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Plasma kallikrein 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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(3R,8R,11S,14S,17S,20S,23S,26S,29S,32S)-3-Amino-23-benzyl-20-[(1-carbamimidoylpiperidin-4-yl)methyl]-26-[3-(diaminomethylideneamino)propyl]-11-(1H-indol-3-ylmethyl)-17,29-dimethyl-14-(2-methylpropyl)-2,10,13,16,19,22,25,28,31-nonaoxo-5,6-dithia-1,9,12,15,18,21,24,27,30-nonazabicyclo[30.3.0]pentatriacontane-8-carboxylic acidKi9.93 [1], 14.0 [2], 31.9 [3], 53.6 [4], 166.0 [5]
(3R,8R,11S,14S,17S,20S,23S,26S,29S,32S)-3-Amino-20-[(1-carbamimidoylpiperidin-4-yl)methyl]-11-(carboxymethyl)-23-(hydroxymethyl)-17,26-bis[(4-hydroxyphenyl)methyl]-29-methyl-14-(2-methylpropyl)-2,10,13,16,19,22,25,28,31-nonaoxo-5,6-dithia-1,9,12,15,18,21,24,27,30-nonazabicyclo[30.3.0]pentatriacontane-8-carboxylic acidKi136.0 [1], 907.0 [2], 938.0 [3], 1580.0 [4], 1694.0 [5]
RazaxabanKi2300.0 [1]
(2R)-2-[[(2R)-2-[[2-[[2-[[2-[[(2S)-2-[[(1R,7S,10S,13S,16S,22S,25S,28S,40R,43S,46S,49S,52S,58S,61S)-40-Acetamido-43,52-bis(2-amino-2-oxoethyl)-13-(carboxymethyl)-46-[(1R)-1-hydroxyethyl]-10,49,61-tris(1H-indol-3-ylmethyl)-16-methyl-25-(2-methylpropyl)-2,8,11,14,17,23,26,41,44,47,50,53,59,62-tetradecaoxo-30,38,65-trithia-3,9,12,15,18,24,27,42,45,48,51,54,60,63-tetradecazahexacyclo[32.29.3.132,36.03,7.018,22.054,58]heptahexaconta-32,34,36(67)-triene-28-carbonyl]amino]propanoyl]-methylamino]acetyl]-methylamino]acetyl]-methylamino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoic acidIC5027.0 [1], 790.0 [2]
(2R)-2-[[(2R)-2-[[2-[[2-[[2-[[(2S)-2-[[(1R,7S,10S,13S,16S,22S,25S,28S,40R,43S,46S,49S,52S,58S,61S)-40-Acetamido-43,52-bis(2-amino-2-oxoethyl)-13-(carboxymethyl)-46-[(1R)-1-hydroxyethyl]-10,49,61-tris(1H-indol-3-ylmethyl)-16-methyl-25-(2-methylpropyl)-2,8,11,14,17,23,26,41,44,47,50,53,59,62-tetradecaoxo-30,38,65-trithia-3,9,12,15,18,24,27,42,45,48,51,54,60,63-tetradecazahexacyclo[32.29.3.132,36.03,7.018,22.054,58]heptahexaconta-32,34,36(67)-triene-28-carbonyl]amino]propanoyl]-methylamino]acetyl]-methylamino]acetyl]-methylamino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoic acidKi3.0 [1]
2-[3-(Aminomethyl)phenyl]-N-[2-fluoro-4-(2-methylsulfonylphenyl)phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide;hydrochlorideKi61.0 [1]
Ethyl N-[(2S)-6-amino-1-oxo-1-[5-[[4-(2-phenylethoxy)phenyl]methyl]-1,2,4-oxadiazol-3-yl]hexan-2-yl]carbamateKi43000.0 [1]
(2S)-2-[[(2S)-2-[[(1R)-1-(4-Bromophenyl)ethyl]carbamoylamino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-3-methylbutanamideIC5010.0 [1]
Bis-triazole derivative 10Ki2.4 [1]
N-[(1S)-1-[4-(3-Amino-1H-indazol-6-yl)pyridin-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexane-1-carboxamideKi24.0 [1]
