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Neurotensin receptor 1 Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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NeurotensinIC501.4 [1], 6.03 [2]
NeurotensinKi1.64 [1], 2.1 [2]
Neurotensin(8-13)IC500.41 [1], 0.8 [2], 0.82 [3]
Neurotensin(8-13)Ki0.24 [1], 1.07 [2], 1.29 [3]
(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC500.3 [1]
(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi0.14 [1], 0.27 [2], 0.29 [3], 1.05 [4]
(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]-methylamino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi5.1 [1], 1400.0 [2], 4100.0 [3], 5100.0 [4], 7100.0 [5]
2-[[5-(2,6-Dimethoxyphenyl)-1-[4-[3-(dimethylamino)propyl-methylcarbamoyl]-2-propan-2-ylphenyl]pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acidIC503.16 [1], 4.0 [2]
2-[[5-(2,6-Dimethoxyphenyl)-1-[4-[3-(dimethylamino)propyl-methylcarbamoyl]-2-propan-2-ylphenyl]pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acidKi1.0 [1]
Demotensin 4IC500.51 [1], 0.85 [2], 2.9 [3]
MeclinertantIC500.99 [1], 82.0 [2]
Nalphame-Arg-Lys-Pro-Trp-Tle-LeuKi95.0 [1], 180.0 [2]
H-Lys-lys-pro-tyr-ile-leu-OHIC500.33 [1]
H-Lys-lys-pro-tyr-ile-leu-OHKi2.7 [1]
(2R)-4-Methyl-2-[[2-[5-(quinolin-8-ylsulfonylamino)indol-1-yl]acetyl]amino]pentanoic acidIC503.76 [1]
(2R)-4-Methyl-2-[[2-[5-(quinolin-8-ylsulfonylamino)indol-1-yl]acetyl]amino]pentanoic acidKi545.0 [1]
2-[[5-(2,6-Dimethoxyphenyl)-1-[4-[3-(dimethylamino)propyl-methylcarbamoyl]-2-propan-2-ylphenyl]pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid;hydrochlorideIC500.24 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[3-(2-Aminoethylamino)-2-[(2-aminoethylamino)methyl]propanoyl]amino]acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC500.14 [1], 0.32 [2]
(2R)-2-[[(2S,3S)-2-[[(2S)-2-[[(2R)-1-[(2R)-2-[[(2S)-2-Amino-5-[[amino-[4-[6-[(2Z)-3,3-dimethyl-2-[(2E,4E)-5-(1,3,3-trimethylindol-1-ium-2-yl)penta-2,4-dienylidene]indol-1-yl]hexanoylamino]butylcarbamoylamino]methylidene]amino]pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid;2,2,2-trifluoroacetic acid;bromideKi4.1 [1], 7.9 [2]
Demotensin 3IC500.66 [1], 1.5 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(3S)-7-Amino-3-azidoheptanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidKi4.5 [1], 5.49 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(3S)-3,7-Diamino-3-methylheptanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidKi9.9 [1], 10.4 [2]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[6-Amino-2-[[2-[[3-(2-aminoethylamino)-2-[(2-aminoethylamino)methyl]propanoyl]amino]acetyl]amino]hexyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC500.18 [1], 0.41 [2]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-[[amino-(4-aminobutylcarbamoylamino)methylidene]amino]pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC501.35 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-[[amino-(4-aminobutylcarbamoylamino)methylidene]amino]pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi0.69 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-[[amino-[4-(propanoylamino)butylcarbamoylamino]methylidene]amino]pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC501.35 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-[[amino-[4-(propanoylamino)butylcarbamoylamino]methylidene]amino]pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi0.63 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-[[amino-[2-[2-[2-(propanoylamino)ethoxy]ethoxy]ethylcarbamoylamino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC501.74 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-[[amino-[2-[2-[2-(propanoylamino)ethoxy]ethoxy]ethylcarbamoylamino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi1.7 [1]
CipargaminIC5010000.0 [1]
4-(4-Butylpiperidin-1-yl)-1-o-tolylbutan-1-oneKi1000.0 [1]
Arg-Pro-Tyr-Ile-LeuIC5019.0 [1]
N-[3-Chloro-4-[[[2-(methylamino)-6-pyridin-2-ylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamideIC5030000.0 [1]
(2S)-2-[[1-(7-Chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]-4-methylpentanoic acidKi3300.0 [1]
2-({[(9H-Fluoren-9-YL)methoxy]carbonyl}amino)-4-methylpentanoic acidIC503.79 [1]
N-[1-[3-(3-Oxo-1,4-benzoxazin-4-yl)propyl]piperidin-4-yl]-2-phenylacetamideKi1000.0 [1]
(2S)-2-[[1-(7-Chloroquinolin-4-yl)-2-(2,6-dimethoxyphenyl)imidazole-4-carbonyl]amino]-4-methylpentanoic acidKi10000.0 [1]
(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi1.81 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[2-[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidin-2-yl]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi47.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-4-(4-hydroxyphenyl)butanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi210.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-Amino-2-[[2-(4-aminobutylamino)acetyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi1.6 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[2-[4-Aminobutyl-[(2S)-2,6-diaminohexanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi17.0 [1]
(2S)-2-[[(2S,3S)-2-[[2-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]-[(4-hydroxyphenyl)methyl]amino]acetyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi30000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-(7-Aminoheptanoylamino)-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidKi2.99 [1]
