General Information of the Protein
Protein ID
PT00914
Protein Name
Melanocortin receptor 4
Gene Name
MC4R
Sequence
MVNSTHRGMHTSLHLWNRSSYRLHSNASESLGKGYSDGGCYEQLFVSPEVFVTLGVISLLENILVIVAIAKNKNLHSPMYFFICSLAVADMLVSVSNGSETIVITLLNSTDTDAQSFTVNIDNVIDSVICSSLLASICSLLSIAVDRYFTIFYALQYHNIMTVKRVGIIISCIWAACTVSGILFIIYSDSSAVIICLITMFFTMLALMASLYVHMFLMARLHIKRIAVLPGTGAIRQGANMKGAITLTILIGVFVVCWAPFFLHLIFYISCPQNPYCVCFMSHFNLYLILIMCNSIIDPLIYALRSQELRKTFKEIICCYPLGGLCDLSSRY
    Show/Hide
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 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:
P32245

Secondarily ID:
B2RAC3
Q16317
Q3MIJ6
    Show/Hide
Ensembl ID
ENSG00000166603
HGNC ID
HGNC:6932
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: CL000023 , BTI-Tn-5B1-4
Compound ID Compound Name Compound Formula
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
   Show/Hide
C33H41ClN6O2
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0404424
(S)-Piperidine-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
   Show/Hide
C29H41ClN6O2
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0404824
N-[(2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxopropan-2-yl]-3-(methylamino)propanamide
   Show/Hide
C27H39ClN6O2
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0408646
N-[(2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxopropan-2-yl]-3-(dimethylamino)propanamide
   Show/Hide
C28H41ClN6O2
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0497230
N-[(2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxopropan-2-yl]-3-[3-(dimethylamino)propanoylamino]propanamide
   Show/Hide
C31H46ClN7O3
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0459885
(R)-Piperidine-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
   Show/Hide
C29H41ClN6O2
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0505816
3-Acetylamino-N-[(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-propionamide
   Show/Hide
C28H39ClN6O3
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0540146
N-[(2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxopropan-2-yl]-3-(3-piperidin-1-ylpropanoylamino)propanamide
   Show/Hide
C34H50ClN7O3
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0559941
3-Benzylamino-N-[(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-propionamide
   Show/Hide
C33H43ClN6O2
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0377157
3-Amino-N-[(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-propionamide
   Show/Hide
C26H37ClN6O2
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0483596
Azetidine-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
   Show/Hide
C27H37ClN6O2
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0553968
3-Amino-N-[(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-3-methyl-butyramide
   Show/Hide
C28H41ClN6O2
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0514527
N-[(2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxopropan-2-yl]-3-[(2-methoxyacetyl)amino]propanamide
   Show/Hide
C29H41ClN6O4
 1
1
IC50 = 21 nM
   TI
   LI
   LO
   TS
CP0442575
(S)-Piperidine-3-carboxylic acid {2-[(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethylcarbamoyl]-ethyl}-amide
   Show/Hide
C32H46ClN7O3
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0523592
N-[(2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxopropan-2-yl]-2-[(2S)-pyrrolidin-2-yl]acetamide
