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Information on EC 3.4.21.6 - coagulation factor Xa and Organism(s) Homo sapiens and UniProt Accession P00742

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     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.6 coagulation factor Xa
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This record set is specific for:
Homo sapiens
UNIPROT: P00742 not found.
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
thromboplastin, factor xa, factor x, fxa, prothrombinase, activated factor x, coagulation factor x, coagulation factor xa, blood coagulation factor xa, blood coagulation factor x, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
blood coagulation factor X
zymogen
blood coagulation factor Xa
-
factor Xa
activated blood-coagulation factor X
-
-
-
-
activated factor X
activated Stuart-Prower factor
-
-
-
-
autoprothrombin C
-
-
-
-
blood coagulation factor Xa
-
-
blood-coagulation factor X, activated
-
-
-
-
clotting factor Xa
-
-
coagulation factor Xa
f.Xa
-
-
factor X
-
zymogen
factor Xa
FXaalpha/beta
-
-
plasma thromboplastin
-
-
-
-
prothrombase
-
-
-
-
prothrombinase
Stuart factor
-
-
-
-
thrombokinase
-
-
-
-
thromboplastin
-
-
-
-
thromboplastin, plasma
-
-
-
-
Trocarin prothrombin activator
-
-
-
-
VAP
-
-
-
-
Virus activating protease
-
-
-
-
additional information
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
show the reaction diagram
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
ester hydrolysis
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY hide
9002-05-5
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
prothrombin + H2O
thrombin + ?
show the reaction diagram
Z-D-Arg-Gly-Arg-4-nitroanilide + H2O
Z-D-Arg-Gly-Arg + 4-nitroaniline
show the reaction diagram
i.e S2765
-
-
?
2-aminobenzoyl-VQFRILGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + ILGDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-VQFRSAGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SAGDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-VQFRSLEDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SLEDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-VQFRSLTDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SLTDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-VQFRSVGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SCGDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-VQFRTLGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + TLGDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-VMIAALPRTMFIQ-ED-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
?
activated factor VIII + H2O
factor VIII
show the reaction diagram
Arg-Gly-Arg-4-nitroanilide + H2O
Arg-Gly-Arg + 4-nitroaniline
show the reaction diagram
benzoyl-Ile-Glu(gamma-O-methyl)-Gly-Arg-4-nitroanilide + N-benzoyl-Ile-Glu-Gly-Arg-4-nitroanilide + H2O
benzoyl-Ile-Glu(gamma-O-methyl)-Gly-Arg + N-benzoyl-Ile-Glu-Gly-Arg + 4-nitroaniline
show the reaction diagram
Boc-L-Asp(OBzl)-L-Pro-L-Arg-7-amido-4-methylcoumarin + H2O
Boc-L-Asp(OBzl)-L-Pro-L-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
I-1560
-
-
?
D-cyclohexyl-Gly-L-Pro-L-Arg-4-nitroanilide + H2O
D-cyclohexyl-Gly-L-Pro-L-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
D-hexahydrotyrosol-L-Ala-L-Arg-4-nitroanilide + H2O
D-hexahydrotyrosol-L-Ala-L-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
D-Phe-Pip-Arg-4-nitroanilide + H2O
D-Phe-Pip-Arg + 4-nitroaniline
show the reaction diagram
-
synthetic substrate S2238
-
-
?
D-phenylalanyl-L-pipecolyl-L-arginine-4-nitroanilide + H2O
D-phenylalanyl-L-pipecolyl-L-arginine + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
factor VIII + H2O
?
show the reaction diagram
-
factor Xa proteolytically activates Factor VIII by cleaving P1 residues Arg372, Arg740, and Arg1689. Factor Xa also catalyzes inactivating cleavages that occur on a slower time scale than the activating ones
-
-
?
factor VIII + H2O
activated factor VIII + B domain
show the reaction diagram
FPR-prothrombin + H2O
meizothrombin
show the reaction diagram
-
i.e. prothrombin specifically active site-labeled with D-Phe-Pro-Arg-CH2Cl is cleaved by prothrombinase to intermediate meizothrombin, but the reaction is then directed to formation of a different FPR-prothrombin 2 intermediate product
-
-
?
fragment 1.2:prethrombin-2 + H2O
thrombin
show the reaction diagram
-
intermediate of prothrombin processing to thrombin, cleavage site is Arg320
-
?
FS-2765 + H2O
?
show the reaction diagram
L-Arg-Gly-Arg-4-nitroanilide + H2O
L-Arg-Gly-Arg + 4-nitroaniline
show the reaction diagram
L-Arg-Gly-L-Arg-4-nitroanilide + H2O
L-Arg-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
meizothrombin + H2O
thrombin
show the reaction diagram
-
intermediate of prothrombin processing to thrombin, cleavage site is Arg271
-
?
methoxycarbonyl-D-cyclohexylglycyl-Gly-L-Arg-4-nitroanilide + H2O
methoxycarbonyl-D-cyclohexylglycyl-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
methoxycarbonyl-D-cyclohexylglycyl-glycyl-L-ariginine-4-nitroanilide + H2O
methoxycarbonyl-D-cyclohexylglycyl-glycyl-L-ariginine + 4-nitroaniline
show the reaction diagram
-
i.e. Spectrozyme fXa, SpfXa
-
?
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide + H2O
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
N-2-benzyloxycarbonyl-D-arginyl-L-arginine-4-nitroanilide + H2O
N-2-benzyloxycarbonyl-D-arginyl-L-arginine + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide + H2O
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine + 4-nitroaniline
show the reaction diagram
N-alpha-benzyloxycarbonyl-Ile-Glu-Gly-Arg-7-amido-4-methylcoumarin + H2O
N-benzyloxycarbonyl-Ile-Glu-Gly-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
N-benzoyl-Arg-4-nitroanilide + H2O
N-benzoyl-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
?
N6-CBZ-D-Lys-L-Pro-L-Arg-4-nitroanilide + H2O
N6-CBZ-D-Lys-L-Pro-L-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
prethrombin 1 + H2O
thrombin + ?
show the reaction diagram
-
activation of prethrombin 1 is slow with cleavages at residues R320 and R271 occuring with similar rates
-
-
?
Prethrombin 2 + H2O
?
show the reaction diagram
prethrombin-1 + H2O
thrombin + ?
show the reaction diagram
-
-
-
-
?
prethrombin-2 + H2O
thrombin-2
show the reaction diagram
-
smallest zymogen form of thrombin containing only the factor Xa cleavage site 2
-
?
protease-activated receptor 1 + H2O
activated protease-activated receptor 1 + ?
show the reaction diagram
protease-activated receptor 2 + H2O
activated protease-activated receptor 2 + ?
show the reaction diagram
prothrombin + H2O
thrombin + ?
show the reaction diagram
prothrombin + H2O
thrombin + propeptide of thrombin
show the reaction diagram
prothrombin + H2O
thrombin + thrombin N-terminal fragment F12
show the reaction diagram
-
at the physiological concentration of prothrombin, thrombin formation results in rapid release of the product into solution due to weak interaction between thrombin and the cleaved N-terminal F12 domain, of which fragment F1 plays an essential role in membrane binding. Thrombin itself interacts with poor affinity with the F12 domain
-
-
?
prothrombin + H2O
thrombin + thrombin propeptide
show the reaction diagram
-
-
-
-
?
prothrombin + H2O
trhombin + ?
show the reaction diagram
-
-
-
-
?
ProTS195A + H2O
?
show the reaction diagram
-
the mutant protein also acts as competitive inhibitor of prothrombin activation
-
-
?
recombinant prothrombin R155A/R284A/R271A mutant rMZ-II + H2O
meizothrombin
show the reaction diagram
-
cleavage site is Arg320
reaction intermediate in the reaction with wild-type prothrombin
?
recombinant prothrombin R155A/R284A/R271A/S525C mutant rMZ-II-F + H2O
meizothrombin
show the reaction diagram
-
labeled with fluorescein at Cys525, cleavage site is Arg320
reaction intermediate in the reaction with wild-type prothrombin
?
recombinant prothrombin R155A/R284A/R320A mutant rP2-II + H2O
fragment 1.2:prethrombin-2
show the reaction diagram
-
cleavage site is Arg271
reaction intermediate in the reaction with wild-type prothrombin
?
recombinant prothrombin S525C mutant + H2O
thrombin
show the reaction diagram
-
labeled with fluorescein at Cys525, cleavage sites are Arg271 and Arg320
-
?
