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(1E)-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-sulfonamide
-
-
(1R)-N2-(4-chlorophenyl)-N1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-1,3-dihydro-2H-isoindole-1,2-dicarboxamide
-
-
(1R,2R)-N-(4-chlorophenyl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-hydroxycyclopentane-1,2-dicarboxamide
-
-
(1R,2S)-N-(4-chlorophenyl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4,4-bis(hydroxymethyl)cyclopentane-1,2-dicarboxamide
-
-
(1R,2S)-N-(5-chloropyridin-2-yl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]cyclopropane-1,2-dicarboxamide
-
-
(1S,3R,4S)-4-[(1H-indol-2-ylcarbonyl)amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
(2-[2-[(4-carbamimidoylbenzyl)amino]azetidin-1-yl]-1-cyclohexyl-2-oxoethoxy)carbamic acid
-
-
(2R)-2-[(3-carbamimidoylphenyl)amino]-2-[2-(beta-L-glucopyranosyloxy)phenyl]-N-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]ethanamide
-
-
(2R)-2-[(3-carbamimidoylphenyl)amino]-2-[2-(beta-L-glucopyranosyloxy)phenyl]-N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]-2-oxoethyl]ethanamide
-
-
(2R)-2-[(5-carbamimidoyl-2-hydroxyphenyl)amino]-2-[2-(beta-L-glucopyranosyloxy)phenyl]-N-[2-(4-methyl-1,4-diazepan-1-yl)-2-oxoethyl]ethanamide
-
-
(2R)-N1-(4-chlorophenyl)-N2-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2,3-dihydro-1H-pyrrolo[2,3-b]pyridine-1,2-dicarboxamide
-
-
(2R)-N1-(5-chloropyridin-2-yl)-4-hydroxy-N2-[5-(3-oxomorpholin-4-yl)pyridin-2-yl]pyrrolidine-1,2-dicarboxamide
-
-
(2R)-N1-(5-chloropyridin-2-yl)-N2-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)pyrrolidine-1,2-dicarboxamide
-
-
(2R)-N1-(5-chloropyridin-2-yl)-N2-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-methoxypyrrolidine-1,2-dicarboxamide
-
-
(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-hydroxypyrrolidine-1,2-dicarboxamide
-
-
(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-methoxypyrrolidine-1,2-dicarboxamide
-
-
(2R,3S)-N2-(5-chloropyridin-2-yl)-N1-(2,2-difluoroethyl)-N3-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-N1-methylcyclopropane-1,2,3-tricarboxamide
-
-
(2R,4R)-N1-(4-chlorophenyl)-4-methoxy-N2-(3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)pyrrolidine-1,2-dicarboxamide
-
-
(2R,4R)-N1-(5-chloropyridin-2-yl)-4-methoxy-N2-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidine-1,2-dicarboxamide
-
-
(2R,4S)-N1-(5-chloropyridin-2-yl)-4-(2,4-difluorophenyl)-4-hydroxy-N2-(2-oxo-2H-1,3'-bipyridin-6'-yl)pyrrolidine-1,2-dicarboxamide
-
-
(2RS)-(3'-amidino-3-biphenyl)-5-(4-pyridylamino)pentanoic acid
i.e. FX-2212, 50% inhibition by 272 nM
(2S)-1-[(2R)-2-[3-chloro-5-(difluoromethoxy)phenyl]-2-hydroxyacetyl]-N-[4-(N'-methoxycarbamimidoyl)benzyl]azetidine-2-carboxamide
-
-
(2S)-N-(2-[[2-(aminomethyl)-5-chlorobenzyl]amino]-2-oxoethyl)-2-[(benzylsulfonyl)amino]-4-(1-oxidopyridin-2-yl)butanamide
-
-
(2S)-N-(4-carbamimidoylbenzyl)-1-[(2R)-2-[3-chloro-5-(difluoromethoxy)phenyl]-2-hydroxyacetyl]azetidine-2-carboxamide
-
-
(2S,4S)-N1-(4-chlorophenyl)-N2-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-methoxypyrrolidine-1,2-dicarboxamide
-
-
(3-[(5-chloropyridin-2-yl)carbamoyl]-4-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]phenoxy)acetic acid
-
-
(3-[[(3-carbamimidoylphenyl)(2-[[4-(1-ethanimidoylpiperidin-4-yl)phenyl]amino]-2-oxoethyl)amino]methyl]phenoxy)acetic acid
-
-
(3R)-N2-(4-chlorophenyl)-N3-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-3,4-dihydroisoquinoline-2,3(1H)-dicarboxamide
-
-
(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
-
-
(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetic acid
-
-
(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)acetic acid
-
-
(4R)-4-[[(5-chlorothiophen-2-yl)carbonyl]amino]-N,N-dimethyl-1-[(3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)carbonyl]-L-prolinamide
-
-
(4S)-4-[[(5-chlorothiophen-2-yl)carbonyl]amino]-N-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-L-prolinamide
-
-
(4S)-N5-(4-chlorophenyl)-N4-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-1-methyl-4,6-dihydropyrrolo[3,4-c]pyrazole-4,5(1H)-dicarboxamide
-
-
(4S,5S)-3-(3-carbamimidoylphenyl)-5-(methoxymethyl)-N-(2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1,2-oxazole-4-carboxamide
-
-
(5R)-N1-(5-chloropyridin-2-yl)-N5-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1H-pyrazole-1,5-dicarboxamide
-
-
(5R,6R)-N-(4-chlorophenyl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]spiro[2.4]heptane-5,6-dicarboxamide
-
-
(5S)-N1-(4-chlorophenyl)-N5-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-5-methyl-4,5-dihydro-1H-pyrazole-1,5-dicarboxamide
-
-
(6R)-N7-(4-chlorophenyl)-N6-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-5,8-dihydro-1,7-naphthyridine-6,7(6H)-dicarboxamide
-
-
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
(E)-2-(5-chlorothiophen-2-yl)-N-(1-[5-[2-(methylsulfonyl)phenyl]pyridin-2-yl]-2-oxopyrrolidin-3-yl)ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(6-fluoro-2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[1-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[[(3R)-1-[[1-(pyridin-4-yl)piperidin-4-yl]carbonyl]pyrrolidin-3-yl]methyl]ethenesulfonamide
-
-
(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
-
potent anticoagulation activities in vitro and ex vivo
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-chlorophenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
-
-
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-fluorophenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
-
-
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-methylphenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
-
-
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]phenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
-
potent anticoagulation activities in vitro and ex vivo
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-4-cyanobenzylpropionamide
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-4-hydroxyphenethylpropionamide
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-aryl-propionamides
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-benzylpropionamide
-
non-substrate-like binding mode
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-ethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-phenpropionyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-propionic acid phenethyl ester
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(2-chloro)-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(3-chloro)-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(4-amino)-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(4-tert-butyl)-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-aryl-propionamides
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamides
-
-
([(2R)-2-(7-carbamimidoylnaphthalen-2-yl)-5-[(1-ethanimidoylpiperidin-4-yl)methyl]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
-
-
([(3'-carbamimidoylbiphenyl-3-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
-
-
([(7-carbamimidoylnaphthalen-2-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
-
-
([2'-(butylsulfonyl)-4-[2-([[2-hydroxy-5-(N'-hydroxycarbamimidoyl)phenyl]sulfonyl]amino)ethyl]biphenyl-3-yl]oxy)acetic acid
-
-
([2-[(E)-2-(5-carbamimidoyl-2-hydroxyphenyl)ethenyl]-5-[(1-ethanimidoylpiperidin-4-yl)oxy]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
-
-
1,1'-(benzene-1,4-diyldimethanediyl)bis(N,N-diethylpiperidine-3-carboxamide)
-
-
1,2-dicaproyl-sn-glycero-3-phospho-L-serine
1,2-dioleoyl-phosphatidylglycerol
-
in vesicles with 1,2-dioleoyl-phosphatidylglycerol, 18fold activation of enzyme activity with prothrombin
1,5-dansyl-Glu-Gly-Arg chloromethyl ketone
-
slow binding inhibitor
1-(1-[(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2-hydroxypropanoyl]piperidin-4-yl)tetrahydropyrimidin-2(1H)-one
-
-
1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[2,3-b]pyridin-2-ylsulfonyl)-piperazin-2-one
-
-
1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[3,2-b]pyridin-2-ylsulfonyl)-piperazin-2-one
-
-
1-(3-amino-1,2-benzisoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[2-[(dimethylamino)methyl]pyridin-3-yl]-2-fluorophenyl)-7-fluoro-1H-indazole-3-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[2-[(dimethylamino)methyl]pyridin-3-yl]phenyl)-7-fluoro-1H-indazole-3-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[[3-(dimethylamino)propyl](pyridin-4-yl)amino]phenyl)-7-fluoro-1H-indazole-3-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-5-methyl-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-7-fluoro-6-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-1H-indazole-3-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-N-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-N-[1-[2-(pyrrolidin-1-ylmethyl)phenyl]piperidin-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-amino-1H-isoindol-5-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-aminophenyl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(3-carbamimidoylphenyl)-3-methyl-N-(2'-sulfamoylbiphenyl-4-yl)-1H-pyrazole-5-carboxamide
-
-
1-(3-carbamoylphenyl)-N-[3-chloro-4-(2-thioxopyrrolidin-1-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-carbamoylphenyl)-N-[4-(5-ethyl-2-imino-1,3,4-thiadiazol-3(2H)-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-carbamoylphenyl)-N-[4-[(2Z)-2-(cyanoimino)imidazolidin-1-yl]phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-[6-[4-(2-chloropyridin-4-yl)piperazin-1-yl]-7-fluoro-3-methyl-1H-indazol-1-yl]phenyl)methanamine
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-4-bromo-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(fluoro)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-(4-aminophthalazin-6-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(4-aminoquinazolin-6-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(4-methoxyphenyl)-3-(methylsulfonyl)-6-(4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
good factor Xa binding ability and good plasma anticoagulant activity
1-(4-methoxyphenyl)-4-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[3,4-d]pyridazin-7-one
-
-
1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(1H-tetrazol-1-ylmethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(2H-tetrazol-2-ylmethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
1-(4-methoxyphenyl)-6-(4-[1-[(methylamino)methyl]cyclopropyl]phenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
good factor Xa binding ability and good plasma anticoagulant activity
1-(4-methoxyphenyl)-6-(4-[1-[(methylamino)methyl]cyclopropyl]phenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-6-[4-(1-[[(1-methylethyl)amino]methyl]cyclopropyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(4-methoxyphenyl)-6-[4-(2-oxopiperidin-1-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(4-methoxyphenyl)-6-[4-[1-(morpholin-4-ylmethyl)cyclopropyl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(4-methoxyphenyl)-6-[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(4-methoxyphenyl)-7-oxo-6-(4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
good factor Xa binding ability and good plasma anticoagulant activity
1-(4-methoxyphenyl)-7-oxo-6-[1-[2-(pyrrolidin-1-ylmethyl)phenyl]piperidin-4-yl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1,3-oxazolidin-3-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[4-[(2-oxopiperidin-1-yl)oxy]phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
good factor Xa binding ability and good plasma anticoagulant activity
1-(4-methoxyphenyl)-7-[2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-6,7-dihydropyrazolo[3,4-c]azepin-8(1H)-one
-
-
1-(4-[1-[3-(aminomethyl)phenyl]-7-fluoro-3-methyl-1H-indazol-6-yl]-3-fluorophenyl)piperidin-2-one
-
-
1-(5-methoxypyridin-2-yl)-6-[4-[2-(methylsulfonyl)pyridin-1(2H)-yl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(6-chloronaphthalen-2-yl)-N-[2'-[(dimethylamino)methyl]-3-fluorobiphenyl-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-carbamimidoyl-N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-3-carboxamide
-
-
1-carbamimidoyl-N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-4-carboxamide
-
-
1-palmitoyl-2-oleoyl-3-sn-phosphatidylcholine
-
in vesicles with 1,2-palmitoyl-2-oleoyl-3-sn-phosphatidylcholine, 18fold activation of enzyme activity with prothrombin
1-[(4-amino-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-piperazin-2-one
-
-
1-[(4-aminoquinazolin-7-yl)methyl]-4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]piperazin-2-one
-
-
1-[(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)methyl]cyclopropanecarboxylic acid
-
-
1-[(6-chloro-2-naphthyl)sulfonyl]-4-[(1-pyridin-4-ylpiperidin-4-yl)carbonyl]piperazine
-
-
1-[1-(3-amino-1,2-benzoxazol-5-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-2-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]phenyl)ethanone
-
-
1-[2-(aminomethyl)phenyl]-N-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-[2-([2-[(5-chloropyridin-2-yl)carbamoyl]-4-methoxyphenyl]carbamoyl)-5-(N,N-dimethylcarbamimidoyl)phenyl]piperidine-4-carboxylic acid
-
-
1-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide
-
-
1-[2-[(5-chlorothiophen-2-yl)amino]-2-oxoethyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]-D-prolinamide
-
-
1-[2-[(aminooxy)sulfinyl]phenyl]-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-[3-(5-amino-1,3,4-thiadiazol-2-yl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-[3-(5-amino-4H-1,2,4-triazol-3-yl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-[3-(aminomethyl)phenyl]-N-3-fluoro-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
i.e. DPC423, highly potent, selective, and orally bioavailable inhibitor
1-[3-(aminomethyl)phenyl]-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
i.e. DPC 423
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-[3-(aminomethyl)phenyl]-N-[4-(2-iminopyrrolidin-1-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-[3-[([1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methyl)sulfonyl]phenyl]pyridinium
-
-
1-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]urea
-
-
1-[3-[amino(imino)methyl]phenyl]-N-[2'-(aminosulfonyl)[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-[4-amino-3-[([1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methyl)sulfonyl]phenyl]pyridinium
-
-
1-[4-[1-(5-methoxypyridin-2-yl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]phenyl]-1,2-dihydropyridine-2-sulfonamide
-
-
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]-2-ethylpropan-2-ol
-
-
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]ethanol
-
-
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]propan-2-ol
-
-
1-[[2-(5-chlorothiophen-2-yl)-1,3-thiazol-5-yl]methyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]-D-prolinamide
-
-
1-[[4-([4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]phenyl]carbamoyl)phenyl]carbonoimidoyl]piperidine-4-carboxylic acid
-
-
1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide
-
-
10-[(5-chloro-1H-indol-2-yl)sulfonyl]-1'-(4,5-dihydro-1,3-oxazol-2-yl)-2-methyldihydro-1H-spiro[imidazo[5',1':2,3]imidazo[1,2-a]pyrazine-5,4'-piperidine]-3,8(2H,9H)-dione
-
-
1H-pyrrolo[3,2-c]pyridine-1-acetamide, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-
-
-
1H-pyrrolo[3,2-c]pyridine-1-acetic acid, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-
-
-
1H-pyrrolo[3,2-c]pyridine-1-acetic acid, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-, methyl ester
-
-
2,2'-ethane-1,2-diylbis(1-benzofuran-5-carboximidamide)
-
-
2,2,4,7-tetramethyl-6-[2-(4-methylphenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]-1,2,3,4-tetrahydroquinoline
89% activity at 0.03 mM
2-(1-[(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2-hydroxypropanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
-
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
2-(2-aminoethoxy)-N-[2-[(5-chloropyridin-2-yl)carbamoyl]-4-fluorophenyl]-4-(morpholin-4-yl)benzamide
-
-
2-(2-hydroxy-5-methylbiphenyl-3-yl)-1H-indole-5-carboxamidine
-
-
2-(2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
-
2-(2-hydroxybiphenyl-3-yl)benzofuran-5-carboxamidine
-
-
2-(2-hydroxyphenyl)1H-benzoimidazole-5-carboxamidine
-
-
2-(2-hydroxyphenyl)1H-indole-5-carboxamidine
-
-
2-(2-hydroxyphenyl)3-methyl-3H-benzoimidazole-5-carboxamidine
-
-
2-(2-methoxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
-
2-(3,5-dibromo-2-hydroxyphenyl)-1H-indole-5-carboxamidine
-
-
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
2-(3-bromo-2-hydroxy-5-methylphenyl)-1H-indole-5-carboxamidine
-
-
2-(3-bromo-2-hydroxy-5-nitrophenyl)-1H-indole-5-carboxamidine
-
-
2-(3-bromo-2-hydroxyphenyl)-1H-indole-5-carboxamidine
-
-
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-bromo-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-chloro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide
-
-
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide
-
-
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide
-
-
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide
-
-
2-(4-[(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2-hydroxypropanoyl]piperazin-1-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
-
2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2-methylpropanoic acid
-
-
2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)propanoic acid
-
-
2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)propanoic acid
-
-
2-(5-bromo-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
-
2-(5-carbamimidoyl-2-hydroxyphenoxy)ethyl 4-(pyrrolidin-1-ylcarbonoimidoyl)benzoate
-
-
2-(5-chloro-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
-
2-(5-nitro-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
-
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
2-biphenyl-3-yl-1H-indole-5-carboxamidine
-
-
2-cyano-1-(2-methyl-1-benzofuran-5-yl)-3-[2-oxo-1-[2-oxo-2-(pyrrolidin-1-yl)ethyl]azepan-3-yl]guanidine
-
-
2-[(3-carbamimidoylphenoxy)amino]-2-[2-(hexopyranosyloxy)phenyl]-N-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]acetamide
-
-
2-[(4-carbamimidoylbenzoyl)amino]-N-[(5-chloropyridin-2-yl)oxy]-5-methoxybenzamide
-
-
2-[(benzylsulfonyl)amino]-N-[2-[(4-carbamimidoylbenzyl)amino]-2-oxoethyl]-4-(1-oxidopyridin-2-yl)butanamide
-
-
2-[(benzylsulfonyl)amino]-N-[2-[(4-carbamimidoylbenzyl)amino]-2-oxoethyl]-4-phenylbutanamide
-
-
2-[3-[(benzylsulfonyl)amino]-2-hydroxyazepan-1-yl]-N-[(2S)-5-carbamimidamido-1-(2,3-dihydro-1,3-thiazol-2-yl)-1-oxopentan-2-yl]acetamide
-
-
2-[3-[(benzylsulfonyl)amino]-2-oxopyridin-1(2H)-yl]-N-[(2S)-5-carbamimidamido-1-(2,3-dihydro-1,3-thiazol-2-yl)-1-oxopentan-2-yl]acetamide
-
-
2-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]propan-2-ol
-
-
2-[5-carbamimidoyl-2-(2-methylpropoxy)phenoxy]ethyl 4-[(1-ethanimidoylpiperidin-4-yl)oxy]benzoate
-
-
2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
2-[6-[3-([[(E)-2-(5-chlorothiophen-2-yl)ethenyl]sulfonyl]amino)-2-oxopyrrolidin-1-yl]pyridin-3-yl]benzenesulfonamide
-
-
2-[N2-(benzylsulfonyl)-D-arginylglycyl-L-arginyl]-1,3-thiazole
-
-
2-[[(4-bromophenyl)carbamoyl]amino]-N-[4-(N,N-dimethylcarbamimidoyl)phenyl]-2-phenylacetamide
-
-
2-[[4-(dimethylamino)benzoyl]amino]-N-(5-methoxypyridin-2-yl)-5-[(methylsulfonyl)amino]benzamide
-
-
2-[[[4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl](methylsulfonyl)amino]methyl]-1-benzothiophene-5-carboximidamide
-
-
2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}-N-(2-methylphenyl)benzamide
-
16% inhibition at 0.00136 mM
2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}-N-(3-methylphenyl)benzamide
-
88% inhibition at 0.00136 mM
2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}-N-(4-methylphenyl)benzamide
-
94% inhibition at 0.00136 mM
2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}-N-(4-methylpyridin-2-yl)benzamide
-
56% inhibition at 0.00136 mM
2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}-N-(4-phenoxyphenyl)benzamide
