM
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CP0493731
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-12-carbamoyl-18-[3-(diaminomethylideneamino)propyl]-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-2-[[(2S)-2-[[2-(hexadecanoylamino)acetyl]amino]-3-hydroxypropanoyl]amino]pentanediamide
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C83H127N21O18
 1
1
Ki = 1.6 nM
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CP0335401
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-18-(3-carbamimidamidopropyl)-12-carbamoyl-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-3-(dimethylamino)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]-2-[[(2S)-3-hydroxy-2-[[2-[[2-[2-[2-[16-(1H-tetrazol-5-yl)hexadecanoylamino]ethoxy]ethoxy]acetyl]amino]acetyl]amino]propanoyl]amino]pentanediamide
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C92H143N27O20
 1
1
Ki = 2.9 nM
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CP0061830
(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-18-[3-(diaminomethylideneamino)propyl]-3-[[(2S)-2-[[2-[[2-[[2-[[2-[[2-(hexadecanoylamino)acetyl]amino]acetyl]amino]acetyl]amino]acetyl]amino]acetyl]amino]hexanoyl]amino]-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosane-12-carboxamide
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C74H114N18O15
 1
1
Ki = 3 nM
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CP0339846
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-18-(3-carbamimidamidopropyl)-12-carbamoyl-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]-2-[[(2S)-3-hydroxy-2-[[2-[[2-[2-[2-[16-(1H-tetrazol-5-yl)hexadecanoylamino]ethoxy]ethoxy]acetyl]amino]acetyl]amino]propanoyl]amino]pentanediamide
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C93H145N29O20
 1
1
Ki = 3 nM
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CP0506416
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-12-carbamoyl-18-[3-(diaminomethylideneamino)propyl]-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-(propan-2-ylamino)propan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-2-[[(2S)-3-hydroxy-2-[[2-[[2-[2-[2-[16-(1H-tetrazol-5-yl)hexadecanoylamino]ethoxy]ethoxy]acetyl]amino]acetyl]amino]propanoyl]amino]pentanediamide
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C93H145N27O20
 1
1
Ki = 3.4 nM
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CP0357038
(2S)-2-[[(2S)-2-[(2-acetamidoacetyl)amino]-3-hydroxypropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-12-carbamoyl-18-[3-(diaminomethylideneamino)propyl]-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-6-(diaminomethylideneamino)-1-oxohexan-2-yl]pentanediamide
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C70H106N22O18
 1
1
Ki = 4.3 nM
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CP0061829
(2S)-2-[[(2S)-2-[(2-acetamidoacetyl)amino]-3-hydroxypropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-12-carbamoyl-18-[3-(diaminomethylideneamino)propyl]-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]pentanediamide
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C69H99N21O18
 1
1
Ki = 5.1 nM
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CP0299139
(2S)-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-12-carbamoyl-18-[3-(diaminomethylideneamino)propyl]-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-2-[[(2S)-3-hydroxy-2-[[2-[[2-[2-[2-[16-(1H-tetrazol-5-yl)hexadecanoylamino]ethoxy]ethoxy]acetyl]amino]acetyl]amino]propanoyl]amino]pentanediamide
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C90H139N27O20
 1
1
Ki = 10 nM
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CP0061831
2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-3-hydroxy-2-[[2-[[2-[2-[2-[16-(1H-tetrazol-5-yl)hexadecanoylamino]ethoxy]ethoxy]acetyl]amino]acetyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-12-carbamoyl-18-[3-(diaminomethylideneamino)propyl]-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-3-oxopropyl]amino]-2-oxoethyl]-(carboxymethyl)amino]acetic acid
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C96H146N28O25
 1
1
Ki = 13 nM
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CP0139298