(7R,10S,13S,21S,24S,27S,30S,33S,36S,39S,42S,45R)-7-Acetamido-36-(3-amino-3-oxopropyl)-13-benzyl-24-(4-carbamimidamidobutyl)-39-(carboxymethyl)-10-(hydroxymethyl)-21-[(4-hydroxyphenyl)methyl]-33-(1H-imidazol-5-ylmethyl)-30-methyl-42-(2-methylpropyl)-8,11,14,19,22,25,28,34,37,40,43-undecaoxo-5,47,52-trithia-9,12,15,20,23,26,29,32,35,38,41,44-dodecazatetracyclo[25.23.3.13,49.015,18]tetrapentaconta-1,3(54),49-triene-45-carboxylic acidIC506.0 [1]
(7R,10S,13S,21S,24S,27S,30S,33S,36S,39S,42S,45R)-7-Acetamido-36-(3-amino-3-oxopropyl)-13-benzyl-24-(4-carbamimidamidobutyl)-39-(carboxymethyl)-10-(hydroxymethyl)-21-[(4-hydroxyphenyl)methyl]-33-(1H-imidazol-5-ylmethyl)-30-methyl-42-(2-methylpropyl)-8,11,14,19,22,25,28,34,37,40,43-undecaoxo-5,47,52-trithia-9,12,15,20,23,26,29,32,35,38,41,44-dodecazatetracyclo[25.23.3.13,49.015,18]tetrapentaconta-1,3(54),49-triene-45-carboxylic acidKi0.36 [1]
(12S,15R)-15-(Benzylsulfonylamino)-N-[(4-carbamimidoylphenyl)methyl]-3,14,24-trioxo-4,13,23-triazatetracyclo[24.2.2.16,10.117,21]dotriaconta-1(29),6,8,10(32),17(31),18,20,26(30),27-nonaene-12-carboxamideKi136.0 [1]
(12S,15R)-15-(Benzylsulfonylamino)-N-[(4-carbamimidoylphenyl)methyl]-3,14,24-trioxo-1,4,13,23,26-pentazatetracyclo[24.2.2.16,10.117,21]dotriaconta-6,8,10(32),17(31),18,20-hexaene-12-carboxamideKi25.3 [1], 31.6 [2]
(13S,16R)-16-(Benzylsulfonylamino)-N-[(4-carbamimidoylphenyl)methyl]-15-oxo-2,7-dioxa-14-azatricyclo[16.2.2.28,11]tetracosa-1(21),8,10,18(22),19,23-hexaene-13-carboxamideKi19.0 [1], 34.2 [2]
(7S,10R)-10-(Benzylsulfonylamino)-N-[(4-carbamimidoylphenyl)methyl]-4,9,13-trioxo-3,8,14-triazabicyclo[14.3.1]icosa-1(19),16(20),17-triene-7-carboxamideKi25.0 [1], 25.4 [2]
(19S,22R)-22-(Benzylsulfonylamino)-N-[(4-carbamimidoylphenyl)methyl]-4,11,21-trioxo-3,12,20-triazatetracyclo[22.2.2.26,9.214,17]dotriaconta-1(27),6,8,14(30),15,17(29),24(28),25,31-nonaene-19-carboxamideKi868.0 [1]
(19S,22R)-22-(Benzylsulfonylamino)-N-[(4-carbamimidoylphenyl)methyl]-4,11,21-trioxo-3,6,9,12,20-pentazatetracyclo[22.2.2.26,9.214,17]dotriaconta-1(27),14(30),15,17(29),24(28),25-hexaene-19-carboxamideKi493.0 [1]
(21S,24R)-24-(Benzylsulfonylamino)-N-[(4-carbamimidoylphenyl)methyl]-4,12,23-trioxo-3,13,22-triazatetracyclo[24.3.1.16,10.115,19]dotriaconta-1(29),6(32),7,9,15,17,19(31),26(30),27-nonaene-21-carboxamideKi17.4 [1]
(8S,11R)-11-(Benzylsulfonylamino)-N-[(4-carbamimidoylphenyl)methyl]-10-oxo-3,4,5,9,14,15,16,22-octazatetracyclo[16.3.1.13,6.113,16]tetracosa-1(21),4,6(24),13(23),14,18(22),19-heptaene-8-carboxamideKi10.1 [1]
2-[[(1R,7S,13S,16S,19S,22R,34R,43S,49S)-34-[(2-Aminoacetyl)amino]-43-[3-(diaminomethylideneamino)propyl]-19-[(4-hydroxyphenyl)methyl]-16-methyl-2,8,14,17,20,35,38,41,44,50-decaoxo-24,32,53-trithia-3,9,15,18,21,36,39,42,45,51-decazahexacyclo[26.23.3.126,30.03,7.09,13.045,49]pentapentaconta-26,28,30(55)-triene-22-carbonyl]amino]acetic acidKi0.3 [1], 120000.0 [2]
