General Information of the Protein
Protein ID
PT01325
Protein Name
Melanocortin receptor 3
Gene Name
MC3R
Sequence
MNASCCLPSVQPTLPNGSEHLQAPFFSNQSSSAFCEQVFIKPEVFLSLGIVSLLENILVILAVVRNGNLHSPMYFFLCSLAVADMLVSVSNALETIMIAIVHSDYLTFEDQFIQHMDNIFDSMICISLVASICNLLAIAVDRYVTIFYALRYHSIMTVRKALTLIVAIWVCCGVCGVVFIVYSESKMVIVCLITMFFAMMLLMGTLYVHMFLFARLHVKRIAALPPADGVAPQQHSCMKGAVTITILLGVFIFCWAPFFLHLVLIITCPTNPYCICYTAHFNTYLVLIMCNSVIDPLIYAFRSLELRNTFREILCGCNGMNLG
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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)
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Melanocortin receptor
Function
Receptor for MSH (alpha, beta and gamma) and ACTH. This receptor is mediated by G proteins which activate adenylate cyclase. Required for expression of anticipatory patterns of activity and wakefulness during periods of limited nutrient availability and for the normal regulation of circadian clock activity in the brain.
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Uniprot ID
Primary ID:
P41968

Secondarily ID:
Q4KN27
Q9H517
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Ensembl ID
ENSG00000124089
HGNC ID
HGNC:6931
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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0041451
 Compound Info 
CAS_75921-69-6
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C78H111N21O19
  1
1
Ki = 0.78 nM
 Bioactivity Info 
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CP0299138
 Compound Info 
(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 = 2 nM
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CP0493731
 Compound Info 
(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 = 2.5 nM
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CP0061830
 Compound Info 
(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 = 8 nM
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CP0304263
 Compound Info 
(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 = 8.2 nM
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CP0335401
 Compound Info 
(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 = 11 nM
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CP0506416
 Compound Info 
(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 = 13 nM
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CP0357038
 Compound Info 
(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 = 22 nM
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CP0339846
 Compound Info 
(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 = 27 nM
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CP0299139
 Compound Info 
(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 = 42 nM
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CP0061829
 Compound Info 
(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 = 45 nM
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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
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C77H109N21O19S
  1
1
Ki = 46 nM
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CP0455645
 Compound Info 
BREMELANOTIDE
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C50H68N14O10
  1
1
Ki = 53 nM
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CP0139298
 Compound Info 
(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 = 67 nM
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CP0061831
 Compound Info 
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 = 71 nM
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CP0317619
 Compound Info 
(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 = 121 nM
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CP0314387
 Compound Info 
(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 = 450 nM
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CP0306904
 Compound Info 
(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 = 1100 nM
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CP0339847
 Compound Info 
(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 = 1600 nM
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Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000154 , HEK293-EBNA1-6E
 Cell Line Info 
Cell Line ID: CL000309 , NCTC clone 929
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Cell Line ID: CL000058 , T-REx-293
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0041451
 Compound Info 
CAS_75921-69-6
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C78H111N21O19
  5
1 EC50 = 0.13 nM
2 IC50 = 1.17 nM
3 IC50 = 3.3 nM