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-12-carbamoyl-18-[3-(diaminomethylideneamino)propyl]-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-2-[[(2S)-3-hydroxy-2-[[2-[[2-[2-[2-[16-(1H-tetrazol-5-yl)hexadecanoylamino]ethoxy]ethoxy]acetyl]amino]acetyl]amino]propanoyl]amino]pentanediamide
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C90H138N26O21
 1
1
Ki = 15 nM
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CP0455645
BREMELANOTIDE
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C50H68N14O10
 1
1
Ki = 17 nM
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CP0317619
(2S)-N-[(2S)-1-[[(2S)-2-amino-3-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-18-(3-carbamimidamidopropyl)-12-carbamoyl-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-3-oxopropyl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]-2-[[(2S)-3-hydroxy-2-[[2-[[2-[2-[2-[16-(1H-tetrazol-5-yl)hexadecanoylamino]ethoxy]ethoxy]acetyl]amino]acetyl]amino]propanoyl]amino]pentanediamide
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C90H139N27O20
 1
1
Ki = 40 nM
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CP0314387
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-18-(3-carbamimidamidopropyl)-12-carbamoyl-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-oxo-4-[[2-[[2-[2-[2-[16-(1H-tetrazol-5-yl)hexadecanoylamino]ethoxy]ethoxy]acetyl]amino]acetyl]amino]pentanoic acid
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C94H141N25O24
 1
1
Ki = 110 nM
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CP0045108
(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
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C77H109N21O19S
 1
1
Ki = 150 nM
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CP0306904
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-18-(3-carbamimidamidopropyl)-12-carbamoyl-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-oxo-4-[[2-[[2-[2-[2-[16-(1H-tetrazol-5-yl)hexadecanoylamino]ethoxy]ethoxy]acetyl]amino]acetyl]amino]pentanoic acid
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C94H146N26O24
 1
1
Ki = 270 nM
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CP0339847
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S,12S,15S,18S,21R,24S,26R)-21-benzyl-12-carbamoyl-18-[3-(diaminomethylideneamino)propyl]-26-hydroxy-15-(1H-indol-3-ylmethyl)-2,6,14,17,20,23-hexaoxo-1,7,13,16,19,22-hexazabicyclo[22.3.0]heptacosan-3-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-oxo-4-[[2-[[2-[2-[2-[16-(1H-tetrazol-5-yl)hexadecanoylamino]ethoxy]ethoxy]acetyl]amino]acetyl]amino]pentanoic acid
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C93H141N23O26
 1
1
Ki = 710 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0050965
21-(2-Acetylamino-hexanoylamino)-7-[3-(diaminomethaniminium)-propyl]-10-(1H-indol-3-ylmethyl)-4-naphthalen-2-ylmethyl-2,5,8,11,19,22-hexaoxo-3,6,9,12,18,23-hexaaza-tricyclo[21.7.0.0*24,29*]triaconta-24(29),25,27
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C54H71N15O9
 2
1 EC50 = 0.12 nM
2 IC50 = 0.09 nM
CP0041451
CAS_75921-69-6
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C78H111N21O19
 2
1 IC50 = 0.86 nM
2 IC50 = 2.2 nM
CP0045108
(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
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C77H109N21O19S
 2
1 IC50 = 18 nM
2 IC50 = 557 nM
CP0135281
(3S,6S,9S,12R,15S,18S,26S)-18-[[(2S)-2-acetamidohexanoyl]amino]-12-benzyl-9-[3-(diaminomethylideneamino)propyl]-15-(1H-imidazol-5-ylmethyl)-6-(1H-indol-3-ylmethyl)-3-methyl-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,21-heptazacyclohexacosane-26-carboxamide
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C53H74N16O10
 1
1 IC50 = 24.8 nM
CP0091326
(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
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C50H69N15O9
 1
1 IC50 = 43.6 nM
CP0083436
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 = 65.3 nM
CP0290684
4-[((R)-N-Cyclohexyl-3-methyl-piperazine-1-carboximidoyl)-amino]-N-[2-(2,4-dichloro-phenyl)-ethyl]-benzamide
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C27H35Cl2N5O
 1
1 IC50 = 70 nM
CP0102543
4-[(N-Cyclohexyl-3,5-dimethyl-piperazine-1-carboximidoyl)-amino]-N-[2-(2,4-dichloro-phenyl)-ethyl]-benzamide
