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Serine protease hepsin 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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▼
NafamostatIC505.0 [1]
NafamostatKi0.53 [1]
(2R)-N-(4-Carbamimidoylphenyl)-2-cyclohexyl-2-[(4-fluorophenyl)sulfonylamino]acetamideIC5090.0 [1], 190.0 [2], 1290.0 [3]
(2R)-N-(4-Carbamimidoylphenyl)-2-cyclohexyl-2-[[4-(trifluoromethyl)phenyl]sulfonylamino]acetamideIC50680.0 [1], 850.0 [2], 3150.0 [3]
(2R)-N-(4-Carbamimidoylphenyl)-2-cyclohexyl-2-[(4-methylphenyl)sulfonylamino]acetamideIC5033.0 [1], 38.0 [2], 990.0 [3]
Chembl4129630IC503000.0 [1], 3350.0 [2], 6490.0 [3]
2-(2-Hydroxyphenyl)-1H-indole-5-carboxamidineIC5044000.0 [1]
2-(2-Hydroxyphenyl)-1H-indole-5-carboxamidineKi35000.0 [1]
2-(3-Methylphenyl)-2,3-dihydro-1H-perimidineIC50350.0 [1]
Benzenebutanamide, N-(4-(aminoiminomethyl)phenyl)-alpha-(((4-methylphenyl)sulfonyl)amino)-IC50870.0 [1], 1130.0 [2]
(2S)-2-[[(2S)-2-Acetamido-6-aminohexanoyl]amino]-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pentanediamideKi0.22 [1], 1.45 [2]
(2R)-N-(4-Carbamimidoylphenyl)-2-[(4-methylphenyl)sulfonylamino]-2-phenylacetamideIC5022.0 [1], 100.0 [2]
1-[(2S)-3-(3-Carbamimidoylphenyl)-2-(naphthalen-2-ylsulfonylamino)propanoyl]-N-(thiophen-2-ylmethyl)piperidine-3-carboxamideIC50330.0 [1], 676.0 [2]
N-Methyl-D-aspartic acidIC50750.0 [1]
DabigatranKi835.0 [1]
ProbucolIC50430.0 [1]
AnthralinIC50230.0 [1]
LeupeptinKi61.0 [1]
GabexateIC50383.0 [1]
CamostatIC5029.0 [1]
MeclizineIC502020.0 [1]
1-[n-(Naphthalen-2-Ylsulfonyl)glycyl-4-Carbamimidoyl-D-Phenylalanyl]piperidineIC504460.0 [1]
1H-Indole-5-carboximidamideKi500000.0 [1]
2-{5-[Amino(iminio)methyl]-1H-benzimidazol-2-YL}benzenolateKi40000.0 [1]
6-Chloro-2-(2-Hydroxybiphenyl-3-yl)-1H-Indole-5-CarboxamidineIC502600.0 [1]
2,7-Bis(4-amidinobenzylidene)cycloheptanoneIC50272.0 [1]
4-[(2R)-3-(3-Carbamimidoylphenyl)-2-(naphthalen-2-ylsulfonylamino)propanoyl]-N,N-dimethylpiperazine-1-carboxamideIC506550.0 [1]
(2S)-2-Acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideKi3.38 [1]
3-[(2S)-3-Oxo-3-[4-(piperidine-4-carbonyl)piperazin-1-yl]-2-[[2,4,6-tri(propan-2-yl)phenyl]sulfonylamino]propyl]benzenecarboximidamideKi7400.0 [1]
2-[[(Tosylamino)acetyl]amino]-3-(3-amidinophenyl)propanoic acid methyl esterIC503140.0 [1]
3-[3-(1-Benzyl-piperidin-4-yl)-ureido]-benzamidineKi53100.0 [1]
Methyl 4-[(2S)-3-(3-carbamimidoylphenyl)-2-(naphthalen-2-ylsulfonylamino)propanoyl]piperazine-1-carboxylateIC506190.0 [1]
3-[(2S)-2-(Naphthalen-2-ylsulfonylamino)-3-oxo-3-(4-phenylpiperazin-1-yl)propyl]benzenecarboximidamideKi7000.0 [1]
4-[4-[(2S)-3-(3-Carbamimidoylphenyl)-2-[[2,4,6-tri(propan-2-yl)phenyl]sulfonylamino]propanoyl]piperazine-1-carbonyl]piperidine-1-carboximidamideKi1580.0 [1]
Inhibitor 1 [Colombo et al., 2012]Ki1.1 [1]
2-(4-Carbamimidoylanilino)-2-(7-ethyl-3-methyl-1-benzofuran-5-yl)-N-(1-methylimidazol-4-yl)sulfonylacetamideKi553.0 [1]
N-[1-[(1-Benzylpiperidin-4-yl)methyl]-3-(3-carbamimidoylphenyl)-2-oxo-1,3-diazinan-5-yl]-2-phenylacetamideKi1120.0 [1]
3-[3-(1-Benzylpiperidin-4-yl)-5-methyl-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamideKi3400.0 [1]
3-[3-[(1-Benzylpiperidin-4-yl)methyl]-5-(methoxymethyl)-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamideKi920.0 [1]
3-[3-[(1-Benzylpiperidin-4-yl)methyl]-5-(hydroxymethyl)-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamideKi690.0 [1]
N-[[1-[(1-Benzylpiperidin-4-yl)methyl]-3-(3-carbamimidoylphenyl)-2-oxo-1,3-diazinan-5-yl]methyl]benzamideKi1100.0 [1]
