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Melanocortin receptor 4 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
Melanotan-1IC500.4 [1], 1.16 [2], 3.6 [3]
ThiqIC501.2 [1]
ThiqKi9.0 [1]
Msh, 2-tyr-alpha-IC5019.0 [1]
Melanotan IIIC500.72 [1], 1.1 [2]
Melanotan IIKi1.26 [1]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-oxo-1-[4-[2-[(2-thiophen-2-ylethylamino)methyl]phenyl]piperazin-1-yl]propan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi10.8 [1], 11.0 [2], 12.0 [3]
1-[4-[2-[(1S)-1-Amino-3-methylbutyl]-4-(trifluoromethyl)phenyl]piperazin-1-yl]-3-(2,4-dichlorophenyl)propan-1-oneKi74.0 [1], 75.0 [2]
N-[2-[(2-Amino-2-oxoethyl)-[(1R)-1-phenylethyl]amino]-2-oxoethyl]-N-benzhydryl-2-[3-(diaminomethylideneamino)propylamino]acetamideIC501900.0 [1], 2100.0 [2], 3100.0 [3]
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]-4-methylsulfanylbutanoyl]amino]acetyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-[[(2S)-1-[[(2S)-1-(carboxymethylamino)-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic acidIC50760.0 [1], 770.0 [2]
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]-4-methylsulfanylbutanoyl]amino]acetyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-[[(2S)-1-[[(2S)-1-(carboxymethylamino)-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic acidKi730.0 [1]
3-Amino-N-[(2R)-3-(2,4-dichlorophenyl)-1-oxo-1-[4-[2-[(2-thiophen-2-ylethylamino)methyl]phenyl]piperazin-1-yl]propan-2-yl]propanamideKi1.8 [1]
2-Amino-N-[(1S)-1-[2-[4-[3-(2,4-dichlorophenyl)propanoyl]piperazin-1-yl]-5-(trifluoromethyl)phenyl]-3-methylbutyl]acetamideIC501300.0 [1]
2-Amino-N-[(1S)-1-[2-[4-[3-(2,4-dichlorophenyl)propanoyl]piperazin-1-yl]-5-(trifluoromethyl)phenyl]-3-methylbutyl]acetamideKi19.0 [1]
(2R)-1-[4-[2-[(1S)-1-Amino-3-methylbutyl]-4-methylphenyl]piperazin-1-yl]-3-(4-chlorophenyl)-2-methylpropan-1-oneIC50560.0 [1], 570.0 [2]
(2R)-1-[4-[2-[(1S)-1-Amino-3-methylbutyl]-4-methylphenyl]piperazin-1-yl]-3-(4-chlorophenyl)-2-methylpropan-1-oneKi25.0 [1]
(2R)-1-[4-[2-[(1S)-1-Amino-2-methylpropyl]-4-methylphenyl]piperazin-1-yl]-3-(4-chlorophenyl)-2-methylpropan-1-oneIC502400.0 [1]
(2R)-1-[4-[2-[(1S)-1-Amino-2-methylpropyl]-4-methylphenyl]piperazin-1-yl]-3-(4-chlorophenyl)-2-methylpropan-1-oneKi69.0 [1]
(2R)-3-(4-Chloro-2-fluorophenyl)-2-methyl-1-[4-[4-methyl-2-[(1S)-2-methyl-1-[2-(methylamino)ethylamino]propyl]phenyl]piperazin-1-yl]propan-1-oneIC50660.0 [1]
(2R)-3-(4-Chloro-2-fluorophenyl)-2-methyl-1-[4-[4-methyl-2-[(1S)-2-methyl-1-[2-(methylamino)ethylamino]propyl]phenyl]piperazin-1-yl]propan-1-oneKi6.0 [1]
N-[(1S)-1-[2-[4-[(2R)-3-(4-Chloro-2-fluorophenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-2-(methylamino)acetamideIC50410.0 [1]
N-[(1S)-1-[2-[4-[(2R)-3-(4-Chloro-2-fluorophenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-2-(methylamino)acetamideKi2.8 [1]
N-[(1S)-1-[2-[4-[(2R)-3-(4-Chloro-2-fluorophenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(dimethylamino)propanamideIC50190.0 [1]
N-[(1S)-1-[2-[4-[(2R)-3-(4-Chloro-2-fluorophenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(dimethylamino)propanamideKi2.2 [1]
N-[(1S)-1-[2-[4-[(2R)-3-(4-Chloro-2-methylphenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(dimethylamino)propanamideIC5092.0 [1]
N-[(1S)-1-[2-[4-[(2R)-3-(4-Chloro-2-methylphenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(dimethylamino)propanamideKi0.6 [1]
N-[(1S)-1-[2-[4-[(2R)-3-(4-Chlorophenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(dimethylamino)propanamideIC5035.0 [1]