S-2765 + H2O
Z-D-Arg-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
S2222 + H2O
?
show the reaction diagram
S2238 + H2O
?
show the reaction diagram
-
-
-
-
?
S2765 + H2O
?
show the reaction diagram
-
-
-
-
?
tosyl-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
tosyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
tosyl-glycyl-prolyl-D-arginine-4-nitroanilide + H2O
tosyl-glycyl-prolyl-D-arginine + 4-nitroaniline
show the reaction diagram
-
i.e. Chz-TH, synthetic chromogenic substrate
-
?
Z-D-Arg-Gly-Arg-4-nitroanilide + H2O
Z-D-Arg-Gly-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
Z-D-Arg-Gly-L-Arg-4-nitroanilide + H2O
Z-D-Arg-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
prothrombin + H2O
thrombin + ?
show the reaction diagram
-
-
?
activated factor VIII + H2O
factor VIII
show the reaction diagram
-
proteolytic inactivation
-
-
?
factor VIII + H2O
?
show the reaction diagram
-
factor Xa proteolytically activates Factor VIII by cleaving P1 residues Arg372, Arg740, and Arg1689. Factor Xa also catalyzes inactivating cleavages that occur on a slower time scale than the activating ones
-
-
?
factor VIII + H2O
activated factor VIII + B domain
show the reaction diagram
-
proteolytic activation by removal of the B domain
-
-
?
protease-activated receptor 1 + H2O
activated protease-activated receptor 1 + ?
show the reaction diagram
-
PAR-1 activation mediates activation of phospholipase C in endothelial cells
-
-
?
protease-activated receptor 2 + H2O
activated protease-activated receptor 2 + ?
show the reaction diagram
-
PAR-2 activation mediates activation of phospholipase C in endothelial cells
-
-
?
prothrombin + H2O
thrombin + ?
show the reaction diagram
prothrombin + H2O
thrombin + propeptide of thrombin
show the reaction diagram
-
proteolytic activation
-
-
?
prothrombin + H2O
trhombin + ?
show the reaction diagram
-
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
vitamin K
dependent on
Factor Va
-
Factor VIIa
-
human plasma factor V activated by thrombin, residues 1-709 and 1546-2196, required for catalytic activity in the prothrombinase complex activating prothrombin to thrombin
-
factor VNN
-
factor V cleaved by the venom of the snake Naja nigricollis nigricollis at Asp697, Asp1509, and Asp1514, 2 fragments of MW 100 and 80 kDa, 7% clotting activity compared to factor VIIa
-
factor VNN/IIa
-
factor VNN cleaved by alpha-thrombin at Arg1545, 48% clotting activity compared to factor VIIa
-
factor VNN/RVV
-
factor VNN cleaved by Russell's viper venom at Arg1545, 48% clotting activity compared to factor VIIa
-
factor VRVV
-
factor V cleaved by Russell's viper venom at Arg1018 and Arg1545, 2 fragments of MW 74 and 150 kDa, 102% clotting activity compared to factor VIIa
-
Phospholipids
-
part of the prothrombinase complex, reduce the inhibitory effect of 3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
additional information
-
dissociation constants for binding to factor Xa for the factor Va variants at pH 7.4 and in presence of phospholipid vesicles containing phosphocholine and phosphatidylserine and Ca2+
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
dependent on, required for coordination of the enzyme domains, residues Asp46, Gly47, Gln49, and Gly64 are involved in Ca2+ binding, modeling of the calcium-binding site within the serine protease domain
additional information
-
divalent cations are required
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2RS)-(3'-amidino-3-biphenyl)-5-(4-pyridylamino)pentanoic acid
i.e. FX-2212, 50% inhibition by 272 nM
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
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
6-[2-(4-chlorophenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]-2,2,4,7-tetramethyl-1,2,3,4-tetrahydroquinoline
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
heparin
inhibition via complex formation with and modulation of the activity of thrombin
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
rivaroxaban
-
RPR128515
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
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
VGY-000010
-
-
VGY-000014
-
-
VGY-000046
-
-
VGY-000049
-
-
VGY-000060
-
-
VGY-000063
-
-
VGY-000073
-
-
VGY-0006201
-
VGY-0006208
-
VGY-0006212
-
VGY-0224586
-
-
VGY-0224865
-
VGY-0224867
-
VGY-0224887
-
VGY-0224908
-
VGY-0224909
-
VGY-0224918
-
VGY-0224933
-
-
VGY-0224945
-
VGY-0224950
-
VGY-0224963
-
-
VGY-0224989
-
VGY-0225108
-
-
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
-
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
(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
-
100% remaining rate after 5 min incubation with human liver microsomes
(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
-
-
(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
-
i.e. GW813893. More than 90fold selective over all enzymes tested, including thrombin, factor IXa, factor XIa, kallikrein, plasmin and several more
(E)-2-(5-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
-
potent anticoagulant activity, no mutagenic potential and high selectivity for factor Xa over trypsin
(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-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
-
presence of 1,2-dicaproyl-sn-glycero-3-phospho-L-serine and 5 mM Ca2+ results in dimerization with concomitant decrease in kcat value. Binding of 1,2-dicaproyl-sn-glycero-3-phospho-L-serine exposes residues K351. K242, and K420
1,5-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-[(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
-
-
2,2'-ethane-1,2-diylbis(1-benzofuran-5-carboximidamide)
-
-
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
-
i.e. FXV673, highly specific fo factor Xa compared to other serine proteases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, no effect on platelet aggregation
2-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-[(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
-
competitive
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-[(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-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
-
i.e. JTV-803, strong, synthetic inhibitor highly specific for factor Xa compared to other serine proteases
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-[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
-
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
-
AT3, a member of the serpin superfamily of protease inhibitors, X-ray crystal structure-based simulations of AT3/FXa, PDB code 2GD4, overview
-
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
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
bivalirudin
-
intravenously applicated inhibitor
BMS-740808
-
-
Bovine pancreatic trypsin inhibitor
-
factor Xa-trypsin hybrid mutants
-
choline
-
positively linked to Na+ binding
CI-1031
-
i.e. ZK-807834, small molecule direct inhibitor of facor Xa
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
-
D13R
-
-
dabigatran etexilate
-
i.e. Rendix, Pradaxa
dansyl-Glu-Gly-Arg
-
-
darexaban
-
-
DEGR-chloromethyl ketone
-
inactivation
DPC-423
-
-
DX-9065a
DX9065a
edoxaban
EDTA
-
-
eisenstasin
-
protein inhibitor isolated from the midgut of Eisenia andrei
-
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
-
FXV673
-
small molecule direct inhibitor of facor Xa
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
LY517717
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
-
i.e. RPR208566, highly specific
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-[[(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-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
-
i.e. DU-176b. Presence prolongs the activated partial thromboplastin time, prothrombin time and thrombin time in plasma. It does not impair human platelet aggregation induced by ADP or thromboxane A2 receptor agonist U46619. Thrombin-induced platelet aggregation is inhibited with IC50 value of 2.9 microM
N-(5-chloropyridin-2-yl)-N'-[(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-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-[(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
-
46% remaining rate after 5 min incubation with human liver microsomes
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
-
63% remaining rate after 5 min incubation with human liver microsomes
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
-
-
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
PD0313052
pefabloc
-
-
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
-
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
RPR208566
-
potent direct inhibitor, overview over effects in vivo
SK549
-
potent direct inhibitor, overview over effects in vivo
Soybean trypsin inhibitor
-
factor Xa-trypsin hybrid mutants
-
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
-
-
tert-butyl [(3S,4R)-1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-4-(trifluoromethyl)pyrrolidin-3-yl]carbamate
-
-
TFPIalpha
-
-
-
tick anticoagulant peptide
-
tirofiban
-
glycoprotein IIb/IIIa receptor-antagonist, 16.9% inhibition at 0.042 mM in absence of heparin, 48% inhibition at 0.14 mM in presence of heparin 1 U/ml
tissue factor pathway inhibitor
-
trans-N'-[2-[(5-chloropyridin-2-yl)carbamoyl]-5-(dihydroxymethyl)-1-benzofuran-3-yl]-N,N-dimethylcyclohexane-1,4-dicarboxamide
-
-
trimethylphenylammonium
-
i.e. TMPA, strong and highly specific inhibition, inhibits substrate hydrolysis competitively, does not inhibit the binding of 4-aminobenzamidine to the S1-pocket, and is positively linked to Na+ binding rsulting in 10fold increase in binding of inhibitor at 0.15 M Na+, interacts with Y99, F174, and W215 via van der Waals interactions, and the charged amine coupling electrostatically with the carboxylates of E97