-
22% inhibition at 0.00136 mM
2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}-N-(5-methylpyridin-2-yl)benzamide
-
73% inhibition at 0.00136 mM
2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}-N-(6-methylpyridin-2-yl)benzamide
-
9% inhibition at 0.00136 mM
2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}-N-(pyridin-2-yl)benzamide
-
38% inhibition at 0.00136 mM
2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}-N-[4-(propan-2-yl)phenyl]benzamide
-
23% inhibition at 0.00136 mM
2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}-N-[4-(trifluoromethoxy)phenyl]benzamide
-
32% inhibition at 0.00136 mM
3-(1-[5-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-pentyl]-2-oxo-1,2-dihydroquinolin-3-yl)-4-hydroxybenzamidine
-
-
3-(1-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-2-oxo-1,2-dihydroquinolin-3-yl)benzamidine
-
-
3-(1-[5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl]-2-oxo-1,2,3,4-tetrahydro-3-quinolinyl)-4-hy-droxybenzenecarboximidamide
-
-
3-(1-[5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl]-2-oxo-1,2,3,4-tetrahydro-3-quinolinyl)benzenecarboximidamide
-
-
3-(1H-imidazol-1-ylmethyl)-1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
3-(3-carbamimidoyl-phenyl)-isoxazole-4-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
i.e. SA862
3-(3-carbamimidoylphenyl)-N-(2'-sulfamoylbiphenyl-4-yl)-1,2-oxazole-4-carboxamide
-
-
3-(4-(5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]pentyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-4-hydroxybenzenecarboximidamide
-
-
3-(4-(5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]pentyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide
-
IC50: 3.0 nM
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-3-oxo-3,4-dihydroquinoxalin-2-yl)benzamidine
-
-
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-3-oxo-3,4-dihydroquinoxolin-2-yl)benzamidine
-
-
3-(4-[5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1-benzenecarboximidamide
-
-
3-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2,2-dimethylpropanoic acid
-
-
3-(aminomethyl)-6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
3-(iminomethyl)-1-(4-methoxyphenyl)-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
3-([(3S)-3-[(naphthalen-2-ylsulfonyl)amino]-2-oxopyrrolidin-1-yl]methyl)benzenecarboximidamide
-
-
3-([4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]-2-oxopiperazin-1-yl]methyl)benzenecarboximidamide
-
-
3-([[3-(4-carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino)-4-(3,4-dihydroisoquinolin-2(1H)-yl)-4-oxobutanoic acid
-
-
3-amino-2,3-dihydro-1,3-benzoxazol-5-yl [1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methanesulfonate
-
-
3-amino-4-chloro-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]benzamide
-
-
3-amino-4-chloro-N-[(1R)-2-[4-[4-fluoro-2-(methylsulfonyl)phenyl]piperazin-1-yl]-2-oxo-1-phenylethyl]benzamide
-
-
3-amino-N-[(1R)-2-oxo-1-phenyl-2-[(2'-sulfamoylbiphenyl-4-yl)amino]ethyl]-1H-indazole-5-carboxamide
-
-
3-carbamimidoyl-N-[(1R)-2-oxo-1-phenyl-2-[(2'-sulfamoylbiphenyl-4-yl)amino]ethyl]benzamide
-
-
3-carbamimidoylbenzamide
-
-
3-chloro-2-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-N-[(3R,4S)-3-fluoro-1-(propan-2-yl)piperidin-4-yl]benzamide
-
-
3-chloro-2-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-N-[1-(propan-2-yl)piperidin-4-yl]benzamide
-
-
3-chloro-4-[3-[(4-chlorophenyl)amino]-3-oxopropyl]-5-([[5-(propan-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]carbonyl]amino)benzoic acid
-
-
3-chloro-N-(4-chloro-2-([(4-chlorophenyl)-amino]carbonyl)phenyl)-4-[(4-methyl-1-piperazinyl)methyl]-2-thiophenecarboxamide
binding structure and mechanism
3-chloro-N-(4-chloro-2-([(5-chloro-2-pyridinyl)amino]carbonyl)-6-methoxyphenyl)-4-([(4,5-dihydro-2-oxazolyl)methylamino]methyl)-2-thiophenecarboxamide
binding structure and mechanism, good bioavailability
3-chloro-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
-
3-chloro-N-[(1R,2S)-2-[[4-(2-oxopyridin-1(2H)-yl)benzoyl]amino]cyclohexyl]-1H-indole-6-carboxamide
-
-
3-chloro-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[2-[(4-chlorophenyl)carbamoyl]-4-methylphenyl]-1-benzothiophene-2-carboxamide
-
-
3-chloro-N-[2-[(4-fluorophenyl)carbamoyl]-4-methylphenyl]-1-benzothiophene-2-carboxamide
-
-
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
highly potent and selective non-amidine inhibitor, reversibel inhibition, 5fold higher affinity for the free factor Xa than for the enzyme/substrate complex, inhibition mechanism, 19fold decreased inhibitory effect in presence of phospholipid
3-chloro-N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]-6-methoxyphenyl]-4-[[2-(methylamino)-1H-imidazol-1-yl]methyl]thiophene-2-carboxamide
-
-
3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]-N-(5-methyl-2-pyridyl)benzamide
-
-
3-hydroxy-4'-methoxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
-
-
3-hydroxy-4'-methoxy-4-methyl-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
-
-
3-hydroxy-4'-methyl-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
-
-
3-hydroxy-N-(5-methoxy-2-pyridyl)-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
-
-
3-methyl-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
3-methyl-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
-
3-[(4-methoxyphenyl)carbamoyl]-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]phenyl beta-D-glucopyranosiduronic acid
-
-
3-[(5-chloropyridin-2-yl)carbamoyl]-2-[[4-(1-methyl-2-oxo-1,2-dihydropyridin-3-yl)benzoyl]amino]phenyl b-D-glucopyranosiduronic acid
-
-
3-[6-(2'-dimethylaminomethyl-biphenyl-4-yl)-7-oxo-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridine-1-yl]-benzamide
-
the inhibitor shows good fXa potency, selectivity, in vivo efficacy and oral bioavailability
3-[6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
3-[7-fluoro-3-methyl-6-[4-(2-oxopiperidin-1-yl)phenyl]-1H-indazol-1-yl]benzenecarboximidamide
-
-
3-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl](methyl)amino]-2-oxopyrrolidin-1-yl]methyl]benzenecarboximidamide
-
-
3-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl]amino]-2-oxopyrrolidin-1-yl]methyl]benzenecarboximidamide
-
-
3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
-
-
3-{4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl}-4-hydroxybenzamidine
-
-
4'-chloro-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
-
-
4'-[1-(4-methoxyphenyl)-4-methyl-7-oxo-3-(trifluoromethyl)-1,7-dihydro-6H-pyrazolo[3,4-d]pyridazin-6-yl]biphenyl-2-sulfonamide
-
-
4'-[1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,7-dihydro-6H-pyrazolo[4,3-d]pyrimidin-6-yl]biphenyl-2-sulfonamide
-
-
4,4'-[(2-oxocycloheptane-1,3-diylidene)di(E)methylylidene]dibenzenecarboximidamide
-
-
4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide)
-
-
4-(3-(aminoiminomethyl)phenyl)-1-(6-chloro-benzo[b]thiophene-2-sulfonyl)-piperazin-2-one
-
-
4-(4-(2-oxopyridin-1(2H)-yl)benzamido)-3-(3,4,5-trimethoxybenzamido)benzoic acid
-
-
4-(4-amino-quinazolin-7-ylmethyl)-1-(6-chloro-benzo[b]thiophene-2-sulfonyl)-piperazin-2-one
-
-
4-(4-[5-[([[(5-chlorothiophen-2-yl)carbonyl]oxy]amino)methyl]-2-oxo-1,3-oxazolidin-3-yl]phenyl)morpholin-3-one
-
-
4-(benzo[b]thien-2-ylsulfonyl)-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-([[(5-chlorothiophen-2-yl)carbonyl]amino]methyl)-3-fluoro-5-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]benzoic acid
-
-
4-acetamido-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-benzamide
-
-
4-bromo-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)benzamide
-
-
4-chloro-3-([[(4-chlorocyclopenta-1,3-dien-1-yl)carbonyl]amino]methyl)-N-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2,3-dihydro-1H-indole-1-carboxamide
-
-
4-chloro-N-[4-(2-[[2-fluoro-4-(2-oxopyrazin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-1,3-thiazol-2-yl]benzamide
-
-
4-chloro-N-[5-(2-oxo-2-[4-[2-oxo-2-(pyrrolidin-1-yl)ethyl]piperazin-1-yl]ethyl)-3H-pyrrol-2-yl]benzamide
-
-
4-hydroxy-3-[2-oxo-3-(S)-(5-pyridin-3-yl-thiophene-2-sulfonylamino)-pyrrolidin-1-ylmethyl]-benzamidine
-
i.e. RPR130737, highly specific inhibitor of factor Xa realtive to other serine proteases, reversible, fast binding, competitive active-site directed inhibitor
4-methoxy-N-[2-[([[1-(pyridin-4-yl)piperidin-4-yl]methyl]carbamoyl)amino]phenyl]benzamide
-
-
4-[(3-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(4'-chloro[1,1'-biphenyl]-4-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(5'-chloro[2,2'-bithiophen]-5-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazine-2-one
-
-
4-[(5-chloro-1H-indol-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
-
4-[(6-bromobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
-
4-[(6-chloro-2-naphthalenyl)sulfonyl]-1-[[1-(4-pyridinyl)-4-piperidinyl]-methyl]piperazinone
-
i.e. M55113, strong inhibitor, highly selective for factor Xa over trypsin and thrombin
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-imidazo[4,5-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-b]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(furo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(1-methyl-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(4,5-dihydro-4-oxo-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(5-oxido-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[[1-(2-hydroxyethyl)-1H-pyrrolo[3,2-c]pyridin-2-yl]methyl]-piperazin-2-one
-
-
4-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorothieno[3,2-b]pyridin-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-3-methoxy-5-[[1-(propan-2-yl)piperidin-4-yl]carbamoyl]benzoic acid
-
-
4-[3-[(4-chlorophenyl)amino]-3-oxopropyl]-3-([[5-(propan-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]carbonyl]amino)-5-(trifluoromethyl)benzoic acid
-
-
4-[[(1E)-2-(4-chlorophenyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[[(1E)-2-(5-chloro-2-thienyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[[(1E)-2-(5-chloro-4-methoxy-2-thienyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl]-1-(pyridin-4-yl)piperidine-4-carboxylic acid
-
-
4-[[(3-carbamimidoylphenyl)amino]methyl]-3-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzoic acid
-
-
4-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl](methyl)amino]-2-oxopyrrolidin-1-yl]methyl]thiophene-2-carboximidamide
-
-
4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
-
-
4-[[(E)-2-(5-chlorothiophen-2-yl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
-
4-[[2-(5-chloro-2-thienyl)ethyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate
5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)-2-methylimidazo[1,2-a]pyridine
-
-
5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridine
-
-
5-bromo-N-([(5S)-3-[4-(3-methylidenemorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-butyl-2-(3-carbamimidoyl-phenyl)-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
5-chloro-3-hydroxy-4'-methoxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
-
-
5-chloro-3-[(5-chloro-2-pyridyl)carbamoyl]-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]phenyl beta-D-glucopyranosiduronic acid
-
-
5-chloro-N-(1-oxo-2-[3-[(pyridin-4-ylamino)methyl]benzyl]-2,3-dihydro-1H-isoindol-4-yl)thiophene-2-carboxamide
-
-
5-chloro-N-(2-[[1-(propan-2-yl)piperidin-4-yl](1,3-thiazol-2-ylmethyl)sulfamoyl]ethyl)thiophene-2-carboxamide
-
-
5-chloro-N-(4-[2-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]-2-oxoethyl]-1,3-thiazol-2-yl)thiophene-2-carboxamide
-
-
5-chloro-N-(5-chloro-2-pyridyl)-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
-
-
5-chloro-N-(5-chloro-2-pyridyl)-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
-
AS1468240, potent inhibitor
5-chloro-N-(5-chloropyridin-2-yl)-2-([4-[(2-imino-1,3-oxazolidin-3-yl)methyl]benzoyl]amino)benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-([4-[(dimethylamino)methyl]benzoyl]amino)benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-([[trans-4-(3-oxomorpholin-4-yl)cyclohexyl]carbonyl]amino)benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-[(4-[[ethanimidoyl(methyl)amino]methyl]benzoyl)amino]benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)benzoyl]amino]-3-methoxybenzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-[[4-(piperidin-1-ylcarbonoimidoyl)benzoyl]amino]benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-3-hydroxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-3-methoxy-2-[[4-(2-oxopiperidin-1-yl)benzoyl]amino]benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-3-methoxy-2-[[4-(2-oxopyridin-1(2H)-yl)benzoyl]amino]benzamide
-
-
5-chloro-N-([(5R)-3-[4-(2-imino-1,3-oxazolidin-3-yl)phenyl]-4,5-dihydro-1,2-oxazol-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-2-imino-3-[4-(2-oxo-1,3-oxazolidin-3-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-2-imino-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-2-oxo-3-[4-(2-oxopyrrolidin-1-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-3-[2-fluoro-4-(3-oxomorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-3-[3-cyclopropyl-4-(5-oxo-1,4-oxazepan-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-3-[3-fluoro-4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-3-[3-fluoro-4-(thiomorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-3-[4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([1-[2-(3-oxopiperazin-1-yl)-4-(2-oxopyridin-1(2H)-yl)phenyl]-1H-imidazol-4-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([1-[2-(methylamino)-4-(2-oxopyridin-1(2H)-yl)phenyl]-1H-1,2,3-triazol-4-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([1-[4-(2-imino-1,3-oxazolidin-3-yl)phenyl]-3-phenyl-1H-pyrazol-4-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([1-[4-(2-oxopyridin-1(2H)-yl)-2-(piperazin-1-yl)phenyl]-1H-1,2,3-triazol-4-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([1-[4-(2-oxopyridin-1(2H)-yl)phenyl]-1H-imidazol-4-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([3-[4-(3-oxomorpholin-4-yl)phenyl]-1,2,4-oxadiazol-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([4-[6-fluoro-7-(methylamino)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl]phenyl]carbamoyl)thiophene-2-sulfonamide
-
-
5-chloro-N-[(1-[3-methyl-4-(3-oxomorpholin-4-yl)phenyl]-2-[[(methylsulfonyl)amino]methyl]-1H-imidazol-4-yl)methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1R,2S)-2-([4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]benzoyl]amino)cyclopentyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1R,2S)-2-[[4-(2-oxopyridin-1(2H)-yl)benzoyl]amino]cyclopentyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1R,4R)-4-[[2-fluoro-4-(2-oxopyrazin-1(2H)-yl)phenyl]carbamoyl]-2-(2-oxopropyl)cyclopentyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1R,4S)-2-ethoxy-4-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]carbamoyl]cyclopentyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1R,4S)-4-[[2-fluoro-4-(2-oxopyrazin-1(2H)-yl)phenyl]carbamoyl]-2-hydroxycyclopentyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1S,2S)-2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]carbamoyl]cyclohexyl]pyridine-2-carboxamide
-
-
5-chloro-N-[(2R)-3-methoxy-1-[[3-methyl-4-(3-oxomorpholin-4-yl)phenyl]amino]-1-oxopropan-2-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[(3R)-1-(3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)-5-oxopyrrolidin-3-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[(3R)-1-[2-fluoro-4-(3-oxomorpholin-4-yl)phenyl]-5-oxopyrrolidin-3-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[(3R,4R)-1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-4-methoxypyrrolidin-3-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[(3R,4S)-4-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]carbamoyl]-1-(methylsulfonyl)pyrrolidin-3-yl]pyridine-2-carboxamide
-
-
5-chloro-N-[(3S)-1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-4-methoxypyrrolidin-3-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[(3S,4S)-3-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]carbamoyl]-1-methylpiperidin-4-yl]pyridine-2-carboxamide
-
-
5-chloro-N-[1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-1H-1,2,4-triazol-3-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[1-oxo-2-[3-(3-oxomorpholin-4-yl)benzyl]-2,3-dihydro-1H-isoindol-4-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[1-[(3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)carbamoyl]cyclopropyl]thiophene-2-carboxamide
-
-
5-chloro-N-[2-[3-(2-imino-1,3-oxazolidin-3-yl)benzyl]-3-oxo-2,3-dihydro-1H-isoindol-4-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[3-oxo-2-[3-(3-oxomorpholin-4-yl)benzyl]-2,3-dihydro-1H-isoindol-4-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[4-(dimethylamino)-2-[[4-(2-imino-1,3-oxazolidin-3-yl)phenyl]carbamoyl]-5-methylphenyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[(5R)-3-[4-[2-(furan-2-yl)-4,5-dihydro-1H-imidazol-1-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[(5S)-3-[2-fluoro-4-[3-(hydroxymethyl)-2-oxopyridin-1(2H)-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[(5S)-3-[4-[3-(hydroxymethyl)-2-oxopyridin-1(2H)-yl]-3-methylphenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[(5S)-3-[4-[3-[2-[(2-hydroxyethyl)amino]ethyl]-2-oxopyridin-1(2H)-yl]-3-(methoxymethyl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[(5S)-3-[4-[3-[2-[(trans-4-hydroxycyclohexyl)amino]ethoxy]-2-oxopyridin-1(2H)-yl]-3-methylphenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[3-(4-cyanophenyl)-4,5-dihydro-1,2-oxazol-5-yl]methyl]thiophene-2-carboxamide
-
-
5-ethynyl-N-(2-methyl-1-[[3-methyl-4-(3-oxomorpholin-4-yl)phenyl]amino]-1-oxopropan-2-yl)thiophene-2-carboxamide
-
-
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-(4-[1-[(dimethylamino)methyl]cyclopropyl]phenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]phenyl)-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-(4-[2-[(dimethylamino)methyl]cyclopenta-2,4-dien-1-yl]phenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-chloro-benzo[b]thiophene-2-sulfonic acid [2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)-pyrrolidin-3-yl]-amide
-
-
6-chloro-benzo[b]thiophene-2-sulfonic acid [2-oxo-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-pyrrolidin-3-yl]-amide
-
-
6-chloro-N-methyl-N-[(3S)-2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pyrrolidin-3-yl]-1-benzothiophene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-(6-fluoro-2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[(1R)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[(1S)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[(1S)-1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[2-fluoro-4-[(1S)-1-(methylamino)ethyl]phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-(2-fluoro-4-piperidin-1-ylphenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-(2-fluoro-4-pyridin-4-ylphenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]thieno[2,3-b]pyridine-2-sulfonamide
-
-
6-chloro-N-[1-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]thieno[2,3-b]pyridine-2-sulfonamide
-
-
6-[2'-(methylsulfonyl)biphenyl-4-yl]-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(aminooxy)sulfinyl]-3-fluorobiphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-4-methyl-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[3,4-d]pyridazin-7-one
-
-
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylic acid
-
-
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(3-nitrophenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-ethylphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(iminomethyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-5-methyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
6-[2-(4-chlorophenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]-2,2,4,7-tetramethyl-1,2,3,4-tetrahydroquinoline
16% activity at 0.005 mM; 35% activity at 0.03 mM; 63% activity at 0.001 mM; 67% activity at 0.03 mM; 76% activity at 0.005 mM; 82% activity at 0.03 mM; 85% activity at 0.005 mM; 87% activity at 0.03 mM; 8% activity at 0.005 mM; 94% activity at 0.03 mM