(2S)-2-[[(3S,6S,11S,14S,17S)-3-(4-Aminobutyl)-6-[3-(diaminomethylideneamino)propyl]-14-(1H-indol-3-ylmethyl)-2,5,8,13,16-pentaoxo-1,4,7,12,15-pentazabicyclo[15.3.0]icosane-11-carbonyl]amino]-4-methylpentanoic acidKi190.0 [1]
H-Arg-N-Me-Arg-Pro-Tyr-Ile-Leu-OHKi0.51 [1]
(2S)-2-[[(2S,3S)-2-[[(3S,6S,12S)-12-[3-(Diaminomethylideneamino)propyl]-5,11,14-trioxo-20-oxa-4,10,13-triazatricyclo[19.2.2.06,10]pentacosa-1(24),21(25),22-triene-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi450.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(5R)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]-3,3-dimethyl-1,3-azasilolidine-5-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC5015.2 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-5-(3-Aminopropylamino)-2-azidopentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC503.9 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[2-[2-[Bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC500.4 [1]
(2S)-2-[[(3S,6S,14S,17S,20S)-3-(4-Aminobutyl)-6-[3-(diaminomethylideneamino)propyl]-17-(1H-indol-3-ylmethyl)-7-methyl-2,5,8,11,16,19-hexaoxo-1,4,7,10,15,18-hexazabicyclo[18.3.0]tricosane-14-carbonyl]amino]-4-methylpentanoic acidKi3500.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2R)-6-Amino-2-[[2-[2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1-carbamimidoylpiperidin-4-yl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidIC502.5 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-3-[4-(Aminomethyl)cyclohexyl]-2-[[2-[2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-2-(1-carbamimidoylpiperidin-4-yl)acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidIC500.3 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2R)-6-Amino-2-[[2-[2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-4-(2-aminopyrimidin-4-yl)butanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC5010.2 [1]
(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2R)-6-Amino-2-[[2-[2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-2-(1-carbamimidoylpiperidin-4-yl)acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidIC500.6 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2R)-6-Amino-2-[[2-[2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-2-(1-carbamimidoylpiperidin-4-yl)acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(3-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidIC50106.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[2-[2-[2-[Bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetyl]amino]-2-piperidin-4-ylacetyl]pyrrolidine-2-carbonyl]amino]-2-(1-carbamimidoylpiperidin-4-yl)acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidIC500.3 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2R)-6-Amino-2-[[2-[2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-4-(1-carbamimidoylpiperidin-4-yl)butanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidIC506.3 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2R)-6-Amino-2-[[2-[2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidIC5024.6 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2R)-6-Amino-2-[[2-[2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-2-(1-carbamimidoylpiperidin-4-yl)acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidIC500.4 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[(5S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]-6-oxo-1,7-diazaspiro[4.4]nonan-7-yl]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi17000.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[(5R)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]-6-oxo-1,7-diazaspiro[4.4]nonan-7-yl]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi12.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-Amino-5-[[amino-[[(2S)-2,7-diaminoheptanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acidIC505.71 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2R)-6-Amino-2-[[2-[2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC500.5 [1]
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-trimethylsilylpropanoyl]amino]-4-methylpentanoic acidIC5093.8 [1]
(2R)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-trimethylsilylpropanoic acidIC500.02 [1]
(2R)-2-[[(2R)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-trimethylsilylpropanoyl]amino]-3-trimethylsilylpropanoic acidIC5015.4 [1]
(2S)-2-[[(2R)-2-[[(2S)-2-[[(5R)-1-[(2S)-6-Amino-2-[[(2S)-2,7-diaminoheptanoyl]amino]hexanoyl]-3,3-dimethyl-1,3-azasilolidine-5-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-trimethylsilylpropanoyl]amino]-4-methylpentanoic acidIC50968.0 [1]
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-5-(diaminomethylideneamino)-2-(methylamino)pentanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-trimethylsilylpropanoyl]amino]-4-methylpentanoic acidIC50246.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2,6-Bis[[3',6'-dihydroxy-6-[(C-sulfanylcarbonimidoyl)amino]spiro[1H-2-benzofuran-3,9'-xanthene]-1-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-carbamimidoylcyclohexyl)acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC503.4 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-Amino-6-[[6-(carbamothioylamino)-3',6'-dihydroxyspiro[1H-2-benzofuran-3,9'-xanthene]-1-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-carbamimidoylcyclohexyl)acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC500.6 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-Amino-2-[[6-(carbamothioylamino)-3',6'-dihydroxyspiro[1H-2-benzofuran-3,9'-xanthene]-1-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-carbamimidoylcyclohexyl)acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidIC501.2 [1]
