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Melanocortin receptor 1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
Melanotan IIIC500.2 [1], 0.25 [2], 0.4 [3], 6.7 [4]
Melanotan IIKi0.11 [1]
ThiqIC502063.0 [1], 2067.0 [2]
ThiqKi300.0 [1], 760.0 [2], 1500.0 [3], 5000.0 [4]
Melanotan-1IC500.51 [1]
Melanotan-1Ki0.05 [1], 0.5 [2], 1.8 [3]
Msh, 2-tyr-alpha-IC500.4 [1], 5.97 [2]
Msh, 2-tyr-alpha-Ki1.5 [1]
Ac-Tyr-D-Phe-Arg-2-Nal-NHCH3Ki4520.0 [1]
BremelanotideKi1.91 [1], 6.4 [2]
Ac-His-DPhe-Arg-Trp-NH2IC50105.0 [1], 615.0 [2]
Ac-His-Phe-Arg-Trp-NH2Ki35.0 [1], 37.0 [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 acidIC501000.0 [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)pentanamideIC50580.0 [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]propanamideKi1300.0 [1]
N-(3-Amino-propyl)-3-[(1H-indol-3-ylmethyl)-amino]-2-[(naphthalen-2-ylmethyl)-amino]-propionamideKi630.96 [1], 700.0 [2]
(2R)-1-[4-[2-[(1S)-1-Amino-3-methylbutyl]-4-methylphenyl]piperazin-1-yl]-3-(4-chlorophenyl)-2-methylpropan-1-oneKi3100.0 [1]
(2S)-2-Amino-5-(diaminomethylideneamino)-N-(naphthalen-1-ylmethyl)-N-(naphthalen-2-ylmethyl)pentanamideKi630.96 [1], 1200.0 [2]
(2S)-5-(Diaminomethylideneamino)-N-[3-(diaminomethylideneamino)propyl]-2-(naphthalen-2-ylmethylamino)pentanamideKi3981.07 [1], 4500.0 [2]
Ac-His-D-Phe-Arg-2-Nal-NHCH3Ki13.0 [1]
(2S)-2-[[(2R)-2-Amino-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)-N-[(2S)-1-(methylamino)-3-naphthalen-2-yl-1-oxopropan-2-yl]pentanamideKi4384.0 [1]
(2S)-2-[(3S)-3-(2-Aminoethyl)-4-[(2R)-2-amino-3-(4-fluorophenyl)propanoyl]-2-oxopiperazin-1-yl]-N-methyl-3-naphthalen-2-ylpropanamideKi5820.0 [1]
(2S)-2-[(3S)-4-[(2R)-2-Amino-3-(4-fluorophenyl)propanoyl]-3-[2-(diaminomethylideneamino)ethyl]-2-oxopiperazin-1-yl]-N-methyl-3-naphthalen-2-ylpropanamideKi1120.0 [1]
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]acetyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-[[(2S)-1-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-oxobutanoic acidIC500.5 [1]
N-[2-[(2-Amino-2-oxoethyl)-[(1R)-1-phenylethyl]amino]-2-oxoethyl]-N-benzhydryl-2-[3-(diaminomethylideneamino)propylamino]acetamideIC509100.0 [1], 25000.0 [2]
(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-carboxamideIC508.7 [1], 100.0 [2]
(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-carboxamideIC504.0 [1], 14.8 [2]
(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-carboxamideIC508.7 [1], 9.9 [2]
CID 137659949IC5026000.0 [1]
CID 137659949Ki30.0 [1]
(2S,5R,8S,11S,14S,22S)-22-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-2-(2-amino-2-oxoethyl)-5-benzyl-8-[3-(diaminomethylideneamino)propyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,19,23-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-14-carboxamideKi155.0 [1]
(2S,5R,8S,11S,14S,22S)-22-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-2-(2-amino-2-oxoethyl)-5-benzyl-8-[3-(diaminomethylideneamino)propyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,17,23-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-14-carboxamideKi688.0 [1]
(2S,5R,8S,11S,14S,22S)-22-[[(2R)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-2-(3-amino-3-oxopropyl)-5-benzyl-8-[3-(diaminomethylideneamino)propyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,17,23-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-14-carboxamideKi120.0 [1]