6-[3-fluoro-2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
6-[4-(1-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]cyclopropyl)phenyl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[4-([(2S)-4-[(3-chloro-1H-indol-6-yl)sulfonyl]-2-methyl-6-oxopiperazin-1-yl]methyl)phenyl]-2-methylpyridazin-3(2H)-one
-
-
6-[4-([4-[(3-chloro-1H-indol-6-yl)sulfonyl]-3-hydroxypiperazin-1-yl]carbonyl)piperidin-1-yl]-2-methylpyridazin-3(2H)-one
-
-
6-[4-([4-[(5-chloro-1H-indol-2-yl)sulfonyl]-2-oxopiperazin-1-yl]methyl)phenyl]-2-[2-(dimethylamino)ethyl]pyridazin-3(2H)-one
-
-
7'-[(6-chloronaphthalen-2-yl)sulfonyl]-8a'-(hydroxymethyl)-1-(pyridin-4-yl)tetrahydro-5'H-spiro[piperidine-4,2'-[1,3]thiazolo[3,2-a]pyrazin]-5'-one
-
-
7-([7-[(1-ethanimidoylpiperidin-4-yl)oxy]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]methyl)naphthalene-2-carboximidamide
-
-
7-oxo-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
7-[(2R)-5-[(1-ethanimidoylpiperidin-4-yl)methyl]-1-(ethylsulfonyl)-2,3-dihydro-1H-indol-2-yl]naphthalene-2-carboximidamide
-
-
8-amino-N-[(1R)-2-oxo-1-phenyl-2-[4-(pyridin-4-yl)piperazin-1-yl]ethyl]naphthalene-2-carboxamide
-
-
8-amino-N-[(1R)-2-[4-[4-fluoro-2-(methylsulfonyl)phenyl]piperazin-1-yl]-2-oxo-1-phenylethyl]naphthalene-2-carboxamide
-
-
abciximab
-
glycoprotein IIb/IIIa receptor-antagonist, 3.8% inhibition at 0.140 mM in absence of heparin, 49% inhibition at 0.14 mM in presence of heparin 1 U/ml
-
actinomycin
-
no remaining enzyme activityafter 20 h
active site-mutated activated protein C
-
-
-
AduNAP4
-
an anticoagulant peptide from the blood-feeding human hookworm, Ancylostoma duodenale, that consits of 104 amino acids including a predicted 23-residue signal peptide. Cloning and recombinant expression of His-tagged and thioredoxin-tagged in Escherichia coli strain BL21, GenBank ID EU552548. Exhibits mixed-type inhibition versus factor Xa
-
Alpha1-proteinase inhibitor
-
engineering of functional exosites in P1 Arg variant increases the association rate constant for the reactions with factors Xa and IXa, without affecting the inhibitor reactions with trypsin and thrombin. Mutation K222Y/L224E in alpha1-proteinase inhibitor increases the association rate constant 14fold
-
amblyomin-X
-
cloning of the inhibitor from the salivary glands of the tick Amblyomma cajennense, the transcript codes for a protein with unique structure containing an N-terminal Kunitz-type domain and a C-terminus, which acts as an inhibitor factor Xa, recombinant inhibitor expression in Escherichia coli, amblyomin-X structure-function relationships, molecular modelling, overview
-
Ancylostoma ceylanicum anticoagulant peptide 1
-
i.e. AcAP1, natural enzyme inhibitor from human specific hookworm, cloned and sequenced, GenBank accession number AF399710, purified, recombinant expression in Escherichia coli, possesses anticoagulant activity in vivo, specific inhibition of factor Xa, no inhibition of other proteases like thrombin, kallikrein, or coagulation factor XIIa, inhibition mechanism
-
Ancylostoma ceylanicum anticoagulant peptide 5
-
i.e. AcAP5, natural enzyme inhibitor from dog specific hookworm, also inhibits the human factor Xa, competitive to AcAP1
-
antithrombin mutant HAT/Proth-1
-
mutant of human antithrombin possessing factor Xa-cleavage site 1 from human thrombin, recombinant from expression in inhuman 293 cells, inactivation of factor Xa is 3-4fold more effective that with mutant HAT/Proth-2, increased inactivation by heparin and 300-500fold by pentasaccharide fragment of heparin
-
antithrombin mutant HAT/Proth-2
-
mutant of human antithrombin possessing factor Xa-cleavage site 2 from human thrombin, recombinant from expression in inhuman 293 cells, increased inactivation by heparin and 300-500fold by pentasaccharide fragment of heparin
-
AP'4
-
nonapeptide comprising amino acids 323-331 of factor Va, strong, inhibition of prothrombinase activity, noncompetitive with respect to prothrombin, inhibition mechanism
Aprotinin
-
95% inhibition of factor Xa and 2% inhibition of prothrombinase complex activity at 10 U/ml
atrial polypeptide
-
promotes factor Xa-antithrombin III complex formation when preincubated with antithrombin III, or when added within 1 min to factor Xa/antithrombin III mixtures. It promotes transformation of free factor Xaalpha into factor Xabeta
-
Bauhinia ungulata factor Xa inhibitor
-
i.e. BuXI, specific Kunitz-type inhibitor of factor Xa, methionine residues at the active site of the inhibitor are involved in the inhibition mechanism, oxidized protein does no longer inhibit factor Xa
-
BIBM1015
4-(1-methyl-benzimidazole-based inhibitor)
BIBR1109
4-(1-methyl-benzimidazole-based inhibitor)
BIBT0871
possesses a 1-methyl-benzimidazole scaffold placing the methyl substitutent into the S2-subsite, pyridinyl moiety interacts with F174, binding structure
bivalirudin
-
intravenously applicated inhibitor
Bovine pancreatic trypsin inhibitor
-
factor Xa-trypsin hybrid mutants
-
choline
-
positively linked to Na+ binding
coronary-dilatory hypothalamic neurohormone C
-
incubation with factor Xa and antithrombin III results in a decrease in total complex formation, a decrease in modified antithrombin III, a decrease in factor Xagamma and little change in the ratio of free factor Xaalpha to factor Xabeta. Neurohormone C retards the hydrolysis of the factor Xa/antithrombin III complexes which forms free factor Xa and modified antithrombin III
-
cycloheximide
-
61% inhibition at 0.01 mg/ml after 3 h, complete inhibition after 20 h
dabigatran etexilate
-
i.e. Rendix, Pradaxa
diisopropylfluorophosphate
eisenstasin
-
protein inhibitor isolated from the midgut of Eisenia andrei
-
endogeneous polypeptide inhibitor
-
8.8fold purification of a 15 kDa polypeptide inhibitor from nymphs of camel tick Hyalomma dromedarii, with potent antocoagulant properties, specific for factor Xa compared to other serine proteases, binds 2 sites of factor Xa, uncompetitive, inhibits blood coagulation, 329 U/mg, complete inhibition by 2 inhibitor units
-
enoxaparin
-
increases the inhibitory effect of abciximab and eptifibatide
epi-N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
3fold less anticoagulant activity than stereoisomer N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
eptifibatide
-
glycoprotein IIb/IIIa receptor-antagonist, 13.5% inhibition at 0.333 mM in absence of heparin, 38% inhibition at 0.14 mM in presence of heparin 1 U/ml
eribaxaban
-
efficacy and safety in oral application, overview
ethyl (4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)acetate
-
-
ethyl 1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
ethyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)-2-methylpropanoate
-
-
ethyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)propanoate
-
-
ethyl 3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]benzoate
-
-
ethyl 4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]benzoate
-
-
ethyl 6-(2'-hydroxybiphenyl-4-yl)-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
ethyl 6-[3-fluoro-2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
ethyl N-[(1R)-1-cyclohexyl-2-[(2S)-2-[[4-(N'-hydroxycarbamimidoyl)benzyl]carbamoyl]azetidin-1-yl]-2-oxoethyl]glycinate
-
-
ethyl N-[(2-[[(4-[N'-[(hexyloxy)carbonyl]carbamimidoyl]phenyl)amino]methyl]-1-methyl-1H-benzimidazol-5-yl)carbonyl]-N-(pyridin-2-yloxy)-b-alaninate
-
-
ethyl N-[(2-[[(4-[N'-[(hexyloxy)carbonyl]carbamimidoyl]phenyl)amino]methyl]-1-methyl-1H-benzimidazol-5-yl)carbonyl]-N-pyridin-2-yl-b-alaninate
-
-
ethyl N-[1-cyclohexyl-2-[2-([2-[4-(N'-hydroxycarbamimidoyl)phenyl]ethoxy]carbamoyl)azetidin-1-yl]-2-oxoethyl]glycinate
-
-
ethyl-(4-(2-oxopyridin-1(2H)-yl)benzamido)-3-(3,4,5-trimethoxybenzamido)benzoate
-
-
factor Va peptide
-
factor Va amino acid residues 697-709, i.e. D13R, competitive inhibition of prothrombinase activity with respect to prothrombin, inhibition mechanism
-
fidexaban
-
a direct FXa inhibitor
fondaparinux
-
an indirect factor Xa inhibitor
fondaparinux sodium
-
a direct FXa inhibitor
FPR-prothrombin
-
i.e. prothrombin specifically active site-labeled with D-Phe-Pro-Arg-CH2Cl, acts as a competitive inhibitor of prothrombin activation. The inhibitory effect of FPR-ProT increases with decreasing phospholipid concentration, with a 5fold decrease in the FPR-ProT concentration required for 50% inhibition at 0.002 mM phospholipid compared with that at 0.030 mM
-
fucoidan
-
brown algae sulfated polysaccharide from Fucus evanescens. Deacetylation of fucoidan does not alter its inhibitory capacities, while purification from protein and polyphenols reduces inhibitory effects. depolymerization of fucoidan increases inhibitory activity
HD1-22
-
bivalent fusion aptamer consisting of 15-base spanning DNA aptamer HD1 which specifically inhibits the procoagulant functions of thrombin, and aptamer HD22 which binds to exosite 2 of thrombin, interconnected by a poly-dA linker. Aptamer HD1-22 binds to (pro)exosite 1 of prothrombin and inhibits the prothrombinase activity nearly 2fold better than HD1. The anticoagulant activities of HD1-22 are fully reversed by addition of antidote-oligodeoxynucleotides
-
heparin pentasaccharide
-
-
hir54-65(SO3+)
-
C-terminal fragment of hirudin. Inhibition of the rate of cleavage at residues R320 of prethrombin 2, thrombin formation, and the activation of prethrombin 2 by prothrombinase
idrabiotaparinux
-
i.e. SSR126517E, an indirect factor Xa inhibitor
idrabiotaparinux sodium
-
a direct FXa inhibitor
idraparinux sodium
-
a direct FXa inhibitor
JTV-803
-
synthetic selective inhibitor of coagulation factor Xa strongly inhibits thrombin generation without affecting initial thrombin forming time necessary for platelet activation in hemostasis
LY-517717
-
a xaban, specific for factor Xa
m-(o-(2-chloro-5-fluorosulfonylphenylureido)phenoxybutoxy)benzamidine
-
-
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-([[4-(1-oxidopyridin-4-yl)benzoyl]amino]oxy)butanoate
-
-
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate
methyl (3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetate
-
-
methyl (4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetate
-
-
methyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2-methylpropanoate
-
-
methyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)propanoate
-
-
methyl 2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzenesulfinate
-
-
methyl 3'-fluoro-4'-(3-[[(3-methoxyphenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-(3-[[(4-fluorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-(3-[[(4-methoxyphenyl)sulfonyl]amino]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-(3-[[(5-isoxazol-3-ylthiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-([[1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]carbonyl]amino)biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[2-oxo-3-[(phenylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[2-oxo-3-[(quinolin-3-ylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[2-oxo-3-[(quinolin-6-ylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[3-(4-methoxyphenoxy)-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[3-(iminomethyl)-1-(4-methoxyphenyl)-5,7-dioxo-1,4,5,7-tetrahydro-6H-pyrazolo[4,3-d]pyrimidin-6-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[3-([[4-(iminomethyl)phenyl]sulfonyl]methyl)-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[3-[(1H-indazol-6-ylsulfamoyl)methyl]-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[3-[(4-methoxyphenyl)amino]-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3-(3-carbamimidoylphenyl)-5-[(4-carbamimidoylphenyl)carbamoyl]-4,5-dihydro-1,2-oxazole-5-carboxylate
-
-
methyl 3-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2,2-dimethylpropanoate
-
-
methyl 3-[3-[amino(imino)methyl]phenyl]-5-[4-[amino(imino)methyl]phenyl]pentanoate
-
-
methyl 3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
-
-
methyl 4'-(3-[[(2,5-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(3,4-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(3,4-difluorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(3,5-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(3-chlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(4-chloro-6-methyl-1-benzothiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(4-chlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(4-ethylphenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(5-chlorothiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(diethylamino)ethyl](methyl)amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(dimethylamino)ethyl](methyl)amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(dimethylamino)ethyl]amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](3-hydroxypropyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl]amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl][2-(4-methylpiperazin-1-yl)-2-oxoethyl]amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(7-chloronaphthalen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-([[4-amino-3-(iminomethyl)-1-(4-methoxyphenyl)-1H-pyrazol-5-yl]carbonyl]amino)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-[1-(2-amino-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[1-(2-carbamoyl-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[1-(2-carbamoylphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[1-[2-[(aminooxy)sulfinyl]-4-methoxyphenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[1-[2-[(aminooxy)sulfinyl]phenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[(2-hydroxyethyl)(methyl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[methyl(1-methylpiperidin-4-yl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-[3-[(cyclohexylsulfonyl)methyl]-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
-
-
methyl 6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
methyl N-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]glycinate
-
-
methyl N-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycinate
-
-
methyl [3-(3-carbamimidoylphenyl)-4-[(2'-sulfamoylbiphenyl-4-yl)carbamoyl]-4,5-dihydro-1,2-oxazol-5-yl]acetate
-
-
methyl [3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]amidosulfite
-
-
N-(2,4-dichlorophenyl)-4-(2,2,4,7-tetramethyl-1,2,3,4-tetrahydroquinolin-6-yl)pyrimidin-2-amine
1% activity at 0.03 mM
N-(2-chlorophenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
11% inhibition at 0.00136 mM
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl](methyl)amino]ethyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl](methyl)amino]ethyl)-N,5-dimethyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]ethyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]ethyl)-N,5-dimethyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]phenyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-(3-chloro-4-methoxyphenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
39% inhibition at 0.00136 mM
N-(3-chlorophenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
76% inhibition at 0.00136 mM
N-(3-methoxyphenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
40% inhibition at 0.00136 mM
N-(3-[[4'-(trifluoromethyl)biphenyl-4-yl]methoxy]phenyl)piperidine-4-carboxamide
-
-
N-(4-butoxyphenyl)piperidine-3-carboxamide
-
slight inhibition
N-(4-carbamoyl-2-(3,4,5-trimethoxybenzamido)phenyl)-2-oxo-1-phenyl-1,2-di-hydropyridine-4-carboxamide
-
-
N-(4-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
-
N-(4-chlorophenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
complete inhibition at 0.00136 mM
N-(4-ethylphenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
15% inhibition at 0.00136 mM
N-(5-carbamoyl-2-(4-(2-oxopiperidin-1-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dichlorobenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dimethoxybenzamide
-
highly potent, selective, direct inhibitor
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-chlorobenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-fluorobenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-formamidobenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-methoxybenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-5-chlorothio-phene-2-carboxamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-6-chloronicotinamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)benzo[d]oxa-zole-6-carboxamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyrrolidin-1-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
-
N-(5-chloro-2-pyridyl)-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
-
-
N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide
-
-
N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]benzamide
-
-
N-(5-chloropyridin-2-yl)-3-hydroxy-2-[[4-(1-methyl-4-oxo-1,4-dihydropyridin-3-yl)benzoyl]amino]benzamide
-
-
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]ethanediamide
-
-
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
N-(5-chloropyridin-2-yl)-N'-[(3R,4S)-1-formyl-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]piperidin-4-yl]ethanediamide
-
-
N-(5-chloropyridin-2-yl)-N'-[4-(3-oxomorpholin-4-yl)phenyl]pyrazine-2,3-dicarboxamide
-
-
N-(5-chlorothiophen-2-yl)-N'-[(3R,4S)-1-formyl-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]piperidin-4-yl]ethanediamide
-
-
N-(6-methoxypyridin-3-yl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
7% inhibition at 0.00136 mM
N-(benzylsulfonyl)-3-(1-carbamimidoylpiperidin-4-yl)-D-alanyl-N-[(2S)-5-carbamimidamido-1-hydroxypentan-2-yl]glycinamide
-
-
N-([1-[4-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-methoxy-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3-fluorophenyl]-1H-imidazol-2-yl]methyl)-2-methoxy-N,N-dimethyl-2-oxoethanaminium
-
-
N-([1-[4-(3-[[(6-chloronaphthalen-2-yl)sulfonyl]amino]-2-oxopiperidin-1-yl)-3-fluorophenyl]-1H-imidazol-2-yl]methyl)-2-methoxy-N,N-dimethyl-2-oxoethanaminium
-
-
N-([3-(1,1'-biphenyl-4-yl)methoxy]phenyl)piperidine-4-carboxamide
-
-
N-1-adamantylaminocarbonyl-D,L-3-amidinophenylalanine methyl ester
-
-
N-1-adamantyloxycarbonyl-(R)-3-amidinophenylalanine-(2-phenyl)-1-ethylamide
-
-
N-1-adamantyloxycarbonyl-(R)-D-3-amidinophenylalanine benzylamide
-
-
N-1-adamantyloxycarbonyl-(R)-D-3-amidinophenylalanine methyl ester
-
-
N-1-adamantyloxycarbonyl-(R)-L-3-amidinophenylalanine methyl ester
-
-
N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine
-
-
N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester
-
-
N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine piperidine
-
-
N-1-adamantyloxycarbonyl-D,L-4-amidinophenylalanine methyl ester
-
-
N-1-adamantyloxycarbonyl-D,L-4-guanidinophenylalanine methyl ester
-
-
N-9-fluorenemethyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester
-
-
N-benzyloxycarbonyl-D,L-3-amidinophenylalanine piperidine
-
-
N-methyl-N-[(3S)-2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
-
N-tert-butyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester
-
-
N-[(1R)-1-(5-chloro-1H-benzimidazol-2-yl)-2-methoxyethyl]-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7-carboxamide
-
-
N-[(1R)-1-(5-chloro-1H-benzimidazol-2-yl)-2-methoxyethyl]-4-(3-oxomorpholin-4-yl)-3-(trifluoromethyl)benzamide
-
-
N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
-
N-[(1R)-2-(4-benzoylpiperidin-1-yl)-2-oxo-1-phenylethyl]-3-carbamimidoylbenzamide
-
-
N-[(1R)-2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
-
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclobutyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cycloheptyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclooctyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
N-[(1R,2S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2S,4R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2S,5S)-2-[(1H-indol-2-ylcarbonyl)amino]-5-(methylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
