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Leukocyte elastase 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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▼
SivelestatIC5044.0 [1]
SivelestatKi37.0 [1], 200.0 [2]
Benzyl N-[(2S)-3-methyl-1-oxo-1-[(2S)-2-[[(3S)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]carbamoyl]pyrrolidin-1-yl]butan-2-yl]carbamateKi1.6 [1]
4-N-(4-Chlorophenyl)sulfonyl-1-N-[(2S)-3-methyl-1-oxo-1-[(2S)-2-[(1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl)carbamoyl]pyrrolidin-1-yl]butan-2-yl]benzene-1,4-dicarboxamideIC5034.0 [1]
4-N-(4-Chlorophenyl)sulfonyl-1-N-[(2S)-3-methyl-1-oxo-1-[(2S)-2-[(1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl)carbamoyl]pyrrolidin-1-yl]butan-2-yl]benzene-1,4-dicarboxamideKi0.2 [1], 0.5 [2], 3.0 [3]
GW311616 hydrochlorideIC5022.0 [1], 350.0 [2], 670.0 [3]
GW311616 hydrochlorideKi0.31 [1]
(2S)-1-[(2S)-2-[(4-Methoxybenzoyl)amino]-3-methylbutanoyl]-N-[(3S)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]pyrrolidine-2-carboxamideKi1.3 [1], 1.9 [2], 3.1 [3]
2-[5-Amino-2-(4-fluorophenyl)-6-oxopyrimidin-1-yl]-N-(1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl)acetamideKi101.0 [1]
Cbz-Val-Pro-Val-(2-benzoxazole)Ki3.0 [1], 4.7 [2]
Benzyl N-[2-oxo-1-[2-oxo-2-[(1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl)amino]ethyl]-6-phenylpyridin-3-yl]carbamateKi4.5 [1], 5.6 [2]
(3Ar,6S,6aS)-4-methylsulfonyl-6-propan-2-yl-1-[2-(pyrrolidin-1-ylmethyl)-1,3-oxazole-4-carbonyl]-3,3a,6,6a-tetrahydro-2H-pyrrolo[3,2-b]pyrrol-5-one;hydrochlorideIC5010.0 [1], 250.0 [2], 390.0 [3]
(3Ar,6S,6aS)-4-methylsulfonyl-6-propan-2-yl-1-[2-(pyrrolidin-1-ylmethyl)-1,3-oxazole-4-carbonyl]-3,3a,6,6a-tetrahydro-2H-pyrrolo[3,2-b]pyrrol-5-one;hydrochlorideKi0.16 [1]
4-N-(4-Bromophenyl)sulfonyl-1-N-[3-methyl-1-oxo-1-[(2S)-2-[[(3S)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]carbamoyl]pyrrolidin-1-yl]butan-2-yl]benzene-1,4-dicarboxamideIC5038.0 [1]
4-N-(4-Bromophenyl)sulfonyl-1-N-[3-methyl-1-oxo-1-[(2S)-2-[[(3S)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]carbamoyl]pyrrolidin-1-yl]butan-2-yl]benzene-1,4-dicarboxamideKi0.4 [1], 0.62 [2]
1,1-Dioxo-2-[(1-phenyltetrazol-5-yl)sulfanylmethyl]-1,2-benzothiazol-3-oneKi15.0 [1]
FreselestatKi12.0 [1], 12.16 [2], 12.2 [3]
Benzyl N-[(2S)-3-methyl-1-[(2S)-2-[[(2S)-3-methyl-1-[5-[(3-methylphenyl)methyl]-1,2,4-oxadiazol-3-yl]-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxobutan-2-yl]carbamateKi0.49 [1]
Unii-X4edb9177RKi0.03 [1]
2-(Diethylamino)-5,6,7,8-tetrahydro-4H-[1]benzothieno[2,3-d][1,3]oxazine-4-oneKi12.59 [1], 13.0 [2], 16.22 [3], 16.3 [4]
(1,1,3-Trioxo-4-propan-2-yl-1,2-benzothiazol-2-yl)methyl 2,6-dichlorobenzoateKi0.03 [1]
(3Ar,6S,6aS)-1-[1-(2,2-dimethylpropyl)azetidine-3-carbonyl]-4-methylsulfonyl-6-propan-2-yl-3,3a,6,6a-tetrahydro-2H-pyrrolo[3,2-b]pyrrol-5-one;hydrochlorideIC5037.0 [1], 170.0 [2], 190.0 [3]