N-[(1S)-1-[2-[4-[(2R)-3-(4-Chlorophenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(dimethylamino)propanamideKi2.8 [1]
N-[(1S)-1-[2-[4-[(2R)-3-(4-Chlorophenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(methylamino)propanamideIC5087.0 [1]
N-[(1S)-1-[2-[4-[(2R)-3-(4-Chlorophenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(methylamino)propanamideKi5.7 [1]
3-Amino-N-[(1S)-1-[2-[4-[(2R)-3-(4-chlorophenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]propanamideIC50280.0 [1]
3-Amino-N-[(1S)-1-[2-[4-[(2R)-3-(4-chlorophenyl)-2-methylpropanoyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]propanamideKi5.9 [1]
1-[(2R)-1-[4-[2-[(1S)-1-(2-Aminoethylamino)-3-methylbutyl]-6-fluorophenyl]piperazin-1-yl]-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl]pyrrolidin-2-oneIC5021.0 [1]
1-[(2R)-1-[4-[2-[(1S)-1-(2-Aminoethylamino)-3-methylbutyl]-6-fluorophenyl]piperazin-1-yl]-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl]pyrrolidin-2-oneKi0.9 [1], 0.94 [2]
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)propanamideIC5019.0 [1]
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)propanamideKi0.59 [1], 0.6 [2]
1-[4-[2-[(1S)-1-Amino-3-methylbutyl]-4-(trifluoromethyl)phenyl]piperazin-1-yl]-3-(4-chloro-2-methoxyphenyl)-2-methylpropan-1-oneIC501700.0 [1]
1-[4-[2-[(1S)-1-Amino-3-methylbutyl]-4-(trifluoromethyl)phenyl]piperazin-1-yl]-3-(4-chloro-2-methoxyphenyl)-2-methylpropan-1-oneKi14.0 [1]
(3S,6S,9R,12S,15R,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-carboxamideIC500.06 [1], 0.6 [2], 1.8 [3]
Ac-His-DPhe-Arg-Trp-NH2IC50359.0 [1], 1153.0 [2], 4600.0 [3]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-oxo-1-[4-[2-[1-(piperidin-3-ylamino)ethyl]phenyl]piperazin-1-yl]propan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi6.4 [1]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-oxo-1-[4-[2-(1,2,4-triazol-1-ylmethyl)phenyl]piperazin-1-yl]propan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi270.0 [1]
N-[(1S)-1-[2-[1-[(3S,4R)-1-Tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamideIC5070.0 [1]
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-6-amino-1-[(2S)-2-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-2-oxoethyl]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-4-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acidIC5015.0 [1], 16.0 [2], 19.0 [3]
(3R)-N-[(2R)-1-[4-[2-(Aminomethyl)phenyl]piperazin-1-yl]-3-(4-chlorophenyl)-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi380.0 [1]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-[4-[2-(diethylaminomethyl)phenyl]piperazin-1-yl]-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi14.0 [1], 34.0 [2], 52.0 [3]
1-[(2R)-1-[4-[2-[(1S)-1-Amino-3-methylbutyl]-6-fluorophenyl]piperazin-1-yl]-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl]pyrrolidin-2-oneKi9.7 [1]
Ac-Tyr-D-Phe-Arg-2-Nal-NHCH3Ki104.0 [1]
(2R)-1-[4-[2-[(1S)-1-Amino-3-methylbutyl]-4-(trifluoromethyl)phenyl]piperazin-1-yl]-3-(4-chlorophenyl)-2-methylpropan-1-oneKi31.0 [1]
(2R)-1-[4-[2-[(1S)-1-Amino-3-methylbutyl]-4-(trifluoromethyl)phenyl]piperazin-1-yl]-3-(2,4-dichlorophenyl)-2-methylpropan-1-oneKi26.0 [1]
3-Amino-N-[(2R)-3-(4-chlorophenyl)-1-oxo-1-[4-[2-[(2-thiophen-2-ylethylamino)methyl]phenyl]piperazin-1-yl]propan-2-yl]propanamideKi20.5 [1], 21.0 [2]
1-[(2R)-1-[4-[2-[(1S)-1-Amino-3-methylbutyl]phenyl]piperazin-1-yl]-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl]pyrrolidin-2-oneIC50220.0 [1]
1-[(2R)-1-[4-[2-[(1S)-1-Amino-3-methylbutyl]phenyl]piperazin-1-yl]-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl]pyrrolidin-2-oneKi6.4 [1]