Trypsin
-
-
-
warfarin
YM-150
-
a xaban, specific for factor Xa
YM-222714
-
-
YM-22714
-
-
YM-60828
YM150
ZK-807191
-
a dihydrochloride salt of fidexaban
[2-([4-[(5S)-5-([[(5-chlorothiophen-2-yl)carbonyl]amino]methyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]amino)ethoxy]acetic acid
-
-
[4-[(5-chloro-1H-indol-2-yl)sulfonyl]piperazin-1-yl](5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)methanone
-
-
[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol
-
selective and orally bioavailable inhibitor
[[4-(2-[[(5-carbamimidoyl-2-hydroxyphenyl)sulfonyl]amino]ethyl)-2'-(methylsulfonyl)biphenyl-3-yl]oxy]acetic acid
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Phospholipids
interaction via Lys14 of the Gla-domain
1,2-dicaproyl-sn-glycero-3-phosphate
-
i.e. C6PA, binding constants in presence of Ca2+
1,2-dicaproyl-sn-glycero-3-phospho-D-homoserine
-
i.e. C6P(homo)S, binding constants in presence of Ca2+
1,2-dicaproyl-sn-glycero-3-phospho-D-serine
-
i.e. C6P(D)S, binding constants in presence of Ca2+
1,2-dicaproyl-sn-glycero-3-phospho-L-N-methylserine
-
i.e. C6P(N-Me)S, binding constants in presence of Ca2+
1,2-dicaproyl-sn-glycero-3-phospho-L-serine
1,2-dicaproyl-sn-glycero-3-phospho-rac-1-glycerol
-
i.e. C6PG, binding constants in presence of Ca2+
1,2-dicaproyl-sn-glycero-3-phosphocholine
-
i.e. C6PC, binding constants in presence of Ca2+
1,2-dicaproylphosphatidylserine
-
soluble, upregulates 60fold, and directs factor Xa to appropriate peptide bonds in prothrombin
1-caproyl-sn-glycero-3-phosphate
-
i.e. C6lysoPA, binding constants in presence of Ca2+
1-caproyl-sn-glycero-3-phospho-L-serine
-
i.e. C6lysoPS, binding constants in presence of Ca2+
1-caproyl-sn-glycero-3-phosphocholine
-
i.e. C6lysoPC, binding constants in presence of Ca2+
Factor V
-
factor V variants 501A/510A/511D, 501A/510A/511D/513A, 513A/577A/578A, and 501A/510A/511D/513A/577A/578A exhibit markedly reduced factor Xa-cofactor activity tested in the prothrombinase assay, and reduced binding affinity as judged by the direct binding assay.These factor Va variants are normally cleaved at Arg-506 by activated protein C, and the interaction between the factor Xa-factor Va complex and prothrombin is unaffected by the introduced mutations. The key factor Xa binding surface is centered on residues Arg-501, Arg-510, Ala-511, Asp-513, Asp-577, and Asp-578 in the factor Va A2 domain
-
Factor Va
-
Glycosaminoglycans
-
bind with higher affinity to factor Xa in presence of Ca2+ than in its absence, while the binding to the Gla-domainless factor Xa shows similar Km-values in absence or presence of Ca2+, binding induces conformational changes in the active site of factor Xa, glycosaminoglycans influence the ability of factor Xa to cleave chromogenic substrates and reduce its factor VII cleaving activity, exosites on the surface of factor Xa are perturbed, the activation effect increass with increasing number of sulfate residues
-
heparin
-
binds to a Ca2+-dependent binding site, reduces Km and kcat for chromogenic substrates dependent on Ca2+
L-alpha-glycerophosphorylserine
-
i.e. GPS, binding constants in presence of Ca2+
Li+
-
can partly replace Na+, less efficient
phospholipid vesicle
-
-
-
Phospholipids
-
-
protein S
-
protein S counteracted the inhibition of activated factor V by FXa of the Arg506 cleavage, whereas protein S and FXa yielded additive stimulatory effect of the cleavage at Arg306
-
short chain phosphatidylserine
-
i.e. C6PS, binding leads to 60fold increased proteolytic activity, location of binding sites and binding structure, partly Ca2+-dependent, kinetics with wild-type enzyme and mutant enzyme fragments
tissue factor
-
i.e. thromboplastin
-
tissue factor TF
-
-
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0507 - 3.9
Arg-Gly-Arg-4-nitroanilide
0.0013
D-cyclohexyl-Gly-L-Pro-L-Arg-4-nitroanilide
-
20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1% (w/v) PEG 8000 at 25°C
0.0022
D-hexahydrotyrosol-L-Ala-L-Arg-4-nitroanilide
-
20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1% (w/v) PEG 8000 at 25°C
0.0013
D-phenylalanyl-L-pipecolyl-L-arginine-4-nitroanilide
-
20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1% (w/v) PEG 8000 at 25°C
0.00016
FPR-prothrombin
-
pH 7.7, 37°C, in presence of phospholipid at 0.025 mM
-
0.00058 - 0.00078
fragment 1.2:prethrombin-2
-
0.036
L-Arg-Gly-L-Arg-4-nitroanilide
-
25°C
0.00065 - 0.00095
meizothrombin
-
0.061
methoxycarbonyl-D-cyclohexylglycyl-Gly-L-Arg-4-nitroanilide
-
20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1% (w/v) PEG 8000 at 25°C
0.072 - 1.38
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
0.042 - 0.122
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
0.0045
N6-CBZ-D-Lys-L-Pro-L-Arg-4-nitroanilide
-
20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1% (w/v) PEG 8000 at 25°C
0.0052 - 0.0069
prethrombin-1
-
0.0088
prethrombin-2
-
prothrombinase complex, pH 7.4, 22°C
-
0.000018 - 0.000985
prothrombin
-
0.000071
ProTS195A
-
pH 7.7, 37°C, versus prothrombin, in absence of phospholipid
-
0.00036 - 0.00045
recombinant prothrombin R155A/R284A/R271A mutant rMZ-II
-
0.00039 - 0.0005
recombinant prothrombin R155A/R284A/R320A mutant rP2-II
-
0.026
S-2765
-
wild type enzyme, at pH 7.5 and 25°C
0.133 - 0.739
S2222
0.052 - 0.112
S2765
0.097 - 0.206
tosyl-glycyl-prolyl-D-arginine-4-nitroanilide
additional information
additional information
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
27.1 - 154.4
Arg-Gly-Arg-4-nitroanilide
0.0057 - 114
fragment 1.2:prethrombin-2
-
6.39 - 150
meizothrombin
-
33 - 210
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
1.4 - 411
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
6.5 - 18.1
prethrombin-1
-
20.5
prethrombin-2
-
prothrombinase complex, pH 7.4, 22°C
-
0.0000000018 - 108
prothrombin
-
0.0068 - 110
recombinant prothrombin R155A/R284A/R271A mutant rMZ-II
-
0.324 - 114
recombinant prothrombin R155A/R284A/R320A mutant rP2-II
-
21
S-2765
-
wild type enzyme, at pH 7.5 and 25°C
139 - 211
S2222
214 - 270
S2765
46 - 79
tosyl-glycyl-prolyl-D-arginine-4-nitroanilide
additional information
meizothrombin
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000272
(2RS)-(3'-amidino-3-biphenyl)-5-(4-pyridylamino)pentanoic acid
i.e. FX-2212
0.000000007
3-chloro-N-(4-chloro-2-([(5-chloro-2-pyridinyl)amino]carbonyl)-6-methoxyphenyl)-4-([(4,5-dihydro-2-oxazolyl)methylamino]methyl)-2-thiophenecarboxamide
-
0.000015
BIBM1015
pH 8.0, 37°C
0.00004
BIBR1109
pH 8.0, 37°C
0.000057
BIBT0871
pH 8.0, 37°C
0.0000009 - 0.003
RPR128515
0.0000007 - 0.004
RPR131247
0.000018
RPR132747
-
0.0000013
RPR200095
-
0.0000018 - 0.004
RPR208707
0.0000022 - 0.004
RPR208815
0.000003
RPR208944
-
0.0000011
RPR209685
-
0.0000017
(3-[[(3-carbamimidoylphenyl)(2-[[4-(1-ethanimidoylpiperidin-4-yl)phenyl]amino]-2-oxoethyl)amino]methyl]phenoxy)acetic acid
-
pH and temperature not specified in the publication
0.00000055
(4S,5S)-3-(3-carbamimidoylphenyl)-5-(methoxymethyl)-N-(2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1,2-oxazole-4-carboxamide
-
pH and temperature not specified in the publication
0.000004 - 0.0000097
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
0.0000003
(E)-2-(5-chlorothiophen-2-yl)-N-(1-[5-[2-(methylsulfonyl)phenyl]pyridin-2-yl]-2-oxopyrrolidin-3-yl)ethenesulfonamide
-
pH and temperature not specified in the publication
0.000001
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000006
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000013
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(6-fluoro-2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000002
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000015
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000006
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000008
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000001
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000005
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000003
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000006
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000002
(E)-2-(5-chlorothiophen-2-yl)-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000002
(E)-2-(5-chlorothiophen-2-yl)-N-[1-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000055
(E)-2-(5-chlorothiophen-2-yl)-N-[[(3R)-1-[[1-(pyridin-4-yl)piperidin-4-yl]carbonyl]pyrrolidin-3-yl]methyl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.00000076
(R)-6-(2'-((3-hydroxypyrrolidin-1-yl)methyl)-[1,1'-biphenyl]-4-yl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-5,6-dihydro-1H-pyrazolo[3,4-c]pyridin-7(4H)-one
-
-
0.0000013
([(7-carbamimidoylnaphthalen-2-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
-
pH and temperature not specified in the publication
0.0012
1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[2,3-b]pyridin-2-ylsulfonyl)-piperazin-2-one
-
above
0.0012
1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[3,2-b]pyridin-2-ylsulfonyl)-piperazin-2-one
-
above
0.00000004
1-(3-amino-1,2-benzisoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.00000003
1-(3-amino-1,2-benzoxazol-5-yl)-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
pH and temperature not specified in the publication
0.0000044
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[2-[(dimethylamino)methyl]pyridin-3-yl]-2-fluorophenyl)-7-fluoro-1H-indazole-3-carboxamide
-
pH and temperature not specified in the publication
0.00000017
1-(3-amino-1,2-benzoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-5-methyl-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
pH and temperature not specified in the publication
0.00000019
1-(3-amino-1,2-benzoxazol-5-yl)-N-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.000002