(2S,5R,8S,11S,14S,22S)-22-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-2-(3-amino-3-oxopropyl)-5-benzyl-8-[3-(diaminomethylideneamino)propyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,17,23-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-14-carboxamideKi130.0 [1]
(3S,6S,9R,12S,15S,23S)-15-[[(2R)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-12-(3-amino-3-oxopropyl)-9-benzyl-6-[3-(diaminomethylideneamino)propyl]-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxamideKi3350.0 [1]
(3S,6S,9R,12S,15S,23S)-15-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-12-(3-amino-3-oxopropyl)-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-carboxamideKi133.0 [1]
(2S,5R,8S,11S,14S,22S)-22-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-2-(2-amino-2-oxoethyl)-5-benzyl-8-[3-(diaminomethylideneamino)propyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,16,23-hexaoxo-1,4,7,10,13,17-hexazacyclotricosane-14-carboxamideKi240.0 [1]
(2S,5R,8S,11S,14S,22S)-22-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-2-(2-amino-2-oxoethyl)-5-benzyl-8-[3-(diaminomethylideneamino)propyl]-11-(naphthalen-2-ylmethyl)-3,6,9,12,16,23-hexaoxo-1,4,7,10,13,17-hexazacyclotricosane-14-carboxamideKi255.0 [1]
(2S,5R,8S,11S,14S,22S)-22-[[(2R)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-2-(2-amino-2-oxoethyl)-5-benzyl-8-[3-(diaminomethylideneamino)propyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,17,23-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-14-carboxamideKi840.0 [1]
(2S,5R,8S,11S,14S,22S)-22-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-2-(2-amino-2-oxoethyl)-5-benzyl-8-[3-(diaminomethylideneamino)propyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,18,23-hexaoxo-1,4,7,10,13,17-hexazacyclotricosane-14-carboxamideKi295.0 [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-carboxamideIC501.0 [1]
N-(1-Naphthylmethyl)-N-(2-naphthylmethyl)amineKi1000000.0 [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-carboxamideKi6000.0 [1]
(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-carboxamideKi1500.0 [1]
(2S)-2-[[(2R)-2-Acetamido-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamideIC5010000.0 [1]
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]acetamideIC501938.0 [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]propanamideKi4200.0 [1]
(3R)-N-[(2R)-1-[4-[2-(Aminomethyl)phenyl]piperazin-1-yl]-3-(4-chlorophenyl)-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi27.0 [1]
Ac-His-Phe-Arg-DTrp-NH2IC506347.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-Amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamideKi51.0 [1]
(2S)-N-[(2R)-1-[4-(Tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-4-methylpiperazine-2-carboxamideIC501700.0 [1]
(2S)-2-Amino-N-[(2R)-1-(4-butanoyl-4-phenylpiperidin-1-yl)-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-3-(3-methylimidazol-4-yl)propanamideIC50120.0 [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-carboxamideKi12000.0 [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-carboxamideIC504900.0 [1]
1-[(2R)-2-[[(1S,2S)-1-Amino-1,2,3,4-tetrahydronaphthalene-2-carbonyl]amino]-3-(4-chlorophenyl)propanoyl]-N-tert-butyl-4-cyclohexylpiperidine-4-carboxamideIC50530.0 [1]
(3S,6S,9R,12S,15S,23S)-15-[[(2S)-2-Acetamidohexanoyl]amino]-9-benzyl-6-[3-(diaminomethylideneamino)propyl]-12-(1H-imidazol-5-ylmethyl)-3-[(1R)-1-(1H-indol-3-yl)ethyl]-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxamideIC5015.0 [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-carboxamideKi2300.0 [1]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-[4-[2-[(dimethylamino)methyl]phenyl]piperazin-1-yl]-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi20000.0 [1]