N-[(1R,2S,5S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
potent inhibition, promising anticoagulant activity and good oral bioavailability
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dipropylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
-
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-[(2-hydroxyethyl)(methyl)carbamoyl]cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
-
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-[(2-methoxyethyl)(methyl)carbamoyl]cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclobutyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cycloheptyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclooctyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(2-[[(4-carbamimidoylphenyl)amino]methyl]-1-methyl-1H-benzimidazol-5-yl)carbonyl]-N-pyridin-2-yl-b-alanine
-
-
N-[(2S)-1-[(2R)-2-[[2-(aminomethyl)-5-chlorobenzyl]carbamoyl]pyrrolidin-1-yl]-4-(1-oxidopyridin-2-yl)-1-oxobutan-2-yl]glycine
-
-
N-[(2S)-1-[(2R)-2-[[2-(aminomethyl)-5-chlorobenzyl]carbamoyl]pyrrolidin-1-yl]-4-(4-hydroxyphenyl)-1-oxobutan-2-yl]glycine
-
-
N-[(2S)-5-carbamimidamido-1-(2,3-dihydro-1,3-thiazol-2-yl)-1-oxopentan-2-yl]-2-[4-[(4-chlorophenyl)sulfonyl]-2-oxopiperazin-1-yl]acetamide
-
-
N-[(3aR,7aR)-2-[3-(2-amino-2-iminoethoxy)benzyl]-1,3-dioxooctahydro-1H-isoindol-4-yl]-5-chlorothiophene-2-carboxamide
-
-
N-[(3R,4S)-1-acetyl-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]piperidin-4-yl]-N'-(5-chloropyridin-2-yl)ethanediamide
-
-
N-[(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-1-methoxypiperidin-3-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-1-[(dimethylamino)oxy]piperidin-3-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(3S)-1-(1-amino-2,3-dihydro-1H-inden-5-yl)-2-oxopyrrolidin-3-yl]-6-chloronaphthalene-2-sulfonamide
-
-
N-[(3S)-1-[(1,6-diaminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
-
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]-7-methoxynaphthalene-2-sulfonamide
-
-
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
-
N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
N-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]glycine
-
-
N-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycine
-
-
N-[1-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-(dimethylamino)-4-oxobutan-2-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[2-([[4-(aminomethyl)cyclohexyl]methyl]amino)-2-oxo-1-phenylethyl]-3-carbamimidoylbenzamide
-
-
N-[2-([[4-(aminomethyl)cyclohexyl]methyl]amino)-2-oxoethyl]-3-carbamimidoylbenzamide
-
-
N-[2-[(4-chlorophenyl)carbamoyl]-4-methoxyphenoxy]benzene-1,4-dicarboxamide
-
-
N-[2-[(4-methoxybenzoyl)amino]phenyl]-1-(pyridin-4-yl)piperidine-4-carboxamide
-
-
N-[2-[(4-tert-butylbenzoyl)amino]phenyl]-3-carbamimidoylbenzamide
-
-
N-[2-[(5-chloropyridin-2-yl)carbamoyl]phenyl]-2'-sulfamoylbiphenyl-4-carboxamide
-
-
N-[2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)phenyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[3-(benzyloxy)phenyl]piperidine-3-carboxamide
-
slight inhibition
N-[3-(benzyloxy)phenyl]piperidine-4-carboxamide
-
slight inhibition
N-[3-(biphenyl-4-ylmethoxy)phenyl]-1-carbamimidoylpiperidine-3-carboxamide
-
-
N-[3-(biphenyl-4-ylmethoxy)phenyl]-1-carbamimidoylpiperidine-4-carboxamide
-
-
N-[3-(biphenyl-4-ylmethoxy)phenyl]piperidine-3-carboxamide
-
-
N-[3-(biphenyl-4-ylmethoxy)phenyl]piperidine-4-carboxamide
-
-
N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-1-[3-(5-methylidene-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-1-[3-[(glycylamino)methyl]phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
N-[3-[(2',3'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
N-[3-[(2',4',6'-trifluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
N-[3-[(2',4'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
N-[3-[(2',5'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
N-[3-[(2',6'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
N-[3-[(2'-fluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
N-[3-[(3',4',5'-trifluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
N-[3-[(3',5'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
N-[3-[(3'-fluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
N-[3-[(4'-fluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-3-carboxamide
-
-
N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-4-carboxamide
-
slight inhibition
N-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]acetamide
-
-
N-[4-(biphenyl-4-ylmethoxy)phenyl]piperidine-3-carboxamide
-
slight inhibition
N-[4-(biphenyl-4-ylmethoxy)phenyl]piperidine-4-carboxamide
-
-
N-[4-(dimethylamino)phenyl]-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
24% inhibition at 0.00136 mM
N-[4-(N,N-dimethylcarbamimidoyl)-2-fluorophenyl]-1-(3-fluoronaphthalen-2-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]-6-hydroxyphenyl]-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7-carboxamide
-
-
N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]phenyl]-2'-[(dimethylamino)methyl]biphenyl-4-carboxamide
-
-
N-[4-[(4-fluorobenzyl)oxy]phenyl]piperidine-3-carboxamide
-
slight inhibition
N-[4-[(4-fluorobenzyl)oxy]phenyl]piperidine-4-carboxamide
-
slight inhibition
N-[4-[2-(2-[[1-(2-fluorobenzoyl)piperidin-4-yl]oxy]phenyl)-2-oxoethyl]pyridin-3-yl]-4-methoxybenzamide
-
-
N1-(4-bromophenyl)-3-methoxy-N2-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)azetidine-1,2-dicarboxamide
-
-
N2,N2-dimethyl-N5-[[(2-methyl-1-benzofuran-5-yl)amino]([2-oxo-1-[2-oxo-2-(pyrrolidin-1-yl)ethyl]azepan-3-yl]amino)methylidene]pyridine-2,5-dicarboxamide
-
-
N2-(benzylsulfonyl)-D-arginyl-N-[(2S)-5-carbamimidamido-1-hydroxypentan-2-yl]glycinamide
-
-
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(1-methyl-4,5-dihydro-1H-imidazol-2-yl)phenyl]glycinamide
-
-
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]-D-norvalinamide
-
-
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]norvalinamide
-
-
N2-[(4-chlorophenyl)carbamoyl]-N2-(cyclopropylmethyl)-N-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]glycinamide
-
-
N2-[(4-chlorophenyl)carbamoyl]-N2-(cyclopropylmethyl)-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]glycinamide
-
-
N2-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
N2-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N2-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycinamide
-
-
N24R
-
peptide comprising amino acids 307-348 of the factor Va heavy chain, binds to membrane-bound factor Xa and inhibits its activity
-
N5-(5-chloropyridin-2-yl)-N4-[4-(2-imino-1,3-oxazolidin-3-yl)phenyl]-2-methyl-1,3-thiazole-4,5-dicarboxamide
-
-
Nalpha-4'-amidinobenzensulfonyl-glycyl-D,L-4-amimidinophenylalanine ethyl ester
-
-
Nalpha-tosylglycyl-D,L-3-amidinophenylalanine alkyl ester
-
-
nematode anticoagulant protein c2
-
i.e. NAPc2, binds either to factor X or factor Xa, tight binding, competitive, binds to a macromolecular substrate binding, exosite site of human prothrombinase complex, recombinantly expressed in Pichia pastoris and purified, inhibition kinetics
-
NH2-RCRFGYR-OH
-
i.e. ESP, small peptide derived from protein inhibitor eisenstasin. ESP exhibits a high level of factor Xa inhibition in chromogenic peptide substrate assays and inhibits proteinase-activated receptor 2-mediated factor Xa activation resulting in significant reduction of endothelial nitric oxide
Nodipecten nodosus HS-like glycosaminoglycan
-
extracted from the mollusk and fractionated by ethanol precipitation, resists degradation with heparinase I but is cleaved by nitrous acid, structure analysis. It shows an anticoagulant activity of 36 IU/mg and inhibits factor Xa with a IC50 of 835 ng/ml in the presence of antithrombin. Exhibits no bleeding effect, or induction factor XIIa-mediated kallikrein activity, or toxic effect on fibroblast cells
-
octamixaban
-
i.e. FXV-673, a potent, reversible and direct FXa inhibitor
p-amidinophenylmethanesulfonyl fluoride
-
-
p-nitrophenylguanidinobenzoate
-
-
phenylmethanesulfonyl fluoride
-
-
platelet factor 4
-
upon preincubation with factor Xa and heparin, platelet factor 4 at about 250 nM decreases the kcat of peptide substrate S2765 hydrolysis about fivefold and that of prothrombin activation about 25fold. In the presence of saturating fVa, inhibition of factor Xa by platelet factor is abolished, while in the presence of limiting factor Va, platelet factor 4 alters the interaction of factor Xa with factor Va. High concentrations of platelet factor 4 restore factor Xa activity toward peptide S2765 and prothrombin, indicating a dual effect of platelet factor 4 on factor Xa activities. Heparin is required to promote the formation of an fXaPF4 complex
-
PMSF
-
complete inhibition of factor Xa and 5% inhibition of prothrombinase complex activity at 1 mM
propan-2-yl 4-[(3-chloro-1H-indol-6-yl)sulfonyl]-1-[[1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl]methyl]-6-oxopiperazine-2-carboxylate
-
-
protein inhibitor C
-
presence of heparin enhances inhibition up to 42fold in the presence of a physiological Ca2+ concentration. In the absence of Ca2+, no enhancement of inhibition is observed
-
protein NAP
-
a known nematode anticoagulant protein/peptide
-
protein S
-
protein S counteracted the inhibition of activated factor V by FXa of the Arg506 cleavage, leading to 50% reduced activity, whereas protein S and FXa yielded a 3fold additive stimulatory effect of the cleavage at Arg306, annihilation of the FXa protection of the Arg506 cleavage by protein S is due to an enhanced rate of Arg506 cleavage of FVa not bound to FXa, resulting in depletion of free FVa and dissociation of FXa-FVa complexes
-
protein Z-dependent protease inhibitor
-
ProTS195A
-
the prothrombin mutant also does inhibit thrombin generation, but with a much smaller effect compared to that with FPR-ProT
-
recombinant tick saliva anticoagulant protein
-
-
-
RNA11F7t
-
a RNA aptamer, that is selected from a combinatorial library based on its ability to bind factor Xa, inhibits thrombin formation catalyzed by prothrombinase without obscuring the active site of Xa within the enzyme complex. Selective inhibition of protein substrate cleavage arises from the ability of the aptamer to bind to factor Xa and exclude interactions between the proteinase and cofactor within prothrombinase. Competition for enzyme complex assembly results from the binding of RNA11F7t to factor Xa with nanomolar affinity in a Ca2+-dependent interaction. RNA11F7t binds equivalently to the zymogen factor X as well as derivatives lacking gamma-carboxyglutamic acid residues, strong Ca2+-dependence of the binding ofRNA1F7t
-
RPR120844
-
potent direct inhibitor, overview over effects in vivo
RPR128515
compound contains a benzamidine moiety and surrogate of the basic group, binds in a canonical fashion typical for synthetic serine protease inhibitors, no direct hydrogen bonding with the carboxylate of Asp189 at the bottom of the S1 pocket, binding mode and inhibition mechanism; i.e. 3-[(3'-aminomethyl-biphenyl-4-carbonyl)-amino]-2-(3-carbamimidoyl-benzyl)-butyric acid methyl ester
RPR131247
compound contains a benzamidine moiety and surrogate of the basic group, binds in a canonical fashion typical for synthetic serine protease inhibitors, no direct hydrogen bonding with the carboxylate of Asp189 at the bottom of the S1 pocket, binding mode and inhibition mechanism
RPR132747
i.e. 3-[4-(6-chloro-benzo[b]thiophene-2-sulfonyl)-2-oxo-piperazin-1-ylmethyl]-benzamidine, non-peptide inhibitor based on a sulfonylpiperazinone scaffold
RPR200095
i.e. 4-[4-(6-chloro-benzo[b]thiophene-2-sulfonyl)-2-oxo-piperazin-1-ylmethyl]-benzamidine
RPR208566
-
potent direct inhibitor, overview over effects in vivo
RPR208707
compound contains a benzamidine moiety and surrogate of the basic group, binds in a canonical fashion typical for synthetic serine protease inhibitors, no direct hydrogen bonding with the carboxylate of Asp189 at the bottom of the S1 pocket, binding mode and inhibition mechanism
RPR208815
compound contains a benzamidine moiety and surrogate of the basic group, binds in a canonical fashion typical for synthetic serine protease inhibitors, no direct hydrogen bonding with the carboxylate of Asp189 at the bottom of the S1 pocket, binding mode and inhibition mechanism
RPR208944
i.e. 4-(6-chloro-benzo[b]thiophene-2-sulfonyl)-1-[1-(2-hydroxy-ethyl)-1H-pyrrolo[3,2-c]pyridin-2-ylmethyl]-piperazin-2-one
RPR209685
i.e. 4-[2-(5-chloro-thiophen-2-yl)-ethenesulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
SK549
-
potent direct inhibitor, overview over effects in vivo
Soybean trypsin inhibitor
-
SR90107A/ORG31540
-
synthetic pentasaccharide, selective, antithrombin-III dependent factor Xa inhibitor, inhibition of platelet and fibrin deposition onshunts in vivo, prevention of thrombosis
tanogitran
-
a direct FXa inhibitor
tert-butyl N-(3-carbamimidoylbenzoyl)-D-tyrosinate
-
-
tert-butyl [(3S,4R)-1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-4-(trifluoromethyl)pyrrolidin-3-yl]carbamate
-
-
therostasin
-
highly specific, natural, tight-binding inhibitor, 5200fold purified from the rhynchobdellid leech Theromyzon tessulatum, DNA and amino acid sequence determination and analysis, protein of 8990 Da encoded by 825 bp, SwissProt accession number P82355, GenBank accession number AF239803, causes a 4fold increase in blood clotting velocity
-
tick anticoagulant peptide
-
tirofiban
-
glycoprotein IIb/IIIa receptor-antagonist, 16.9% inhibition at 0.042 mM in absence of heparin, 48% inhibition at 0.14 mM in presence of heparin 1 U/ml
tissue factor pathway inhibitor
-
trans-N'-[2-[(5-chloropyridin-2-yl)carbamoyl]-5-(dihydroxymethyl)-1-benzofuran-3-yl]-N,N-dimethylcyclohexane-1,4-dicarboxamide
-
-
trimethylphenylammonium
-
i.e. TMPA, strong and highly specific inhibition, inhibits substrate hydrolysis competitively, does not inhibit the binding of 4-aminobenzamidine to the S1-pocket, and is positively linked to Na+ binding rsulting in 10fold increase in binding of inhibitor at 0.15 M Na+, interacts with Y99, F174, and W215 via van der Waals interactions, and the charged amine coupling electrostatically with the carboxylates of E97
Triton X-100
-
complete inactivation at 0.05%
Viperidae snake venom group IIA secreted phospholipases A2
i.e. SVPLA2, different isoforms, overview, FXa strong-binding SVPLA2s CBc, MtxII, CbII and CBa2 inactivate factor Xa by direct binding and by interacting with FXa by the non-catalytic phospholipid-independent mechanism, identification of the potential FXa binding site, overview
-
vitamin K
-
induction of enzyme activity
YM-150
-
a xaban, specific for factor Xa
ZK-807191
-
a dihydrochloride salt of fidexaban
ZK-816042
CI-1031, 183305-24-0, amidine-imidazole inhibitor, inhibitor conformation and binding mode to the enzyme is investigated by NMR structure determination of the lyophilized enzyme-inhibitor complex formed in presence of stabilizing excipients
[2-([4-[(5S)-5-([[(5-chlorothiophen-2-yl)carbonyl]amino]methyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]amino)ethoxy]acetic acid
-
-
[4-[(5-chloro-1H-indol-2-yl)sulfonyl]piperazin-1-yl](5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)methanone
-
-
[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol
[[4-(2-[[(5-carbamimidoyl-2-hydroxyphenyl)sulfonyl]amino]ethyl)-2'-(methylsulfonyl)biphenyl-3-yl]oxy]acetic acid
-
-
(1S,3R,4S)-4-[(1H-indol-2-ylcarbonyl)amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
-
100% remaining rate after 5 min incubation with human liver microsomes
(1S,3R,4S)-4-[(1H-indol-2-ylcarbonyl)amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
-
less oral availability than compound N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, more metabolically stable
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
i.e. GW813893. More than 90fold selective over all enzymes tested, including thrombin, factor IXa, factor XIa, kallikrein, plasmin and several more
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
i.e. GW813893. Suppresses thrombotic activity correlating with the suppression of plasma-based clotting activity and the inhibition of plasma factor Xa activity. Inhibitor is orally active
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
i.e. GW813893. Suppresses thrombotic activity correlating with the suppression of plasma-based clotting activity and the inhibition of plasma factor Xa activity. Inhibitor is orally active
(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid
-
i.e. R-142086. Exhibits potent anti-factor Xa activity and anticoagulant activity when administered orally
(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid
-
potent anticoagulant activity, no mutagenic potential and high selectivity for factor Xa over trypsin
1,2-dicaproyl-sn-glycero-3-phospho-L-serine
-
i.e. C6PS, soluble phospholipid, inhibition of amidolytic activity of factor Xa in absence of Ca2+
1,2-dicaproyl-sn-glycero-3-phospho-L-serine
-
presence of 1,2-dicaproyl-sn-glycero-3-phospho-L-serine and 5 mM Ca2+ results in dimerization with concomitant decrease in kcat value. Binding of 1,2-dicaproyl-sn-glycero-3-phospho-L-serine exposes residues K351. K242, and K420
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
i.e. SN429
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
selective for factor Xa over thrombin, trypsin, plasmin, and tissue plasminogen activator
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
-
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
inhibitor shows bioavailability under both fasted and fed conditions
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
inhibitor shows bioavailability under both fasted and fed conditions and antithrombotic efficacy in a rat model of venous thrombosis after oral administration, without a significant increase in bleeding time
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
i.e. FXV673, highly specific fo factor Xa compared to other serine protesases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, inhibition of thrombus formation in vivo in the acute arterial and venous electrolytic injury canine model, no effect on platelet aggregation
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
i.e. FXV673, highly specific fo factor Xa compared to other serine proteases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, no effect on platelet aggregation
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
i.e. FXV673, highly specific fo factor Xa compared to other serine protesases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, no effect on platelet aggregation
4-aminobenzamidine
-
competitive
4-aminobenzamidine
-
90% inhibition of factor Xa and 2% inhibition of prothrombinase complex activity at 1 mM
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate
-
i.e. JTV-803, strong, synthetic inhibitor highly specific for factor Xa compared to other serine proteases
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate
-
i.e. JTV-803, synthetic the enzyme in vitro and thrombus formation in rats in vivo
antistasin
-
naturally occurring inhibitor, anticoagulant isolated from Mexican leech Haementeria officinalis, slow, tight-binding, selective inhibitor protein
-
antistasin
-
the inhibitor exerts its inhibitory effect at a site removed from the active site of factor Xa
-
antithrombin
-
complete inhibition
-
antithrombin
-
Arg150 of the autolysis loop is involved in specific interaction with the activated conformation of antithrombin
-
antithrombin
-
i.e. HAT, serpin, human, recombinant from expression in human 293 cells, inhibition is increased by heparin
-
antithrombin
-
inhibition is enhanced by heparin. Ca2+ increases about 3fold the inhibition rate of wild-type recombinant enzyme over that in presence of EDTA
-
antithrombin
-
complete inhibition
-
antithrombin
-
