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Tryptase beta-1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
Bis(5-amidino-2-benzimidazolyl)methaneIC5051.0 [1]
Bis(5-amidino-2-benzimidazolyl)methaneKi140.0 [1]
Ethyl N-[(2S)-6-amino-1-oxo-1-[5-[[4-(2-phenylethoxy)phenyl]methyl]-1,2,4-oxadiazol-3-yl]hexan-2-yl]carbamateKi5.4 [1], 46.5 [2]
[4-[3-(Aminomethyl)phenyl]piperidin-1-yl]-(1-butyl-7-methylindol-3-yl)methanoneIC5068.0 [1], 3694.0 [2]
[4-[3-(Aminomethyl)phenyl]piperidin-1-yl]-(1-butyl-7-methylindol-3-yl)methanoneKi68.0 [1]
Benzyl N-[(2S)-6-amino-1-oxo-1-[5-[[4-(2-phenylethoxy)phenyl]methyl]-1,2,4-oxadiazol-3-yl]hexan-2-yl]carbamateKi12.0 [1]
(2R)-1-Acetyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]pyrrolidine-2-carboxamideIC502.0 [1]
(2R)-1-Acetyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]pyrrolidine-2-carboxamideKi14000.0 [1]
N-[(2S)-6-Amino-1-[5-[[4-[2-(3,4-dichlorophenyl)ethoxy]phenyl]methyl]-1,2,4-oxadiazol-3-yl]-1-oxohexan-2-yl]-3,4-difluorobenzamide;hydrochlorideKi7.6 [1], 400.0 [2]
N-[(2S)-6-Amino-1-[5-[[4-[2-(3,4-dichlorophenyl)ethoxy]phenyl]methyl]-1,2,4-oxadiazol-3-yl]-1-oxohexan-2-yl]-4-fluorobenzamideKi2.5 [1], 400.0 [2]
Grassystatin AIC5010000.0 [1]
[5-[4-[[4-(Diaminomethylideneamino)phenyl]methylcarbamoyl]piperazine-1-carbonyl]oxycyclooctyl] 4-[[4-(diaminomethylideneamino)phenyl]methylcarbamoyl]piperazine-1-carboxylateKi0.07 [1]
4-[2-[4-(Diaminomethylideneamino)phenyl]-4-oxo-4-(2-phenylethylamino)butanoyl]-N-(3,3-diphenylpropyl)piperazine-1-carboxamideKi210.0 [1]
1,4-Bis[[4-(4-amidinobenzoylaminomethyl)piperidino]carbonyloxymethyl]benzeneKi0.4 [1]
[5-[4-[[4-(Diaminomethylideneamino)phenyl]methylcarbamoyl]piperazine-1-carbonyl]oxycyclooctyl] 4-(benzylcarbamoyl)piperazine-1-carboxylateKi15000.0 [1]
[5-[4-(Benzylcarbamoyl)piperazine-1-carbonyl]oxycyclooctyl] 4-(benzylcarbamoyl)piperazine-1-carboxylateKi101000.0 [1]
N-[(2S)-6-Amino-1-[5-[[4-[2-(3-chlorophenyl)ethylcarbamoyl]phenyl]methyl]-1,2,4-oxadiazol-3-yl]-1-oxohexan-2-yl]-3,5-difluorobenzamideKi1.5 [1]
Ethyl N-[(2S)-6-amino-1-[5-[[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)phenyl]methyl]-1,2,4-oxadiazol-3-yl]-1-oxohexan-2-yl]carbamateKi2.8 [1]
1,4-Bis[[2-oxo-2-[4-(aminomethyl)benzylamino]ethyl]carbamoyloxymethyl]benzeneKi0.6 [1]
4-[[(4-Carbamimidoylbenzoyl)amino]methyl]-N-(3,3-diphenylpropyl)piperidine-1-carboxamideKi84.0 [1]
N-[2-[3-[4-(Aminomethyl)phenyl]propylamino]ethyl]-1,2,3,4-tetrahydroisoquinoline-7-sulfonamideIC50190.0 [1]
