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Insulin-degrading enzyme 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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(4S)-5-Amino-4-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2R,3S)-3-hydroxy-4-(hydroxyamino)-2-(naphthalen-2-ylmethyl)-4-oxobutanoyl]amino]pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-oxopentanoic acidKi25.9 [1], 70.3 [2], 275.0 [3]
(4S)-5-Amino-4-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2R,3R)-3-hydroxy-4-(hydroxyamino)-2-(naphthalen-2-ylmethyl)-4-oxobutanoyl]amino]pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-oxopentanoic acidKi103.0 [1], 927.0 [2], 1890.0 [3]
Prop-2-enyl (2S)-5-(diaminomethylideneamino)-2-[[(2R)-4-(hydroxyamino)-2-(naphthalen-2-ylmethyl)-4-oxobutanoyl]amino]pentanoateKi87.0 [1], 107.0 [2], 1280.0 [3]
(4R)-4-Amino-5-[[(2R)-1-[[(2R)-5-(diaminomethylideneamino)-1-[[(2R)-1-(hydroxyamino)-3-naphthalen-2-yl-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acidKi85.1 [1], 365.0 [2], 833.0 [3]
5-[2-[[(4S)-4-Acetamido-5-[[(2R)-1-[benzoyl-[(2R)-1-[[(2R)-1-(hydroxyamino)-3-naphthalen-2-yl-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-oxopentanoyl]amino]ethylamino]naphthalene-1-sulfonic acidKi1.4 [1], 43.7 [2], 410.0 [3]
(4R)-4-Amino-5-[[(2R)-1-[[(2R)-5-(diaminomethylideneamino)-1-[[(2R)-1-(hydroxyamino)-3-naphthalen-2-yl-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acidKi49.8 [1], 228.0 [2], 3260.0 [3]
2-[(2R,5R,8R,11R,14R,17R)-8-Benzyl-11-[(2R)-butan-2-yl]-17-[[(2R)-1-[[(2R)-5-carbamimidamido-1-[[(2R)-1-(hydroxyamino)-3-naphthalen-2-yl-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]carbamoyl]-14-(3-carbamimidamidopropyl)-5-(1H-imidazol-5-ylmethyl)-3,6,9,12,15,20-hexaoxo-1,4,7,10,13,16-hexazacycloicos-2-yl]acetic acidKi23.1 [1], 171.0 [2], 246.0 [3]
(4S)-5-Amino-4-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2R)-4-(hydroxyamino)-2-(naphthalen-2-ylmethyl)-4-oxobutanoyl]amino]pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-oxopentanoic acidKi2.96 [1], 21.7 [2], 37.9 [3]
N-(Carboxymethyl)-N-(3-Phenylpropyl)glycyl-N-Methyl-L-HistidinamideIC50100.0 [1], 3100.0 [2]
2-[Benzoyl-[2-[[(2S)-3-(1H-imidazol-5-yl)-1-methoxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]acetic acidIC50100000.0 [1]
2-[Benzyl-[2-[[(2S)-1-methoxy-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]acetic acidIC50100000.0 [1]
Methyl N-(Carboxymethyl)-N-(2-Phenylethyl)glycyl-L-HistidinateIC501400.0 [1]
2-[Benzyl-[2-[[(2S)-3-(1H-imidazol-5-yl)-1-(methylamino)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]acetic acidIC50600.0 [1]
Methyl 2-[[2-[[(2S)-3-(1H-imidazol-5-yl)-1-(methylamino)-1-oxopropan-2-yl]amino]-2-oxoethyl]-(3-phenylpropyl)amino]acetateIC50100000.0 [1]
Methyl N-(Carboxymethyl)-N-(3-Phenylpropyl)glycyl-L-HistidinateIC50600.0 [1]
(2R,3S)-N-[(2S)-1-Amino-6-(diaminomethylideneamino)-1-oxohexan-2-yl]-N',3-dihydroxy-2-(naphthalen-2-ylmethyl)butanediamideKi33000.0 [1]
(2R)-N-[(2S)-1-Amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-N'-hydroxy-2-(naphthalen-2-ylmethyl)butanediamideKi1150.0 [1]
(2S)-N-[(2S)-1-Amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-N'-hydroxy-2-(naphthalen-2-ylmethyl)butanediamideKi33000.0 [1]