(3Ar,6S,6aS)-1-[1-(2,2-dimethylpropyl)azetidine-3-carbonyl]-4-methylsulfonyl-6-propan-2-yl-3,3a,6,6a-tetrahydro-2H-pyrrolo[3,2-b]pyrrol-5-one;hydrochlorideKi1.73 [1]
(3Ar,6S,6aS)-1-[5-[(cyclopropylamino)methyl]pyrazine-2-carbonyl]-4-methylsulfonyl-6-propan-2-yl-3,3a,6,6a-tetrahydro-2H-pyrrolo[3,2-b]pyrrol-5-one;hydrochlorideIC5011.0 [1], 150.0 [2], 260.0 [3]
(3Ar,6S,6aS)-1-[5-[(cyclopropylamino)methyl]pyrazine-2-carbonyl]-4-methylsulfonyl-6-propan-2-yl-3,3a,6,6a-tetrahydro-2H-pyrrolo[3,2-b]pyrrol-5-one;hydrochlorideKi0.01 [1]
BoceprevirIC5010000.0 [1], 17000.0 [2], 100000.0 [3]
(2S)-N-[(1R)-1-(1,3-Benzodioxol-5-yl)butyl]-3,3-diethyl-2-[4-(4-methylpiperazine-1-carbonyl)phenoxy]-4-oxoazetidine-1-carboxamideIC500.45 [1], 23.0 [2], 36.0 [3]
2-(Furan-2-yl)-4H-3,1-benzoxazin-4-oneIC505500.0 [1]
2-(Furan-2-yl)-4H-3,1-benzoxazin-4-oneKi1778.28 [1], 562341000000000.0 [2]
(2S)-1-[(2S)-3-Methyl-2-[[4-(morpholine-4-carbonyl)benzoyl]amino]butanoyl]-N-(5,5,6,6,6-pentafluoro-2-methyl-4-oxohexan-3-yl)pyrrolidine-2-carboxamideKi20.0 [1], 25.0 [2]
N-(Methoxycarbonyl)-L-valyl-N-((1S)-3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl)-L-prolinamideIC5010.0 [1]
N-(Methoxycarbonyl)-L-valyl-N-((1S)-3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl)-L-prolinamideKi13.0 [1]
BentranilIC5017000.0 [1]
BentranilKi9549.93 [1], 104713000000000.0 [2]
Sivelestat sodiumIC5044.0 [1], 50.0 [2]
Sivelestat sodiumKi200.0 [1]
Benzyl N-[2-oxo-1-[2-oxo-2-[(1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl)amino]ethyl]pyridin-3-yl]carbamateKi280.0 [1]
Benzyl N-[(2S)-3-methyl-1-[(2S)-2-[[(2S)-3-methyl-1-oxo-1-(1,3-thiazol-2-yl)butan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxobutan-2-yl]carbamateKi270.0 [1]
Benzyl N-[(2S)-3-methyl-1-[(2S)-2-[[(2S)-3-methyl-1-(1-methylimidazol-2-yl)-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxobutan-2-yl]carbamateKi80000.0 [1]
Benzyl N-[(2S)-3-methyl-1-[(2S)-2-[[(2S)-3-methyl-1-oxo-1-pyridin-2-ylbutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxobutan-2-yl]carbamateKi22000.0 [1]
Benzyl N-[(2S)-1-[(2S)-2-[[(2S)-1-(1H-benzimidazol-2-yl)-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamateKi5600.0 [1]
2-[5-Amino-2-(4-fluorophenyl)-6-oxopyrimidin-1-yl]-N-[(2S)-1-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-3-methyl-1-oxobutan-2-yl]acetamideKi6.38 [1], 6.4 [2]
2-[5-Amino-2-(4-fluorophenyl)-6-oxopyrimidin-1-yl]-N-[(2S)-3-methyl-1-[5-[2-(3-methylphenyl)propan-2-yl]-1,3,4-oxadiazol-2-yl]-1-oxobutan-2-yl]acetamideKi1.37 [1], 1.4 [2]
Pyridin-4-ylmethyl N-[2-oxo-1-[2-oxo-2-[(1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl)amino]ethyl]-6-phenylpyridin-3-yl]carbamateKi8.0 [1]
2-[3-(2-Methyl-1-phenylpropan-2-yl)-2,4,8-trioxo-6-phenyl-1H-pyrido[3,4-d]pyrimidin-7-yl]-N-(1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl)acetamideKi0.93 [1], 0.95 [2]
2-[5-Amino-2-(4-fluorophenyl)-6-oxopyrimidin-1-yl]-N-[(2S)-3-methyl-1-oxo-1-[5-(2-phenylpropan-2-yl)-1,3,4-oxadiazol-2-yl]butan-2-yl]acetamideKi0.52 [1]