N-(2-((3-(4-(Aminomethyl)phenyl)propyl)(methyl)amino)ethyl)naphthalene-2-sulfonamideIC50120.0 [1]
N-[2-[3-[4-(Aminomethyl)phenyl]propylamino]ethyl]-2,3-dihydro-1H-indene-5-sulfonamideIC50200.0 [1]
N-(2-(3-(4-(Aminomethyl)phenyl)propylamino)ethyl)naphthalene-2-sulfonamideIC5073.0 [1]
N-(2-(3-(4-(Aminomethyl)phenyl)propylamino)ethyl)benzo[b]thiophene-5-sulfonamideIC50210.0 [1]
N-(2-(3-(4-(Aminomethyl)phenyl)propylamino)ethyl)-1-chloronaphthalene-2-sulfonamideIC505.0 [1]
Benzyl N-[(2S)-5-(diaminomethylideneamino)-1-[4-[(2S,5S)-5-[4-[4-(diaminomethylideneamino)butanoylamino]butyl]-3,6-dioxopiperazin-2-yl]butylamino]-1-oxopentan-2-yl]carbamateIC502200.0 [1]
N-[(2S)-5-(Diaminomethylideneamino)-1-[4-[(2S,5S)-5-[4-[4-(diaminomethylideneamino)butanoylamino]butyl]-3,6-dioxopiperazin-2-yl]butylamino]-1-oxopentan-2-yl]benzamideIC502400.0 [1]
3-[4-[5-(Aminomethyl)-2-fluorophenyl]piperidine-1-carbonyl]-5-(3-thiophen-2-yl-1,2,4-oxadiazol-5-yl)benzamideKi1.3 [1]
2-[5-[[5-(Aminomethyl)-2,4-dimethylphenyl]methylamino]-3-chloro-2-methyl-6-oxopyrazin-1-yl]-N-[3-(aminomethyl)phenyl]acetamide;2,2,2-trifluoroacetic acidKi93.0 [1]
(2S,4R)-1-Acetyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-hydroxypyrrolidine-2-carboxamide;nitric acidKi10.0 [1]
4-[[(4-Carbamimidoylbenzoyl)amino]methyl]-N-(3,3-diphenylpropyl)benzamideKi340.0 [1]
4-N-[[4-(Diaminomethylideneamino)phenyl]methyl]-1-N-(3,3,3-triphenylpropyl)piperazine-1,4-dicarboxamideKi6900.0 [1]
4-N-[[4-(Diaminomethylideneamino)phenyl]methyl]-1-N-(3,3-diphenylpropyl)piperazine-1,4-dicarboxamideKi870.0 [1]
4-[2-(4-Carbamimidoylanilino)-2-oxoethyl]-N-(3,3-diphenylpropyl)piperidine-1-carboxamideKi300.0 [1]
4-N-[[4-(Diaminomethylideneamino)phenyl]methyl]-1-N-(2-naphthalen-1-ylethyl)piperazine-1,4-dicarboxamideKi7400.0 [1]
4-[2-[(4-Carbamimidoylbenzoyl)amino]ethyl]-N-(3,3-diphenylpropyl)piperidine-1-carboxamideKi11000.0 [1]
4-[[(3-Carbamimidoylbenzoyl)amino]methyl]-N-(3,3-diphenylpropyl)piperidine-1-carboxamideKi24000.0 [1]
4-[[[4-(Diaminomethylideneamino)benzoyl]amino]methyl]-N-(3,3-diphenylpropyl)piperidine-1-carboxamideKi9800.0 [1]
4-[[(4-Carbamimidoylphenyl)sulfonylamino]methyl]-N-(3,3-diphenylpropyl)piperidine-1-carboxamideKi9700.0 [1]
4-N-Benzyl-1-N-[[4-(diaminomethylideneamino)phenyl]methyl]-4-N-methylpiperazine-1,4-dicarboxamideKi80000.0 [1]
4-N-Benzyl-1-N-[[4-(diaminomethylideneamino)phenyl]methyl]-4-N-(3-phenylpropyl)piperazine-1,4-dicarboxamideKi12000.0 [1]
4-N-[[4-(Diaminomethylideneamino)phenyl]methyl]-1-N-(4-phenylbutyl)piperazine-1,4-dicarboxamideKi11000.0 [1]