1-(3-aminophenyl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000013
1-(3-carbamimidoylphenyl)-3-methyl-N-(2'-sulfamoylbiphenyl-4-yl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.000000015
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
0.000000013
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00000016
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
0.00000029
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-4-bromo-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt
-
-
0.0000008
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt
-
-
0.00000046
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(fluoro)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.000000008
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00000004
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.0000013
1-(3-[amino(imino)methyl]phenyl)-N-[2'-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00000011
1-(4-methoxyphenyl)-3-(methylsulfonyl)-6-(4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000018
1-(4-methoxyphenyl)-4-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[3,4-d]pyridazin-7-one
-
-
0.0000014
1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(1H-tetrazol-1-ylmethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.0000029
1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(2H-tetrazol-2-ylmethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.000000054
1-(4-methoxyphenyl)-6-(4-[1-[(methylamino)methyl]cyclopropyl]phenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000055
1-(4-methoxyphenyl)-6-(4-[1-[(methylamino)methyl]cyclopropyl]phenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.000000042
1-(4-methoxyphenyl)-6-[4-(1-[[(1-methylethyl)amino]methyl]cyclopropyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000064
1-(4-methoxyphenyl)-6-[4-[1-(morpholin-4-ylmethyl)cyclopropyl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000021
1-(4-methoxyphenyl)-6-[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.00000024
1-(4-methoxyphenyl)-7-oxo-6-(4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.0000011
1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
0.00000008
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
pH and temperature not specified in the publication
0.000000074
1-(4-methoxyphenyl)-7-oxo-6-[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.0000015
1-(6-chloronaphthalen-2-yl)-N-[2'-[(dimethylamino)methyl]-3-fluorobiphenyl-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.057
1-carbamimidoyl-N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-3-carboxamide
-
pH 8.0, 25°C
0.0338
1-carbamimidoyl-N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00122
1-[(4-amino-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-piperazin-2-one
-
-
0.0000008
1-[(4-aminoquinazolin-7-yl)methyl]-4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]piperazin-2-one
-
pH and temperature not specified in the publication
0.00000097
1-[1-(3-amino-1,2-benzoxazol-5-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-2-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]phenyl)ethanone
-
pH and temperature not specified in the publication
0.00000091
1-[2-(aminomethyl)phenyl]-N-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.000001
1-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide
-
pH and temperature not specified in the publication
0.0000012
1-[2-[(aminooxy)sulfinyl]phenyl]-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.021
1-[3-(5-amino-1,3,4-thiadiazol-2-yl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
above
0.0049
1-[3-(5-amino-4H-1,2,4-triazol-3-yl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
0.0000004
1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000027
1-[3-(aminomethyl)phenyl]-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
0.000000013
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-(2'-(methylsulfonyl))-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
0.00000015
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
0.00000015
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.0026
1-[3-[([1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methyl)sulfonyl]phenyl]pyridinium
-
-
0.000054
1-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]urea
-
-
0.000011
1-[3-[amino(imino)methyl]phenyl]-N-[2'-(aminosulfonyl)[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00026
1-[4-amino-3-[([1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methyl)sulfonyl]phenyl]pyridinium
-
-
0.000003
1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide
-
pH and temperature not specified in the publication
0.00057
2,2'-ethane-1,2-diylbis(1-benzofuran-5-carboximidamide)
-
pH and temperature not specified in the publication
0.0000005
2-(1-[(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2-hydroxypropanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
pH and temperature not specified in the publication
0.000002
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
pH and temperature not specified in the publication
0.00021
2-(2-hydroxy-5-methylbiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.000078
2-(2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.0068
2-(2-hydroxybiphenyl-3-yl)benzofuran-5-carboxamidine
-
pH 7.4, 22°C
0.014
2-(2-hydroxyphenyl)1H-benzoimidazole-5-carboxamidine
-
pH 7.4, 22°C
0.0027
2-(2-hydroxyphenyl)1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.03
2-(2-hydroxyphenyl)3-methyl-3H-benzoimidazole-5-carboxamidine
-
pH 7.4, 22°C
0.019
2-(2-methoxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.000089
2-(3,5-dibromo-2-hydroxyphenyl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.00000089
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.00000048
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.0000016
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.00000038
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.00000091
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.00000036
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.000052
2-(3-bromo-2-hydroxy-5-methylphenyl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.000078
2-(3-bromo-2-hydroxy-5-nitrophenyl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.000043
2-(3-bromo-2-hydroxyphenyl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.00000001
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-bromo-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.000000009
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-chloro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.00000002
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.000000005
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.000000007
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide
-
-
0.000000041
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide
-
-
0.000000008
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.000000005
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide
-
below
0.000000005
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
below
0.000000009
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide
-
-
0.00000001
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide
-
-
0.00021
2-(5-bromo-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.00034
2-(5-chloro-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.000014
2-(5-nitro-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.00000052
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
pH 7.5, 37°C
0.043
2-biphenyl-3-yl-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.0000065
2-cyano-1-(2-methyl-1-benzofuran-5-yl)-3-[2-oxo-1-[2-oxo-2-(pyrrolidin-1-yl)ethyl]azepan-3-yl]guanidine
-
pH and temperature not specified in the publication
0.0000027
2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
0.0000004
2-[6-[3-([[(E)-2-(5-chlorothiophen-2-yl)ethenyl]sulfonyl]amino)-2-oxopyrrolidin-1-yl]pyridin-3-yl]benzenesulfonamide
-
pH and temperature not specified in the publication
0.00000013
2-[N2-(benzylsulfonyl)-D-arginylglycyl-L-arginyl]-1,3-thiazole
-
pH and temperature not specified in the publication
0.0000115
2-[[4-(dimethylamino)benzoyl]amino]-N-(5-methoxypyridin-2-yl)-5-[(methylsulfonyl)amino]benzamide
-
pH and temperature not specified in the publication
0.0000235
3-(1-[5-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-pentyl]-2-oxo-1,2-dihydroquinolin-3-yl)-4-hydroxybenzamidine
-
-
0.0000189
3-(1-[5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl]-2-oxo-1,2,3,4-tetrahydro-3-quinolinyl)-4-hydroxybenzenecarboximidamide
-
-
0.0000129
3-(1-[5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl]-2-oxo-1,2,3,4-tetrahydro-3-quinolinyl)benzenecarboximidamide
-
-
0.0000021
3-(1H-imidazol-1-ylmethyl)-1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00000015
3-(3-carbamimidoyl-phenyl)-isoxazole-4-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.00000015
3-(3-carbamimidoylphenyl)-N-(2'-sulfamoylbiphenyl-4-yl)-1,2-oxazole-4-carboxamide
-
pH and temperature not specified in the publication
0.00000016
3-(4-(5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]pentyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-4-hydroxybenzenecarboximidamide
-
-
0.0000605
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl)-4-hydroxybenzamidine
-
-
0.0000008 - 0.000067
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-3-oxo-3,4-dihydroquinoxolin-2-yl)benzamidine
0.0000023
3-(4-[5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1-benzenecarboximidamide
-
-
0.000022
3-(aminomethyl)-6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.0000017
3-(iminomethyl)-1-(4-methoxyphenyl)-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00023