   Show/Hide
C29H41ClN6O2
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0540104
(R)-Piperidine-3-carboxylic acid {2-[(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethylcarbamoyl]-ethyl}-amide
   Show/Hide
C32H46ClN7O3
 1
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0493706
3-Amino-N-[(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-2,2-dimethyl-propionamide
   Show/Hide
C28H41ClN6O2
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0554490
N-[3-[[(2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxopropan-2-yl]amino]-3-oxopropyl]benzamide
   Show/Hide
C33H41ClN6O3
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0415193
N-[(2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxopropan-2-yl]-3-(dibenzylamino)propanamide
   Show/Hide
C40H49ClN6O2
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0514529
N-[(2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxopropan-2-yl]-3-[(2,2,2-trifluoroacetyl)amino]propanamide
   Show/Hide
C28H36ClF3N6O3
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0041451
CAS_75921-69-6
   Show/Hide
C78H111N21O19
 11
1 EC50 = 0.017 nM
2 IC50 = 0.2 nM
3 IC50 = 0.4 nM
4 IC50 = 0.48 nM
5 IC50 = 0.52 nM
6 IC50 = 1.16 nM
7 IC50 = 3.6 nM
8 Ki = 0.3 nM
9 Ki = 0.44 nM
10 Ki = 0.47 nM
11 Ki = 0.95 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
   Show/Hide
C50H69N15O9
 3
1 EC50 = 0.057 nM
2 IC50 = 0.72 nM
3 IC50 = 2 nM
CP0166249
(4S)-5-[(2S)-1-[(2S)-1-[(2S)-1-[(2S)-1-[2-[(2S)-6-amino-1-[(2S)-2-[N-[(2S)-1-(carboxymethylimino)-1-hydroxy-3-methylbutan-2-yl]-C-hydroxycarbonimidoyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]imino-2-hydroxyethyl]imino-1-hydroxy-3-(1H-indol-3-yl)propan-2-yl]imino-5-carbamimidamido-1-hydroxypentan-2-yl]imino-1-hydroxy-3-phenylpropan-2-yl]imino-1-hydroxy-3-(1H-imidazol-5-yl)propan-2-yl]imino-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[[(2S)-1-[(2S)-2-[[(2S)-2-amino-1,4-dihydroxy-4-iminobutylidene]amino]-3-carboxypropanoyl]pyrrolidin-2-yl]-hydroxymethylidene]amino]-1,3-dihydroxypropylidene]amino]-1-hydroxy-3-(4-hydroxyphenyl)propylidene]amino]-1,3-dihydroxypropylidene]amino]-1-hydroxy-4-methylsulfanylbutylidene]amino]-5-hydroxypentanoic acid
   Show/Hide
C90H127N25O26S
 1
1 EC50 = 0.19 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
   Show/Hide
C77H109N21O19S
 4
1 EC50 = 0.21 nM
2 IC50 = 5 nM
3 IC50 = 38.7 nM
4 Ki = 26 nM
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
   Show/Hide
C54H71N15O9
 3
1 IC50 = 0.06 nM
2 Kd = 0.5012 nM
3 Kd = 0.7943 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
   Show/Hide
C53H74N16O10
 1
1 IC50 = 0.89 nM
CP0082819
(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
   Show/Hide
C47H63N15O9
 1
1 IC50 = 2.03 nM
CP0123950
(4S,15R,18S,21S,24S)-5-((S)-2-Acetylamino-hexanoylamino)-22-benzyl-19-(3-guanidino-propyl)-16-(1H-indol-3-ylmethyl)-4,7,15,18,21,24-hexaoxo-tetracosahydro-3a,8,14,17,20,23-hexaaza-cyclopentacyclotricosene-13-carboxylic acid amide
   Show/Hide
C49H69N13O9
 1
1 IC50 = 3 nM
CP0213531
(S)-4-(4-{2-[1-(Acetyl-ethyl-amino)-ethyl]-phenyl}-piperazin-1-yl)-3-(4-chloro-benzyl)-N-cyclobutyl-4-oxo-butyramide
   Show/Hide
C31H41ClN4O3
 2
1 IC50 = 5.8 nM
2 Ki = 6 nM
CP0266933
(+/-)-1-(1-(4-fluorophenyl)-2-{4-[4-(2-methoxy-1-naphthyl)butyl]piperazin-1-yl}ethyl)-4-methylpiperazine
   Show/Hide
