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Proteasome Macropain subunit MB1 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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BortezomibIC504.68 [1]
BortezomibKi0.55 [1], 0.6 [2], 9.8 [3]
Z-Leu-leu-leu-alIC509.0 [1], 11.0 [2], 25.0 [3], 37.0 [4]
Z-Leu-leu-leu-alKi1.4 [1], 3.7 [2], 4.0 [3], 70.0 [4]
5-Aminoquinolin-8-olIC50600.0 [1]
LactacystinIC50160.0 [1], 370.0 [2], 500.0 [3], 4960.0 [4], 10090.0 [5]
1-[2-[4-[1-[4-[2-(Azepan-1-yl)ethoxy]phenyl]-2-phenylbut-1-enyl]phenoxy]ethyl]azepaneIC50640.0 [1], 1020.0 [2], 11000.0 [3], 100000.0 [4]
1-[2-[4-[1-[4-[2-(Azepan-1-yl)ethoxy]phenyl]-2-phenylbut-1-enyl]phenoxy]ethyl]azepaneKi580.0 [1]
(2S)-N-[(2S)-1-[[(E,2S)-1-[4-(Aminomethyl)phenyl]-4-methylsulfonylbut-3-en-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-2-[[(2S)-2-azido-3-phenylpropanoyl]amino]-4-methylpentanamideIC501200.0 [1], 1700.0 [2], 2600.0 [3], 5800.0 [4], 50000.0 [5]
N-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-Amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]-3-[1,1-bis[4-[2-(azepan-1-yl)ethoxy]phenyl]but-1-en-2-yl]benzamideIC502400.0 [1], 5500.0 [2], 5700.0 [3], 6300.0 [4], 50000.0 [5]
N-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-Acetamido-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]-3-[1,1-bis[4-[2-(azepan-1-yl)ethoxy]phenyl]but-1-en-2-yl]benzamideIC502100.0 [1], 6000.0 [2], 9400.0 [3], 40000.0 [4]
IxazomibIC503.0 [1], 3.4 [2], 7.73 [3], 9.0 [4]
Tert-butyl N-[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]carbamateIC503190.0 [1], 7970.0 [2]
Tert-butyl N-[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]carbamateKi2430.0 [1], 5030.0 [2]
(2S)-N-[(E,2S)-1-[4-(Aminomethyl)phenyl]-4-methylsulfonylbut-3-en-2-yl]-2-[[(2S)-3-(4-aminophenyl)-2-[[(2S)-2-azido-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanamideIC502800.0 [1], 3600.0 [2], 7200.0 [3], 50000.0 [4]
(2S)-2-[[(2S)-3-[4-(Aminomethyl)phenyl]-2-[[(2S)-2-azido-3-phenylpropanoyl]amino]propanoyl]amino]-N-[(E,2S)-1-[4-(aminomethyl)phenyl]-4-methylsulfonylbut-3-en-2-yl]-4-methylpentanamideIC5010500.0 [1], 21000.0 [2], 27000.0 [3], 50000.0 [4]
Tert-butyl N-[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]carbamateIC50252.0 [1], 460.0 [2]
Tert-butyl N-[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]carbamateKi101.0 [1], 316.0 [2]
(2S)-N-[(2S)-1-[(2-Chlorophenyl)methylamino]-1-oxo-3-pyridin-4-ylpropan-2-yl]-N'-(2,2-dimethylpropyl)-2-[[2-(1H-indol-3-yl)-2-oxoacetyl]amino]butanediamideIC501.1 [1], 1.2 [2], 9.5 [3]
VorinostatIC5025000.0 [1]
CarfilzomibIC508.4 [1], 9.6 [2]
EpoxomicinIC503.7 [1], 26.0 [2], 47.0 [3]
RicolinostatIC5025000.0 [1]
Onx-0914 (PR-957)IC50150.0 [1], 422.0 [2], 1000.0 [3]
[4-[(1E,6E)-7-[4-[(2S)-2-Amino-3-methylbutanoyl]oxy-3-methoxyphenyl]-3,5-dioxohepta-1,6-dienyl]-2-methoxyphenyl] (2S)-2-amino-3-methylbutanoateIC505000.0 [1], 10000.0 [2]