3-([(3S)-3-[(naphthalen-2-ylsulfonyl)amino]-2-oxopyrrolidin-1-yl]methyl)benzenecarboximidamide
-
pH and temperature not specified in the publication
0.000004
3-([4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]-2-oxopiperazin-1-yl]methyl)benzenecarboximidamide
-
pH and temperature not specified in the publication
0.039
3-([[3-(4-carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino)-4-(3,4-dihydroisoquinolin-2(1H)-yl)-4-oxobutanoic acid
-
pH and temperature not specified in the publication
0.000019
3-amino-2,3-dihydro-1,3-benzoxazol-5-yl [1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methanesulfonate
-
-
0.000004
3-amino-4-chloro-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]benzamide
-
pH and temperature not specified in the publication
0.000002
3-amino-4-chloro-N-[(1R)-2-[4-[4-fluoro-2-(methylsulfonyl)phenyl]piperazin-1-yl]-2-oxo-1-phenylethyl]benzamide
-
pH and temperature not specified in the publication
0.25
3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.0000007
3-chloro-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.00000076
3-chloro-N-[(1R,2S)-2-[[4-(2-oxopyridin-1(2H)-yl)benzoyl]amino]cyclohexyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.000002
3-chloro-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
3-chloro-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
3-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.0000003
3-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
3-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000015
3-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.0000008
3-chloro-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000002
3-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.00000032
3-chloro-N-[2-[(4-chlorophenyl)carbamoyl]-4-methylphenyl]-1-benzothiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.000011
3-chloro-N-[2-[(4-fluorophenyl)carbamoyl]-4-methylphenyl]-1-benzothiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.000015 - 0.000464
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
0.000000005
3-chloro-N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]-6-methoxyphenyl]-4-[[2-(methylamino)-1H-imidazol-1-yl]methyl]thiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.0000081
3-methyl-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000009
3-methyl-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.00000072
3-[6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
0.00000018
3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
0.000022
3-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl](methyl)amino]-2-oxopyrrolidin-1-yl]methyl]benzenecarboximidamide
-
pH and temperature not specified in the publication
0.000047
3-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl]amino]-2-oxopyrrolidin-1-yl]methyl]benzenecarboximidamide
-
pH and temperature not specified in the publication
0.00061
4,4'-[(2-oxocycloheptane-1,3-diylidene)di(E)methylylidene]dibenzenecarboximidamide
-
pH and temperature not specified in the publication
0.000592 - 0.000649
4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide)
0.0000013
4-(3-(aminoiminomethyl)phenyl)-1-(6-chloro-benzo[b]thiophene-2-sulfonyl)-piperazin-2-one
-
-
0.0000008
4-(4-amino-quinazolin-7-ylmethyl)-1-(6-chloro-benzo[b]thiophene-2-sulfonyl)-piperazin-2-one
-
-
0.000959
4-(benzo[b]thien-2-ylsulfonyl)-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.085
4-aminobenzamidine
-
pH 8.0, 25°C, with wild-type enzyme
0.0000024
4-hydroxy-3-[2-oxo-3-(S)-(5-pyridin-3-yl-thiophene-2-sulfonylamino)-pyrrolidin-1-ylmethyl]-benzamidine
-
pH 7.5, 22°C
0.0012
4-[(3-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.0012
4-[(4'-chloro[1,1'-biphenyl]-4-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000023
4-[(5'-chloro[2,2'-bithiophen]-5-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazine-2-one
-
-
0.0000019
4-[(5-chloro-1H-indol-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
pH and temperature not specified in the publication
0.000003
4-[(6-bromobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000004
4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
pH and temperature not specified in the publication
0.0012
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-imidazo[4,5-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000045
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0012
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-b]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000004
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.00122
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(furo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.00122
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(4,5-dihydro-4-oxo-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
above
0.000038
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(5-oxido-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
-
0.000004
4-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0012
4-[(6-chlorothieno[3,2-b]pyridin-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000048
4-[[(1E)-2-(4-chlorophenyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0000011
4-[[(1E)-2-(5-chloro-2-thienyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0012
4-[[(1E)-2-(5-chloro-4-methoxy-2-thienyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000019
4-[[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl]-1-(pyridin-4-yl)piperidine-4-carboxylic acid
-
pH and temperature not specified in the publication
0.000007
4-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl](methyl)amino]-2-oxopyrrolidin-1-yl]methyl]thiophene-2-carboximidamide
-
pH and temperature not specified in the publication
0.0000011
4-[[(E)-2-(5-chlorothiophen-2-yl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
pH and temperature not specified in the publication
0.000128
4-[[2-(5-chloro-2-thienyl)ethyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000019
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate
-
-
0.00000006
5-butyl-2-(3-carbamimidoyl-phenyl)-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.0000015
5-chloro-N-(5-chloropyridin-2-yl)-2-([4-[(2-imino-1,3-oxazolidin-3-yl)methyl]benzoyl]amino)benzamide
-
pH and temperature not specified in the publication
0.0000013
5-chloro-N-(5-chloropyridin-2-yl)-2-([4-[(dimethylamino)methyl]benzoyl]amino)benzamide
-
pH and temperature not specified in the publication
0.0000006
5-chloro-N-(5-chloropyridin-2-yl)-2-[(4-[[ethanimidoyl(methyl)amino]methyl]benzoyl)amino]benzamide
-
pH and temperature not specified in the publication
0.00000044
5-chloro-N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.0002
5-chloro-N-(5-chloropyridin-2-yl)-2-[[4-(piperidin-1-ylcarbonoimidoyl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.000000057
5-chloro-N-(5-chloropyridin-2-yl)-3-methoxy-2-[[4-(2-oxopiperidin-1-yl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.00000051
5-chloro-N-[(1R,2S)-2-([4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]benzoyl]amino)cyclopentyl]thiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.000003
5-chloro-N-[(3S)-1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-4-methoxypyrrolidin-3-yl]thiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.0000015
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.00000084
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000035
6-(4-[1-[(dimethylamino)methyl]cyclopropyl]phenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000002
6-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]phenyl)-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000043
6-chloro-benzo[b]thiophene-2-sulfonic acid [2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)-pyrrolidin-3-yl]-amide
-
-
0.000096
6-chloro-benzo[b]thiophene-2-sulfonic acid [2-oxo-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-pyrrolidin-3-yl]-amide
-
-
0.000043
6-chloro-N-methyl-N-[(3S)-2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pyrrolidin-3-yl]-1-benzothiophene-2-sulfonamide
-
pH and temperature not specified in the publication
0.0000013
6-chloro-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.0000008
6-chloro-N-[(3S)-1-(6-fluoro-2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000003
6-chloro-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-1-[(1R)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000009
6-chloro-N-[(3S)-1-[(1S)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-1-[(1S)-1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000003
6-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000005
6-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-1-[2-fluoro-4-[(1S)-1-(methylamino)ethyl]phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000006
6-chloro-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000001
6-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.00001
6-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.0000008
6-chloro-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000004
6-chloro-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000016
6-chloro-N-[1-(2-fluoro-4-piperidin-1-ylphenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.000028
6-chloro-N-[1-(2-fluoro-4-pyridin-4-ylphenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.0000024
6-chloro-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.0000006
6-chloro-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000006
6-chloro-N-[1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.00001
6-chloro-N-[1-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.00000011
6-chloro-N-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.000000016
6-chloro-N-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]thieno[2,3-b]pyridine-2-sulfonamide