3-[3-[(1-Benzylpiperidin-4-yl)methyl]-5-hydroxy-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamideKi210.0 [1]
3-[3-[(1-Benzylpiperidin-4-yl)methyl]-5-methoxy-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamideKi760.0 [1]
3-[3-[(1-Benzylpiperidin-4-yl)methyl]-5-(methanesulfonamido)-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamideKi720.0 [1]
3-[5-(Benzenesulfonamido)-3-[(1-benzylpiperidin-4-yl)methyl]-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamideKi670.0 [1]
N-[[1-[(1-Benzylpiperidin-4-yl)methyl]-3-(3-carbamimidoylphenyl)-2-oxo-1,3-diazinan-5-yl]methyl]-2-phenylacetamideKi310.0 [1]
3-[3-[(1-Benzylpiperidin-4-yl)methyl]-5-(benzylsulfonylamino)-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamideKi530.0 [1]
(2S)-2-Acetamido-6-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]hexanamideKi0.41 [1]
(2S)-2-[[(2S)-2-Acetamido-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pentanediamideKi0.21 [1]
(2S)-2-[[(2S)-2-Acetamido-6-aminohexanoyl]amino]-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pentanediamideKi0.58 [1]
(2S)-2-Acetamido-6-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]hexanamideKi2.1 [1]
(2S)-2-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pentanediamideKi0.28 [1]
(2S)-2-[[(2S)-2-Acetamido-3-hydroxypropanoyl]amino]-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pentanediamideKi0.34 [1]
(2S)-2-Acetamido-6-amino-N-[(2S)-5-(diaminomethylideneamino)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]hexanamideKi0.57 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-3-(1H-indol-3-yl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-4-methylpentanamideKi0.21 [1]
(2S)-2-[[(2S)-2-Acetamido-3-hydroxypropanoyl]amino]-6-amino-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]hexanamideKi1.2 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-3-hydroxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-4-methylpentanamideKi0.6 [1]
(2S)-2-[[(2S)-2-Acetamido-3-(1H-indol-3-yl)propanoyl]amino]-6-amino-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]hexanamideKi0.55 [1]
(2S)-2-[[(2S)-2-Acetamido-3-hydroxypropanoyl]amino]-6-amino-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]hexanamideKi8.5 [1]
(2S)-2-Acetamido-N-[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]butanediamideKi1.4 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-3-hydroxypropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-4-methylpentanamideKi0.68 [1]
(2S)-2-[[(2S,3R)-2-Acetamido-3-hydroxybutanoyl]amino]-6-amino-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]hexanamideKi0.61 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-4-methylpentanamideKi1.2 [1]
(2S)-2-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-6-amino-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]hexanamideKi0.47 [1]
4-[(2S)-3-(3-Carbamimidoylphenyl)-2-(naphthalen-2-ylsulfonylamino)propanoyl]-N-hexylpiperazine-1-carboxamideKi1200.0 [1]
3-[(2S)-3-[4-(1-Benzothiophene-3-carbonyl)piperazin-1-yl]-2-(naphthalen-2-ylsulfonylamino)-3-oxopropyl]benzenecarboximidamideKi3500.0 [1]
Benzyl N-[(3R)-1-[(2S)-3-(3-carbamimidoylphenyl)-2-(naphthalen-2-ylsulfonylamino)propanoyl]piperidin-3-yl]carbamateKi2600.0 [1]
Benzyl 4-[(2S)-3-(3-carbamimidoylphenyl)-2-[(4-methylphenyl)sulfonylamino]propanoyl]piperazine-1-carboxylateKi2400.0 [1]
3-[(2S)-3-Oxo-3-(4-phenylpiperazin-1-yl)-2-[[2,4,6-tri(propan-2-yl)phenyl]sulfonylamino]propyl]benzenecarboximidamideKi7400.0 [1]
3-[(2S)-2-(Naphthalen-2-ylsulfonylamino)-3-oxo-3-(4-phenylpiperidin-1-yl)propyl]benzenecarboximidamideKi3300.0 [1]
N-Benzyl-4-[(2S)-3-(3-carbamimidoylphenyl)-2-(naphthalen-2-ylsulfonylamino)propanoyl]piperazine-1-carboxamideKi1000.0 [1]