[(1R)-3-Methyl-1-[[2-(5-oxo-1,6-naphthyridin-6-yl)acetyl]amino]butyl]boronic acidKi440.0 [1]
[(1R)-1-[[2-(8-Bromo-5-oxo-1,6-naphthyridin-6-yl)acetyl]amino]-3-methylbutyl]boronic acidKi170.0 [1]
(2S)-2-Amino-N-[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-3-(4-phenylmethoxyphenyl)propanamideIC5011600.0 [1]
(2S)-2-Amino-N-[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-3-(4-phenylmethoxyphenyl)propanamideKi24500.0 [1]
1-N-[(2S)-1-[[(2S)-1-(Benzylamino)-1-oxopropan-2-yl]amino]-4-(2,2-dimethylpropylamino)-1,4-dioxobutan-2-yl]-4-N-hydroxybenzene-1,4-dicarboxamideIC50260.0 [1], 394.2 [2], 820.5 [3]
(2S)-N-[(E,2S)-1-[4-(Aminomethyl)phenyl]-4-methylsulfonylbut-3-en-2-yl]-2-[[(2S)-2-[[(2S)-2-azido-3-phenylpropanoyl]amino]-3-pyridin-4-ylpropanoyl]amino]-4-methylpentanamideIC505500.0 [1], 10500.0 [2], 50000.0 [3]
Tert-butyl N-[6-[[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]carbamateIC50707.0 [1]
Tert-butyl N-[6-[[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]carbamateKi67.0 [1], 200.0 [2]
N'-[(2S)-1-[[(2S)-1-[[(2S)-1-(Benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]-N-[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]hexanediamideIC5025.8 [1], 541.0 [2]
N'-[(2S)-1-[[(2S)-1-[[(2S)-1-(Benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]-N-[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]hexanediamideKi10.3 [1]
N'-[(2S)-1-[[(2S)-1-[[(2S)-1-(Benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]-N-[6-[[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]hexanediamideIC5025.9 [1], 756.0 [2]
N'-[(2S)-1-[[(2S)-1-[[(2S)-1-(Benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]-N-[6-[[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]hexanediamideKi10.8 [1]
N'-[(2S)-1-[[(2S)-1-[[(2S)-1-(Benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]-N-[6-[[6-[[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]hexanediamideIC5022.7 [1], 472.0 [2]
N'-[(2S)-1-[[(2S)-1-[[(2S)-1-(Benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]-N-[6-[[6-[[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]hexanediamideKi11.4 [1]
N,N'-Bis[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]hexanediamideIC5019.1 [1], 476.0 [2]
N,N'-Bis[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]hexanediamideKi10.6 [1]
VincaleukoblastineIC504580.0 [1], 40000.0 [2]
MarizomibIC503.5 [1], 22.0 [2]
[(1R)-3-Methyl-1-[[(2S)-3-phenyl-2-(5,6,7,8-tetrahydronaphthalene-1-carbonylamino)propanoyl]amino]butyl]boronic acidIC501.6 [1], 616595001.86 [2]
[(1R)-3-Methyl-1-[[(2S)-3-phenyl-2-[[(1S)-1,2,3,4-tetrahydronaphthalene-1-carbonyl]amino]propanoyl]amino]butyl]boronic acidIC501.2 [1], 831763771.1 [2]
(2E)-2-(Quinolin-2-ylmethylidene)hydrazinecarbothioamideIC5010000.0 [1]
[(1R)-3-Methyl-1-[[2-(1-methyl-5-oxo-3,4-dihydro-2H-1,6-naphthyridin-6-yl)acetyl]amino]butyl]boronic acidKi1620.0 [1]
[(1R)-1-[[2-[4-(Diethylamino)-2-oxopyridin-1-yl]acetyl]amino]-3-methylbutyl]boronic acidKi800.0 [1]