-
-
0.0000001
6-chloro-N-[1-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.00000005
6-chloro-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]thieno[2,3-b]pyridine-2-sulfonamide
-
-
0.0000022
6-[2'-(methylsulfonyl)biphenyl-4-yl]-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000012 - 0.0000017
6-[2'-[(aminooxy)sulfinyl]-3-fluorobiphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
0.0000028
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-4-methyl-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[3,4-d]pyridazin-7-one
-
-
0.0000018
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.000038
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylic acid
-
-
0.0000019
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00002
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(3-nitrophenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000026
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-ethylphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.00000035
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000011
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000012
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(iminomethyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000021
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.0000018
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-5-methyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00000074
6-[3-fluoro-2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.000000038
6-[4-(1-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]cyclopropyl)phenyl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000012
7'-[(6-chloronaphthalen-2-yl)sulfonyl]-8a'-(hydroxymethyl)-1-(pyridin-4-yl)tetrahydro-5'H-spiro[piperidine-4,2'-[1,3]thiazolo[3,2-a]pyrazin]-5'-one
-
pH and temperature not specified in the publication
0.000006
7-([7-[(1-ethanimidoylpiperidin-4-yl)oxy]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]methyl)naphthalene-2-carboximidamide
-
pH and temperature not specified in the publication
0.00000025
7-oxo-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.0001
8-amino-N-[(1R)-2-oxo-1-phenyl-2-[4-(pyridin-4-yl)piperazin-1-yl]ethyl]naphthalene-2-carboxamide
-
pH and temperature not specified in the publication
0.000003
8-amino-N-[(1R)-2-[4-[4-fluoro-2-(methylsulfonyl)phenyl]piperazin-1-yl]-2-oxo-1-phenylethyl]naphthalene-2-carboxamide
-
pH and temperature not specified in the publication
0.00000734
AduNAP4
-
-
-
0.0000001
Ancylostoma ceylanicum anticoagulant peptide 1
-
25°C
-
0.0000003 - 0.0000006
antistasin
-
-
-
0.0057
AP'4
-
pH 7.4
0.00000008
apixaban
0.00000003
BMS-740808
-
-
0.000014
BuXI
-
-
-
0.0064
D13R
-
-
0.00000015
DPC423
-
-
0.0000357 - 0.000041
DX-9065a
0.0000038
ethyl 1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
0.000045
ethyl 6-(2'-hydroxybiphenyl-4-yl)-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
0.0000036
ethyl 6-[3-fluoro-2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
0.000057 - 0.00028
FPR-prothrombin
-
0.0000013
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate
-
37°C
0.00000082
methyl 2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzenesulfinate
-
-
0.0001
methyl 3'-fluoro-4'-(3-[[(3-methoxyphenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.0000445
methyl 3'-fluoro-4'-(3-[[(4-fluorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.000053
methyl 3'-fluoro-4'-(3-[[(4-methoxyphenyl)sulfonyl]amino]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.000026
methyl 3'-fluoro-4'-(3-[[(5-isoxazol-3-ylthiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.0000036
methyl 3'-fluoro-4'-([[1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]carbonyl]amino)biphenyl-2-sulfinate
-
-
0.00037
methyl 3'-fluoro-4'-[2-oxo-3-[(phenylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000028
methyl 3'-fluoro-4'-[2-oxo-3-[(quinolin-3-ylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000073
methyl 3'-fluoro-4'-[2-oxo-3-[(quinolin-6-ylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
0.0002
methyl 3'-fluoro-4'-[3-(4-methoxyphenoxy)-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000003
methyl 3'-fluoro-4'-[3-(iminomethyl)-1-(4-methoxyphenyl)-5,7-dioxo-1,4,5,7-tetrahydro-6H-pyrazolo[4,3-d]pyrimidin-6-yl]biphenyl-2-sulfinate
-
-
0.00042
methyl 3'-fluoro-4'-[3-([[4-(iminomethyl)phenyl]sulfonyl]methyl)-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000019
methyl 3'-fluoro-4'-[3-[(1H-indazol-6-ylsulfamoyl)methyl]-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.00056
methyl 3'-fluoro-4'-[3-[(4-methoxyphenyl)amino]-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000094
methyl 3-(3-carbamimidoylphenyl)-5-[(4-carbamimidoylphenyl)carbamoyl]-4,5-dihydro-1,2-oxazole-5-carboxylate
-
pH and temperature not specified in the publication
0.00065
methyl 4'-(3-[[(2,5-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000061
methyl 4'-(3-[[(3,4-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00027
methyl 4'-(3-[[(3,4-difluorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00073
methyl 4'-(3-[[(3,5-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00038
methyl 4'-(3-[[(3-chlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00016
methyl 4'-(3-[[(4-chloro-6-methyl-1-benzothiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000023
methyl 4'-(3-[[(4-chlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000078
methyl 4'-(3-[[(4-ethylphenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000053
methyl 4'-(3-[[(5-chlorothiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000011
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(diethylamino)ethyl](methyl)amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00000084
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(dimethylamino)ethyl](methyl)amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000022
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(dimethylamino)ethyl]amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000023
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](3-hydroxypropyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000022
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl]amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate2
-
-
0.00000071
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl][2-(4-methylpiperazin-1-yl)-2-oxoethyl]amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000018
methyl 4'-(3-[[(7-chloronaphthalen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000084
methyl 4'-([[4-amino-3-(iminomethyl)-1-(4-methoxyphenyl)-1H-pyrazol-5-yl]carbonyl]amino)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000002
methyl 4'-[1-(2-amino-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000018
methyl 4'-[1-(2-carbamoyl-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.000002
methyl 4'-[1-(2-carbamoylphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000018
methyl 4'-[1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000012
methyl 4'-[1-[2-[(aminooxy)sulfinyl]-4-methoxyphenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000074
methyl 4'-[1-[2-[(aminooxy)sulfinyl]phenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.0000027
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[(2-hydroxyethyl)(methyl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
0.00000043
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[methyl(1-methylpiperidin-4-yl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
0.0032
methyl 4'-[3-[(cyclohexylsulfonyl)methyl]-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000028
methyl 6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
0.00000088
methyl N-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]glycinate
-
-
0.000000043
methyl N-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycinate
-
-
0.0000063
methyl [3-(3-carbamimidoylphenyl)-4-[(2'-sulfamoylbiphenyl-4-yl)carbamoyl]-4,5-dihydro-1,2-oxazol-5-yl]acetate
-
pH and temperature not specified in the publication
0.000047
methyl [3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]amidosulfite
-
-
0.000057
N-(3-[[4'-(trifluoromethyl)biphenyl-4-yl]methoxy]phenyl)piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00000012
N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide
-
pH and temperature not specified in the publication
0.000003
N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.00000056
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]ethanediamide
-
pH and temperature not specified in the publication
0.000000561
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
pH 7.4, 30°C
0.00000021
N-([1-[4-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-methoxy-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3-fluorophenyl]-1H-imidazol-2-yl]methyl)-2-methoxy-N,N-dimethyl-2-oxoethanaminium
-
-
0.00000035
N-([1-[4-(3-[[(6-chloronaphthalen-2-yl)sulfonyl]amino]-2-oxopiperidin-1-yl)-3-fluorophenyl]-1H-imidazol-2-yl]methyl)-2-methoxy-N,N-dimethyl-2-oxoethanaminium
-
-
0.000018
N-methyl-N-[(3S)-2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
pH and temperature not specified in the publication
0.000004
N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.000016
N-[(1R)-2-(4-benzoylpiperidin-1-yl)-2-oxo-1-phenylethyl]-3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.002
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclobutyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0000113
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cycloheptyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000013
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclooctyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000086
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.1