human recombinant protein, competitive inhibition, heparin-activated antithrombin, interaction and inhibition mechanism involving inhibitor residues Tyr253, as well as Glu255, Glu237, and Arg399, and exosites generated via heparin binding, rapid kinetic studies, wild-type and mutant antithrombins, overview
-
antithrombin
-
allosteric activation of antithrombin as a factor IXa and Xa inhibitor requires binding of a high-affinity heparin pentasaccharide and involves mitigation of repression rather than positive enhancement, via a mechanism in which heparin activates antithrombin by mitigating an unfavorable surface interaction, by altering its nature, and by moving the attached proteinase away from the site of the unfavorable interaction through RCL expulsion, detailed overview
-
antithrombin
-
heparin and antithrombin-binding sulfated pentasaccharide DEFGH, and derivatives thereof, activate antithrombin, design of two tetra-sulfated N-arylacyl tetrahydroisoquinoline variants as potential nonsaccharide activators of antithrombin, binding affinities, kinetics, and binding sites, modeling, overview. Second-order rate constants of antithrombin inhibition of factor Xa in the presence and absence of the designed activators show antithrombin activation in the range of 8-80fold at pH 6.0
-
antithrombin
-
irreversible inhibition
-
antithrombin III
-
AT3, a member of the serpin superfamily of protease inhibitors, X-ray crystal structure-based simulations of AT3/FXa, PDB code 2GD4, overview
-
antithrombin III
-
90% inhibition of factor Xa at 0.01 mg/ml in presence of heparin and 5% inhibition of prothrombinase complex activity at 1 U/ml
-
apixaban
-
-
apixaban
-
inhibitor does not alter platelet aggregation to ADP, gamma-thrombin, and collagen
apixaban
-
i.e. BMS-562247
apixaban
-
an oral, direct, and highly selective factor Xa inhibitor in late-stage clinical development for the prevention and treatment of thromboembolic diseases. Evaluation of the metabolic drug-drug interaction potential of apixaban in vitro, overview. Apixaban shows a slow metabolic turnover in incubations of human liver microsomes with formation of O-demethylation and hydroxylation products as prominent in vitro metabolites
apixaban
-
i.e. BMS-562247-1, a xaban, specific for factor Xa
apixaban
-
efficacy and safety in oral application, overview
apixaban
-
i.e. BMS-562247, a small molecule able to inhibit in a selective and reversible manner the active site of both free and prothrombinase-bound factor Xa, requires oraladministration, bleeding rates of 0.69%
apixaban
-
a direct oral factor Xa inhibitor
apixaban
-
a direct, oral applicable, selective factor Xa inhibitor and activated prothrombinase, reversible and potent inhibition of both free and cell bound factor Xa. It has low potential for drug-drug interactions and is predominantly eliminated through metabolic pathways and non-renal mechanisms
apixaban
-
highly selective inhibitor
apixaban
-
highly selective inhibitor
apixaban
-
study on use for prevention of arterial thrombosis in rabbit models of electrically induced carotid artery thrombosis and cuticle bleeding time. Addition of aspirin to apixaban significally reduces the thrombus weight with no significant increase in bleeding time. Addition of aspirin and apixaban to clopidogrel produces a further significant reduction in thrombus weight. Combination of clopidogrel and aspirin with apixaban produces a significant but moderate 2.1fold increase in bleeding time
apixaban
-
inhibitor does not alter platelet aggregation to ADP, gamma-thrombin, and collagen. In vivo, apixaban is effective in the prevention of experimental thrombosis at doses that preserve hemostasis
apixaban
-
i.e. BMS-562247 or 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5-dihydropyrazolo[5,4-c]pyridine-3-carboxamide. Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban. Oxidative metabolism of radiolabeled apixaban by liver microsomes is approximately 20times faster in rabbits than in rats or humans. Prominant metabolites are O-demethyl apixaban, O-demethyl apixaban glucuronide and O-demethyl apixaban sulfate, metabolic profiles, overview
betrixaban
-
-
betrixaban
-
a xaban, specific for factor Xa; i.e. PRT-054021
betrixaban
-
efficacy and safety in oral application, overview
Ca2+
-
maximal inhibition at 2 mM
Ca2+
-
presence of heparin enhances inhibition by protein inhibitor C up to 42fold in the presence of a physiological Ca2+ concentration. In the absence of Ca2+, no enhancement of inhibition is observed
Ca2+
-
the strength of the dimer interaction is strongly Ca2+-concentration-dependent, such that significant dimer forms in solution only at or above 5 mM Ca2+
CI-1031
-
i.e. ZK-807834, small molecule direct inhibitor of facor Xa, prevention of thrombosis when administered in vivo
CI-1031
-
i.e. ZK-807834, small molecule direct inhibitor of facor Xa
DEGR-chloromethyl ketone
-
inactivation
DEGR-chloromethyl ketone
-
inactivation
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
2.5 mM: 10% inhibition of factor Xa and 95% inhibition of prothrombinase complex activity, 10 mM: 90% inhibition of factor Xa and 95% inhibition of prothrombinase complex activity
DX-9065a
-
fast-binding inhibitor
DX-9065a
-
competitive, factor Xa
DX-9065a
-
synthetic selective inhibitor of coagulation factor Xa strongly inhibits thrombin generation without affecting initial thrombin forming time necessary for platelet activation in hemostasis
DX-9065a
-
inhibits factor Xa increased thymidine incorporation in mesangial cells, inhibits activation of extracellular regulated kinase in mesangial cells
DX-9065a
-
a low-molecular selective fXa inhibitor
DX-9065a
-
a direct FXa inhibitor
DX-9065a
-
i.e. (2S)-2[4-[[(3S)-1-acetimidoyl-3-pyrrolidinyl]oxy]phenyl]-3-(7-amidino-2-naphthyl) propanoic acid hydrochloride pentahydrate, a specific factor Xa inhibitor, DX-9065a treatment significantly ameliorated proteinuria in vivo in rats with a significant reduction in the size of glomeruli, the total number of glomerular cells, and crescent formation, as well as abolishing the phosphorylation of p44/42 MAP kinase on day 8
DX9065a
-
small, potent and selective direct inhibitor of fXa, prevents thrombosis in vivo
DX9065a
-
requires system administration
edoxaban
-
a xaban, specific for factor Xa; i.e. DU-176b
edoxaban
-
efficacy and safety in oral application, overview
EDTA
-
-
EDTA
-
complete inhibition at 10 mM
FXV673
-
small molecule direct inhibitor of facor Xa, prevention of thrombosis when administered in vivo
FXV673
-
small molecule direct inhibitor of facor Xa
heparin
-
alos induces thrombocytopenia
heparin
-
highly increases the inhibitory effects of glycoprotein IIb/IIIa receptor-antagonists
heparin
inhibition via complex formation with and modulation of the activity of thrombin
idraparinux
-
an indirect factor Xa inhibitor
idraparinux
-
a synthetic pentasaccharide and long-acting, indirect, specific antithrombin-dependent factor Xa inhibitor, population pharmacokinetic modelling and analysis from phase III clinical trials, investigation in the treatment and prevention of thromboembolic events
LY517717
-
efficacy and safety in oral application, overview
LY517717
-
a direct factor Xa inhibitor, requires oraladministration, with an oral bioavailability of 25-82%. LY517717 is apparently primarily cleared via a gastrointestinal route
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate
-
i.e. RPR208566, highly specific
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate
-
i.e. RPR208566, inhibits thrombus formation in the rat artery model, highly specific
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
i.e. DU-176b. Presence prolongs the activated partial thromboplastin time, prothrombin time and thrombin time in plasma. It does not impair human platelet aggregation induced by ADP or thromboxane A2 receptor agonist U46619. Thrombin-induced platelet aggregation is inhibited with IC50 value of 2.9 microM
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
i.e. DU-176b. Dose-dependently inhibits thrombus formation in a rabbit thrombosis model
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
i.e. DU-176b dose-dependently inhibits thrombus formation in a rat thrombosis model. Bleeding time in rats is not significantly prolonged at an antithrombotic dose
N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
46% remaining rate after 5 min incubation with human liver microsomes
N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
higher oral availability than compounds (1S,3R,4S)-4-[(1H-indol-2-ylcarbonyl)amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid, N-[(1R,2S,5S)-2-[(1H-indol-2-ylcarbonyl)amino]-5-(methylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, less metabolically stable
N-[(1R,2S,5S)-2-[(1H-indol-2-ylcarbonyl)amino]-5-(methylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
63% remaining rate after 5 min incubation with human liver microsomes
N-[(1R,2S,5S)-2-[(1H-indol-2-ylcarbonyl)amino]-5-(methylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
less oral availability than compound N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, more metabolically stable
otamixaban
-
i.e. FXV-673
otamixaban
-
requires system administration
PD0313052
-
slow, tight-binding mechanism, factor Xa; slow, tight-binding mechanism, prothrombinase
PD0313052
-
i.e. [(2R, 6S)-2-(5-carbamimidoyl-2-hydroxy-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-quinoxaline-6-carboxylic acid]
protein Z-dependent protease inhibitor
-
inhibition by branched pathway acyl-intermediate trapping mechanism. Reaction proceeds by the initial assembly of a membrane-associated protein Z-protein Z-dependent protease inhibitor-factor Xa Michaelis complex followed by conversion to a stable protein Z-dependent protease inhibitor-factor Xa complex. Assembly of the Michaelis complex is rate-limiting. For every factor Xa molecule inhibited, two inhibitor molecules are cleaved. Protein Z dissociates from protein Z-dependent inhibitor once a stable complex with factor Xa is formed. It acts catalytically to accelerate the membrane-dependent protein Z-dependent protease-factor Xa reaction
-
protein Z-dependent protease inhibitor
-
ZPI, UniProt ID Q9UK55, a member of the serpin superfamily of protease inhibitors, ZPI can produce rapid inhibition of FXa in the presence of the not-essential cofactor protein Z, negatively charged phospholipids and Ca2+ ions, mechanism. Generation of a three-dimensional structural model of the Michaelis complex of human ZPI/FXa using homology modeling, protein-protein docking and molecular dynamics simulation methods, overview
-
razaxaban
-
-
razaxaban
-
i.e. BMS-561389
rivaroxaban
-
i.e. 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide or BAY 597939, an oral, direct factor Xa inhibitor for the prevention and treatment of thromboembolic disorders, in vitro metabolism and pathways, detailed overview
rivaroxaban
-
sensitive and specific quantification in human plasma by high-performance liquid chromatography-tandem mass spectrometry. Concentrations between 0.5 and 500 micrograms per liter can be detected. Inter-assay precision is below 7.4% and inter-assay accuracy is between 96.3% and 102.9%
rivaroxaban
-
an oral direct factor Xa inhibitor, in advanced development as an alternative to warfarin for the prevention and treatment of thromboembolic disorders
rivaroxaban
-
i.e. 5-chloro-N-[[(2S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxaziolidin-5-yl]methyl]thiophene-2-carboxamide, an small molecule oral factor Xa inhibitor, binds factor Xa rapidly and reversibly, mode of binding, pharmacodynamics and pharmacokinetics, overview
rivaroxaban
-
an oral inhibitor, safety, pharmacokinetics and pharmacodynamics of single/multiple doses of the oral, direct factor Xa inhibitor rivaroxaban in healthy male Chinese individuals, overview
rivaroxaban
-
i.e. Xarelto
rivaroxaban
-
i.e. 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide or BAY 597939, an oral, direct factor Xa inhibitor for the prevention and treatment of thromboembolic disorders, in vitro metabolism and pathways, detailed overview
rivaroxaban
-
i.e. BAY 59-7939, a xaban, specific for factor Xa
rivaroxaban
-
efficacy and safety in oral application, overview
rivaroxaban
-
i.e. BAY 59-7939, requires oraladministration. It is absorbed in the gastrointestinal tract, is primarily excreted by the kidneys, and has a bioavailability of more than 80%, and bleeding rates of 4.3-10.2%
rivaroxaban
-
a direct oral factor Xa inhibitor
rivaroxaban
-
i.e. 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide or BAY 597939, an oral, direct factor Xa inhibitor for the prevention and treatment of thromboembolic disorders, in vitro metabolism and pathways, detailed overview
Soybean trypsin inhibitor
-
factor Xa-trypsin hybrid mutants
-
Soybean trypsin inhibitor
-
complete inhibition of factor Xa and 5% inhibition of prothrombinase complex activity at 0.01 mg/ml
-
TAK-442
-
a xaban, specific for factor Xa
TAK-442
-
efficacy and safety in oral application, overview
TAK-442
-
potent factor Xa/prothrombinase inhibitor, acts synergistically with aspirin or clopidogrel in preventing arterial thrombosis and whole blood coagulation. TAK-442, aspirin, or clopidogrel alone have no significant effect on thrombus formation, whereas the combination of TAK-442 with aspirin and clopidogrel remarkably prolonge the time to thrombus formation without additional significant prolongation of bleeding time
tick anticoagulant peptide
-
inhibition is thermodynamically favored when the enzyme is assembled in the prothrombinase complex
-
tick anticoagulant peptide
-
i.e. TAP, 60 amino acid peptide, isolated from the tick Ornithodoros moubata, reversible, slow, tight-binding inhibitor, short-term inhibition of clot-associated procoagulant activity in vitro and in vivo
-
tick anticoagulant peptide
-
TAP
-
tick anticoagulant peptide
-
a slow, tight-binding specific inhibitor. The inhibitor is purified from extracts of Ornithodoros moubata
-
tick anticoagulant peptide
-
TAP
-
tissue factor pathway inhibitor
-
i.e. TFPI, plasma fXa inhibitor
-
tissue factor pathway inhibitor
-
-
-
warfarin
-
-
warfarin
-
a vitamin K antagonist, inhibits factors Xa and VII, and thrombin
warfarin
-
62% inhibition at 0.02 mg/ml after 3 h, and 90% after 20 h
YM-60828
-
potent direct inhibitor, overview over effects in vivo
YM150
-
efficacy and safety in oral application, overview
YM150
-
a direct inhibitor of factor Xa, requires oraladministration,bleeding rate is 11.8-23.5%
[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol
-
selective and orally bioavailable inhibitor
[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol
-
good oral bioavailability after oral administration at a dose of 3 mg/kg in fasted monkeys. Pharmakokinetics study
additional information
-
inhibition mechanism, inhibitor binding
-
additional information
-
not affected by NH4+ and Li+
-
additional information
-
inhibition potential of overlapping peptides within the region of amino acids 307-348 of factor Va heavy chain
-
additional information
-
no inhibition by the Bauhinia variegata trypsin inhibitor BvTI
-
additional information
neutral groups such as chlorobenzohtiophene or chlorothiophene and basic groups such as benzamidine interact in the S1 pocket through the neutral group whereas the S4 pocket is occupied by the basic moiety
-
additional information
-
neutral groups such as chlorobenzohtiophene or chlorothiophene and basic groups such as benzamidine interact in the S1 pocket through the neutral group whereas the S4 pocket is occupied by the basic moiety
-
additional information
-
structure-activity relationship, development and synthesis of zinc-binding independent inhibitors, overview
-
additional information
-
inhibitory effect, oral bioavailability and pharmakokinetic profile of DPC423 derivatives, overview
-
additional information
binding mode of dual specific inhibitors, with a N-methyl-benzimidazole scaffold, of thrombin and factor Xa, overview
-
additional information
-
binding mode of dual specific inhibitors, with a N-methyl-benzimidazole scaffold, of thrombin and factor Xa, overview
-
additional information
-
potencies of inhibitor molecules and anticoagulant activities, overview
-
additional information
-
no inhibition by hirudin
-
additional information
-
inhibitors of blood coagulation factors Xa and IIa, i.e. PD0313052 and argatroban, synergize to reduce thrombus weight and thrombin generation in vivo and in vitro
-
additional information
-
development of phenyltriazolinone inhibitors, X-ray structure analysis and binding structure, overview
-
additional information
-
rational design of small-molecule direct fXa inhibitors, synthesis, overview
-
additional information
-
clinical studies, efficacy and safety of factor Xa inhibitors, overview
-
additional information
-
factor Xa acts as anticoagulants, clinical studies, overview
-
additional information
-
synthesis of a series of benzyloxy anilides of nipecotic and isonipecotic acids, as inhibitors of ADP-induced platelet aggregation and the blood coagulation enzyme factor Xa
-
additional information
-
structure and property based design of factor Xa pyrrolidin-2-one inhibitors with aminoindane and phenylpyrrolidine P4 motifs, rational design, syntheses and evaluation, overview
-
additional information
-
evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs, overview
-
additional information
-
design, synthesis, and structure-activity relationship of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors
-
additional information
-
development of direct FXa inhibitors, overview. Selectivity is a significant issue in the development of factor Xa inhibitors, since several trypsin-like serine proteases play key regulatory roles in the coagulation cascade, among them FVIIa, FIXa, FXa, FXIa, and thrombin
-
additional information
-
sulfated low-molecular weight lignins CDSO3, FDSO3, SDSO3, and unfractionated heparin inhibit thrombin and factor Xa through allosteric disruption of the catalytic apparatus, specifically through the catalytic step
-
additional information
not inhibited by VGY-000058
-
additional information
-
benzamidine functionally is a common theme in most classes of inhibitors, with many of the most potent compounds requiring two basic functional groups to afford potent inhibition. Reliance on this structural feature may afford difficulty in obtaining inhibitors with acceptable oral absorption and with sufficiant duration of action to qualify as clinical candidates for oral anticoagulant trials
-
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0.000272
(2RS)-(3'-amidino-3-biphenyl)-5-(4-pyridylamino)pentanoic acid
i.e. FX-2212
0.0000017
(3-[[(3-carbamimidoylphenyl)(2-[[4-(1-ethanimidoylpiperidin-4-yl)phenyl]amino]-2-oxoethyl)amino]methyl]phenoxy)acetic acid
-
pH and temperature not specified in the publication
0.00000055
(4S,5S)-3-(3-carbamimidoylphenyl)-5-(methoxymethyl)-N-(2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1,2-oxazole-4-carboxamide
-
pH and temperature not specified in the publication
0.000004 - 0.0000097
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
0.0000003
(E)-2-(5-chlorothiophen-2-yl)-N-(1-[5-[2-(methylsulfonyl)phenyl]pyridin-2-yl]-2-oxopyrrolidin-3-yl)ethenesulfonamide
-
pH and temperature not specified in the publication
0.000001
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000006
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000013
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(6-fluoro-2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000002
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000015
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000006
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000008
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000001
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000005
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000003