4-N,4-N-Dibenzyl-1-N-[[4-(diaminomethylideneamino)phenyl]methyl]piperazine-1,4-dicarboxamideKi29000.0 [1]
4-[[(4-Carbamimidoylbenzoyl)-methylamino]methyl]-N-(3,3-diphenylpropyl)piperidine-1-carboxamideKi50000.0 [1]
2-(4-Guanidinophenyl)-3-oxo-3-[4-(3,3-diphenylpropylcarbamoyl)piperazino]propionic acid methyl esterKi160.0 [1]
4-N-[(4-Carbamimidoylphenyl)methyl]-1-N-(3,3-diphenylpropyl)piperazine-1,4-dicarboxamideKi400.0 [1]
4-[2-[4-(Diaminomethylideneamino)phenyl]acetyl]-N-(3,3-diphenylpropyl)piperazine-1-carboxamideKi7000.0 [1]
4-N-[[4-(Diaminomethylideneamino)phenyl]methyl]-1-N-[2-(9H-fluoren-9-yl)ethyl]piperazine-1,4-dicarboxamideKi6900.0 [1]
1-N-[[4-(Diaminomethylideneamino)phenyl]methyl]-4-N-(4,4-diphenylcyclohexyl)piperazine-1,4-dicarboxamideKi890.0 [1]
1-N-[[4-(Diaminomethylideneamino)phenyl]methyl]-4-N-(naphthalen-2-ylmethyl)piperazine-1,4-dicarboxamideKi1300.0 [1]
3-[[(4-Carbamimidoylbenzoyl)amino]methyl]-N-(3,3-diphenylpropyl)piperidine-1-carboxamideKi13000.0 [1]
1-N-Benzyl-4-N-[[4-(diaminomethylideneamino)phenyl]methyl]piperazine-1,4-dicarboxamideKi16000.0 [1]
4-[(4-Carbamimidoylbenzoyl)amino]-N-(3,3-diphenylpropyl)piperidine-1-carboxamideKi2600.0 [1]
4-N-[[4-(Diaminomethylideneamino)phenyl]methyl]-1-N-ethylpiperazine-1,4-dicarboxamideKi370000.0 [1]
4-N-[[4-(Diaminomethylideneamino)phenyl]methyl]-1-N-(3-phenylpropyl)piperazine-1,4-dicarboxamideKi7300.0 [1]
4-N-[[4-(Diaminomethylideneamino)phenyl]methyl]-1-N-(2-phenylethyl)piperazine-1,4-dicarboxamideKi42000.0 [1]
1,4-Bis[1,4-dioxo-4-[4-(aminomethyl)benzylamino]butylaminomethyl]benzeneKi3.0 [1]
1,4-Bis[methyl[1,4-dioxo-4-[4-(aminomethyl)benzylamino]butyl]aminomethyl]benzeneKi5.0 [1]
1,4-Bis[1,4-dioxo-4-[methyl[4-(aminomethyl)benzyl]amino]butylaminomethyl]benzeneKi2000.0 [1]
1,4-Bis[1,3-dioxo-3-(4-guanidinobenzylamino)propylaminomethyl]benzeneKi680.0 [1]
1,4-Bis[1,3-dioxo-3-[4-(aminomethyl)benzylamino]propylaminomethyl]benzeneKi150.0 [1]
1,4-Bis[1,5-dioxo-5-(4-guanidinobenzylamino)pentylaminomethyl]benzeneKi100.0 [1]
[5-[2-[[4-(Diaminomethylideneamino)phenyl]methylcarbamoylamino]acetyl]oxycyclooctyl] 2-[[4-(diaminomethylideneamino)phenyl]methylcarbamoylamino]acetateKi2.0 [1]
1,4-Bis[[3-oxo-3-(4-guanidinobenzylamino)propyl]carbamoyloxymethyl]benzeneKi90.0 [1]
1,4-Bis[[2-oxo-2-(4-guanidinobenzylamino)ethyl]carbamoyloxymethyl]benzeneKi10.0 [1]
1,4-Bis[1,4-dioxo-4-(4-guanidinobenzylamino)butylaminomethyl]benzeneKi40.0 [1]
1,4-Bis[1,5-dioxo-5-[4-(aminomethyl)benzylamino]pentylaminomethyl]benzeneKi9.0 [1]