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.00000285
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
pH 7.4
0.000265
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclobutyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000175
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cycloheptyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000041
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0014
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclooctyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000118
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000187
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0044
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0032
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.00027
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000005
N-[(3S)-1-(1-amino-2,3-dihydro-1H-inden-5-yl)-2-oxopyrrolidin-3-yl]-6-chloronaphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000006
N-[(3S)-1-[(1,6-diaminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
pH and temperature not specified in the publication
0.00018
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]-7-methoxynaphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000022
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
pH and temperature not specified in the publication
0.0001
N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
N-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]glycine
-
-
0.00000013
N-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycine
-
-
0.00021
N-[2-([[4-(aminomethyl)cyclohexyl]methyl]amino)-2-oxo-1-phenylethyl]-3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.011
N-[2-([[4-(aminomethyl)cyclohexyl]methyl]amino)-2-oxoethyl]-3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.002
N-[3-(biphenyl-4-ylmethoxy)phenyl]-1-carbamimidoylpiperidine-3-carboxamide
-
pH 8.0, 25°C
0.0052
N-[3-(biphenyl-4-ylmethoxy)phenyl]-1-carbamimidoylpiperidine-4-carboxamide
-
pH 8.0, 25°C
0.0025
N-[3-(biphenyl-4-ylmethoxy)phenyl]piperidine-3-carboxamide
-
pH 8.0, 25°C
0.001
N-[3-(biphenyl-4-ylmethoxy)phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.021
N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-1-[3-(5-methylidene-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
above
0.021
N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-1-[3-[(glycylamino)methyl]phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
above
0.000548
N-[3-[(2',3'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00947
N-[3-[(2',4',6'-trifluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.000512
N-[3-[(2',4'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00127
N-[3-[(2',5'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00145
N-[3-[(2',6'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.000767
N-[3-[(2'-fluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.000666
N-[3-[(3',4',5'-trifluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00013
N-[3-[(3',5'-difluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.000177
N-[3-[(3'-fluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00387
N-[3-[(4'-fluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.26
N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-3-carboxamide
-
pH 8.0, 25°C
0.000088
N-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]acetamide
-
-
0.126
N-[4-(biphenyl-4-ylmethoxy)phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.0000007
N-[4-(N,N-dimethylcarbamimidoyl)-2-fluorophenyl]-1-(3-fluoronaphthalen-2-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.0000001
N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]phenyl]-2'-[(dimethylamino)methyl]biphenyl-4-carboxamide
-
pH and temperature not specified in the publication
0.0000017
N2-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.00000002
N2-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.00000013
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.00000037
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.0000001
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N2-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycinamide
-
-
0.0000001
octamixaban
-
pH and temperature not specified in the publication
0.00000017 - 0.00000029
PD0313052
0.00005 - 0.0017
pefabloc
0.000098
ProTS195A
-
pH 7.7, 37°C, versus prothrombin, in absence of phospholipid
-
0.00000018 - 0.00000019
razaxaban
0.0000007
recombinant tick saliva anticoagulant protein
-
wild type enzyme, at pH 7.5 and 25°C
-
0.000026
tanogitran
-
pH and temperature not specified in the publication
0.016
tert-butyl N-(3-carbamimidoylbenzoyl)-D-tyrosinate
-
pH and temperature not specified in the publication
0.00000162
TFPIalpha
-
wild type enzyme, at pH 7.5 and 25°C
-
0.0000005
tick anticoagulant peptide
-
-
-
0.00000009 - 0.00000024
tissue factor pathway inhibitor
-
5 - 107
trimethylphenylammonium
0.01
Trypsin
-
above
-
0.0000001
ZK-807191
-
pH and temperature not specified in the publication
0.000005
[[4-(2-[[(5-carbamimidoyl-2-hydroxyphenyl)sulfonyl]amino]ethyl)-2'-(methylsulfonyl)biphenyl-3-yl]oxy]acetic acid
-
pH and temperature not specified in the publication
additional information
additional information
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000075
(1S,3R,4S)-4-[(1H-indol-2-ylcarbonyl)amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.000018
(2R)-N1-(5-chloropyridin-2-yl)-N2-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)pyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00000032
(2R)-N1-(5-chloropyridin-2-yl)-N2-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-methoxypyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00000038
(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-hydroxypyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00000016
(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-methoxypyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000001
(2R,4S)-N1-(5-chloropyridin-2-yl)-4-(2,4-difluorophenyl)-4-hydroxy-N2-(2-oxo-2H-1,3'-bipyridin-6'-yl)pyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000075
(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000025
(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000019
(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000008
(5R)-N1-(5-chloropyridin-2-yl)-N5-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1H-pyrazole-1,5-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000012
(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
37°C, pH 8.4
0.0000071
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000074
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-chlorophenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000037
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-fluorophenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.000005
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-methylphenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000064
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]phenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000039
([(2R)-2-(7-carbamimidoylnaphthalen-2-yl)-5-[(1-ethanimidoylpiperidin-4-yl)methyl]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000007
([(3'-carbamimidoylbiphenyl-3-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000044
([2-[(E)-2-(5-carbamimidoyl-2-hydroxyphenyl)ethenyl]-5-[(1-ethanimidoylpiperidin-4-yl)oxy]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.045
1,1'-(benzene-1,4-diyldimethanediyl)bis(N,N-diethylpiperidine-3-carboxamide)
Homo sapiens
-
pH 8.0, 25°C
0.0000035
1-(1-[(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2-hydroxypropanoyl]piperidin-4-yl)tetrahydropyrimidin-2(1H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.0000027
1-[(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)methyl]cyclopropanecarboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000022
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]-2-ethylpropan-2-ol
Homo sapiens
-
pH 8.3, 37°C
0.00002
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]ethanol
Homo sapiens
-
pH 8.3, 37°C
0.000018
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]propan-2-ol
Homo sapiens
-
pH 8.3, 37°C
0.0000048
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
Homo sapiens
-
37°C
0.0000022
2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2-methylpropanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000035
2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)propanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000011
2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)propanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
2-[3-[(benzylsulfonyl)amino]-2-hydroxyazepan-1-yl]-N-[(2S)-5-carbamimidamido-1-(2,3-dihydro-1,3-thiazol-2-yl)-1-oxopentan-2-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
2-[3-[(benzylsulfonyl)amino]-2-oxopyridin-1(2H)-yl]-N-[(2S)-5-carbamimidamido-1-(2,3-dihydro-1,3-thiazol-2-yl)-1-oxopentan-2-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000018
2-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]propan-2-ol
Homo sapiens
-
pH 8.3, 37°C
0.000006
2-[[[4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl](methylsulfonyl)amino]methyl]-1-benzothiophene-5-carboximidamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
3-(4-(5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]pentyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide
Homo sapiens
-
IC50: 3.0 nM
0.0000019
3-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2,2-dimethylpropanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00345
3-amino-N-[(1R)-2-oxo-1-phenyl-2-[(2'-sulfamoylbiphenyl-4-yl)amino]ethyl]-1H-indazole-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000035