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000006
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000002
(E)-2-(5-chlorothiophen-2-yl)-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000002
(E)-2-(5-chlorothiophen-2-yl)-N-[1-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000055
(E)-2-(5-chlorothiophen-2-yl)-N-[[(3R)-1-[[1-(pyridin-4-yl)piperidin-4-yl]carbonyl]pyrrolidin-3-yl]methyl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.00054
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-4-cyanobenzylpropionamide
-
pH 8.0, 25°C
0.00017
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-4-hydroxyphenethylpropionamide
-
pH 8.0, 25°C
0.00022
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-benzylpropionamide
-
pH 8.0, 25°C
0.00034
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-ethyl-propionamide
-
pH 8.0, 25°C
0.000074
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamide
-
pH 8.0, 25°C
0.00049
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-phenpropionyl-propionamide
-
pH 8.0, 25°C
0.00023
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-propionic acid phenethyl ester
-
pH 8.0, 25°C
0.000074
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(2-chloro)-phenethyl-propionamide
-
pH 8.0, 25°C
0.000074
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(3-chloro)-phenethyl-propionamide
-
pH 8.0, 25°C
0.00095
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(4-amino)-phenethyl-propionamide
-
pH 8.0, 25°C
0.002
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(4-tert-butyl)-phenethyl-propionamide
-
pH 8.0, 25°C
0.000025
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamides
-
pH 8.0, 25°C
0.00000076
(R)-6-(2'-((3-hydroxypyrrolidin-1-yl)methyl)-[1,1'-biphenyl]-4-yl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-5,6-dihydro-1H-pyrazolo[3,4-c]pyridin-7(4H)-one
-
-
0.0000013
([(7-carbamimidoylnaphthalen-2-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
-
pH and temperature not specified in the publication
0.0012
1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[2,3-b]pyridin-2-ylsulfonyl)-piperazin-2-one
-
above
0.0012
1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[3,2-b]pyridin-2-ylsulfonyl)-piperazin-2-one
-
above
0.00000004
1-(3-amino-1,2-benzisoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.00000003
1-(3-amino-1,2-benzoxazol-5-yl)-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
pH and temperature not specified in the publication
0.0000044
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[2-[(dimethylamino)methyl]pyridin-3-yl]-2-fluorophenyl)-7-fluoro-1H-indazole-3-carboxamide
-
pH and temperature not specified in the publication
0.00000017
1-(3-amino-1,2-benzoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-5-methyl-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
pH and temperature not specified in the publication
0.00000019
1-(3-amino-1,2-benzoxazol-5-yl)-N-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.000002
1-(3-aminophenyl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000013
1-(3-carbamimidoylphenyl)-3-methyl-N-(2'-sulfamoylbiphenyl-4-yl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.000000015
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
0.000000013
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00000016
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
0.00000029
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-4-bromo-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt
-
-
0.0000008
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt
-
-
0.00000046
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(fluoro)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.000000008
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00000004
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.0000013
1-(3-[amino(imino)methyl]phenyl)-N-[2'-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00000011
1-(4-methoxyphenyl)-3-(methylsulfonyl)-6-(4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000018
1-(4-methoxyphenyl)-4-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[3,4-d]pyridazin-7-one
-
-
0.0000014
1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(1H-tetrazol-1-ylmethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.0000029
1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(2H-tetrazol-2-ylmethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.000000054
1-(4-methoxyphenyl)-6-(4-[1-[(methylamino)methyl]cyclopropyl]phenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000055
1-(4-methoxyphenyl)-6-(4-[1-[(methylamino)methyl]cyclopropyl]phenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.000000042
1-(4-methoxyphenyl)-6-[4-(1-[[(1-methylethyl)amino]methyl]cyclopropyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000064
1-(4-methoxyphenyl)-6-[4-[1-(morpholin-4-ylmethyl)cyclopropyl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000021
1-(4-methoxyphenyl)-6-[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.00000024
1-(4-methoxyphenyl)-7-oxo-6-(4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.0000011
1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
0.00000008
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
pH and temperature not specified in the publication
0.000000074
1-(4-methoxyphenyl)-7-oxo-6-[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.0000015
1-(6-chloronaphthalen-2-yl)-N-[2'-[(dimethylamino)methyl]-3-fluorobiphenyl-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.057
1-carbamimidoyl-N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-3-carboxamide
-
pH 8.0, 25°C
0.0338
1-carbamimidoyl-N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00122
1-[(4-amino-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-piperazin-2-one
-
-
0.0000008
1-[(4-aminoquinazolin-7-yl)methyl]-4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]piperazin-2-one
-
pH and temperature not specified in the publication
0.00000097
1-[1-(3-amino-1,2-benzoxazol-5-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-2-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]phenyl)ethanone
-
pH and temperature not specified in the publication
0.00000091
1-[2-(aminomethyl)phenyl]-N-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.000001
1-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide
-
pH and temperature not specified in the publication
0.0000012
1-[2-[(aminooxy)sulfinyl]phenyl]-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.021
1-[3-(5-amino-1,3,4-thiadiazol-2-yl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
above
0.0049
1-[3-(5-amino-4H-1,2,4-triazol-3-yl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
0.0000004
1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000027
1-[3-(aminomethyl)phenyl]-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
0.000000013
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-(2'-(methylsulfonyl))-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
0.00000015
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
0.00000015
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.0026
1-[3-[([1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methyl)sulfonyl]phenyl]pyridinium
-
-
0.000054
1-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]urea
-
-
0.000011
1-[3-[amino(imino)methyl]phenyl]-N-[2'-(aminosulfonyl)[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00026
1-[4-amino-3-[([1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methyl)sulfonyl]phenyl]pyridinium
-
-
0.000003
1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide
-
pH and temperature not specified in the publication
0.000008
1H-pyrrolo[3,2-c]pyridine-1-acetamide, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-
-
-
0.000154
1H-pyrrolo[3,2-c]pyridine-1-acetic acid, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-
-
-
0.000018
1H-pyrrolo[3,2-c]pyridine-1-acetic acid, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-, methyl ester
-
-
0.00057
2,2'-ethane-1,2-diylbis(1-benzofuran-5-carboximidamide)
-
pH and temperature not specified in the publication
0.0000005
2-(1-[(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2-hydroxypropanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
pH and temperature not specified in the publication
0.000002
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
pH and temperature not specified in the publication
0.00021
2-(2-hydroxy-5-methylbiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.000078
2-(2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.0068
2-(2-hydroxybiphenyl-3-yl)benzofuran-5-carboxamidine
-
pH 7.4, 22°C
0.014
2-(2-hydroxyphenyl)1H-benzoimidazole-5-carboxamidine
-
pH 7.4, 22°C
0.0027
2-(2-hydroxyphenyl)1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.03
2-(2-hydroxyphenyl)3-methyl-3H-benzoimidazole-5-carboxamidine
-
pH 7.4, 22°C
0.019
2-(2-methoxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.000089
2-(3,5-dibromo-2-hydroxyphenyl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.00000089
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.00000048
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.0000016
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.00000038
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.00000091
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.00000036
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.000052
2-(3-bromo-2-hydroxy-5-methylphenyl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.000078
2-(3-bromo-2-hydroxy-5-nitrophenyl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.000043
2-(3-bromo-2-hydroxyphenyl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.00000001
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-bromo-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.000000009
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-chloro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.00000002
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.000000005
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.000000007
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide
-
-
0.000000041
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide
-
-
0.000000008
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.000000005
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide
-
below
0.000000005
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
below
0.000000009
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide
-
-
0.00000001
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide
-
-
0.00021
2-(5-bromo-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.00034
2-(5-chloro-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.000014
2-(5-nitro-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.00000027 - 0.00000141
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
0.043
2-biphenyl-3-yl-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.0000065
2-cyano-1-(2-methyl-1-benzofuran-5-yl)-3-[2-oxo-1-[2-oxo-2-(pyrrolidin-1-yl)ethyl]azepan-3-yl]guanidine
-
pH and temperature not specified in the publication
0.0000027
2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
0.0000004
2-[6-[3-([[(E)-2-(5-chlorothiophen-2-yl)ethenyl]sulfonyl]amino)-2-oxopyrrolidin-1-yl]pyridin-3-yl]benzenesulfonamide
-
pH and temperature not specified in the publication
0.00000013
2-[N2-(benzylsulfonyl)-D-arginylglycyl-L-arginyl]-1,3-thiazole
-
pH and temperature not specified in the publication
0.0000115
2-[[4-(dimethylamino)benzoyl]amino]-N-(5-methoxypyridin-2-yl)-5-[(methylsulfonyl)amino]benzamide
-
pH and temperature not specified in the publication
0.0000235
3-(1-[5-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-pentyl]-2-oxo-1,2-dihydroquinolin-3-yl)-4-hydroxybenzamidine
-
-
0.0000189
3-(1-[5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl]-2-oxo-1,2,3,4-tetrahydro-3-quinolinyl)-4-hydroxybenzenecarboximidamide
-
-
0.0000129
3-(1-[5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl]-2-oxo-1,2,3,4-tetrahydro-3-quinolinyl)benzenecarboximidamide
-
-
0.0000021
3-(1H-imidazol-1-ylmethyl)-1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00000015
3-(3-carbamimidoyl-phenyl)-isoxazole-4-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.00000015
3-(3-carbamimidoylphenyl)-N-(2'-sulfamoylbiphenyl-4-yl)-1,2-oxazole-4-carboxamide
-
pH and temperature not specified in the publication
0.00000016
3-(4-(5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]pentyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-4-hydroxybenzenecarboximidamide
-
-
0.0000605
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl)-4-hydroxybenzamidine
-
-
0.0000008 - 0.000067
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-3-oxo-3,4-dihydroquinoxolin-2-yl)benzamidine
0.0000023
3-(4-[5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1-benzenecarboximidamide
-
-
0.000022
3-(aminomethyl)-6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.0000017
3-(iminomethyl)-1-(4-methoxyphenyl)-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00023
3-([(3S)-3-[(naphthalen-2-ylsulfonyl)amino]-2-oxopyrrolidin-1-yl]methyl)benzenecarboximidamide
-
pH and temperature not specified in the publication
0.000004
3-([4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]-2-oxopiperazin-1-yl]methyl)benzenecarboximidamide
-
pH and temperature not specified in the publication
0.039
3-([[3-(4-carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino)-4-(3,4-dihydroisoquinolin-2(1H)-yl)-4-oxobutanoic acid
-
pH and temperature not specified in the publication
0.000019
3-amino-2,3-dihydro-1,3-benzoxazol-5-yl [1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methanesulfonate
-
-
0.000004
3-amino-4-chloro-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]benzamide
-
pH and temperature not specified in the publication
0.000002
3-amino-4-chloro-N-[(1R)-2-[4-[4-fluoro-2-(methylsulfonyl)phenyl]piperazin-1-yl]-2-oxo-1-phenylethyl]benzamide
-
pH and temperature not specified in the publication
0.25
3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.000000007
3-chloro-N-(4-chloro-2-([(5-chloro-2-pyridinyl)amino]carbonyl)-6-methoxyphenyl)-4-([(4,5-dihydro-2-oxazolyl)methylamino]methyl)-2-thiophenecarboxamide
-
0.0000007
3-chloro-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.00000076
3-chloro-N-[(1R,2S)-2-[[4-(2-oxopyridin-1(2H)-yl)benzoyl]amino]cyclohexyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.000002
3-chloro-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
3-chloro-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
3-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.0000003
3-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
3-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000015
3-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.0000008
3-chloro-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000002
3-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.00000032
3-chloro-N-[2-[(4-chlorophenyl)carbamoyl]-4-methylphenyl]-1-benzothiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.000011
3-chloro-N-[2-[(4-fluorophenyl)carbamoyl]-4-methylphenyl]-1-benzothiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.000015 - 0.000464
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
0.000000005
3-chloro-N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]-6-methoxyphenyl]-4-[[2-(methylamino)-1H-imidazol-1-yl]methyl]thiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.0000081
3-methyl-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000009
3-methyl-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.00000072
3-[6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
0.00000018
3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
0.000022
3-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl](methyl)amino]-2-oxopyrrolidin-1-yl]methyl]benzenecarboximidamide
-
pH and temperature not specified in the publication
0.000047
3-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl]amino]-2-oxopyrrolidin-1-yl]methyl]benzenecarboximidamide
-
pH and temperature not specified in the publication
0.00061
4,4'-[(2-oxocycloheptane-1,3-diylidene)di(E)methylylidene]dibenzenecarboximidamide
-
pH and temperature not specified in the publication
0.000592 - 0.000649
4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide)
0.0000013
4-(3-(aminoiminomethyl)phenyl)-1-(6-chloro-benzo[b]thiophene-2-sulfonyl)-piperazin-2-one
-
-
0.0000008
4-(4-amino-quinazolin-7-ylmethyl)-1-(6-chloro-benzo[b]thiophene-2-sulfonyl)-piperazin-2-one
-
-
0.000959
4-(benzo[b]thien-2-ylsulfonyl)-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.085
4-aminobenzamidine
-
pH 8.0, 25°C, with wild-type enzyme
0.0000024
4-hydroxy-3-[2-oxo-3-(S)-(5-pyridin-3-yl-thiophene-2-sulfonylamino)-pyrrolidin-1-ylmethyl]-benzamidine
-
pH 7.5, 22°C
0.0012
4-[(3-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.0012
4-[(4'-chloro[1,1'-biphenyl]-4-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000023
4-[(5'-chloro[2,2'-bithiophen]-5-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazine-2-one
-
-
0.0000019
4-[(5-chloro-1H-indol-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
pH and temperature not specified in the publication
0.000003
4-[(6-bromobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000004
4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
pH and temperature not specified in the publication
0.0012
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-imidazo[4,5-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000045
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0012
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-b]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000004
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
0.00122
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(furo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000003
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(1-methyl-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
-
0.00122
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(4,5-dihydro-4-oxo-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
above
0.000038
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(5-oxido-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
-
0.000003
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[[1-(2-hydroxyethyl)-1H-pyrrolo[3,2-c]pyridin-2-yl]methyl]-piperazin-2-one
-
-
0.000004
4-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0012
4-[(6-chlorothieno[3,2-b]pyridin-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000048
4-[[(1E)-2-(4-chlorophenyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0000011
4-[[(1E)-2-(5-chloro-2-thienyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0012
4-[[(1E)-2-(5-chloro-4-methoxy-2-thienyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000019
4-[[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl]-1-(pyridin-4-yl)piperidine-4-carboxylic acid
-
pH and temperature not specified in the publication
0.000007
4-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl](methyl)amino]-2-oxopyrrolidin-1-yl]methyl]thiophene-2-carboximidamide
-
pH and temperature not specified in the publication
0.0000011
4-[[(E)-2-(5-chlorothiophen-2-yl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
pH and temperature not specified in the publication
0.000128
4-[[2-(5-chloro-2-thienyl)ethyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000019
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate
-
-
0.00000006
5-butyl-2-(3-carbamimidoyl-phenyl)-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.0000015
5-chloro-N-(5-chloropyridin-2-yl)-2-([4-[(2-imino-1,3-oxazolidin-3-yl)methyl]benzoyl]amino)benzamide
-
pH and temperature not specified in the publication
0.0000013
5-chloro-N-(5-chloropyridin-2-yl)-2-([4-[(dimethylamino)methyl]benzoyl]amino)benzamide
-
pH and temperature not specified in the publication
0.0000006
5-chloro-N-(5-chloropyridin-2-yl)-2-[(4-[[ethanimidoyl(methyl)amino]methyl]benzoyl)amino]benzamide