C32H43FN4O
 1
1 IC50 = 7.9 nM
CP0057668
1-Pentanoylamino-4-phenyl-cyclohexanecarboxylic acid ((R)-1-{(S)-1-[(S)-1-(carbamoylmethyl-carbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-4-guanidino-butylcarbamoyl}-2-phenyl-ethyl)-amide
   Show/Hide
C46H60N10O6
 1
1 IC50 = 13 nM
CP0036043
4-(4-Ethoxy-phenyl)-1-pentanoylamino-cyclohexanecarboxylic acid ((R)-1-{(S)-1-[(S)-1-(carbamoylmethyl-carbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-4-guanidino-butylcarbamoyl}-2-phenyl-ethyl)-amide
   Show/Hide
C48H64N10O7
 1
1 IC50 = 43 nM
CP0238510
1'-[3-(4-chlorophenyl)-2-[(3R)-1,2-dihydro-3-isoquinolinylcarboxamido]-(2R)-propanoyl]-1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]
   Show/Hide
C32H35ClN4O4S
 1
1 IC50 = 66 nM
CP0316843
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40ClF2N3O2
 1
1 IC50 = 70 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
   Show/Hide
C53H74N16O10
 1
1 IC50 = 71.5 nM
CP0135404
(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
   Show/Hide
C53H74N16O10
 1
1 IC50 = 77.8 nM
CP0164490
(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
   Show/Hide
C53H74N16O10
 1
1 IC50 = 91 nM
CP0193753
5-Bromo-2-pentanoylamino-1,2,3,4-tetrahydro-naphthalene-2-carboxylic acid ((S)-1-{(S)-1-[(S)-1-(carbamoylmethyl-carbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-4-guanidino-butylcarbamoyl}-2-phenyl-ethyl)-amide
   Show/Hide
C44H55BrN10O6
 2
1 IC50 = 105 nM
2 IC50 = 200 nM
CP0044562
(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
   Show/Hide
C38H50N12O6
 1
1 IC50 = 150 nM
CP0353786
2-(2-(5-bromo-2-methoxyphenethyl)-3-fluorophenyl)-4,5-dihydro-1H-imidazole
   Show/Hide
C18H18BrFN2O
 1
1 IC50 = 160 nM
CP0288934
N-[(2R)-3-(4-chlorophenyl)-1-oxo-1-[4-[2-[1-(piperidin-3-ylamino)ethyl]phenyl]piperazin-1-yl]propan-2-yl]quinoline-3-carboxamide
   Show/Hide
C36H41ClN6O2
 1
1 IC50 = 300 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
   Show/Hide
C34H43N11O5
 1
1 IC50 = 1153 nM
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
   Show/Hide
C93H145N29O20
 1
1 Ki = 0.08 nM
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
   Show/Hide
C87H134N22O21S
 1
1 Ki = 0.11 nM
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
   Show/Hide
C83H127N21O18
 1
1 Ki = 0.12 nM
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
   Show/Hide
C92H143N27O20
 1
1 Ki = 0.13 nM
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
   Show/Hide
C90H139N27O20
 1
1 Ki = 0.17 nM
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
   Show/Hide
C90H139N27O20
 1
1 Ki = 0.17 nM
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
   Show/Hide
C90H138N26O21
 1
1 Ki = 0.2 nM
CP0726156
H-Tyr-Val-Nle-Gly-Pro-D-Nal(2')-Arg-Trp-Asp-Arg-Phe-Gly-NH2
   Show/Hide
C78H104N20O15
 1
1 Ki = 0.22 nM
CP0455645
BREMELANOTIDE
   Show/Hide
C50H68N14O10
 1
1 Ki = 0.25 nM
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
   Show/Hide
C93H145N27O20
 1
1 Ki = 0.26 nM
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
   Show/Hide
C74H114N18O15
 1
1 Ki = 0.33 nM
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
   Show/Hide
C84H134N22O18
 1
1 Ki = 0.37 nM
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
   Show/Hide
C96H146N28O25
 1
1 Ki = 0.58 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
   Show/Hide
C34H47Cl2N5O3
 1
1 Ki = 0.59 nM
CP0309779