Benzyl N-[(2S)-1-[(2S)-2-[[(2S)-1-(1-benzofuran-2-yl)-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamateKi3400.0 [1]
Freselestat, (S)-Ki3.59 [1], 3.6 [2]
Benzyl N-[(2S)-3-methyl-1-[(2S)-2-[[(2S)-3-methyl-1-(1-methylbenzimidazol-2-yl)-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxobutan-2-yl]carbamateKi12000.0 [1]
2-[5-Amino-2-(4-fluorophenyl)-6-oxopyrimidin-1-yl]-N-[(2S)-3-methyl-1-[5-[(3-methylphenyl)methyl]-1,3,4-oxadiazol-2-yl]-1-oxobutan-2-yl]acetamideKi0.64 [1]
Benzyl N-[(2S)-3-methyl-1-[(2S)-2-[[(2S)-3-methyl-1-(1,3-oxazol-2-yl)-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxobutan-2-yl]carbamateKi28.0 [1]
Benzyl N-[(2S)-3-methyl-1-[(2S)-2-[[(2S)-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxobutan-2-yl]carbamateKi41.0 [1]
N-[(2S)-3-Methyl-1-oxo-1-[(2S)-2-[[(3S)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]carbamoyl]pyrrolidin-1-yl]butan-2-yl]morpholine-4-carboxamideKi190.0 [1], 195.0 [2]
Benzyl N-[(2S)-3-methyl-1-[(2S)-2-[[(3S)-2-methyl-4-oxopentan-3-yl]carbamoyl]pyrrolidin-1-yl]-1-oxobutan-2-yl]carbamateKi8000.0 [1]
2-Isopropylamino-5-methyl-4H-3,1-benzoxazin-4-oneIC5033.0 [1]
2-Isopropylamino-5-methyl-4H-3,1-benzoxazin-4-oneKi1.5 [1], 6.61e+17 [2]
Benzyl N-[(2S)-1-[(2S)-2-[[(2S)-1-(1,3-benzothiazol-2-yl)-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamateKi25.0 [1]
Benzyl (3aS,6R,6aR)-5-oxo-6-prop-2-enyl-2,3,3a,4,6,6a-hexahydropyrrolo[3,2-b]pyrrole-1-carboxylateIC50500.0 [1], 500000.0 [2]
Phenyl N-[(2S)-3-methyl-1-oxo-1-[(2S)-2-[[(3S)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]carbamoyl]pyrrolidin-1-yl]butan-2-yl]carbamateKi1.3 [1], 1.5 [2], 2.3 [3]
Benzyl N-[(2S)-1-[2,3-dihydro-1H-inden-2-yl-[2-oxo-2-[(1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl)amino]ethyl]amino]-3-methyl-1-oxobutan-2-yl]carbamateIC50365.0 [1]
Benzyl (3aS,6R,6aR)-4-methylsulfonyl-5-oxo-6-prop-2-enyl-3,3a,6,6a-tetrahydro-2H-pyrrolo[3,2-b]pyrrole-1-carboxylateIC500.05 [1], 56.0 [2], 370.0 [3]
3,1-Benzoxazin-4-one, 2-diethylamino-Ki302.0 [1], 310.0 [2], 2691530000000000.0 [3]
4-N-(4-Chlorophenyl)sulfonyl-1-N-[(2S)-1-[2,3-dihydro-1H-inden-2-yl-[2-oxo-2-[(1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl)amino]ethyl]amino]-3-methyl-1-oxobutan-2-yl]benzene-1,4-dicarboxamideIC5084.0 [1]
2-[[(2,6-Dichlorobenzoyl)oxy]methyl]-3-oxo-2,3-dihydro-1,2-benzisothiazole 1,1-dioxideKi2.0 [1], 2.7 [2]
Methyl 4-oxo-4-[[(2S)-1-oxo-1-[[(2S)-1-oxo-1-[(2S)-2-[[(3S)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]carbamoyl]pyrrolidin-1-yl]propan-2-yl]amino]propan-2-yl]amino]butanoateKi7.0 [1], 14.0 [2], 92.0 [3]
(2S,3S)-N-[(1S)-1-[[3-(Butylamino)-3-oxopropyl]-dihydroxysilyl]-3-methylbutyl]-3-methyl-2-[(2-naphthalen-2-ylacetyl)amino]pentanamideIC50300.0 [1], 18000.0 [2]
(2S,3S)-N-[(1S)-1-[[3-(Butylamino)-3-oxopropyl]-dihydroxysilyl]-3-methylbutyl]-3-methyl-2-[(2-naphthalen-2-ylacetyl)amino]pentanamideKi3500.0 [1]
4-[(4R)-2,5-Dioxo-1-[3-(trifluoromethyl)phenyl]-3,4,6,7-tetrahydrocyclopenta[d]pyrimidin-4-yl]benzonitrileIC5011.5 [1], 22.0 [2]