-
pH and temperature not specified in the publication
0.00000044
5-chloro-N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.0002
5-chloro-N-(5-chloropyridin-2-yl)-2-[[4-(piperidin-1-ylcarbonoimidoyl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.000000057
5-chloro-N-(5-chloropyridin-2-yl)-3-methoxy-2-[[4-(2-oxopiperidin-1-yl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.00000051
5-chloro-N-[(1R,2S)-2-([4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]benzoyl]amino)cyclopentyl]thiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.000003
5-chloro-N-[(3S)-1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-4-methoxypyrrolidin-3-yl]thiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.0000015
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.00000084
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000035
6-(4-[1-[(dimethylamino)methyl]cyclopropyl]phenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000002
6-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]phenyl)-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000043
6-chloro-benzo[b]thiophene-2-sulfonic acid [2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)-pyrrolidin-3-yl]-amide
-
-
0.000096
6-chloro-benzo[b]thiophene-2-sulfonic acid [2-oxo-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-pyrrolidin-3-yl]-amide
-
-
0.000043
6-chloro-N-methyl-N-[(3S)-2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pyrrolidin-3-yl]-1-benzothiophene-2-sulfonamide
-
pH and temperature not specified in the publication
0.0000013
6-chloro-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.0000008
6-chloro-N-[(3S)-1-(6-fluoro-2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000003
6-chloro-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-1-[(1R)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000009
6-chloro-N-[(3S)-1-[(1S)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-1-[(1S)-1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000003
6-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000005
6-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-1-[2-fluoro-4-[(1S)-1-(methylamino)ethyl]phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000006
6-chloro-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000001
6-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.00001
6-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.0000008
6-chloro-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000004
6-chloro-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000016
6-chloro-N-[1-(2-fluoro-4-piperidin-1-ylphenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.000028
6-chloro-N-[1-(2-fluoro-4-pyridin-4-ylphenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.0000024
6-chloro-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.0000006
6-chloro-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000006
6-chloro-N-[1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.00001
6-chloro-N-[1-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.00000011
6-chloro-N-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.000000016
6-chloro-N-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]thieno[2,3-b]pyridine-2-sulfonamide
-
-
0.0000001
6-chloro-N-[1-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.00000005
6-chloro-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]thieno[2,3-b]pyridine-2-sulfonamide
-
-
0.0000022
6-[2'-(methylsulfonyl)biphenyl-4-yl]-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000012 - 0.0000017
6-[2'-[(aminooxy)sulfinyl]-3-fluorobiphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
0.0000028
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-4-methyl-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[3,4-d]pyridazin-7-one
-
-
0.0000018
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.000038
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylic acid
-
-
0.0000019
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00002
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(3-nitrophenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000026
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-ethylphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.00000035
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000011
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000012
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(iminomethyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000021
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.0000018
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-5-methyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00000074
6-[3-fluoro-2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.000000038
6-[4-(1-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]cyclopropyl)phenyl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000012
7'-[(6-chloronaphthalen-2-yl)sulfonyl]-8a'-(hydroxymethyl)-1-(pyridin-4-yl)tetrahydro-5'H-spiro[piperidine-4,2'-[1,3]thiazolo[3,2-a]pyrazin]-5'-one
-
pH and temperature not specified in the publication
0.000006
7-([7-[(1-ethanimidoylpiperidin-4-yl)oxy]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]methyl)naphthalene-2-carboximidamide
-
pH and temperature not specified in the publication
0.00000025
7-oxo-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.0001
8-amino-N-[(1R)-2-oxo-1-phenyl-2-[4-(pyridin-4-yl)piperazin-1-yl]ethyl]naphthalene-2-carboxamide
-
pH and temperature not specified in the publication
0.000003
8-amino-N-[(1R)-2-[4-[4-fluoro-2-(methylsulfonyl)phenyl]piperazin-1-yl]-2-oxo-1-phenylethyl]naphthalene-2-carboxamide
-
pH and temperature not specified in the publication
0.0000001
Ancylostoma ceylanicum anticoagulant peptide 1
-
25°C
-
0.0000003 - 0.0000006
antistasin
-
-
-
0.000000016 - 0.00000017
apixaban
0.000015
BIBM1015
pH 8.0, 37°C
0.00004
BIBR1109
pH 8.0, 37°C
0.000057
BIBT0871
pH 8.0, 37°C
0.00000003
BMS-740808
-
-
0.0000357 - 0.000041
DX-9065a
0.000134
endogeneous polypeptide inhibitor
-
pH 7.4, 25°C, kinetics
-
0.0000038
ethyl 1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
0.000045
ethyl 6-(2'-hydroxybiphenyl-4-yl)-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
0.0000036
ethyl 6-[3-fluoro-2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
0.000057 - 0.00028
FPR-prothrombin
-
0.0000013
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate
-
37°C
0.00000082
methyl 2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzenesulfinate
-
-
0.0001
methyl 3'-fluoro-4'-(3-[[(3-methoxyphenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.0000445
methyl 3'-fluoro-4'-(3-[[(4-fluorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.000053
methyl 3'-fluoro-4'-(3-[[(4-methoxyphenyl)sulfonyl]amino]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.000026
methyl 3'-fluoro-4'-(3-[[(5-isoxazol-3-ylthiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.0000036
methyl 3'-fluoro-4'-([[1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]carbonyl]amino)biphenyl-2-sulfinate
-
-
0.00037
methyl 3'-fluoro-4'-[2-oxo-3-[(phenylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000028
methyl 3'-fluoro-4'-[2-oxo-3-[(quinolin-3-ylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000073
methyl 3'-fluoro-4'-[2-oxo-3-[(quinolin-6-ylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
0.0002
methyl 3'-fluoro-4'-[3-(4-methoxyphenoxy)-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000003
methyl 3'-fluoro-4'-[3-(iminomethyl)-1-(4-methoxyphenyl)-5,7-dioxo-1,4,5,7-tetrahydro-6H-pyrazolo[4,3-d]pyrimidin-6-yl]biphenyl-2-sulfinate
-
-
0.00042
methyl 3'-fluoro-4'-[3-([[4-(iminomethyl)phenyl]sulfonyl]methyl)-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000019
methyl 3'-fluoro-4'-[3-[(1H-indazol-6-ylsulfamoyl)methyl]-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.00056
methyl 3'-fluoro-4'-[3-[(4-methoxyphenyl)amino]-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000094
methyl 3-(3-carbamimidoylphenyl)-5-[(4-carbamimidoylphenyl)carbamoyl]-4,5-dihydro-1,2-oxazole-5-carboxylate
-
pH and temperature not specified in the publication
0.0000034
methyl 3-[3-[amino(imino)methyl]phenyl]-5-[4-[amino(imino)methyl]phenyl]pentanoate
-
pH 8.0, 25°C
0.00065
methyl 4'-(3-[[(2,5-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000061
methyl 4'-(3-[[(3,4-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00027
methyl 4'-(3-[[(3,4-difluorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00073
methyl 4'-(3-[[(3,5-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00038
methyl 4'-(3-[[(3-chlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00016
methyl 4'-(3-[[(4-chloro-6-methyl-1-benzothiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000023
methyl 4'-(3-[[(4-chlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000078
methyl 4'-(3-[[(4-ethylphenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000053
methyl 4'-(3-[[(5-chlorothiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000011
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(diethylamino)ethyl](methyl)amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00000084
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(dimethylamino)ethyl](methyl)amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000022
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(dimethylamino)ethyl]amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000023
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](3-hydroxypropyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000022
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl]amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate2
-
-
0.00000071
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl][2-(4-methylpiperazin-1-yl)-2-oxoethyl]amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000018
methyl 4'-(3-[[(7-chloronaphthalen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000084
methyl 4'-([[4-amino-3-(iminomethyl)-1-(4-methoxyphenyl)-1H-pyrazol-5-yl]carbonyl]amino)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000002
methyl 4'-[1-(2-amino-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000018
methyl 4'-[1-(2-carbamoyl-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.000002
methyl 4'-[1-(2-carbamoylphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000018
methyl 4'-[1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000012
methyl 4'-[1-[2-[(aminooxy)sulfinyl]-4-methoxyphenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000074
methyl 4'-[1-[2-[(aminooxy)sulfinyl]phenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.0000027
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[(2-hydroxyethyl)(methyl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
0.00000043
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[methyl(1-methylpiperidin-4-yl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
0.0032
methyl 4'-[3-[(cyclohexylsulfonyl)methyl]-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000028
methyl 6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
0.00000088
methyl N-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]glycinate
-
-
0.000000043
methyl N-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycinate
-
-
0.0000063
methyl [3-(3-carbamimidoylphenyl)-4-[(2'-sulfamoylbiphenyl-4-yl)carbamoyl]-4,5-dihydro-1,2-oxazol-5-yl]acetate
-
pH and temperature not specified in the publication
0.000047
methyl [3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]amidosulfite
-
-
0.000057
N-(3-[[4'-(trifluoromethyl)biphenyl-4-yl]methoxy]phenyl)piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00000012
N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide
-
pH and temperature not specified in the publication
0.000003
N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.00000056
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]ethanediamide
-
pH and temperature not specified in the publication
0.000000561 - 0.000007
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
0.00000021
N-([1-[4-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-methoxy-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3-fluorophenyl]-1H-imidazol-2-yl]methyl)-2-methoxy-N,N-dimethyl-2-oxoethanaminium
-
-
0.00000035
N-([1-[4-(3-[[(6-chloronaphthalen-2-yl)sulfonyl]amino]-2-oxopiperidin-1-yl)-3-fluorophenyl]-1H-imidazol-2-yl]methyl)-2-methoxy-N,N-dimethyl-2-oxoethanaminium
-
-
0.0009
N-1-adamantylaminocarbonyl-D,L-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.000074
N-1-adamantyloxycarbonyl-(R)-3-amidinophenylalanine-(2-phenyl)-1-ethylamide
-
pH 8.0, 25°C
0.00022
N-1-adamantyloxycarbonyl-(R)-D-3-amidinophenylalanine benzylamide
-
pH 8.0, 25°C
0.00039
N-1-adamantyloxycarbonyl-(R)-D-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.0046
N-1-adamantyloxycarbonyl-(R)-L-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.0021
N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine
-
pH 8.0, 25°C
0.00062
N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.0017
N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine piperidine
-
pH 8.0, 25°C
0.0014
N-1-adamantyloxycarbonyl-D,L-4-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
1
N-1-adamantyloxycarbonyl-D,L-4-guanidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.0034
N-9-fluorenemethyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.033
N-benzyloxycarbonyl-D,L-3-amidinophenylalanine piperidine
-
pH 8.0, 25°C
0.000018
N-methyl-N-[(3S)-2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
pH and temperature not specified in the publication
0.016
N-tert-butyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.000004
N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.000016
N-[(1R)-2-(4-benzoylpiperidin-1-yl)-2-oxo-1-phenylethyl]-3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.002
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclobutyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0000113
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cycloheptyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000013
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclooctyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000086
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.1
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.00000285
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
pH 7.4
0.000265
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclobutyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000175
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cycloheptyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000041
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0014
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclooctyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000118
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000187
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0044
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0032
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.00027
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000005
N-[(3S)-1-(1-amino-2,3-dihydro-1H-inden-5-yl)-2-oxopyrrolidin-3-yl]-6-chloronaphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000006
N-[(3S)-1-[(1,6-diaminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
pH and temperature not specified in the publication
0.00018
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]-7-methoxynaphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000022
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
pH and temperature not specified in the publication
0.0001
N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
N-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]glycine
-
-
0.00000013
N-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycine
-
-
0.00021
N-[2-([[4-(aminomethyl)cyclohexyl]methyl]amino)-2-oxo-1-phenylethyl]-3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.011
N-[2-([[4-(aminomethyl)cyclohexyl]methyl]amino)-2-oxoethyl]-3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.002
N-[3-(biphenyl-4-ylmethoxy)phenyl]-1-carbamimidoylpiperidine-3-carboxamide
-
pH 8.0, 25°C
0.0052
N-[3-(biphenyl-4-ylmethoxy)phenyl]-1-carbamimidoylpiperidine-4-carboxamide
-
pH 8.0, 25°C
0.0025
N-[3-(biphenyl-4-ylmethoxy)phenyl]piperidine-3-carboxamide
-
pH 8.0, 25°C
0.001
N-[3-(biphenyl-4-ylmethoxy)phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.021
N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-1-[3-(5-methylidene-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
above
0.021
N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-1-[3-[(glycylamino)methyl]phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
above
0.000548
N-[3-[(2',3'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00947
N-[3-[(2',4',6'-trifluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.000512
N-[3-[(2',4'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00127
N-[3-[(2',5'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00145
N-[3-[(2',6'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.000767
N-[3-[(2'-fluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.000666
N-[3-[(3',4',5'-trifluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00013
N-[3-[(3',5'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.000177
N-[3-[(3'-fluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00387
N-[3-[(4'-fluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.26
N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-3-carboxamide
-
pH 8.0, 25°C
0.000088
N-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]acetamide
-
-
0.126
N-[4-(biphenyl-4-ylmethoxy)phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.0000007
N-[4-(N,N-dimethylcarbamimidoyl)-2-fluorophenyl]-1-(3-fluoronaphthalen-2-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.0000001
N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]phenyl]-2'-[(dimethylamino)methyl]biphenyl-4-carboxamide
-
pH and temperature not specified in the publication
0.0000017
N2-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.00000002
N2-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.00000013
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.00000037
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.0000001
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N2-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycinamide
-
-
0.0005
Nalpha-4'-amidinobenzensulfonyl-glycyl-D,L-4-amimidinophenylalanine ethyl ester
-
pH 8.0, 25°C
0.00084
Nalpha-tosylglycyl-D,L-3-amidinophenylalanine alkyl ester
-
pH 8.0, 25°C
0.0000001
octamixaban
-
pH and temperature not specified in the publication
0.00000017 - 0.00000029
PD0313052
0.00005 - 0.0017
pefabloc
0.000098
ProTS195A
-
pH 7.7, 37°C, versus prothrombin, in absence of phospholipid
-
0.00000018 - 0.00000019
razaxaban
0.0000007
recombinant tick saliva anticoagulant protein
-
wild type enzyme, at pH 7.5 and 25°C
-
0.0000009 - 0.003
RPR128515
0.0000007 - 0.004
RPR131247
0.0000018 - 0.004
RPR208707
0.0000022 - 0.004
RPR208815
0.000026
tanogitran
-
pH and temperature not specified in the publication
0.016
tert-butyl N-(3-carbamimidoylbenzoyl)-D-tyrosinate
-
pH and temperature not specified in the publication
0.00000162
TFPIalpha
-
wild type enzyme, at pH 7.5 and 25°C
-
0.000000034
therostasin
-
-
-
0.0000005
tick anticoagulant peptide
-
-
-
0.00000009 - 0.00000024
tissue factor pathway inhibitor
-
5 - 107
trimethylphenylammonium
0.0000001
ZK-807191
-
pH and temperature not specified in the publication
0.000005
[[4-(2-[[(5-carbamimidoyl-2-hydroxyphenyl)sulfonyl]amino]ethyl)-2'-(methylsulfonyl)biphenyl-3-yl]oxy]acetic acid
-
pH and temperature not specified in the publication
additional information
additional information
-
0.000004
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
factor Xa, pH 7.5, 22°C
0.0000097
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