1,4-Bis[[(S)-1-methyl-2-oxo-2-[4-(aminomethyl)benzylamino]ethyl]carbamoyloxymethyl]benzeneKi366.0 [1]
1,4-Bis[[(R)-1-methyl-2-oxo-2-[4-(aminomethyl)benzylamino]ethyl]carbamoyloxymethyl]benzeneKi31.0 [1]
1,4-Bis[methyl[2-oxo-2-[4-(aminomethyl)benzylamino]ethyl]carbamoyloxymethyl]benzeneKi5.0 [1]
2-Acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]acetamide;2,2,2-trifluoroacetic acidKi470.0 [1]
(2S)-2-Acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamide;2,2,2-trifluoroacetic acidKi41.0 [1]
(2S)-1-Acetyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]azetidine-2-carboxamide;2,2,2-trifluoroacetic acidKi20.0 [1]
1-[(2S)-5-(Diaminomethylideneamino)-2-[(1-hydroxynaphthalene-2-carbonyl)amino]pentanoyl]pyrrolidine-2-carboxamideKi330.0 [1]
(2S)-1-Acetyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2,5-dihydropyrrole-2-carboxamide;2,2,2-trifluoroacetic acidKi38.0 [1]
N-[1-(1,3-Benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]cyclopentanecarboxamide;2,2,2-trifluoroacetic acidKi88.0 [1]
(2S)-1-Acetyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]pyrrolidine-2-carboxamide;2,2,2-trifluoroacetic acidKi19.0 [1]
(2S)-1-Acetyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-oxopyrrolidine-2-carboxamide;2,2,2-trifluoroacetic acidKi73.0 [1]
(2S)-N-[(2S)-1-(1,3-Benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamide;2,2,2-trifluoroacetic acidKi6.5 [1]
Methyl 3-[3-(aminomethyl)phenyl]-2-[4-[[2-[(2S,5R)-5-[2-[[4-[[3-[3-(aminomethyl)phenyl]-1-methoxy-1-oxopropan-2-yl]amino]-4-oxobutyl]amino]-2-oxoethyl]-3,6-dioxopiperazin-2-yl]acetyl]amino]butanoylamino]propanoateKi350.0 [1]
Methyl 3-[3-(aminomethyl)phenyl]-2-[3-[[2-[(2S,5R)-5-[2-[[3-[[3-[3-(aminomethyl)phenyl]-1-methoxy-1-oxopropan-2-yl]amino]-3-oxopropyl]amino]-2-oxoethyl]-3,6-dioxopiperazin-2-yl]acetyl]amino]propanoylamino]propanoateKi10.0 [1]
Methyl 3-[3-(aminomethyl)phenyl]-2-[3-[(2S,5R)-5-[2-[[2-[[3-[3-(aminomethyl)phenyl]-1-methoxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]-3,6-dioxopiperazin-2-yl]propanoylamino]propanoateKi180.0 [1]
(R)-2-Acetylamino-3-(3-aminomethyl-phenyl)-propionic acid methyl esterKi13700.0 [1]
Methyl 3-[3-(aminomethyl)phenyl]-2-[3-[(5R)-5-[3-[[3-[3-(aminomethyl)phenyl]-1-methoxy-1-oxopropan-2-yl]amino]-3-oxopropyl]-3,6-dioxopiperazin-2-yl]propanoylamino]propanoateKi2400.0 [1]
(R)-2-Acetylamino-3-(4-aminomethyl-phenyl)-propionic acid methyl esterKi213000.0 [1]