(2S)-2-[[2-[[(2R,3S)-3-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-hydroxyphenyl)oxolane-3-carbonyl]amino]acetyl]amino]-4-methylpentanoic acidKi20000.0 [1]
(2S)-2-[[2-[[3-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-bromophenyl)oxolane-3-carbonyl]amino]acetyl]amino]-4-methylpentanoic acidKi50000.0 [1]
(2S)-2-[[3-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-bromophenyl)oxolane-3-carbonyl]amino]-4-methylpentanoic acidKi95500.0 [1]
(2S)-2-[[2-(4-Bromophenyl)-3-[[(2S)-1-[(2S)-2-[[(2S)-2,6-diaminohexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]oxolane-3-carbonyl]amino]-4-methylpentanoic acidKi53000.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2R,3S)-3-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-bromophenyl)oxolane-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi13000.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2R,3S)-3-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-bromophenyl)oxolane-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi10000.0 [1]
(2S)-2-[[3-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-bromophenyl)oxolane-3-carbonyl]amino]-4-methylpentanoic acidKi91500.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2R,3S)-2-(4-Bromophenyl)-3-[[(2S)-1-[(2S)-2-[[(2S)-2,6-diaminohexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]oxolane-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi5000.0 [1]
(2S)-2-[[(2S,3S)-2-[[3-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-bromophenyl)oxolane-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi870.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2R,3S)-3-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-bromophenyl)oxolane-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi10000.0 [1]
(2S)-2-[[3-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-bromophenyl)oxolane-3-carbonyl]amino]-4-methylpentanoic acidKi70500.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2R)-2-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-bromophenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi2170.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-bromophenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi93.0 [1]
(2S)-2-[[2-[[(2S,3R)-3-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-hydroxyphenyl)oxolane-3-carbonyl]amino]acetyl]amino]-4-methylpentanoic acidKi35000.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2R,3S)-3-[[(2S)-1-[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-2-(4-hydroxyphenyl)oxolane-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi7.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi10000.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-6-Amino-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi5700.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi10000.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-Amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi455.6 [1]
(2S)-2-[[(2S,3S)-2-[[5-Amino-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi10000.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-6-Amino-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]-3-trimethylsilylpropanoic acidKi662.7 [1]
(2S)-2-[[(2S,3S)-2-[[(3R,6S,12S,15R)-15-Amino-12-(4-aminobutyl)-26-hydroxy-5,11,14-trioxo-4,10,13,20-tetrazatricyclo[23.3.1.06,10]nonacosa-1(29),22,25,27-tetraene-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi772.0 [1]
(2S)-2-[[(2S,3S)-2-[[(3R,6S,12S,15S)-15-Amino-12-(4-aminobutyl)-24-hydroxy-5,11,14-trioxo-4,10,13,18-tetrazatricyclo[21.3.1.06,10]heptacosa-1(27),20,23,25-tetraene-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi155.0 [1]
(2S)-2-[[(2S,3S)-2-[[(3R,6S,12R)-12-(4-Aminobutyl)-25-hydroxy-5,11,14-trioxo-4,10,13-triazatricyclo[22.3.1.06,10]octacosa-1(28),21,24,26-tetraene-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi5600.0 [1]
(2S)-2-[[(2S,3S)-2-[[(3R,6S,12S,15S)-15-Amino-12-(4-aminobutyl)-26-hydroxy-20-(2-nitrophenyl)sulfonyl-5,11,14-trioxo-4,10,13,20-tetrazatricyclo[23.3.1.06,10]nonacosa-1(29),22,25,27-tetraene-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi328.0 [1]
2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-Amino-2-(non-8-enoylamino)hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxy-3-prop-2-enylphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi10000.0 [1]
(2S)-2-[[(2S,3S)-2-[[(3R,6S,12S,15S)-15-Amino-12-(4-aminobutyl)-26-hydroxy-5,11,14-trioxo-4,10,13,20-tetrazatricyclo[23.3.1.06,10]nonacosa-1(29),22,25,27-tetraene-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi43.0 [1]
(2S)-2-[[(2S,3S)-2-[[(3R,6S,12S,15S)-15-Amino-12-(4-aminobutyl)-28-hydroxy-5,11,14-trioxo-4,10,13,20-tetrazatricyclo[25.3.1.06,10]hentriaconta-1(31),24,27,29-tetraene-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acidKi903.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Neurotensin receptor 1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 22 Feb. 2025, https://www.aatbio.com/data-sets/neurotensin-receptor-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 22). Quest Database™ Neurotensin receptor 1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/neurotensin-receptor-1-inhibitors-ic50-ki.
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