1-((R)-1-(4-(2-((S)-1-(3-aminopropylamino)-3-methylbutyl)-6-fluorophenyl)piperazin-1-yl)-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl)pyrrolidin-2-one
   Show/Hide
C31H42Cl2FN5O2
 1
1 Ki = 0.9 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
   Show/Hide
C30H40Cl2FN5O2
 1
1 Ki = 0.94 nM
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
   Show/Hide
C70H106N22O18
 1
1 Ki = 1 nM
CP0354019
N-[(1S)-1-[2-[4-[(2R)-3-(2,4-dichlorophenyl)-2-(2-oxopyrrolidin-1-yl)propanoyl]piperazin-1-yl]-5-methylphenyl]-3-methylbutyl]-3-(methylamino)propanamide
   Show/Hide
C33H45Cl2N5O3
 1
1 Ki = 1.4 nM
CP0197233
N-[(1S)-1-[2-[4-[(2R)-3-(2,4-dichlorophenyl)-2-(2-oxopyrrolidin-1-yl)propanoyl]piperazin-1-yl]phenyl]-3-methylbutyl]-3-(dimethylamino)propanamide
   Show/Hide
C33H45Cl2N5O3
 1
1 Ki = 1.5 nM
CP0288154
1-((R)-1-(4-(2-((S)-1-((2-aminoethyl)(methyl)amino)-3-methylbutyl)-6-fluorophenyl)piperazin-1-yl)-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl)pyrrolidin-2-one
   Show/Hide
C31H42Cl2FN5O2
 1
1 Ki = 1.5 nM
CP0234419
(R)-3-amino-N-(3-(2,4-dichlorophenyl)-1-oxo-1-(4-(2-((2-(thiophen-2-yl)ethylamino)methyl)phenyl)piperazin-1-yl)propan-2-yl)propanamide
   Show/Hide
C29H35Cl2N5O2S
 1
1 Ki = 1.8 nM
CP0197234
3-amino-N-((S)-1-(2-(4-((R)-3-(2,4-dichlorophenyl)-2-(2-oxopyrrolidin-1-yl)propanoyl)piperazin-1-yl)-3-fluorophenyl)-3-methylbutyl)propanamide
   Show/Hide
C31H40Cl2FN5O3
 1
1 Ki = 1.9 nM
CP0288155
3-amino-N-((S)-1-(2-(4-((R)-3-(2,4-dichlorophenyl)-2-(2-oxopyrrolidin-1-yl)propanoyl)piperazin-1-yl)phenyl)-3-methylbutyl)propanamide
   Show/Hide
C31H41Cl2N5O3
 1
1 Ki = 2 nM
CP0348895
N-[(1S)-1-[2-[4-[(2R)-3-(2,4-dichlorophenyl)-2-(2-oxopyrrolidin-1-yl)propanoyl]piperazin-1-yl]phenyl]-3-methylbutyl]-2-(methylamino)acetamide
   Show/Hide
C31H41Cl2N5O3
 1
1 Ki = 2.4 nM
CP0214845
N-[(1S)-1-[2-[4-[(2R)-3-(2,4-dichlorophenyl)-2-(2-oxopyrrolidin-1-yl)propanoyl]piperazin-1-yl]phenyl]-3-methylbutyl]-3-(methylamino)propanamide
   Show/Hide
C32H43Cl2N5O3
 1
1 Ki = 2.6 nM
CP0309763
1-((R)-3-(2,4-dichlorophenyl)-1-(4-(2-((S)-3-methyl-1-(2-(methylamino)ethylamino)butyl)phenyl)piperazin-1-yl)-1-oxopropan-2-yl)pyrrolidin-2-one
   Show/Hide
C31H43Cl2N5O2
 1
1 Ki = 3.8 nM
CP0135959
1-((R)-1-(4-(2-((S)-1-amino-3-methylbutyl)-4-(trifluoromethyl)phenyl)piperazin-1-yl)-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl)pyrrolidin-2-one
   Show/Hide
C29H35Cl2F3N4O2
 1
1 Ki = 4.5 nM
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
   Show/Hide
C69H99N21O18
 1
1 Ki = 4.6 nM
CP0182893
(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
   Show/Hide
C40H46ClN11O5
 1
1 Ki = 5 nM
CP0674615
H-Tyr-Val-Nle-Gly-His-D-Nal(2)-Arg-D-Trp-Asp-Arg-Phe-Gly-NH2
   Show/Hide
C79H104N22O15
 1
1 Ki = 5.7 nM
CP0167498
1-((R)-1-(4-(2-((S)-1-amino-3-methylbutyl)phenyl)piperazin-1-yl)-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl)pyrrolidin-2-one
   Show/Hide
C28H36Cl2N4O2
 1
1 Ki = 6.4 nM
CP0084312
(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
   Show/Hide
C42H51N11O5
 1
1 Ki = 7.3 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
   Show/Hide
C33H41ClN6O2
 2
1 Ki = 9 nM
2 Ki = 80 nM
CP0348893
(1S)-(2-{4-[(2R)-(2-oxo-1-pyrrolidinyl)-3-(2,4-dichlorophenyl)propionyl]-1-piperazinyl}-3-fluorophenyl)-3-methylbutylamine
   Show/Hide
C28H35Cl2FN4O2
 1
1 Ki = 9.7 nM
CP0081762
(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