4-[(4S)-3-(Cyanomethyl)-2,5-dioxo-1-[3-(trifluoromethyl)phenyl]-6,7-dihydro-4H-cyclopenta[d]pyrimidin-4-yl]-3-methylsulfonylbenzonitrileIC501.0 [1], 3.4 [2]
(4S)-4-(4-Cyano-2-methylsulfonylphenyl)-N-methyl-2,5-dioxo-1-[3-(trifluoromethyl)phenyl]-6,7-dihydro-4H-cyclopenta[d]pyrimidine-3-carboxamideIC501.0 [1]
6-Methoxy-1,1-dioxo-2-[(1-phenyltetrazol-5-yl)sulfanylmethyl]-4-propan-2-yl-1,2-benzothiazol-3-oneKi0.27 [1]
(2S)-1-[(2S)-2-[[(2S)-2-[[5-(Dimethylamino)naphthalen-1-yl]sulfonylamino]propanoyl]amino]propanoyl]-N-[(3S)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]pyrrolidine-2-carboxamideKi6.3 [1], 10.0 [2], 110.0 [3]
4-Ethyl-1,1-dioxo-2-[(1-phenyltetrazol-5-yl)sulfanylmethyl]-1,2-benzothiazol-3-oneKi2.0 [1]
1,1-Dioxo-2-[(1-phenyltetrazol-5-yl)sulfanylmethyl]-4-propyl-1,2-benzothiazol-3-oneKi0.7 [1]
4-Methoxy-1,1-dioxo-2-[(1-phenyltetrazol-5-yl)sulfanylmethyl]-1,2-benzothiazol-3-oneKi13.6 [1], 14.0 [2]
1,1-Dioxo-4-pentan-3-yl-2-[(1-phenyltetrazol-5-yl)sulfanylmethyl]-1,2-benzothiazol-3-oneKi60.0 [1]
4-Butan-2-yl-1,1-dioxo-2-[(1-phenyltetrazol-5-yl)sulfanylmethyl]-1,2-benzothiazol-3-oneKi0.6 [1]
1,1-Dioxo-2-[(1-phenyltetrazol-5-yl)sulfanylmethyl]-4-propan-2-yl-1,2-benzothiazol-3-oneKi0.3 [1]
QuercetinIC5014300.0 [1]
QuercetinKi11900.0 [1]
Phenylmethylsulfonyl fluorideIC5052161.7 [1], 95219.3 [2]
ApigeninIC5046100.0 [1]
ApigeninKi49900.0 [1]
LuteolinIC5012700.0 [1]
LuteolinKi10100.0 [1]
TelaprevirIC50680.0 [1], 8000.0 [2]
3,4-DichloroisocoumarinIC50100.0 [1], 3000.0 [2]
(2S)-1-[(6R,7S)-3-(Acetyloxymethyl)-7-methoxy-5,5,8-trioxo-5lambda6-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carbonyl]pyrrolidine-2-carboxylic acidKi2.2 [1], 1700.0 [2]
AlvelestatIC5012.0 [1]
AlvelestatKi12.0 [1]
Nymphaeol AIC5022800.0 [1]
Nymphaeol AKi15700.0 [1]
(1R,21S,24S)-21-Tert-butyl-N-[(1R,2S)-1-(cyclopropylsulfonylcarbamoyl)-2-ethenylcyclopropyl]-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6(11),7,9-triene-24-carboxamideIC5010000.0 [1], 100000.0 [2]
MidesteineIC501000.0 [1]
MidesteineKi1400.0 [1]
3'-O-MethyldiplaconeIC507800.0 [1]
3'-O-MethyldiplaconeKi4300.0 [1]
N-[(1S,15S,18S,21Z,24S,27R,29S,34S,37S)-29-Benzyl-21-ethylidene-5,6,27-trihydroxy-31,37-dimethyl-10,16,19,22,30,32,35,38-octaoxo-34-propan-2-yl-36-oxa-9,11,17,20,23,28,31,33-octazatetracyclo[16.13.6.124,28.03,8]octatriaconta-3,5,7-trien-15-yl]-2-methylpropanamideIC50180.0 [1]
N-[(1S,15S,18S,21Z,24S,27R,29S,34S,37S)-29-Benzyl-21-ethylidene-5,6,27-trihydroxy-31,37-dimethyl-10,16,19,22,30,32,35,38-octaoxo-34-propan-2-yl-36-oxa-9,11,17,20,23,28,31,33-octazatetracyclo[16.13.6.124,28.03,8]octatriaconta-3,5,7-trien-15-yl]-2-methylpropanamideKi12.0 [1]
Tanariflavanone DIC5015400.0 [1]
Items per page: 1 - 10 of 100
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References

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MLA

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

APA

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