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C28H37Cl2N5O
 1
1 IC50 = 80 nM
CP0202447
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 IC50 = 129.4 nM
CP0714126
(3S,6S,9S,12S,15S,18S,26S)-18-((S)-2-Acetylamino-hexanoylamino)-12-benzyl-9-(3-guanidino-propyl)-15-(3H-imidazol-4-ylmethyl)-6-(1H-indol-3-ylmethyl)-3-methyl-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,21heptaaza-cyclohexacosane-26-carboxylic acid amide
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C53H74N16O10
 1
1 IC50 = 141 nM
CP0161427
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-(2-fluoro-4-methoxyphenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
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C32H43ClFN3O3
 1
1 IC50 = 205 nM
CP0083437
N-[(1S)-1-[2-[1-[(3R,4S)-1-tert-butyl-4-(2,4-dichlorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
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C31H40Cl3N3O2
 1
1 IC50 = 245.4 nM
CP0162604
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 = 280.3 nM
CP0077679
4-[((S)-N-Cyclohexyl-3-methyl-piperazine-1-carboximidoyl)-amino]-N-[2-(2,4-dichloro-phenyl)-ethyl]-benzamide
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C27H35Cl2N5O
 1
1 IC50 = 380 nM
CP0149427
4-[((S)-N-(R)-Cyclohexyl-2,5-dimethyl-piperazine-1-carboximidoyl)-amino]-N-[2-(2,4-dichloro-phenyl)-ethyl]-benzamide
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C28H37Cl2N5O
 1
1 IC50 = 380 nM
CP0052754
4-[(N-Cyclohexyl-piperazine-1-carboximidoyl)-amino]-N-[2-(2,4-dichloro-phenyl)-ethyl]-benzamide
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C26H33Cl2N5O
 1
1 IC50 = 460 nM
CP0210565
4-[N''-(2-Amino-2-methyl-propyl)-N''''-cyclohexyl-guanidino]-N-[2-(2,4-dichloro-phenyl)-ethyl]-benzamide
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C26H35Cl2N5O
 1
1 IC50 = 530 nM
CP0278410
4-(N''-Cyclohexyl-N''''-pyrrolidin-3-yl-guanidino)-N-[2-(2,4-dichloro-phenyl)-ethyl]-benzamide
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C26H33Cl2N5O
 1
1 IC50 = 530 nM
CP0277007
4-[(N-Cyclohexyl-3-methylamino-pyrrolidine-1-carboximidoyl)-amino]-N-[2-(2,4-dichloro-phenyl)-ethyl]-benzamide
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C27H35Cl2N5O
 1
1 IC50 = 630 nM
CP0156912
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-naphthalen-2-ylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
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C35H44ClN3O2
 1
1 IC50 = 675 nM
CP0045745
(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
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C34H43N11O5
 1
1 IC50 > 10000 nM
CP0058748
15-(2-Acetylamino-hexanoylamino)-6-(3-guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid amide
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C54H71N15O9
 1
1 Ki = 0.09 nM
CP0291923
3-[25-Acetylamino-4-carbamoyl-13-(3-guanidino-propyl)-19-(3H-imidazol-4-ylmethyl)-10-(1H-indol-3-ylmethyl)-16-naphthalen-2-ylmethyl-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptaaza-cyclohexacos-22-yl]-propionic acid
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C51H63N15O11S2
 1
1 Ki = 0.39 nM
CP0674615
H-Tyr-Val-Nle-Gly-His-D-Nal(2)-Arg-D-Trp-Asp-Arg-Phe-Gly-NH2
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C79H104N22O15
 1
1 Ki = 1 nM
CP0274905
15-Acetylamino-6-(3-guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid
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C48H60N14O8
 1
1 Ki = 4.3 nM
CP0726156
H-Tyr-Val-Nle-Gly-Pro-D-Nal(2')-Arg-Trp-Asp-Arg-Phe-Gly-NH2
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C78H104N20O15
 1
1 Ki = 14 nM
CP0685081
Cyclo Ac-Cys-Glu-His-D-(2')Nal-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2
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C70H93N19O16S2
 1
1 Ki = 16 nM
CP0201251
15-Amino-6-(3-guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid
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C46H58N14O7
 1
1 Ki = 18 nM
CP0061104
12-(2-Acetylamino-hexanoylamino)-6-(3-guanidino-propyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14-pentaoxo-1,4,7,10,15pentaaza-cycloicosane-20-carboxylic acid
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C48H64N12O8
 1
1 Ki = 20 nM
CP0793638
Cyclo Ac-Cys-Glu-His-D-Phe-(3,4-di-Cl)-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2