   Show/Hide
C30H36FN7O3
 1
1 Ki = 11 nM
CP0234420
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-oxo-2-(4-{2-[(2-thiophen-2-yl-ethylamino)-methyl]-phenyl}-piperazin-1-yl)-ethyl]-amide
   Show/Hide
C36H40ClN5O2S
 1
1 Ki = 11 nM
CP0370128
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-diethylaminomethyl-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C34H42ClN5O2
 1
1 Ki = 14 nM
CP0133486
(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
   Show/Hide
C41H49N11O6
 1
1 Ki = 15.5 nM
CP0309765
1-((R)-1-(4-(2-((S)-1-amino-3-methylbutyl)-4-fluorophenyl)piperazin-1-yl)-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl)pyrrolidin-2-one
   Show/Hide
C28H35Cl2FN4O2
 1
1 Ki = 26 nM
CP0234962
(R)-1-(4-(2-((S)-1-amino-3-methylbutyl)-4-(trifluoromethyl)phenyl)piperazin-1-yl)-3-(2,4-dichlorophenyl)-2-methylpropan-1-one
   Show/Hide
C26H32Cl2F3N3O
 1
1 Ki = 26 nM
CP0308798
2-((S)-1-(2-(4-((R)-3-(2,4-dichlorophenyl)-2-(2-oxopyrrolidin-1-yl)propanoyl)piperazin-1-yl)-5-(trifluoromethyl)phenyl)-3-methylbutylamino)acetic acid
   Show/Hide
C31H37Cl2F3N4O4
 1
1 Ki = 27 nM
CP0044734
(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
   Show/Hide
C37H46N10O5
 1
1 Ki = 29 nM
CP0103117
(R)-1-(4-(2-((S)-1-amino-3-methylbutyl)-4-(trifluoromethyl)phenyl)piperazin-1-yl)-3-(4-chlorophenyl)-2-methylpropan-1-one
   Show/Hide
C26H33ClF3N3O
 1
1 Ki = 31 nM
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
   Show/Hide
C94H146N26O24
 1
1 Ki = 35 nM
CP0350169
(R)-2-amino-1-(4-(2-((S)-1-amino-3-methylbutyl)-4-(trifluoromethyl)phenyl)piperazin-1-yl)-3-(2,4-dichlorophenyl)propan-1-one
   Show/Hide
C25H31Cl2F3N4O
 1
1 Ki = 39 nM
CP0309777
4-((S)-1-(2-(4-((R)-3-(2,4-dichlorophenyl)-2-(2-oxopyrrolidin-1-yl)propanoyl)piperazin-1-yl)-5-(trifluoromethyl)phenyl)-3-methylbutylamino)butanoic acid
   Show/Hide
C33H41Cl2F3N4O4
 1
1 Ki = 40 nM
CP0040024
(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
   Show/Hide
C41H49N11O5
 1
1 Ki = 49 nM
CP0050698
(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
   Show/Hide
C38H44ClN11O6S
 1
1 Ki = 66.5 nM
CP0047872
(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
   Show/Hide
C40H46ClN11O6
 1
1 Ki = 68 nM
CP0037014
(1S)-[2-{4-[3-(2,4-dichlorophenyl)propionyl]-1-piperazinyl}-5-(trifluoromethyl)phenyl]-3-methylbutylamine
   Show/Hide
C25H30Cl2F3N3O
 1
1 Ki = 74 nM
CP0182921
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
   Show/Hide
C36H45N11O5
 1
1 Ki = 87 nM
CP0336462
(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
   Show/Hide
C36H47N11O5
 1
1 Ki = 97.5 nM
CP0178413
(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
   Show/Hide
C36H47N11O6
 1
1 Ki = 100 nM
CP0228189
(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
   Show/Hide
C40H47N11O5
 1
1 Ki = 100 nM
CP0034706
(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
   Show/Hide
C40H48N8O6
 1
1 Ki = 104 nM
CP0100500
(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
   Show/Hide
C35H42N12O5
 1
1 Ki = 110 nM
CP0228609
(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
   Show/Hide
C37H49N11O5
 1
1 Ki = 120 nM
CP0257564
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
   Show/Hide
C34H42N12O6
 1
1 Ki = 140 nM
CP0034718
(S)-1-(4-(2-((S)-1-amino-3-methylbutyl)-4-(trifluoromethyl)phenyl)piperazin-1-yl)-3-(2,4-dichlorophenyl)-2-methylpropan-1-one