1-[(2R)-1-[4-[2-[(1S)-1-Amino-3-methylbutyl]-4-(trifluoromethyl)phenyl]piperazin-1-yl]-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl]pyrrolidin-2-oneIC50360.0 [1]
1-[(2R)-1-[4-[2-[(1S)-1-Amino-3-methylbutyl]-4-(trifluoromethyl)phenyl]piperazin-1-yl]-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl]pyrrolidin-2-oneKi4.5 [1]
N-[(2S)-1-[[(2R)-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]-6-(4-butyltriazol-1-yl)hexanamideKi350.0 [1], 990.0 [2], 1900.0 [3]
3-Amino-N-[(2R)-3-(2,4-dichlorophenyl)-1-[4-[1-[[[2-(4-methoxyphenyl)acetyl]amino]methyl]cyclohexyl]piperazin-1-yl]-1-oxopropan-2-yl]propanamideKi2.8 [1], 4.2 [2]
5-[[2-[4-[3-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-Amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-oxopropyl]triazol-1-yl]acetyl]amino]-2-[[2-[[2-[4-[3-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-oxopropyl]triazol-1-yl]acetyl]amino]acetyl]amino]-2-[3-[[2-[4-[3-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-oxopropyl]triazol-1-yl]acetyl]amino]propyl]-N-(3-amino-3-oxopropyl)pentanamideIC5014.0 [1]
5-[[2-[4-[3-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-Amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-oxopropyl]triazol-1-yl]acetyl]amino]-2-[[2-[[2-[4-[3-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-oxopropyl]triazol-1-yl]acetyl]amino]acetyl]amino]-2-[3-[[2-[4-[3-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-oxopropyl]triazol-1-yl]acetyl]amino]propyl]-N-(3-amino-3-oxopropyl)pentanamideKi4.3 [1], 11.0 [2]
[(3R,4S)-4-(4-Chlorophenyl)-1-propan-2-ylpyrrolidin-3-yl]-[4-[1-[[(3-fluoro-4-methoxyphenyl)methylamino]methyl]cyclohexyl]piperazin-1-yl]methanoneIC5048.0 [1]
[(3R,4S)-4-(4-Chlorophenyl)-1-propan-2-ylpyrrolidin-3-yl]-[4-[1-[[(3-fluoro-4-methoxyphenyl)methylamino]methyl]cyclohexyl]piperazin-1-yl]methanoneKi0.5 [1], 540.0 [2]
N-[(2R)-3-(2,4-Dichlorophenyl)-1-[4-[2-(1-hydroxy-3-methylbutyl)phenyl]piperazin-1-yl]-1-oxopropan-2-yl]-2-(methylamino)acetamideIC50420.0 [1]
N-[(2R)-3-(2,4-Dichlorophenyl)-1-[4-[2-(1-hydroxy-3-methylbutyl)phenyl]piperazin-1-yl]-1-oxopropan-2-yl]-2-(methylamino)acetamideKi8.3 [1], 500.0 [2]
(3S,6S,9R,12S,15S,23S)-15-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-9-benzyl-6-[3-(diaminomethylideneamino)propyl]-12-(1H-imidazol-5-ylmethyl)-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxamideKi22.0 [1], 87.0 [2]
(2S,5R,8S,11S,18S)-N-[(2S)-1-Amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-benzyl-8-[3-(diaminomethylideneamino)propyl]-2-(1H-imidazol-5-ylmethyl)-3,6,9,15,19-pentaoxo-18-(pentanoylamino)-1,4,7,10,14-pentazacyclononadecane-11-carboxamideKi365.0 [1]
(3S,6S,9R,12S,15S,23S)-15-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-12-(2-aminoethyl)-9-benzyl-6-[3-(diaminomethylideneamino)propyl]-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,19-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxamideKi4.0 [1], 35.0 [2]
BremelanotideKi0.25 [1], 24.55 [2]
Ac-His-Phe-Arg-Trp-NH2Ki246.0 [1], 280.0 [2]
N-[2-[(1R)-1'-[(3S,4R)-1-Tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]propan-2-yl]acetamideIC5013.0 [1]
(3S)-4-[4-[2-[1-[Acetyl(ethyl)amino]ethyl]phenyl]piperazin-1-yl]-3-[(4-chlorophenyl)methyl]-N-cyclobutyl-4-oxobutanamideIC505.8 [1]
(3S)-4-[4-[2-[1-[Acetyl(ethyl)amino]ethyl]phenyl]piperazin-1-yl]-3-[(4-chlorophenyl)methyl]-N-cyclobutyl-4-oxobutanamideKi6.0 [1]
(2S)-N-[(2S)-1-[(2-Amino-2-oxoethyl)amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-[[(2S)-2-(butanoylamino)-3-(1H-imidazol-5-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanamideIC50150.0 [1]