Benzyl N-[(3S)-1-[(2S)-3-(3-carbamimidoylphenyl)-2-[(4-methylphenyl)sulfonylamino]propanoyl]piperidin-3-yl]carbamateKi2300.0 [1]
N-[(4-Bromophenyl)methyl]-4-[(2S)-3-(3-carbamimidoylphenyl)-2-(naphthalen-2-ylsulfonylamino)propanoyl]piperazine-1-carboxamideKi48.0 [1]
3-[(2S)-2-[(4-Methylphenyl)sulfonylamino]-3-oxo-3-(4-phenylpiperidin-1-yl)propyl]benzenecarboximidamideKi4700.0 [1]
4-[(2S)-3-(3-Carbamimidoylphenyl)-2-[(4-methylphenyl)sulfonylamino]propanoyl]-N-(2-phenylethyl)piperazine-1-carboxamideKi670.0 [1]
2-[6-(1-Hydroxycyclohexyl)pyridin-2-Yl]-1h-Indole-5-CarboximidamideKi100.0 [1]
2-(2-Hydroxy-3-propan-2-ylphenyl)-1H-indole-5-carboximidamideKi4900.0 [1]
2-(5-Chloro-2-hydroxy-3-propan-2-ylphenyl)-1H-indole-5-carboximidamideKi4800.0 [1]
2-(2-Hydroxy-3-piperidin-1-ylphenyl)-1H-indole-5-carboximidamideKi1400.0 [1]
2-(6-Piperidin-1-ylpyridin-2-yl)-1H-indole-5-carboximidamideKi600.0 [1]
2-[6-(1-Fluorocyclohexyl)pyridin-2-yl]-1H-indole-5-carboximidamideKi400.0 [1]
(2Z)-2-[1-Hydroxy-6-(1-hydroxycyclohexyl)pyridin-2-ylidene]indole-5-carboximidamideKi100.0 [1]
3-[3-[(1-Benzylpiperidin-4-yl)methyl]-2-oxo-5-phenylmethoxy-1,3-diazinan-1-yl]benzenecarboximidamideKi760.0 [1]
3-[3-[(1-Benzylpiperidin-4-yl)methyl]-2-oxo-5-(phenylmethoxymethyl)-1,3-diazinan-1-yl]benzenecarboximidamideKi560.0 [1]
(2R)-1-[(2R)-5-(Diaminomethylideneamino)-2-[(1-hydroxynaphthalene-2-carbonyl)amino]pentanoyl]pyrrolidine-2-carboxamideIC5010000.0 [1]
4-[3-(1-Benzylpiperidin-4-yl)-5-methyl-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamideKi61200.0 [1]
3-[[3-(1-Benzylpiperidin-4-yl)-5-methyl-2-oxo-1,3-diazinan-1-yl]methyl]benzenecarboximidamideKi15100.0 [1]
4-[[3-(1-Benzylpiperidin-4-yl)-5-methyl-2-oxo-1,3-diazinan-1-yl]methyl]benzenecarboximidamideKi20800.0 [1]
3-[3-[2-(1-Benzylpiperidin-4-yl)ethyl]-5-methyl-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamideKi2120.0 [1]
(2S)-2-Acetamido-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-phenylpentan-2-yl]-4-methylpentanamideKi10000.0 [1]
(2S)-2-Acetamido-N-[(2R)-5-(diaminomethylideneamino)-1-oxo-1-phenylpentan-2-yl]-4-methylpentanamideKi10000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-6-aminohexanoyl]amino]-5-amino-5-oxopentanoyl]amino]-4-methylpentanoic acidKi10000.0 [1]
(2S)-2-[[(2S)-2-Acetamido-6-aminohexanoyl]amino]-N-[(2S)-1-[[(2R)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pentanediamideKi0.83 [1]
(2S)-2-Acetamido-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pentanediamideKi1.04 [1]
(2S)-2-Acetamido-N-[(2S)-1-[[(2R)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pentanediamideKi2.88 [1]
(2S)-2-Acetamido-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-4-methylpentanamideKi22.4 [1]
(2S)-2-Acetamido-N-[(2R)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-4-methylpentanamideKi21.5 [1]
N-[(2S)-5-(Diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]acetamideKi10000.0 [1]
(2S)-2-Acetamido-N-[(2R)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideKi2.91 [1]
2-[5-(4-Chlorophenyl)-2-hydroxyphenyl]-1H-indole-5-carboximidamideIC5023000.0 [1]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

"Quest Database™ Serine protease hepsin Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 20 Feb. 2025, https://www.aatbio.com/data-sets/serine-protease-hepsin-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 20). Quest Database™ Serine protease hepsin Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/serine-protease-hepsin-inhibitors-ic50-ki.
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