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C66H89Cl2N19O16S2
 1
1 Ki = 22 nM
CP0047335
12-Amino-6-(3-guanidino-propyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14-pentaoxo-1,4,7,10,15pentaaza-cycloicosane-20-carboxylic acid
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C40H51N11O6
 1
1 Ki = 24 nM
CP0281018
(3R,6S,9R,12S,15S,23R)-15-((S)-2-Acetylamino-hexanoylamino)-6-(3-guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid amide
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C54H71N15O9
 1
1 Ki = 26 nM
CP0137537
16-(2-Acetylamino-hexanoylamino)-6-(3-guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid
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C54H71N15O9
 1
1 Ki = 28 nM
CP0110629
9-(3-Guanidino-propyl)-15-(3H-imidazol-4-ylmethyl)-6-(1H-indol-3-ylmethyl)-12-naphthalen-2-ylmethyl-5,8,11,14,17,20-hexaoxo-1,4,7,10,13,16hexaaza-cycloicosane-3-carboxylic acid
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C43H51N13O7
 1
1 Ki = 65 nM
CP0167616
5-(3-Guanidino-propyl)-8-(1H-indol-3-ylmethyl)-2-naphthalen-2-ylmethyl-3,6,9,16,19-pentaoxo-1,4,7,10,15pentaaza-cyclononadecane-11-carboxylic acid
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C39H48N10O6
 1
1 Ki = 130 nM
CP0168805
6-(3-Guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid
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C46H57N13O7
 1
1 Ki = 150 nM
CP0058986
1-{2-[(1S)-(methylaminoacetamido)-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(2-fluoro-4-chlorophenyl)propionyl]piperazine
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C28H38ClFN4O2
 1
1 Ki = 180 nM
CP0136197
1-{2-[(1S)-(aminopropionyl)amino-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
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C28H39ClN4O2
 1
1 Ki = 320 nM
CP0058988
1-{2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
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C30H43ClN4O2
 1
1 Ki = 340 nM
CP0296428
1-{2-[(1S)-(methylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
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C29H41ClN4O2
 1
1 Ki = 360 nM
CP0135976
N-[(1S)-1-[2-[4-[(2R)-3-(2,4-dichlorophenyl)-2-(2-oxopyrrolidin-1-yl)propanoyl]piperazin-1-yl]-5-methylphenyl]-3-methylbutyl]-3-(dimethylamino)propanamide
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C34H47Cl2N5O3
 1
1 Ki = 520 nM
CP0129840
6-(3-Guanidino-propyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14-pentaoxo-1,4,7,10,15pentaaza-cycloicosane-20-carboxylic acid
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C40H51N11O6
 1
1 Ki = 540 nM
CP0039210
12-Acetylamino-6-(3-guanidino-propyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14-pentaoxo-1,4,7,10,15pentaaza-cycloicosane-20-carboxylic acid
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C42H53N11O7
 1
1 Ki = 720 nM
CP0197235
1-((R)-1-(4-(2-((S)-1-(2-aminoethylamino)-3-methylbutyl)-6-fluorophenyl)piperazin-1-yl)-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl)pyrrolidin-2-one
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C30H40Cl2FN5O2
 1
1 Ki = 850 nM
CP0099822
CAS_72711-43-4
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C74H99N21O16S
 1
1 Ki = 2100 nM
CP0039213
8-(3-Guanidino-propyl)-2-(3H-imidazol-4-ylmethyl)-11-(1H-indol-3-ylmethyl)-5-naphthalen-2-ylmethyl-3,6,9,12,17-pentaoxo-1,4,7,10,13pentaaza-cyclooctadecane-14-carboxylic acid amide
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C42H50N12O6
 1
1 Ki = 2400 nM
CP0201349
9-(3-Guanidino-propyl)-6-(1H-indol-3-ylmethyl)-12-naphthalen-2-ylmethyl-5,8,11,14,17-pentaoxo-1,4,7,10,13pentaaza-cycloheptadecane-3-carboxylic acid
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C37H44N10O6
 1
1 Ki = 4800 nM
CP0149367
(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 Ki = 5000 nM
Clinical Information about the Protein
Target 1 ( Melanocortin receptor 5 (MC5R) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Female sexual arousal dysfunction [ICD-11: HA01.1]
Investigative Drug(s) 1 Investigative Drug  1
1 MT-II Investigative
Female sexual arousal dysfunction
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02450 Melanocortin receptor 3 Mus musculus, Mouse