(2R,3S)-N-[(2S)-1-[[(2S)-1-Amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-N',3-dihydroxy-2-(naphthalen-2-ylmethyl)butanediamideKi18000.0 [1]
(2R,3R)-N-[(2S)-1-[[(2S)-1-Amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-N',3-dihydroxy-2-(naphthalen-2-ylmethyl)butanediamideKi498.0 [1]
(2R,3S)-N-[(2S)-1-Amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-N',3-dihydroxy-2-(naphthalen-2-ylmethyl)butanediamideKi7750.0 [1]
(2R,3R)-N-[(2S)-1-Amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-N',3-dihydroxy-2-(naphthalen-2-ylmethyl)butanediamideKi7020.0 [1]
(2R)-N-[(2S)-1-Amino-6-(diaminomethylideneamino)-1-oxohexan-2-yl]-N'-hydroxy-2-(naphthalen-2-ylmethyl)butanediamideKi33000.0 [1]
(2S)-N-[(2S)-1-Amino-6-(diaminomethylideneamino)-1-oxohexan-2-yl]-N'-hydroxy-2-(naphthalen-2-ylmethyl)butanediamideKi33000.0 [1]
Prop-2-enyl (2S)-5-(diaminomethylideneamino)-2-[[(2S)-4-(hydroxyamino)-2-(naphthalen-2-ylmethyl)-4-oxobutanoyl]amino]pentanoateKi5280.0 [1]
(4S)-5-Amino-4-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-4-(hydroxyamino)-2-(naphthalen-2-ylmethyl)-4-oxobutanoyl]amino]pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-oxopentanoic acidKi73.3 [1]
(4S)-4-Acetamido-5-[[(2S)-1-[[(4S,6S)-1-(diaminomethylideneamino)-8-(hydroxyamino)-6-(naphthalen-2-ylmethyl)-5,8-dioxooctan-4-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acidKi78.0 [1]
4-Fluoro-N-[[1-[(2R)-4-(hydroxyamino)-1-naphthalen-2-yl-4-oxobutan-2-yl]triazol-4-yl]methyl]benzamideIC5056.0 [1]
(4S,7R,17E)-7-[(4-Benzoylphenyl)methyl]-4-(cyclohexylmethyl)-2,5,8,16,19-pentaoxo-1,3,6,9,15-pentazacyclononadec-17-ene-14-carboxamideIC5020000.0 [1]
(6S,9S,12E,16S)-9-(3-Amino-3-oxopropyl)-6-(cyclohexylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC50100000.0 [1]
(6S,10R,11S,14E,18S)-6,11-Bis(cyclohexylmethyl)-10-hydroxy-2,5,8,13,16-pentaoxo-1,4,7,12,17-pentazacyclodocos-14-ene-18-carboxamideIC50100000.0 [1]
(5S,8S,11R,18S)-5-(3-Amino-3-oxopropyl)-11-[(4-benzoylphenyl)methyl]-8-(cyclohexylmethyl)-3,6,9,12,20-pentaoxo-2,21-dioxa-4,7,10,13,19,25-hexazabicyclo[20.2.1]pentacosane-18-carboxamideIC50570.0 [1]
(6S,9S,12E,16S)-9-(3-Amino-3-oxopropyl)-3-benzyl-6-(cyclohexylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC5010000.0 [1]
(3R,9S,12E,16S)-9-(3-Amino-3-oxopropyl)-3-[(4-benzoylphenyl)methyl]-6-benzyl-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC506000.0 [1]
(3R,9S,12E,16S)-9-(3-Amino-3-oxopropyl)-3-[(4-benzoylphenyl)methyl]-6-butyl-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC501500.0 [1]
(3R,9S,12E,16S)-9-(3-Amino-3-oxopropyl)-3-[(4-benzoylphenyl)methyl]-6-(2-methylpropyl)-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC502100.0 [1]
(2S)-2-[[(E)-4-[[(2S)-1-Amino-6-[[(2R)-3-(4-benzoylphenyl)-2-(2-methylpropanoylamino)propanoyl]amino]-1-oxohexan-2-yl]amino]-4-oxobut-2-enoyl]amino]pentanediamideIC5010000.0 [1]
(3R,6S,9R,12E)-3-[(4-Benzoylphenyl)methyl]-6-(cyclohexylmethyl)-9-methyl-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC5020000.0 [1]
(3R,6S,12E)-3-[(4-Benzoylphenyl)methyl]-6-(cyclohexylmethyl)-9-(hydroxymethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC5060.0 [1]
(3R,6S,12E)-3-[(4-Benzoylphenyl)methyl]-6-(cyclohexylmethyl)-9,9-dimethyl-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC50370.0 [1]