[(1R)-1-[[2-(4-Anilino-2-oxopyridin-1-yl)acetyl]amino]-3-methylbutyl]boronic acidKi98.0 [1]
[(1R)-3-Methyl-1-[[(2S)-2-(5-oxo-1,6-naphthyridin-6-yl)propanoyl]amino]butyl]boronic acidKi1340.0 [1]
N,N-Dimethyl-2,3-diphenylquinolin-6-amineIC502300.0 [1], 25000.0 [2]
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-Acetamido-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[2-[[3-[1,1-bis[4-[2-(azepan-1-yl)ethoxy]phenyl]but-1-en-2-yl]phenyl]methylamino]-2-oxoethyl]amino]-5-(diaminomethylideneamino)pentanamideIC508000.0 [1], 40000.0 [2]
N-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2-Amino-2-oxoethyl)amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-3-[1,1-bis[4-[2-(azepan-1-yl)ethoxy]phenyl]but-1-en-2-yl]benzamideIC50890.0 [1], 9100.0 [2]
N-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[2-[[2-[(2-Amino-2-oxoethyl)amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-3-[1,1-bis[4-[2-(azepan-1-yl)ethoxy]phenyl]but-1-en-2-yl]benzamideIC501100.0 [1], 5000.0 [2]
2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]acetic acidIC508000.0 [1], 40000.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-Aminoacetyl)amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanamideIC508000.0 [1], 40000.0 [2]
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-Acetamido-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[2-[[3-[1,1-bis[4-[2-(azepan-1-yl)ethoxy]phenyl]but-1-en-2-yl]phenyl]methylamino]-2-oxoethyl]amino]-5-(diaminomethylideneamino)pentanamideIC508000.0 [1], 40000.0 [2]
N-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-Amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]-3-[1,1-bis[4-[2-(azepan-1-yl)ethoxy]phenyl]but-1-en-2-yl]benzamideIC508000.0 [1], 40000.0 [2]
(4S)-5-Amino-4-[[(2S)-2-[[(2S)-2-[[2-[[3-[1,1-bis[4-[2-(azepan-1-yl)ethoxy]phenyl]but-1-en-2-yl]benzoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoic acidIC506100.0 [1], 24000.0 [2]
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-Acetamido-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-2-[[2-[[3-[1,1-bis[4-[2-(azepan-1-yl)ethoxy]phenyl]but-1-en-2-yl]phenyl]methylamino]-2-oxoethyl]amino]-4-methylpentanamideIC50370.0 [1], 40000.0 [2]
N-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-Amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]-3-[1,1-bis[4-[2-(azepan-1-yl)ethoxy]phenyl]but-1-en-2-yl]benzamideIC508000.0 [1], 40000.0 [2]
N-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-Amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-3-[1,1-bis[4-[2-(azepan-1-yl)ethoxy]phenyl]but-1-en-2-yl]benzamideIC50890.0 [1], 26000.0 [2]
5-Methyl-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[(4-methylphenyl)methylamino]-1-oxo-4-phenylbutan-2-yl]amino]-1-oxo-4-phenylbutan-2-yl]amino]-1-oxo-4-phenylbutan-2-yl]pyrazine-2-carboxamideIC5016.0 [1], 53.0 [2]
N-[(2S)-1-[[(2S)-1-[[(2S)-5-(Diaminomethylideneamino)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-3-hydroxy-2-methylbenzamideIC5030000.0 [1]