4-[[2-[4-(5-Chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1-yl]-3-(4-methoxycyclohexyl)propanoyl]amino]benzoic acidIC505.2 [1], 45.0 [2]
LeupeptinIC5040000.0 [1]
GabexateIC501350.0 [1]
5-(N,N-Hexamethylene)amilorideIC5050000.0 [1]
DarexabanKi11000.0 [1]
5,5'-Methylenedisalicylic acidIC5067900.0 [1]
SepimostatKi570.0 [1]
Naphthalene-2-carboximidamideKi22500.0 [1]
(2S,3S,4S,5R,6S)-3,4,5-Trihydroxy-6-[3-[(4-methoxybenzoyl)amino]-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]phenoxy]oxane-2-carboxylic acidKi17000.0 [1]
LetaxabanIC5012000.0 [1]
(3R,8R,11S,14S,17S,20S,23S,26S,29S,32S)-3-Amino-11-(carboxymethyl)-20-[3-(diaminomethylideneamino)propyl]-23-(hydroxymethyl)-17,26-bis[(4-hydroxyphenyl)methyl]-29-methyl-14-(2-methylpropyl)-2,10,13,16,19,22,25,28,31-nonaoxo-5,6-dithia-1,9,12,15,18,21,24,27,30-nonazabicyclo[30.3.0]pentatriacontane-8-carboxylic acidKi1000000.0 [1]
Wx-uk1 free baseKi7200.0 [1]
4-(2,5-Dimethyl-1H-pyrrol-1-yl)-2-hydroxybenzoic acidIC5030100.0 [1]
Bms-740808Ki2800.0 [1]
Unii-1Y3JD5pemsIC5015800.0 [1]
Grassystatin AIC5010000.0 [1]
6-Chloro-2-(2-Hydroxybiphenyl-3-yl)-1H-Indole-5-CarboxamidineKi800.0 [1]
3-{5-[Amino(iminio)methyl]-1H-indol-2-YL}-1,1'-biphenyl-2-olateKi1.9 [1]
Unii-vwj4vvz3OUKi310.0 [1]
4-{[(4-Chloroanilino)carbonyl]amino}-N-(5-ethyl-1,3,4-thiadiazol-2-yl)benzenesulfonamideIC5028100.0 [1]
6-(N-Phenylcarbamyl)-2-naphthalenecarboxamidineKi2500.0 [1]
(3-Methyl-pyrazol-1-yl)-(3,4,5-trimethoxy-phenyl)-methanoneIC5042200.0 [1]
3-Chloro-N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]-6-methoxyphenyl]-4-[[4,5-dihydro-1,3-oxazol-2-yl(methyl)amino]methyl]thiophene-2-carboxamideKi37.0 [1]
Methyl N-[4-[5-chloro-2-[(1S)-1-[[(E)-3-[5-chloro-2-(tetrazol-1-yl)phenyl]prop-2-enoyl]amino]-2-phenylethyl]-1H-imidazol-4-yl]phenyl]carbamateKi519.0 [1]
4-Chloro-1-(4-fluorobenzoyl)-1H-pyrazoleIC506600.0 [1]
[4-(2,5-Dimethyl-pyrrol-1-yl)-phenyl]-acetic acidIC5060500.0 [1]
2-[2-(Aminomethyl)phenyl]-N-[2-fluoro-4-(2-sulfamoylphenyl)phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamideKi58.0 [1]
5-Chloro-N-(5-chloro-pyridin-2-yl)-2-[4-(2-imino-oxazolidin-3-ylmethyl)-benzoylamino]-benzamideIC50560.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-4-hydroxy-5-phenylphenyl]butanedioic acidKi8.0 [1]
4-[(E)-(5-Oxo-2-phenyl-1,3-oxazol-4-ylidene)methyl]benzenecarboximidamideIC501340.0 [1]
4-[5-[(Z)-(5-Cyano-4-methyl-2,6-dioxopyridin-3-ylidene)methyl]furan-2-yl]benzenesulfonamideIC505500.0 [1]
(3S)-2-[(2S)-2-[[(2S)-2-Cyclohexyl-2-(pyrazine-2-carbonylamino)acetyl]amino]-3,3-dimethylbutanoyl]-N-[1-(cyclopropylamino)-5,5-difluoro-1,2-dioxopentan-3-yl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-3-carboxamideKi50000.0 [1]