factor Xa assembled in prothrombinase complex, pH 7.5, 22°C
0.0000011
1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.0000011
1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
pH and temperature not specified in the publication
0.00000027
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
pH 7.5, 37°C
0.00000052
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
pH 7.5, 37°C
0.00000141
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
pH 7.5, 37°C
0.0000008
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-3-oxo-3,4-dihydroquinoxolin-2-yl)benzamidine
-
-
0.000067
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-3-oxo-3,4-dihydroquinoxolin-2-yl)benzamidine
-
-
0.000015
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
pH 7.5, 22°C, factor Xa
0.000016
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
pH 7.5, 22°C, Gla-domainless factor Xa
0.000318
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
pH 7.5, 22°C, factor Xa in presence of 0.02 mM phospholipid vesicles containing 80% phosphocholine and 20% phosphatidylserine
0.000454
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
pH 7.5, 22°C, prothrombinase complex
0.000464
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
pH 7.5, 22°C, Gla-domainless factor Xa in presence of 0.02 mM phospholipid vesicles containing 80% phosphocholine and 20% phosphatidylserine
0.00000018
3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
0.00000018
3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
pH and temperature not specified in the publication
0.000592
4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide)
-
pH 7.5, 22°C, factor Xa
0.000649
4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide)
-
pH 7.5, 22°C, factor Xa in presence of 0.02 mM phospholipid vesicles containing 80% phosphocholine and 20% phosphatidylserine
0.000004
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000004
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0000012
6-[2'-[(aminooxy)sulfinyl]-3-fluorobiphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.0000017
6-[2'-[(aminooxy)sulfinyl]-3-fluorobiphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.000000016
apixaban
-
25°C
0.00000008
apixaban
-
25°C
0.00000013
apixaban
-
25°C
0.00000017
apixaban
-
25°C
0.0000357
DX-9065a
-
substrate: FS-2765, factor Xa
0.000041
DX-9065a
-
pH and temperature not specified in the publication
0.000057
FPR-prothrombin
-
pH 7.7, 37°C, versus prothrombin, in absence of phospholipid
-
0.00028
FPR-prothrombin
-
pH 7.7, 37°C, versus prothrombin, in presence of phospholipid at 0.025 mM
-
0.000000561
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
pH 7.4, 30°C
0.000000715
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
pH 7.4, 30°C
0.000007
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
pH 7.4, 30°C
0.00000017
PD0313052
-
prothrombinase, substrate: FS-2765
0.00000025
PD0313052
-
prothrombinase, substrate: prothrombin
0.00000029
PD0313052
-
substrate: FS-2765, factor Xa
0.00005
pefabloc
-
prothrombinase assembled with recombinant factor Xa, pH 7.5
0.000053
pefabloc
-
prothrombinase assembled with native factor Xa, pH 7.5
0.000064
pefabloc
-
native factor Xa, pH 7.5
0.00007
pefabloc
-
recombinant factor Xa, pH 7.5
0.00021
pefabloc
-
prothrombinase assembled with mutant I16L, pH 7.5
0.00029
pefabloc
-
prothrombinase assembled with mutant V17A, pH 7.5
0.00169
pefabloc
-
mutant V17A, pH 7.5
0.0017
pefabloc
-
mutant I16L, pH 7.5
0.00000018
razaxaban
-
-
0.0000009
RPR128515
-
0.0000009
RPR128515
with respect to factor Xa
0.003
RPR128515
above, with respect to thrombin
0.0000007
RPR131247
with respect to factor Xa
0.004
RPR131247
above, with respect to thrombin
0.0000018
RPR208707
with respect to factor Xa
0.004
RPR208707
above, with respect to thrombin
0.0000022
RPR208815
with respect to factor Xa
0.004
RPR208815
above, with respect to thrombin
0.00000009
tissue factor pathway inhibitor
-
recombinant mutant R150A, 22°C
-
0.00000011
tissue factor pathway inhibitor
-
recombinant wild-type enzyme, 22°C
-
0.00000014
tissue factor pathway inhibitor
-
recombinant mutant R143A, 22°C
-
0.00000015
tissue factor pathway inhibitor
-
native wild-type enzyme, 22°C
-
0.00000021
tissue factor pathway inhibitor
-
recombinant mutant R154A, 22°C
-
0.00000024
tissue factor pathway inhibitor
-
recombinant mutant K147A, 22°C
-
5
trimethylphenylammonium
-
pH 8.0, 25°C, with wild-type enzyme
20
trimethylphenylammonium
-
pH 8.0, 25°C, with mutant F174N enzyme
107
trimethylphenylammonium
-
pH 8.0, 25°C, with mutant Y99T enzyme
additional information
additional information
-
-
-
additional information
additional information
-
inhibition kinetics
-
additional information
additional information
-
inactivation kinetics of wild-type and mutant antithrombins
-
additional information
additional information
-
Ki values for derivatives of (R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-aryl-propionamides and (R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-aryl-propionamides, overview
-
additional information
additional information
-
kinetics
-
additional information
additional information
-
the Gla-domainless factor Xa shows a higher Ki in presence of phospholipids
-
additional information
additional information
-
rapid inhibition kinetic studies, wild-type and mutant antithrombins, overview
-
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0.0000075
(1S,3R,4S)-4-[(1H-indol-2-ylcarbonyl)amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.000018
(2R)-N1-(5-chloropyridin-2-yl)-N2-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)pyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00000032
(2R)-N1-(5-chloropyridin-2-yl)-N2-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-methoxypyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00000038
(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-hydroxypyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00000016
(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-methoxypyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000001
(2R,4S)-N1-(5-chloropyridin-2-yl)-4-(2,4-difluorophenyl)-4-hydroxy-N2-(2-oxo-2H-1,3'-bipyridin-6'-yl)pyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000075
(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000025
(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000019
(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000008
(5R)-N1-(5-chloropyridin-2-yl)-N5-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1H-pyrazole-1,5-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000012
(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
37°C, pH 8.4
0.0000071
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000074
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-chlorophenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000037
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-fluorophenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.000005
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-methylphenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000064
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]phenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000039
([(2R)-2-(7-carbamimidoylnaphthalen-2-yl)-5-[(1-ethanimidoylpiperidin-4-yl)methyl]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000007
([(3'-carbamimidoylbiphenyl-3-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000044
([2-[(E)-2-(5-carbamimidoyl-2-hydroxyphenyl)ethenyl]-5-[(1-ethanimidoylpiperidin-4-yl)oxy]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.045
1,1'-(benzene-1,4-diyldimethanediyl)bis(N,N-diethylpiperidine-3-carboxamide)
Homo sapiens
-
pH 8.0, 25°C
0.0000035
1-(1-[(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2-hydroxypropanoyl]piperidin-4-yl)tetrahydropyrimidin-2(1H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.0000027
1-[(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)methyl]cyclopropanecarboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000022
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]-2-ethylpropan-2-ol
Homo sapiens
-
pH 8.3, 37°C
0.00002
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]ethanol
Homo sapiens
-
pH 8.3, 37°C
0.000018
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]propan-2-ol
Homo sapiens
-
pH 8.3, 37°C
0.0000048
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
Homo sapiens
-
37°C
0.0000022
2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2-methylpropanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000035
2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)propanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000011
2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)propanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
2-[3-[(benzylsulfonyl)amino]-2-hydroxyazepan-1-yl]-N-[(2S)-5-carbamimidamido-1-(2,3-dihydro-1,3-thiazol-2-yl)-1-oxopentan-2-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
2-[3-[(benzylsulfonyl)amino]-2-oxopyridin-1(2H)-yl]-N-[(2S)-5-carbamimidamido-1-(2,3-dihydro-1,3-thiazol-2-yl)-1-oxopentan-2-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000018
2-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]propan-2-ol
Homo sapiens
-
pH 8.3, 37°C
0.000006
2-[[[4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl](methylsulfonyl)amino]methyl]-1-benzothiophene-5-carboximidamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
3-(4-(5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]pentyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide
Homo sapiens
-
IC50: 3.0 nM
0.0000019
3-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2,2-dimethylpropanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00345
3-amino-N-[(1R)-2-oxo-1-phenyl-2-[(2'-sulfamoylbiphenyl-4-yl)amino]ethyl]-1H-indazole-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000035
3-carbamimidoyl-N-[(1R)-2-oxo-1-phenyl-2-[(2'-sulfamoylbiphenyl-4-yl)amino]ethyl]benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00029
3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]-N-(5-methyl-2-pyridyl)benzamide
Homo sapiens
-
at pH 8.4 and 37°C
0.00015
3-hydroxy-4'-methoxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
Homo sapiens
-
at pH 8.4 and 37°C
0.000061
3-hydroxy-4'-methoxy-4-methyl-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
Homo sapiens
-
at pH 8.4 and 37°C
0.000068
3-hydroxy-4'-methyl-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
Homo sapiens
-
at pH 8.4 and 37°C
0.00022
3-hydroxy-N-(5-methoxy-2-pyridyl)-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
Homo sapiens
-
at pH 8.4 and 37°C
0.000066
3-[(4-methoxyphenyl)carbamoyl]-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]phenyl beta-D-glucopyranosiduronic acid
Homo sapiens
-
at pH 8.4 and 37°C
0.00046 - 0.00061
3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
0.0000069
4'-chloro-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
Homo sapiens
-
at pH 8.4 and 37°C
0.0000156
4-acetamido-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-benzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.0000259
4-bromo-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)benzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.0000035
4-[[(3-carbamimidoylphenyl)amino]methyl]-3-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0002 - 0.0021
4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
0.000012
5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)-2-methylimidazo[1,2-a]pyridine
Homo sapiens
-
pH 8.3, 37°C
0.000021
5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridine
Homo sapiens
-
pH 8.3, 37°C
0.000068
5-chloro-3-hydroxy-4'-methoxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
Homo sapiens
-
at pH 8.4 and 37°C
0.0000015
5-chloro-3-[(5-chloro-2-pyridyl)carbamoyl]-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]phenyl beta-D-glucopyranosiduronic acid
Homo sapiens
-
at pH 8.4 and 37°C
0.000008
5-chloro-N-(1-oxo-2-[3-[(pyridin-4-ylamino)methyl]benzyl]-2,3-dihydro-1H-isoindol-4-yl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000036
5-chloro-N-(5-chloro-2-pyridyl)-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
Homo sapiens
-
at pH 8.4 and 37°C
14
5-chloro-N-(5-chloro-2-pyridyl)-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
Homo sapiens
-
at pH 8.4 and 37°C
0.0000087
5-chloro-N-(5-chloropyridin-2-yl)-3-hydroxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
Homo sapiens
-
at pH 8.4 and 37°C
0.000004
5-chloro-N-([(5S)-2-oxo-3-[4-(2-oxopyrrolidin-1-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000007
5-chloro-N-([(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000032
5-chloro-N-([(5S)-3-[3-fluoro-4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00009
5-chloro-N-([(5S)-3-[3-fluoro-4-(thiomorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000076
7-[(2R)-5-[(1-ethanimidoylpiperidin-4-yl)methyl]-1-(ethylsulfonyl)-2,3-dihydro-1H-indol-2-yl]naphthalene-2-carboximidamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000005 - 0.000616
apixaban
0.0000546
darexaban
Homo sapiens
-
at pH 6.0 and 25°C
0.0000024
DPC423
Homo sapiens
-
at pH 8.4 and 37°C
0.000002
edoxaban
Homo sapiens
-
wild type enzyme, at pH 7.5 and 25°C
0.0000018
epi-N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.00017
ethyl (4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
ethyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)-2-methylpropanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.000065
ethyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)propanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.01
ethyl 3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]benzoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00069
ethyl 4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]benzoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00011
methyl (3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0000056
methyl (4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.000072
methyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2-methylpropanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.000029
methyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)propanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.0001 - 0.00012
methyl 3-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2,2-dimethylpropanoate
0.00097
methyl 3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00007 - 0.0012
methyl 4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
0.0016
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl](methyl)amino]ethyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.003945
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl](methyl)amino]ethyl)-N,5-dimethyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000221
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]ethyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0041
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]ethyl)-N,5-dimethyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000074
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]phenyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.075
N-(4-butoxyphenyl)piperidine-3-carboxamide
Homo sapiens
-
pH 8.0, 25°C
0.0000286
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.0000065
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dichlorobenzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.0000171
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dimethoxybenzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.000016
N-(5-chloro-2-pyridyl)-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
Homo sapiens
-
at pH 8.4 and 37°C
0.00000083
N-(benzylsulfonyl)-3-(1-carbamimidoylpiperidin-4-yl)-D-alanyl-N-[(2S)-5-carbamimidamido-1-hydroxypentan-2-yl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH 7.4, 22°C
0.0000028
N-[(1R,2S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
N-[(1R,2S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000051
N-[(1R,2S,5S)-2-[(1H-indol-2-ylcarbonyl)amino]-5-(methylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH 7.4, 22°C
0.0000023
N-[(1R,2S,5S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000023
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.0000023
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dipropylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.0000025
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-[(2-hydroxyethyl)(methyl)carbamoyl]cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.0000022
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-[(2-methoxyethyl)(methyl)carbamoyl]cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.000002
N-[(2S)-5-carbamimidamido-1-(2,3-dihydro-1,3-thiazol-2-yl)-1-oxopentan-2-yl]-2-[4-[(4-chlorophenyl)sulfonyl]-2-oxopiperazin-1-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00012
N-[(3aR,7aR)-2-[3-(2-amino-2-iminoethoxy)benzyl]-1,3-dioxooctahydro-1H-isoindol-4-yl]-5-chlorothiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000086
N-[(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-1-methoxypiperidin-3-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000084
N-[(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-1-[(dimethylamino)oxy]piperidin-3-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000047 - 0.00077
N-[1-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-(dimethylamino)-4-oxobutan-2-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
0.0000077
N-[2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)phenyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
N2,N2-dimethyl-N5-[[(2-methyl-1-benzofuran-5-yl)amino]([2-oxo-1-[2-oxo-2-(pyrrolidin-1-yl)ethyl]azepan-3-yl]amino)methylidene]pyridine-2,5-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000015
N2-(benzylsulfonyl)-D-arginyl-N-[(2S)-5-carbamimidamido-1-hydroxypentan-2-yl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000056
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]-D-norvalinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000085
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]norvalinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
N2-[(4-chlorophenyl)carbamoyl]-N2-(cyclopropylmethyl)-N-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
N2-[(4-chlorophenyl)carbamoyl]-N2-(cyclopropylmethyl)-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000497
PD0313052
Homo sapiens
-
-
0.0000065
rivaroxaban
Homo sapiens
-
at pH 6.0 and 25°C
0.0000286
YM-222714
Homo sapiens
-
at pH 6.0 and 25°C
0.000009
[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol
Homo sapiens
-
pH 8.3, 37°C
0.00046
3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00061
3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0002
4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0021
4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
apixaban
Homo sapiens
-
wild type enzyme, at pH 7.5 and 25°C
0.000034
apixaban
Homo sapiens
-
mutant enzyme Y99A, at pH 7.5 and 25°C
0.000045
apixaban
Homo sapiens
-
mutant enzyme F174A, at pH 7.5 and 25°C
0.00022
apixaban
Oryctolagus cuniculus
-
inhibition of FXa activity ex vivo
0.000616
apixaban
Homo sapiens
-
mutant enzyme Y99A/F174A, at pH 7.5 and 25°C
0.0001
methyl 3-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2,2-dimethylpropanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00012
methyl 3-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2,2-dimethylpropanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00007
methyl 4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.0012
methyl 4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.000047
N-[1-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-(dimethylamino)-4-oxobutan-2-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00077
N-[1-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-(dimethylamino)-4-oxobutan-2-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
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