| (3S)-3-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-oxo-1-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]hexan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(4-aminobutyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 2.0 [1], 150.0 [2] |
| (3S)-3-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-12-(1H-indol-3-ylmethyl)-26-methyl-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 10000000.0 [1] |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-18-[[(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-methylbutanoyl]amino]-15-(2-amino-2-oxoethyl)-6-[(1R)-1-hydroxyethyl]-12-[(4-hydroxyphenyl)methyl]-26-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontane-23-carbonyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]pentanediamide | IC50 | 19000.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-4-[[(2S,3S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(4-aminobutyl)-9-[(2S)-butan-2-yl]-6-(3-carbamimidamidopropyl)-12-[(4-hydroxyphenyl)methyl]-26-(1H-imidazol-5-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acid | IC50 | 9000.0 [1] |
| (3S)-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-Amino-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(4-aminobutyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxo-3-[[(2S)-2-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]-3-phenylpropanoyl]amino]butanoic acid | IC50 | 1000.0 [1] |
| 2-[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-18-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-Acetamido-3-(1H-indol-3-yl)propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]-12-[(2S)-butan-2-yl]-23-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]carbamoyl]-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-3,9-bis(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-15-yl]acetic acid | IC50 | 100000.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 9000.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-15-(4-aminobutyl)-23-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 5000.0 [1] |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-3-carboxypropanoyl]amino]propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]-5-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2R,3R)-1-[[(2R)-1-[[(2R)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-9-[(2S)-butan-2-yl]-12-[(4-hydroxyphenyl)methyl]-15,26-bis(1H-imidazol-5-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-6-[4-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]butyl]-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid | IC50 | 1.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-4-[[(2S,3S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-15-(4-aminobutyl)-23-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-9-[(2S)-butan-2-yl]-6-(3-carbamimidamidopropyl)-12-[(4-hydroxyphenyl)methyl]-26-(1H-imidazol-5-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acid | IC50 | 9000.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(4R,7S,10S,13S,19S,22S,25S,28R)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-25-(2-amino-2-oxoethyl)-7-(1H-imidazol-5-ylmethyl)-22-(1H-indol-3-ylmethyl)-10-methyl-13-(2-methylpropyl)-6,9,12,15,18,21,24,27-octaoxo-19-propan-2-yl-1,2-dithia-5,8,11,14,17,20,23,26-octazacyclononacos-28-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 5000.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-15-(4-aminobutyl)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1,6-dioxohexan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 1000.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1,6-dioxohexan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 1000.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-methyl-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 10000000.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(4-aminobutyl)-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 6000.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(4-aminobutyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 1000.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 1000.0 [1] |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Acetamidopropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]-methylamino]-5-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2R,3R)-1-[[(2R)-1-[[(2R)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-9-[(2S)-butan-2-yl]-12-[(4-hydroxyphenyl)methyl]-15,26-bis(1H-imidazol-5-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-6-[4-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]butyl]-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid | IC50 | 3.0 [1] |
| (3S)-3-[[(2S)-2-Acetamido-4-methylpentanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]-6-(hydroxymethyl)-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3,15-bis(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | IC50 | 100000.0 [1] |
| (3S)-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-Acetamido-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxo-6-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]hexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-oxobutanoic acid | IC50 | 4.0 [1] |
| (4S)-5-[[(2S)-1-[[(4R,7S,13S,16S,19S,22S,25S,28R)-4-[[(2R,3R)-1-[[(2S)-6-Acetamido-1-[(1-amino-2-methyl-1-oxopropan-2-yl)amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-19-[(2S)-butan-2-yl]-22-[(4-hydroxyphenyl)methyl]-7,25-bis(1H-imidazol-5-ylmethyl)-10,10-dimethyl-13-(2-methylpropyl)-6,9,12,15,18,21,24,27-octaoxo-16-[4-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]butyl]-1,2-dithia-5,8,11,14,17,20,23,26-octazacyclononacos-28-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamidopropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]-methylamino]-5-oxopentanoic acid | IC50 | 0.4 [1] |
| (3S)-3-[[(2S)-2-Acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-4-[[(2S,3S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]-9-[(2S)-butan-2-yl]-6-(3-carbamimidamidopropyl)-12-[(4-hydroxyphenyl)methyl]-15,26-bis(1H-imidazol-5-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acid | IC50 | 100000.0 [1] |