4 IC50 = 3.8 nM
5 Ki = 0.68 nM
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
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C50H69N15O9
  2
1 EC50 = 0.27 nM
2 IC50 = 8.56 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
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C77H109N21O19S
  3
1 EC50 = 0.67 nM
2 IC50 = 30 nM
3 IC50 = 50.4 nM
CP0050965
 Compound Info 
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
  3
1 IC50 = 0.23 nM
2 Kd = 1.995 nM
3 Kd = 5.012 nM
CP0135281
 Compound Info 
(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 = 25.5 nM
CP0082819
 Compound Info 
(3R,6S,9R,12S,15R,18R,26R)-18-Acetylamino-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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C47H63N15O9
  1
1 IC50 = 102 nM
CP0714126
 Compound Info 
(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 = 137 nM
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 IC50 = 482.7 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 = 1050 nM
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 IC50 = 1492 nM
CP0135404
 Compound Info 
(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 = 2400 nM
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 = 2951 nM
CP0161427
 Compound Info 
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 = 2958 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
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C34H43N11O5
  1
1 IC50 > 10000 nM
CP0726156
 Compound Info 
H-Tyr-Val-Nle-Gly-Pro-D-Nal(2')-Arg-Trp-Asp-Arg-Phe-Gly-NH2
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C78H104N20O15
  1
1 Ki = 0.2 nM
CP0674615
 Compound Info 
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 = 0.81 nM
CP0084312
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-3-(3H-imidazol-4-yl)-2-(4-phenyl-butyrylamino)-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C42H51N11O5
  1
1 Ki = 13.5 nM
CP0182893
 Compound Info 
(S)-2-{(S)-2-[(S)-2-[2-(4-Chloro-phenyl)-acetylamino]-3-(3H-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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C40H46ClN11O5
  1
1 Ki = 20 nM
CP0040024
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-3-(3H-imidazol-4-yl)-2-(3-phenyl-propionylamino)-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C41H49N11O5
  1
1 Ki = 65 nM
CP0228189
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-3-(3H-imidazol-4-yl)-2-phenylacetylamino-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C40H47N11O5
  1
1 Ki = 66.5 nM
CP0047872
 Compound Info 
(S)-2-{(S)-2-[(S)-2-[2-(4-Chloro-phenoxy)-acetylamino]-3-(3H-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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C40H46ClN11O6
  1
1 Ki = 110 nM
CP0217814
 Compound Info 
(S)-2-{(S)-2-[(S)-2-(2,2-Dimethyl-propionylamino)-3-(3H-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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C37H49N11O5
  1
1 Ki = 130 nM
CP0133486
 Compound Info 
(D)-(S)-5-Guanidino-2-{(S)-2-[(S)-2-(2-hydroxy-3-phenyl-propionylamino)-3-(3H-imidazol-4-yl)-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C41H49N11O6
  1
1 Ki = 140 nM
CP0257564
 Compound Info 
N'-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]oxamide
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C34H42N12O6
  1
1 Ki = 160 nM
CP0228609
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-3-(3H-imidazol-4-yl)-2-pentanoylamino-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C37H49N11O5
  1
1 Ki = 170 nM
CP0182921
 Compound Info 
N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]cyclopropanecarboxamide
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C36H45N11O5
  1
1 Ki = 210 nM
CP0049442
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-3-(3H-imidazol-4-yl)-2-(2-methylsulfanyl-acetylamino)-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C35H45N11O5S
  1
1 Ki = 230 nM
CP0058986
 Compound Info 
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 = 230 nM
CP0101637
 Compound Info 
N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]benzamide
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C39H45N11O5
  1
1 Ki = 260 nM
CP0136197
 Compound Info 
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 = 270 nM
CP0336462
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-3-(3H-imidazol-4-yl)-2-isobutyrylamino-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C36H47N11O5
  1
1 Ki = 280 nM
CP0100500
 Compound Info 