2-(1H-Indol-3-yl)-N-(1H-indol-3-ylmethyl)ethanamineKi32000.0 [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)propanamideKi8400.0 [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]methanoneKi3350.0 [1]
(2S)-2-[[(2S)-6-Amino-2-[[(2S)-1-[(2S)-1-[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-carboxypropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-carboxybutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]butanedioic acidKi0.89 [1]
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]propanamideKi5700.0 [1]
(1R,4S,6R)-N-[(2R)-1-[4-(Tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamideIC50750000.0 [1]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-[4-[2-(diethylamino)-1-(2-fluorophenyl)ethyl]piperazin-1-yl]-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi5800.0 [1]
(2S)-N-[(2S)-1-[(2-Amino-2-oxoethyl)amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]-2-[[(2R)-2-[[(2S)-2-(butanoylamino)-3-(1H-imidazol-5-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanamideIC50600.0 [1]
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]acetyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-[[(2S)-1-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic acidIC500.3 [1]
(2S)-2-[[(2R)-2-Acetamido-3-phenylpropanoyl]amino]-N-[(2R)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamideIC5010000.0 [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]-1-(pentanoylamino)-4-phenylcyclohexane-1-carboxamideIC507100.0 [1]
(2S)-N-[(2S)-1-Amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)-2-[[(2R)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(4-phenylbutanoylamino)propanoyl]amino]-3-phenylpropanoyl]amino]pentanamideKi0.17 [1]
N-[2-[4-[(3S,4R)-1-Tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperazin-1-yl]-2-cyclohexylethyl]-N-propan-2-ylmethanesulfonamideIC501000.0 [1]
2-(4-Acetylanilino)-N,N-bis(3-methylbutyl)-3-(3-piperidin-1-ylpropyl)benzimidazole-5-carboxamideKi5200.0 [1]
(3S,9S,17S,20S,23S,26R,29S)-9-[[(2S)-2-Acetamidohexanoyl]amino]-26-benzyl-23-[3-(diaminomethylideneamino)propyl]-20-(1H-indol-3-ylmethyl)-2,8,11,19,22,25,28-heptaoxo-1,7,12,18,21,24,27-heptazatricyclo[27.3.0.03,7]dotriacontane-17-carboxamideIC505000.0 [1]
(3S,9S,17S,20S,23S,26R,29S)-9-[[(2S)-2-Acetamidohexanoyl]amino]-23-[3-(diaminomethylideneamino)propyl]-20-(1H-indol-3-ylmethyl)-26-(naphthalen-2-ylmethyl)-2,8,11,19,22,25,28-heptaoxo-1,7,12,18,21,24,27-heptazatricyclo[27.3.0.03,7]dotriacontane-17-carboxamideIC505000.0 [1]
1-[(2R)-2-[(1-Amino-2,3-dihydro-1H-indene-2-carbonyl)amino]-3-(4-chlorophenyl)propanoyl]-N-tert-butyl-4-cyclohexylpiperidine-4-carboxamideIC501400.0 [1]
N-[(2R)-3-(4-Chlorophenyl)-1-[4-[2-(diethylamino)-1-(2-fluorophenyl)ethyl]piperazin-1-yl]-1-oxopropan-2-yl]-2-(1-methyl-2,3-dihydroisoindol-1-yl)acetamideKi20000.0 [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]-4-(4-ethoxyphenyl)-1-(pentanoylamino)cyclohexane-1-carboxamideIC504700.0 [1]
N-[(2R)-3-(4-Chlorophenyl)-1-[4-[2-(diethylamino)-1-(2-fluorophenyl)ethyl]piperazin-1-yl]-1-oxopropan-2-yl]-2-(2,3-dihydro-1H-isoindol-1-yl)acetamideKi6000.0 [1]
N-[2-[4-[(3S,4R)-1-Tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperazin-1-yl]-2-cyclohexylethyl]-N-propan-2-ylacetamideIC501800.0 [1]