   Show/Hide
C26H32Cl2F3N3O
 1
1 Ki = 140 nM
CP0049389
(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
   Show/Hide
C36H47N11O5
 1
1 Ki = 150 nM
CP0089083
(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
   Show/Hide
C35H45N11O5
 1
1 Ki = 160 nM
CP0101637
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
   Show/Hide
C39H45N11O5
 1
1 Ki = 160 nM
CP0217814
(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
   Show/Hide
C37H49N11O5
 1
1 Ki = 160 nM
CP0184237
(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
   Show/Hide
C33H43N11O6S
 1
1 Ki = 170 nM
CP0204764
(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
   Show/Hide
C35H42F3N11O5
 1
1 Ki = 170 nM
CP0048619
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
   Show/Hide
C32H41N11O4
 1
1 Ki = 180 nM
CP0081758
(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
   Show/Hide
C29H34FN5O3
 1
1 Ki = 189 nM
CP0049442
(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
   Show/Hide
C35H45N11O5S
 1
1 Ki = 210 nM
CP0370229
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-methanesulfonylamino-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C30H34ClN5O4S
 1
1 Ki = 220 nM
CP0269557
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-oxo-2-[4-(2-[1,2,4]triazol-1-ylmethyl-phenyl)-piperazin-1-yl]-ethyl}-amide
   Show/Hide
C32H34ClN7O2
 1
1 Ki = 270 nM
CP0308897
(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
   Show/Hide
C34H43N11O5
 1
1 Ki = 280 nM
CP0182484
(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
   Show/Hide
C35H45N11O6
 1
1 Ki = 350 nM
CP0160526
(R)-N-((R)-1-(4-(2-(aminomethyl)phenyl)piperazin-1-yl)-3-(4-chlorophenyl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C30H34ClN5O2
 1
1 Ki = 380 nM
CP0190200
(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
   Show/Hide
C34H43N11O6
 1
1 Ki = 440 nM
CP0207102
1-(4-(2-(1-aminoethyl)-4-(trifluoromethyl)phenyl)piperazin-1-yl)-3-(2,4-dichlorophenyl)propan-1-one
   Show/Hide
C22H24Cl2F3N3O
 1
1 Ki = 490 nM
CP0195338
(4-(1-((3-fluoro-4-methoxybenzylamino)methyl)cyclohexyl)piperazin-1-yl)((3R,4S)-4-(4-chlorophenyl)-1-isopropylpyrrolidin-3-yl)methanone
   Show/Hide
C33H46ClFN4O2
 1
1 Ki = 540 nM
CP0099822
CAS_72711-43-4
   Show/Hide
C74H99N21O16S
 1
1 Ki = 730 nM
CP0135132
(2S)-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)-N-[(2S)-1-(methylamino)-3-naphthalen-2-yl-1-oxopropan-2-yl]pentanamide
   Show/Hide
C29H37N7O3
 1
1 Ki = 1248 nM
Clinical Information about the Protein
Target 1 ( Melanocortin receptor 4 (MC4R) )
Target Type Successful Target
Disease 7 Target-related Diseases  7
1 Opioid-induced constipation [ICD-11: DB32.1]
2 Hypoactive sexual desire dysfunction [ICD-11: HA00]
3 Atopic dermatitis [ICD-11: EA80]
4 Malnutrition [ICD-11: 5B50-5B71]
5 Obesity [ICD-11: 5B81]
6 Female sexual arousal dysfunction [ICD-11: HA01.1]
7 Erectile dysfunction [ICD-11: HA01.1]
Approved Drug(s) 3 Approved Drugs  3
1 Methylnaltrexone bromide Approved
Opioid-induced constipation
2 Bremelanotide Approved
Hypoactive sexual desire dysfunction
3 Setmelanotide Approved
Obesity
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 PMX-53 Phase 2
Atopic dermatitis
2 PF-07258669 Phase 1
Malnutrition
Investigative Drug(s) 2 Investigative Drugs  2
1 MT-II Investigative
Female sexual arousal dysfunction
2 THIQ Investigative
Erectile dysfunction