(S)-2-{(S)-2-[(S)-2-(2-Cyano-acetylamino)-3-(3H-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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C35H42N12O5
  1
1 Ki = 350 nM
CP0182484
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-3-(3H-imidazol-4-yl)-2-(2-methoxy-acetylamino)-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C35H45N11O6
  1
1 Ki = 380 nM
CP0058988
 Compound Info 
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 = 420 nM
CP0050698
 Compound Info 
(S)-2-{(S)-2-[(S)-2-(4-Chloro-benzenesulfonylamino)-3-(3H-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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C38H44ClN11O6S
  1
1 Ki = 440 nM
CP0178413
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-2-(4-hydroxy-butyrylamino)-3-(3H-imidazol-4-yl)-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C36H47N11O6
  1
1 Ki = 440 nM
CP0081762
 Compound Info 
(S)-2-((S)-4-((R)-2-amino-3-(4-fluorophenyl)propanoyl)-3-(2-guanidinoethyl)-2-oxopiperazin-1-yl)-N-methyl-3-(naphthalen-2-yl)propanamide
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C30H36FN7O3
  1
1 Ki = 470 nM
CP0089083
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-3-(3H-imidazol-4-yl)-2-propionylamino-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C35H45N11O5
  1
1 Ki = 540 nM
CP0204764
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-3-(3H-imidazol-4-yl)-2-(3,3,3-trifluoro-propionylamino)-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C35H42F3N11O5
  1
1 Ki = 540 nM
CP0049389
 Compound Info 
(S)-2-{(S)-2-[(S)-2-Butyrylamino-3-(3H-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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C36H47N11O5
  1
1 Ki = 580 nM
CP0190200
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-2-(2-hydroxy-acetylamino)-3-(3H-imidazol-4-yl)-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C34H43N11O6
  1
1 Ki = 630 nM
CP0099822
 Compound Info 
CAS_72711-43-4
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C74H99N21O16S
  1
1 Ki = 690 nM
CP0296428
 Compound Info 
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 = 710 nM
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
  2
1 Ki = 736 nM
2 Ki = 4500 nM
CP0197235
 Compound Info 
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 = 750 nM
CP0308897
 Compound Info 
(S)-2-{(S)-2-[(S)-2-acetylamino-3-(3H-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 Ki = 770 nM
CP0135976
 Compound Info 
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 = 820 nM
CP0048619
 Compound Info 
2-{(S)-2-[(S)-2-Amino-3-(3H-imidazol-4-yl)-propionylamino]-1-oxo-3-phenyl-propylamino}-5-guanidino-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C32H41N11O4
  1
1 Ki = 890 nM
CP0044734
 Compound Info 
(S)-2-{(R)-2-[(S)-2-acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-phenyl-propionylamino}-5-guanidino-pentanoic acid ((S)-1-methylcarbamoyl-2-naphthalen-2-yl-ethyl)-amide
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C37H46N10O5
  1
1 Ki = 1195 nM
CP0034706
 Compound Info 
(S)-2-{(R)-2-[(S)-2-acetylamino-3-(4-hydroxy-phenyl)-propionylamino]-3-phenyl-propionylamino}-5-guanidino-pentanoic acid ((S)-1-methylcarbamoyl-2-naphthalen-2-yl-ethyl)-amide
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C40H48N8O6
  1
1 Ki = 1727 nM
CP0184237
 Compound Info 
(S)-5-Guanidino-2-{(S)-2-[(S)-3-(3H-imidazol-4-yl)-2-methanesulfonylamino-propionylamino]-3-phenyl-propionylamino}-pentanoic acid [(S)-1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide
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C33H43N11O6S
  1
1 Ki = 1900 nM
CP0081758
 Compound Info 
(S)-2-((S)-4-((R)-2-amino-3-(4-fluorophenyl)propanoyl)-3-(2-aminoethyl)-2-oxopiperazin-1-yl)-N-methyl-3-(naphthalen-2-yl)propanamide
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C29H34FN5O3
  1
1 Ki = 4122 nM
CP0135132
 Compound Info 
(2S)-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)-N-[(2S)-1-(methylamino)-3-naphthalen-2-yl-1-oxopropan-2-yl]pentanamide
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C29H37N7O3
  1
1 Ki = 22562 nM
Clinical Information about the Protein
Target 1 ( Melanocortin receptor 3 (MC3R) )
Target Type Literature-reported 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
 Drug Info 
Investigative
Female sexual arousal dysfunction
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT05047 Melanocortin receptor 3 Rattus norvegicus, Rat
 Protein Info 
50% Identity
Protein ID Protein Name Protein Organism
PT01528 Melanocortin receptor 5 Mus musculus, Mouse
 Protein Info 
PT07463 Melanocortin receptor 5 Rattus norvegicus, Rat
 Protein Info