(3R,6S,12E)-3-[(4-Benzoylphenyl)methyl]-6-(cyclohexylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC50500.0 [1]
(3R,6S,12E)-3-[(4-Benzoylphenyl)methyl]-9-benzyl-6-(cyclohexylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC503200.0 [1]
(3R,6S,9S,12E)-9-(4-Aminobutyl)-3-[(4-benzoylphenyl)methyl]-6-(cyclohexylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC5065.0 [1]
3-[(3R,6S,12E)-3-[(4-Benzoylphenyl)methyl]-16-carbamoyl-6-(cyclohexylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-en-9-yl]propanoic acidIC5085.0 [1]
(4Z,8S,11S,14R)-8-(3-Amino-3-oxopropyl)-14-[(4-benzoylphenyl)methyl]-11-(cyclohexylmethyl)-3,6,9,12,15-pentaoxo-1,2,7,10,13,16,21-heptazacyclohexacos-4-ene-22-carboxamideIC507000.0 [1]
5-[(3As,4S,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]-N-[3-[2-[2-[2-[(4Z,8S,11S,14R)-8-(3-amino-3-oxopropyl)-14-[(4-benzoylphenyl)methyl]-11-(cyclohexylmethyl)-3,6,9,12,15-pentaoxo-1,2,7,10,13,16,21-heptazacyclohexacos-4-en-22-yl]-2-oxoethoxy]ethoxy]ethoxy]propyl]pentanamideIC5080.0 [1]
(4Z,8S,11S,14R)-8-(3-Amino-3-oxopropyl)-14-[(4-benzoylphenyl)methyl]-11-(cyclohexylmethyl)-3,6,9,12,15-pentaoxo-1,2,7,10,13,16,21-heptazacyclohexacos-4-ene-22-carboxylic acidIC5054.0 [1]
(4Z,8S,11S,14R)-8-(3-Amino-3-oxopropyl)-14-[(4-benzoylphenyl)methyl]-11-(cyclohexylmethyl)-3,6,9,12,15-pentaoxo-1,2,7,10,13,16,21-heptazacyclopentacos-4-ene-22-carboxamideIC505000.0 [1]
(4Z,8S,11S,14R)-8-(3-Amino-3-oxopropyl)-14-[(4-benzoylphenyl)methyl]-11-(cyclohexylmethyl)-N-ethyl-3,6,9,12,15-pentaoxo-1,2,7,10,13,16,21-heptazacyclopentacos-4-ene-22-carboxamideIC5060.0 [1]
3-[(4Z,8S,11S,14R)-14-[(4-Benzoylphenyl)methyl]-11-(cyclohexylmethyl)-22-[2-[2-[2-(6'-hydroxy-3-oxospiro[2-benzofuran-1,9'-xanthene]-3'-yl)peroxyethoxy]ethoxy]acetyl]-3,6,9,12,15-pentaoxo-1,2,7,10,13,16,21-heptazacyclohexacos-4-en-8-yl]propanamideIC50100.0 [1]
(6S,9S,12E,16S)-9-(3-Amino-3-oxopropyl)-3-[(4-benzoylphenyl)methyl]-6-(cyclohexylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC5060.0 [1]
(3R,6S,9S,12E)-3-[(4-Benzoylphenyl)methyl]-6-(cyclohexylmethyl)-9-methyl-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC5060.0 [1]
(3R,6S,9S,12E,16S)-9-(3-Amino-3-oxopropyl)-3-[(4-benzoylphenyl)methyl]-6-(cyclohexylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC5060.0 [1]
(3R,6S,10R,11S,14E,18S)-3-[(4-Benzoylphenyl)methyl]-6,11-bis(cyclohexylmethyl)-10-hydroxy-2,5,8,13,16-pentaoxo-1,4,7,12,17-pentazacyclodocos-14-ene-18-carboxamideIC5020000.0 [1]
(3R,6S,9S,12E,16S)-3-[(4-Benzoylphenyl)methyl]-6-(cyclohexylmethyl)-9-[3-(diaminomethylideneamino)propyl]-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC50150.0 [1]
(3R,6S,9S,12E,16S)-3-[(4-Benzoylphenyl)methyl]-6-(cyclohexylmethyl)-9-(cyclopropylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,15-pentazacycloicos-12-ene-16-carboxamideIC501000.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Insulin-degrading enzyme Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 8 May. 2024, https://www.aatbio.com/data-sets/insulin-degrading-enzyme-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, May 8). Quest Database™ Insulin-degrading enzyme Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/insulin-degrading-enzyme-inhibitors-ic50-ki.
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