(3S)-3-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]-4-methylsulfanylbutanoyl]amino]acetyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-[[(2S)-1-[[(2S)-1-(carboxymethylamino)-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic acidIC50600.0 [1]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-[4-[2-(methanesulfonamido)phenyl]piperazin-1-yl]-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi220.0 [1]
3-[4-[2-(4-Fluorophenyl)-2-(4-methylpiperazin-1-yl)ethyl]piperazin-1-yl]-2-methyl-1-phenylpropan-1-oneIC5052.0 [1], 217.0 [2]
N-(3-Amino-propyl)-3-[(1H-indol-3-ylmethyl)-amino]-2-[(naphthalen-2-ylmethyl)-amino]-propionamideKi25118.86 [1], 27000.0 [2]
1-[4-[4-[4-Fluoro-beta-(4-isopropylpiperazino)phenethyl]piperazino]butyl]-2-methoxynaphthaleneIC5012.7 [1]
1-[4-[4-[4-Fluoro-beta-(4-isopropylpiperazino)phenethyl]piperazino]butyl]-2-methoxynaphthaleneKi7.9 [1]
N-[(2R)-1-[[(2S)-1-[[(2S)-1-[(2-Amino-2-oxoethyl)amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-5-bromo-2-(pentanoylamino)-3,4-dihydro-1H-naphthalene-2-carboxamideIC50105.0 [1], 200.0 [2]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-[4-cyclohexyl-4-[(2-methyltetrazol-5-yl)methyl]piperidin-1-yl]-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideIC501.2 [1]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-[4-cyclohexyl-4-[(2-methyltetrazol-5-yl)methyl]piperidin-1-yl]-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi1.2 [1]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-[4-cyclohexyl-4-(2H-tetrazol-5-ylmethyl)piperidin-1-yl]-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideIC50238.0 [1]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-[4-cyclohexyl-4-[(1-methyltetrazol-5-yl)methyl]piperidin-1-yl]-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideIC500.3 [1]
N-[(2R)-3-(4-Chlorophenyl)-1-oxo-1-[4-[2-[(2-thiophen-2-ylethylamino)methyl]phenyl]piperazin-1-yl]propan-2-yl]piperidine-3-carboxamideKi15.0 [1]
N-[2-[(1S)-1'-[(3S,4R)-1-Tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]propan-2-yl]acetamideIC504.3 [1], 4.5 [2]
2-Amino-N-[(2R)-3-(4-chlorophenyl)-1-oxo-1-[4-[2-[(2-thiophen-2-ylethylamino)methyl]phenyl]piperazin-1-yl]propan-2-yl]acetamideKi44.0 [1]
N-[(2R)-3-(4-Chlorophenyl)-1-oxo-1-[4-[2-[(2-thiophen-2-ylethylamino)methyl]phenyl]piperazin-1-yl]propan-2-yl]-2-methoxyacetamideKi69.5 [1], 70.0 [2]
(2R)-1-[4-[2-[(1S)-1-Amino-2-methylpropyl]-4-methylphenyl]piperazin-1-yl]-3-(4-chloro-2-fluorophenyl)-2-methylpropan-1-oneKi35.0 [1]
(2R)-1-[4-[2-[(1S)-1-Amino-2-methylpropyl]-4-methylphenyl]piperazin-1-yl]-3-(4-chloro-2-methylphenyl)-2-methylpropan-1-oneKi9.7 [1]
[4-[2-[(1S)-1-Amino-2-methylpropyl]-4-methylphenyl]piperazin-1-yl]-[(3S,4R)-4-(4-chlorophenyl)-1-(oxan-4-yl)pyrrolidin-3-yl]methanoneKi11.0 [1], 12.0 [2]
(2S)-2-Amino-5-(diaminomethylideneamino)-N-(naphthalen-1-ylmethyl)-N-(naphthalen-2-ylmethyl)pentanamideKi2100.0 [1], 5011.87 [2]
(2S)-5-(Diaminomethylideneamino)-N-[3-(diaminomethylideneamino)propyl]-2-(naphthalen-2-ylmethylamino)pentanamideKi30000.0 [1], 31622.78 [2]



References

This online tool may be cited as follows

MLA

"Quest Database™ Melanocortin receptor 4 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/melanocortin-receptor-4-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ Melanocortin receptor 4 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/melanocortin-receptor-4-inhibitors-ic50-ki.
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