N-[(2R)-3-(4-Chlorophenyl)-1-oxo-1-[4-[(1R,2R)-2-(1,2,4-triazol-1-yl)cyclohexyl]piperazin-1-yl]propan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi2000.0 [1]
1-[(2R)-2-[[(1S,2S)-1-Amino-1-methyl-3,4-dihydro-2H-naphthalene-2-carbonyl]amino]-3-(4-chlorophenyl)propanoyl]-N-tert-butyl-4-cyclohexylpiperidine-4-carboxamideIC50620.0 [1]
N-[(2R)-3-(4-Chlorophenyl)-1-[4-[2-(diethylamino)-1-(2-fluorophenyl)ethyl]piperazin-1-yl]-1-oxopropan-2-yl]-1,1-dimethyl-3,4-dihydro-2H-isoquinoline-3-carboxamideKi7000.0 [1]
N-[(2R)-3-(4-Chlorophenyl)-1-[4-[2-(diethylamino)-1-(2-fluorophenyl)ethyl]piperazin-1-yl]-1-oxopropan-2-yl]isoquinoline-3-carboxamideKi7000.0 [1]
1-[(2R)-2-[(5-Amino-6,7,8,9-tetrahydro-5H-benzo[7]annulene-6-carbonyl)amino]-3-(4-chlorophenyl)propanoyl]-N-tert-butyl-4-cyclohexylpiperidine-4-carboxamideIC50220.0 [1]
(3R)-N-[(2R)-3-(4-Chlorophenyl)-1-[4-[2-(imidazol-1-ylmethyl)phenyl]piperazin-1-yl]-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi4000.0 [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-(dimethylamino)-2-(pentanoylamino)-3,4-dihydro-1H-naphthalene-2-carboxamideIC5025500.0 [1]
(3S,6S,9S,12S,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-carboxamideIC5022.4 [1]
(3R,5R)-N-[(2R)-1-[4-(Tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,5-dimethylpiperazine-1-carboxamideIC502100.0 [1]
(3S,6S,9R,12S,15S,23S)-15-[[(2S)-2-Acetamidohexanoyl]amino]-9-benzyl-6-[3-(diaminomethylideneamino)propyl]-12-(1H-imidazol-5-ylmethyl)-3-[(1S)-1-(1H-indol-3-yl)ethyl]-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxamideIC500.5 [1]
(3R,6S,9R,12S,15S,23S)-15-[[(2S)-2-Acetamidohexanoyl]amino]-9-benzyl-6-[3-(diaminomethylideneamino)propyl]-12-(1H-imidazol-5-ylmethyl)-3-[(1S)-1-(1H-indol-3-yl)ethyl]-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxamideIC503.0 [1]
(2R)-2-Amino-N-[(2R)-1-(4-butanoyl-4-phenylpiperidin-1-yl)-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-3-(1H-imidazol-5-yl)propanamideIC5032.0 [1]
4-[[N-Cyclohexyl-C-[(2R,5S)-2,5-dimethylpiperazin-1-yl]carbonimidoyl]amino]-N-[2-(2,4-dichlorophenyl)ethyl]benzamideKi360.0 [1]
(2S,4R)-N,4-Dibenzyl-1-[(2S)-5-(diaminomethylideneamino)-2-[(2-naphthalen-1-ylacetyl)amino]pentanoyl]pyrrolidine-2-carboxamideKi5000.0 [1]
4-[(N-Cyclohexyl-C-piperazin-1-ylcarbonimidoyl)amino]-N-[2-(2,4-dichlorophenyl)ethyl]benzamideKi400.0 [1]
4-[(N'-Cyclohexyl-N-pyrrolidin-3-ylcarbamimidoyl)amino]-N-[2-(2,4-dichlorophenyl)ethyl]benzamideKi1900.0 [1]
(2S,5S,8R,11S,14S,17S)-5-(3-Amino-3-oxopropyl)-2-butyl-11-[3-(diaminomethylideneamino)propyl]-14-(1H-indol-3-ylmethyl)-8-(naphthalen-2-ylmethyl)-3,6,9,12,15,20-hexaoxo-1,4,7,10,13,16-hexazacycloicosane-17-carboxamideIC501000.0 [1]
3-[(2S,5S,8R,11S,14S,17S)-2-Butyl-17-carbamoyl-11-[3-(diaminomethylideneamino)propyl]-14-(1H-indol-3-ylmethyl)-8-(naphthalen-2-ylmethyl)-3,6,9,12,15,20-hexaoxo-1,4,7,10,13,16-hexazacycloicos-5-yl]propanoic acidIC5010000.0 [1]
c[Nle-His-D-Phe-Arg-Trp-Glu]-NH2IC5010000.0 [1]
c[Nle-Val-D-Phe-Arg-Trp-Glu]-NH2IC5010000.0 [1]
c[Nle-Asp-D-Phe-Arg-Trp-Glu]-NH2IC5010000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Melanocortin receptor 1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/melanocortin-receptor-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ Melanocortin receptor 1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/melanocortin-receptor-1-inhibitors-ic50-ki.
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