N-[(2S)-1-[[(2S)-1-[[(E,2S)-1-[4-(Aminomethyl)phenyl]-4-methylsulfonylbut-3-en-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-3-hydroxy-2-methylbenzamideIC5013000.0 [1], 15000.0 [2]
N,N'-Bis[6-[[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]hexanediamideIC5020.0 [1]
N,N'-Bis[6-[[6-[[6-[[6-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-3-[(3R)-3-hydroxy-2-oxo-1H-indol-3-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-(4-phenylmethoxyphenyl)propan-2-yl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]amino]-6-oxohexyl]hexanediamideKi6.0 [1]
(10S,11R,12S,15S,18S)-15-(2-Amino-2-oxoethyl)-10,11,23-trihydroxy-18-[[(3S)-3-methyl-2-oxopentanoyl]amino]-9,14,17-trioxo-N-[(Z)-prop-1-enyl]-8,13-diazatetracyclo[18.3.1.02,7.06,10]tetracosa-1(23),2(7),3,5,20(24),21-hexaene-12-carboxamideIC505.4 [1]
(10S,11R,12S,15S,18S)-15-(2-Amino-2-oxoethyl)-10,11,23-trihydroxy-18-[[(3S)-3-methyl-2-oxopentanoyl]amino]-9,14,17-trioxo-N-[(Z)-prop-1-enyl]-8,13-diazatetracyclo[18.3.1.02,7.06,10]tetracosa-1(23),2(7),3,5,20(24),21-hexaene-12-carboxamideKi2.3 [1]
1-[2-[4-[1-[4-[2-(Azepan-1-yl)ethoxy]phenyl]-2,2-diphenylethenyl]phenoxy]ethyl]azepaneIC501180.0 [1]
1-[2-[4-[1-[4-[2-(Azepan-1-yl)ethoxy]phenyl]-2,2-diphenylethenyl]phenoxy]ethyl]azepaneKi1100.0 [1]
1-[2-[4-[1-[4-[2-(Azepan-1-yl)ethoxy]phenyl]-2-phenylethenyl]phenoxy]ethyl]azepaneIC50580.0 [1]
1-[2-[4-[1-[4-[2-(Azepan-1-yl)ethoxy]phenyl]-2-phenylethenyl]phenoxy]ethyl]azepaneKi870.0 [1]
5-(3,4-Dimethoxybenzylidene)-3-phenyl-2-thioxo-4-imidazolidinoneKi2010.0 [1], 13600.0 [2]
(2S)-N-[(2S)-1-[(2-Chlorophenyl)methylamino]-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-[(5-methyl-1,2-oxazole-3-carbonyl)amino]butanediamideIC502.1 [1], 13.0 [2]
N-[(2S)-3-(3-Tert-butyl-1,2,4-oxadiazol-5-yl)-1-[[(2S)-1-[(4-methylphenyl)methylamino]-1-oxo-4-phenylbutan-2-yl]amino]-1-oxopropan-2-yl]-5-methyl-1,2-oxazole-3-carboxamideIC5093.0 [1], 1700.0 [2]
5-(4-Hydroxy-3-methoxybenzylidene)-2-mercapto-3-phenyl-3,5-dihydro-4H-imidazol-4-oneKi11500.0 [1], 23600.0 [2]
(2S)-2-Acetamido-N-[(2S)-1-(benzylamino)-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)butanediamideIC5050.0 [1], 960.0 [2]
(2S)-N-[(2S)-1-(Benzylamino)-1-oxo-4-phenylbutan-2-yl]-2-(2,2-dimethylpropanoylamino)-N'-(2,2-dimethylpropyl)butanediamideIC5025.0 [1], 610.0 [2]
(2S)-N-[(2S)-1-(Benzylamino)-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-[(2-piperidin-1-ylacetyl)amino]butanediamideIC5012.0 [1], 30.0 [2]
(2S)-N-[(2S)-1-(Benzylamino)-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-[[2-(4-fluorophenyl)acetyl]amino]butanediamideIC508.4 [1], 73.0 [2]
(2S)-N-[(2S)-1-(Benzylamino)-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-(3-phenylpropanoylamino)butanediamideIC505.4 [1], 17.0 [2]
(2S)-N-[(2S)-1-(Benzylamino)-1-oxo-4-phenylbutan-2-yl]-2-[(4-tert-butylbenzoyl)amino]-N'-(2,2-dimethylpropyl)butanediamideIC5022.0 [1], 40.0 [2]