N-[4-[(2S,5S)-5-[4-[[2-(2-Amino-4,5-dihydroimidazol-1-yl)acetyl]amino]butyl]-3,6-dioxopiperazin-2-yl]butyl]-4-(diaminomethylideneamino)benzamideIC504400.0 [1]
N-(3-Carbamimidoylphenyl)-2-[(2S,5S)-5-[4-[[2-(diaminomethylideneamino)acetyl]amino]butyl]-3,6-dioxopiperazin-2-yl]acetamideIC5019900.0 [1]
N-[4-[(2S,5S)-5-[2-(3-Carbamimidoylanilino)-2-oxoethyl]-3,6-dioxopiperazin-2-yl]butyl]-3-(diaminomethylideneamino)propanamideIC5023600.0 [1]
N-[4-[(2S,5S)-5-[2-(3-Carbamimidoylanilino)-2-oxoethyl]-3,6-dioxopiperazin-2-yl]butyl]-3-[carbamimidoyl(methyl)amino]propanamideIC5012800.0 [1]
N-[4-[(2S,5S)-5-[2-(3-Carbamimidoylanilino)-2-oxoethyl]-3,6-dioxopiperazin-2-yl]butyl]-4-(diaminomethylideneamino)butanamideIC5021300.0 [1]
9H-Fluoren-9-ylmethyl N-[1-[4-[(2S,5S)-5-[2-(3-carbamimidoylanilino)-2-oxoethyl]-3,6-dioxopiperazin-2-yl]butylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamateIC509090.0 [1]
N-[(2S)-1-[4-[(2S,5S)-5-[2-(3-Carbamimidoylanilino)-2-oxoethyl]-3,6-dioxopiperazin-2-yl]butylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]benzamideIC5012400.0 [1]
4-(Diaminomethylideneamino)-N-[4-[(2S,5S)-5-[4-[4-(diaminomethylideneamino)butanoylamino]butyl]-3,6-dioxopiperazin-2-yl]butyl]butanamideIC504700.0 [1]
N-[(2S)-5-(Diaminomethylideneamino)-1-[4-[(2S,5S)-5-[4-[5-(diaminomethylideneamino)pentanoylamino]butyl]-3,6-dioxopiperazin-2-yl]butylamino]-1-oxopentan-2-yl]benzamideIC509300.0 [1]
Benzyl N-[(2S)-5-(diaminomethylideneamino)-1-[4-[(2S,5S)-5-[4-[5-(diaminomethylideneamino)pentanoylamino]butyl]-3,6-dioxopiperazin-2-yl]butylamino]-1-oxopentan-2-yl]carbamateIC505700.0 [1]
Benzyl N-[(2S)-5-(diaminomethylideneamino)-1-[4-[(2S,5S)-5-[4-[[(2S)-5-(diaminomethylideneamino)-2-(phenylmethoxycarbonylamino)pentanoyl]amino]butyl]-3,6-dioxopiperazin-2-yl]butylamino]-1-oxopentan-2-yl]carbamateIC504100.0 [1]
N-[4-[(2S,5S)-5-[4-[3-[Carbamimidoyl(methyl)amino]propanoylamino]butyl]-3,6-dioxopiperazin-2-yl]butyl]-3-(diaminomethylideneamino)propanamideIC505900.0 [1]
N-[3-(Aminomethyl)phenyl]-2-[3-chloro-2-methyl-6-oxo-5-(piperidin-3-ylmethylamino)pyrazin-1-yl]acetamideKi518.0 [1]
3-[4-[3-(Aminomethyl)phenyl]piperidine-1-carbonyl]-5-(3-thiophen-2-yl-1,2,4-oxadiazol-5-yl)benzamideKi1.5 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Tryptase beta-1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/tryptase-beta-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Tryptase beta-1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/tryptase-beta-1-inhibitors-ic50-ki.
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