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3.4.21.6: coagulation factor Xa

This is an abbreviated version!
For detailed information about coagulation factor Xa, go to the full flat file.

Word Map on EC 3.4.21.6

Reaction

selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin =

Synonyms

activated blood-coagulation factor X, activated factor X, activated Stuart-Prower factor, autoprothrombin C, blood coagulation factor X, blood coagulation factor Xa, blood-coagulation factor X, activated, clotting factor Xa, coagulation factor X, coagulation factor Xa, f.Xa, factor X, factor Xa, Fgl2 protein, fX, FXa, FXaalpha/beta, hXa, More, oscutarin, plasma thromboplastin, procoagulant factor X, prothrombase, prothrombin activator, prothrombinase, Stuart factor, thrombokinase, thromboplastin, thromboplastin, plasma, trocarin, Trocarin prothrombin activator, VAP, Virus activating protease, Xa

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.6 coagulation factor Xa

Inhibitors

Inhibitors on EC 3.4.21.6 - coagulation factor Xa

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(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-aminobenzamidine
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
-
antistasin
-
antithrombin
-
antithrombin III
-
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
apixaban
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
-
betrixaban
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
BMS-740808
-
-
Bovine pancreatic trypsin inhibitor
-
factor Xa-trypsin hybrid mutants
-
choline
-
positively linked to Na+ binding
CI-1031
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
D13R
-
-
dabigatran etexilate
-
i.e. Rendix, Pradaxa
dansyl-Glu-Gly-Arg
-
-
darexaban
-
-
DEGR-chloromethyl ketone
diisopropylfluorophosphate
DPC-423
-
-
DX-9065a
DX9065a
edoxaban
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
FXV673
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
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
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
lepiprudin
-
-
-
LY-517717
-
a xaban, specific for factor Xa
LY517717
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
otamixaban
p-amidinophenylmethanesulfonyl fluoride
-
-
p-nitrophenylguanidinobenzoate
-
-
PD0313052
pefabloc
-
-
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
-
razaxaban
recombinant tick saliva anticoagulant protein
-
-
-
rivaroxaban
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
TAK-442
tanogitran
-
a direct FXa inhibitor
tert-butyl N-(3-carbamimidoylbenzoyl)-D-tyrosinate
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-
tert-butyl [(3S,4R)-1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-4-(trifluoromethyl)pyrrolidin-3-yl]carbamate
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TFPIalpha
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therostasin
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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
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tick anticoagulant peptide
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tirofiban
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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
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trans-N'-[2-[(5-chloropyridin-2-yl)carbamoyl]-5-(dihydroxymethyl)-1-benzofuran-3-yl]-N,N-dimethylcyclohexane-1,4-dicarboxamide
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trimethylphenylammonium
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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
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complete inactivation at 0.05%
Trypsin
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VGY-000010
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VGY-000014
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VGY-000046
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VGY-000049
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VGY-000060
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VGY-000063
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VGY-000073
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VGY-0006201
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VGY-0006208
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VGY-0006212
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VGY-0224586
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VGY-0224865
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VGY-0224867
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VGY-0224887
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VGY-0224908
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VGY-0224909
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VGY-0224918
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VGY-0224933
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VGY-0224945
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VGY-0224950
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VGY-0224963
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VGY-0224989
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VGY-0225108
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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
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vitamin K
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induction of enzyme activity
warfarin
YM-150
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a xaban, specific for factor Xa
YM-222714
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YM-22714
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YM-60828
YM150
ZK-807191
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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
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[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
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[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
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additional information
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