(2S)-N-[(2S)-1-(Benzylamino)-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-[(4-phenylmethoxybenzoyl)amino]butanediamideIC506.8 [1], 11.0 [2]
(2S)-N-[(2S)-1-(Benzylamino)-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-[[2-(1H-indol-3-yl)-2-oxoacetyl]amino]butanediamideIC504.8 [1], 9.7 [2]
(2S)-N-[(2S)-1-(Benzylamino)-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-[(5-methyl-1,2-oxazole-3-carbonyl)amino]butanediamideIC504.7 [1], 25.0 [2]
(2S)-N-[(2S)-1-(Cyclopropylmethylamino)-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-(3-phenylpropanoylamino)butanediamideIC5012.0 [1], 360.0 [2]
(2S)-N-[(2S)-1-[(2-Chlorophenyl)methylamino]-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-[[2-(4-fluorophenyl)acetyl]amino]butanediamideIC504.0 [1], 85.0 [2]
(2S)-N-[(2S)-1-[(2-Chlorophenyl)methylamino]-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-(3-phenylpropanoylamino)butanediamideIC503.0 [1], 18.0 [2]
(2S)-N-[(2S)-1-[(2-Chlorophenyl)methylamino]-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-[(4-phenylmethoxybenzoyl)amino]butanediamideIC5011.0 [1], 12.0 [2]
(2S)-N-[(2S)-1-[(2-Chlorophenyl)methylamino]-1-oxo-4-phenylbutan-2-yl]-N'-(2,2-dimethylpropyl)-2-[[2-(1H-indol-3-yl)-2-oxoacetyl]amino]butanediamideIC503.7 [1], 11.0 [2]
(2S)-N-[(2S)-1-[(2-Chlorophenyl)methylamino]-1-oxopropan-2-yl]-N'-(2,2-dimethylpropyl)-2-(3-phenylpropanoylamino)butanediamideIC504.0 [1], 35.0 [2]
(2S)-N-[(2S)-1-[(2-Chlorophenyl)methylamino]-1-oxo-3-pyridin-3-ylpropan-2-yl]-N'-(2,2-dimethylpropyl)-2-(3-phenylpropanoylamino)butanediamideIC503.9 [1], 24.0 [2]
(2S)-N-[(2S)-1-[(2-Chlorophenyl)methylamino]-1-oxo-3-pyridin-4-ylpropan-2-yl]-N'-(2,2-dimethylpropyl)-2-[(5-methyl-1,2-oxazole-3-carbonyl)amino]butanediamideIC5033.3 [1], 940.0 [2]
(2S)-N-[(2S)-1-[(2-Chlorophenyl)methylamino]-1-oxo-3-pyridin-3-ylpropan-2-yl]-N'-(2,2-dimethylpropyl)-2-[(5-methyl-1,2-oxazole-3-carbonyl)amino]butanediamideIC5022.6 [1], 690.0 [2]
(2S)-N-[(2S)-1-[(2-Chlorophenyl)methylamino]-1-oxopropan-2-yl]-N'-(2,2-dimethylpropyl)-2-[(5-methyl-1,2-oxazole-3-carbonyl)amino]butanediamideIC5023.0 [1], 1400.0 [2]
(2S)-2-[[(2S)-3-(3-Tert-butyl-1,2,4-oxadiazol-5-yl)-2-[[2-(1H-indol-3-yl)-2-oxoacetyl]amino]propanoyl]amino]-N-[(4-methylphenyl)methyl]-4-phenylbutanamideIC5011.6 [1], 30.0 [2]
(5Z)-5-[(3-Methoxyphenyl)methylidene]-3-phenyl-2-sulfanylideneimidazolidin-4-oneKi17500.0 [1], 17900.0 [2]
OrlistatIC50100000.0 [1]
Mln9708IC508.44 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Proteasome Macropain subunit MB1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 20 Feb. 2025, https://www.aatbio.com/data-sets/proteasome-macropain-subunit-mb1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 20). Quest Database™ Proteasome Macropain subunit MB1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/proteasome-macropain-subunit-mb1-inhibitors-ic50-ki.
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