6-[N-(4-(Aminomethyl)phenyl)carbamyl]-2-naphthalenecarboxamidineKi7170.0 [1]
6-[(Z)-Amino(imino)methyl]-N-[3-(cyclopentyloxy)phenyl]-2-naphthamideKi2720.0 [1]
2-[(2-Amino-2-carboxyethylthio)methyl]-5-phenylfuran-3-carboxylic acidIC5035400.0 [1]
1-Benzoyl-N-phenyl-1H-pyrazole-3-carboxamideIC5012300.0 [1]
5-Chloro-N-((1R,2S)-2-(4-(2-oxopyridin-1(2H)-YL)benzamido) cyclopentyl)thiophene-2-carboxamideKi16000.0 [1]
(E)-2-(5-Chlorothiophen-2-yl)-N-[(3S)-1-[(2S)-1-morpholin-4-yl-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]prop-1-ene-1-sulfonamideIC505010.0 [1]
3-(6-Chloronaphthalen-2-yl)sulfonyl-N-methyl-N-[1-(2-methylpyridin-4-yl)piperidin-4-yl]propanamideKi3000.0 [1]
2-(3-Amino-1,2-benzoxazol-5-yl)-N-[4-[2-[(dimethylamino)methyl]phenyl]-2-fluorophenyl]-5-(trifluoromethyl)pyrazole-3-carboxamideKi2300.0 [1]
2-(5-Chlorothiophen-2-yl)-N-[(3S)-1-[(2S)-1-morpholin-4-yl-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethanesulfonamideIC5025100.0 [1]
(2S)-N-[(4-Aminocyclohexyl)methyl]-1-[(2R)-2-amino-3,3-dicyclohexylpropanoyl]pyrrolidine-2-carboxamideKi5000.0 [1]
5-[4-[3-(6-Chloro-2-naphthylsulfonyl)propanoyl]piperazino]imidazo[1,2-a]pyridine-2-methanolKi14000.0 [1]
6-Methyl-2-oxo-N-phenylchromene-3-carboxamideIC5050000.0 [1]
(3S,3As,6aR)-N-[1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-2-[(2S)-3,3-dimethyl-2-[[(2S)-3-methyl-2-(pyrazine-2-carbonylamino)butanoyl]amino]butanoyl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-3-carboxamideKi50000.0 [1]
(2S)-1-[(2R)-2-Amino-2-cyclohexylacetyl]-N-[[5-chloro-2-[2-(cyclopropylamino)-2-oxoethoxy]phenyl]methyl]pyrrolidine-2-carboxamideKi79000.0 [1]
4-[(2R)-3-(3-Carbamimidoylphenyl)-2-(naphthalen-2-ylsulfonylamino)propanoyl]-N,N-dimethylpiperazine-1-carboxamideKi7300.0 [1]
(S)-1-(2-Amino-2-cyclohexyl-acetyl)-pyrrolidine-2-carboxylic acid 2,5-dichloro-benzylamideKi586000.0 [1]
(2S)-1-[(2R)-2-Cyclohexyl-2-[[2-(diethylamino)-2-oxoethyl]amino]acetyl]-N-[(2,5-dichlorophenyl)methyl]pyrrolidine-2-carboxamideKi399000.0 [1]
3-Chloro-N-((1R,2S)-2-(4-(2-oxopyridin-1(2H)-YL)benzamido)cyclohexyl)-1H-indole-6-carboxamideKi8458.0 [1]
6-Carbamimidoyl-N-(1-propan-2-yl-1,2,3,4-tetrahydroisoquinolin-7-yl)naphthalene-2-carboxamideKi230.0 [1]
6-Carbamimidoyl-N-(3-propan-2-yloxyphenyl)naphthalene-2-carboxamideKi1370.0 [1]
N-[(1S)-1-[4-(3-Amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexane-1-carboxamideKi5.0 [1]
6-Carbamimidoyl-N-(1,2,3,4-tetrahydroisoquinolin-6-yl)naphthalene-2-carboxamideKi112.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-5-(2-fluorophenyl)-4-hydroxyphenyl]butanedioic acidKi12.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-4-hydroxy-5-(2-hydroxyphenyl)phenyl]butanedioic acidKi13.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-5-(3-acetylphenyl)-4-hydroxyphenyl]butanedioic acidKi6.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-4-hydroxy-5-(3-methylphenyl)phenyl]butanedioic acidKi4.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-4-hydroxy-5-(2-methylphenyl)phenyl]butanedioic acidKi6.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-4-hydroxy-5-(3-hydroxyphenyl)phenyl]butanedioic acidKi3.0 [1]
