General Information of the Protein
Protein ID
PT00911
Protein Name
Melanocyte-stimulating hormone receptor
Secondarily
Protein Name
Melanocortin receptor 1
Gene Name
MC1R
Secondarily
Gene Name
MSHR
Sequence
MAVQGSQRRLLGSLNSTPTAIPQLGLAANQTGARCLEVSISDGLFLSLGLVSLVENALVVATIAKNRNLHSPMYCFICCLALSDLLVSGSNVLETAVILLLEAGALVARAAVLQQLDNVIDVITCSSMLSSLCFLGAIAVDRYISIFYALRYHSIVTLPRARRAVAAIWVASVVFSTLFIAYYDHVAVLLCLVVFFLAMLVLMAVLYVHMLARACQHAQGIARLHKRQRPVHQGFGLKGAVTLTILLGIFFLCWGPFFLHLTLIVLCPEHPTCGCIFKNFNLFLALIICNAIIDPLIYAFHSQELRRTLKEVLTCSW
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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 (PubMed:1325670, PubMed:8463333, PubMed:1516719, PubMed:11442765, PubMed:11707265). The activity of this receptor is mediated by G proteins which activate adenylate cyclase (PubMed:1325670, PubMed:11707265, PubMed:16463023, PubMed:19737927). Mediates melanogenesis, the production of eumelanin (black/brown) and phaeomelanin (red/yellow), via regulation of cAMP signaling in melanocytes (PubMed:31097585).
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Uniprot ID
Primary ID:
Q01726

Secondarily ID:
Q66K38
Q6UR93
Q8WWX6
Q8WWX7
Q96I33
Q96RU4
Q9UBF7
Q9UN58
Q9UN59
Q9UN60
Q9UN61
Q9UN62
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HGNC ID
HGNC:6929
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: CL000045 , A-375
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0388945
 Compound Info 
(3S,6S,9R,12S,15S,23S)-15-[[(2R)-2-acetamidohexanoyl]amino]-6-[3-(diaminomethylideneamino)propyl]-12-(1H-imidazol-5-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-(naphthalen-2-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxamide
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C54H71N15O9
  2
1
EC50 = 3.3 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0382074
 Compound Info 
(3S,6S,9R,12S,15S,23S)-15-[[(2R)-2-acetamidohexanoyl]amino]-6-[3-(diaminomethylideneamino)propyl]-12-(1H-imidazol-5-ylmethyl)-3-(1H-indol-3-ylmethyl)-1,4,7,13-tetramethyl-9-(naphthalen-2-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxamide
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C58H79N15O9
  2
1
EC50 = 20 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 8.7 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0382073
 Compound Info 
(3S,6S,9R,12S,15S,23S)-15-[[(2R)-2-acetamidohexanoyl]amino]-6-[3-(diaminomethylideneamino)propyl]-12-(1H-imidazol-5-ylmethyl)-3-(1H-indol-3-ylmethyl)-7,13-dimethyl-9-(naphthalen-2-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxamide
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C56H75N15O9
  2
1
EC50 = 22 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 14.8 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
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 = 110 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 6.7 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000404 , BHK570
 Cell Line Info 
Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Cell Line ID: CL000680 , HBL
 Cell Line Info 
Cell Line ID: CL000067 , HCT 116
 Cell Line Info 
Cell Line ID: CL000025 , HEK-293T
 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: CL000099 , SaOS-2
 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
  3
1 EC50 = 0.023 nM
2 IC50 = 0.51 nM
3 Ki = 0.5 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
  1
1 EC50 = 0.036 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 = 0.091 nM
2 EC50 = 0.1 nM
3 IC50 = 5.97 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
  3
1 EC50 = 0.1 nM
2 IC50 = 0.25 nM
3 IC50 = 1 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 = 0.35 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 = 0.91 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 = 1.94 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 = 22.4 nM
CP0164490
 Compound Info 
(3S,6R,9S,12S,15S,18R,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 = 264 nM
CP0044562
 Compound Info 
(S)-2-{(R)-2-[(S)-2-Butyrylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-phenyl-propionylamino}-5-guanidino-pentanoic acid [(S)-1-(carbamoylmethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide
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C38H50N12O6
  1
1 IC50 = 580 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 = 615 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 = 3.5 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 = 6 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 = 6 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 = 11.5 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 = 13 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 = 17.5 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 = 20.5 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 = 30 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 = 34 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 = 37 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 = 37.5 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 = 40 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 = 43 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 = 43 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 = 47.5 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 = 51 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 = 57.5 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 = 62 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 = 63.5 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 = 86.5 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 = 91.5 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 = 125 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 = 170 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 = 260 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 = 760 nM
2 Ki > 5000 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 = 1120 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 = 4384 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 = 4520 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 = 5820 nM
Clinical Information about the Protein
Target 1 ( Melanocortin receptor 1 (MC1R) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Hypoactive sexual desire dysfunction [ICD-11: HA00]
2 Erythropoietic porphyrias [ICD-11: 5C58.12]
3 Female sexual arousal dysfunction [ICD-11: HA01.1]
Approved Drug(s) 2 Approved Drugs  2
1 Bremelanotide
 Drug Info 
Approved
Hypoactive sexual desire dysfunction
2 Afamelanotide
 Drug Info 
Approved
Erythropoietic porphyrias
Investigative Drug(s) 1 Investigative Drug  1
1 MT-II
 Drug Info 
Investigative
Female sexual arousal dysfunction
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01440 Melanocyte-stimulating hormone receptor Mus musculus, Mouse
 Protein Info