2-[3-(6-Carbamimidoyl-1H-benzimidazol-2-yl)-5-(3-carbamoylphenyl)-4-hydroxyphenyl]butanedioic acidKi0.5 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-5-(3-cyanophenyl)-4-hydroxyphenyl]butanedioic acidKi10.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-5-(3-chlorophenyl)-4-hydroxyphenyl]butanedioic acidKi3.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-4-hydroxy-5-(2-methoxyphenyl)phenyl]butanedioic acidKi6.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-4-hydroxy-5-(4-methylphenyl)phenyl]butanedioic acidKi18.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-5-(4-chlorophenyl)-4-hydroxyphenyl]butanedioic acidKi37.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-4-hydroxy-5-(4-hydroxyphenyl)phenyl]butanedioic acidKi65.0 [1]
2-[3-(5-Carbamimidoyl-1H-1,3-benzodiazol-2-yl)-4-hydroxy-5-(4-methoxyphenyl)phenyl]butanedioic acidKi27.0 [1]
(3S)-N-[(3S)-1-(Cyclopropylamino)-1,2-dioxohexan-3-yl]-2-[(2S)-2-[[(2S)-3,3-dimethyl-2-(pyrazine-2-carbonylamino)butanoyl]amino]-3,3-dimethylbutanoyl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-3-carboxamideKi50000.0 [1]
3-Chloro-N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]-6-methoxyphenyl]-4-(methylaminomethyl)thiophene-2-carboxamideKi1000.0 [1]
3-Chloro-N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]-6-methoxyphenyl]-4-[[2-(methylamino)imidazol-1-yl]methyl]thiophene-2-carboxamideKi45.0 [1]
(3S,3As,6aR)-2-[(2S)-2-[[(2S)-2-cyclohexyl-2-(pyrazine-2-carbonylamino)acetyl]amino]-3,3-dimethylbutanoyl]-N-[1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-3-carboxamideKi50000.0 [1]
3-[[2-[[4-(Aminomethyl)cyclohexanecarbonyl]amino]-3-(4-pyrimidin-2-yloxyphenyl)propanoyl]amino]benzoic acidIC50710.0 [1]
5-Chloro-N-(5-chloro-pyridin-2-yl)-2-[4-(2-imino-imidazolidin-1-ylmethyl)-benzoylamino]-benzamideIC50210.0 [1]
5-Chloro-N-(5-chloro-pyridin-2-yl)-2-(4-dimethylaminomethyl-benzoylamino)-benzamideIC50500.0 [1]
5-Chloro-N-(5-chloropyridin-2-yl)-2-[[4-[[ethanimidoyl(methyl)amino]methyl]benzoyl]amino]benzamideIC50500.0 [1]
5-Chloro-N-[(1R,2S)-2-[[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]benzoyl]amino]cyclopentyl]thiophene-2-carboxamideKi10000.0 [1]
6-[N-(1-Isopropyl-3,4-dihydro-7-isoquinolinyl)carbamyl]-2-naphthalenecarboxamidineKi436.0 [1]
CID 46899577Ki8.3 [1]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

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

APA

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