3-carbamimidoyl-N-[(1R)-2-oxo-1-phenyl-2-[(2'-sulfamoylbiphenyl-4-yl)amino]ethyl]benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00029
3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]-N-(5-methyl-2-pyridyl)benzamide
Homo sapiens
-
at pH 8.4 and 37°C
0.00015
3-hydroxy-4'-methoxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
Homo sapiens
-
at pH 8.4 and 37°C
0.000061
3-hydroxy-4'-methoxy-4-methyl-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
Homo sapiens
-
at pH 8.4 and 37°C
0.000068
3-hydroxy-4'-methyl-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
Homo sapiens
-
at pH 8.4 and 37°C
0.00022
3-hydroxy-N-(5-methoxy-2-pyridyl)-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
Homo sapiens
-
at pH 8.4 and 37°C
0.000066
3-[(4-methoxyphenyl)carbamoyl]-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]phenyl beta-D-glucopyranosiduronic acid
Homo sapiens
-
at pH 8.4 and 37°C
0.00046 - 0.00061
3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
0.0000069
4'-chloro-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
Homo sapiens
-
at pH 8.4 and 37°C
0.0000156
4-acetamido-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-benzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.0000259
4-bromo-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)benzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.0000035
4-[[(3-carbamimidoylphenyl)amino]methyl]-3-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0002 - 0.0021
4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
0.000012
5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)-2-methylimidazo[1,2-a]pyridine
Homo sapiens
-
pH 8.3, 37°C
0.000021
5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridine
Homo sapiens
-
pH 8.3, 37°C
0.000068
5-chloro-3-hydroxy-4'-methoxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
Homo sapiens
-
at pH 8.4 and 37°C
0.0000015
5-chloro-3-[(5-chloro-2-pyridyl)carbamoyl]-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]phenyl beta-D-glucopyranosiduronic acid
Homo sapiens
-
at pH 8.4 and 37°C
0.000008
5-chloro-N-(1-oxo-2-[3-[(pyridin-4-ylamino)methyl]benzyl]-2,3-dihydro-1H-isoindol-4-yl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000036
5-chloro-N-(5-chloro-2-pyridyl)-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
Homo sapiens
-
at pH 8.4 and 37°C
14
5-chloro-N-(5-chloro-2-pyridyl)-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
Homo sapiens
-
at pH 8.4 and 37°C
0.0000087
5-chloro-N-(5-chloropyridin-2-yl)-3-hydroxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
Homo sapiens
-
at pH 8.4 and 37°C
0.000004
5-chloro-N-([(5S)-2-oxo-3-[4-(2-oxopyrrolidin-1-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000007
5-chloro-N-([(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000032
5-chloro-N-([(5S)-3-[3-fluoro-4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00009
5-chloro-N-([(5S)-3-[3-fluoro-4-(thiomorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000076
7-[(2R)-5-[(1-ethanimidoylpiperidin-4-yl)methyl]-1-(ethylsulfonyl)-2,3-dihydro-1H-indol-2-yl]naphthalene-2-carboximidamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000005 - 0.000616
apixaban
0.0000546
darexaban
Homo sapiens
-
at pH 6.0 and 25°C
0.0000024
DPC423
Homo sapiens
-
at pH 8.4 and 37°C
0.000002
edoxaban
Homo sapiens
-
wild type enzyme, at pH 7.5 and 25°C
0.0000018
epi-N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.00017
ethyl (4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
ethyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)-2-methylpropanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.000065
ethyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)propanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.01
ethyl 3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]benzoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00069
ethyl 4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]benzoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00011
methyl (3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0000056
methyl (4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.000072
methyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2-methylpropanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.000029
methyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)propanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.0001 - 0.00012
methyl 3-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2,2-dimethylpropanoate
0.00097
methyl 3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00007 - 0.0012
methyl 4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
0.0016
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl](methyl)amino]ethyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.003945
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl](methyl)amino]ethyl)-N,5-dimethyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000221
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]ethyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0041
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]ethyl)-N,5-dimethyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000074
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]phenyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.075
N-(4-butoxyphenyl)piperidine-3-carboxamide
Homo sapiens
-
pH 8.0, 25°C
0.0000286
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.0000065
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dichlorobenzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.0000171
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dimethoxybenzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.000016
N-(5-chloro-2-pyridyl)-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
Homo sapiens
-
at pH 8.4 and 37°C
0.00000083
N-(benzylsulfonyl)-3-(1-carbamimidoylpiperidin-4-yl)-D-alanyl-N-[(2S)-5-carbamimidamido-1-hydroxypentan-2-yl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH 7.4, 22°C
0.0000028
N-[(1R,2S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
N-[(1R,2S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000051
N-[(1R,2S,5S)-2-[(1H-indol-2-ylcarbonyl)amino]-5-(methylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH 7.4, 22°C
0.0000023
N-[(1R,2S,5S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000023
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.0000023
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dipropylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.0000025
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-[(2-hydroxyethyl)(methyl)carbamoyl]cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.0000022
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-[(2-methoxyethyl)(methyl)carbamoyl]cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.000002
N-[(2S)-5-carbamimidamido-1-(2,3-dihydro-1,3-thiazol-2-yl)-1-oxopentan-2-yl]-2-[4-[(4-chlorophenyl)sulfonyl]-2-oxopiperazin-1-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00012
N-[(3aR,7aR)-2-[3-(2-amino-2-iminoethoxy)benzyl]-1,3-dioxooctahydro-1H-isoindol-4-yl]-5-chlorothiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000086
N-[(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-1-methoxypiperidin-3-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000084
N-[(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-1-[(dimethylamino)oxy]piperidin-3-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000047 - 0.00077
N-[1-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-(dimethylamino)-4-oxobutan-2-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
0.0000077
N-[2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)phenyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
N2,N2-dimethyl-N5-[[(2-methyl-1-benzofuran-5-yl)amino]([2-oxo-1-[2-oxo-2-(pyrrolidin-1-yl)ethyl]azepan-3-yl]amino)methylidene]pyridine-2,5-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000015
N2-(benzylsulfonyl)-D-arginyl-N-[(2S)-5-carbamimidamido-1-hydroxypentan-2-yl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000056
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]-D-norvalinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000085
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]norvalinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
N2-[(4-chlorophenyl)carbamoyl]-N2-(cyclopropylmethyl)-N-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
N2-[(4-chlorophenyl)carbamoyl]-N2-(cyclopropylmethyl)-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000497
PD0313052
Homo sapiens
-
-
0.0000065
rivaroxaban
Homo sapiens
-
at pH 6.0 and 25°C
0.0000286
YM-222714
Homo sapiens
-
at pH 6.0 and 25°C
0.000009
[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol
Homo sapiens
-
pH 8.3, 37°C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.8
-
assay at
7.6
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
23
-
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
bound to
Manually annotated by BRENDA team
-
coagulation factors from plasma bind to tissue factor TF-expressing cells, e.g. lung fibroblast, become activated, dissociate, and diffuse into plasma to form enzymatic complexes on the membranes of activated platelets, overview
Manually annotated by BRENDA team
-
factor Xa is part of the prothrombinase complex formed by factor Xa, nonenzymatic cofacor Va and Ca2+ on the phospholipid surface of platelets or endothelial cells
Manually annotated by BRENDA team
-
primary
Manually annotated by BRENDA team
-
annexin 2 acts as a receptor for factor Xa on the cell surface. It facilitates factor Xa activation of receptor PAR-1 but does not enhance coagulant function of factor Xa. Overexpression of tissue factor abolishes annexin 2 dependence on factor Xa signaling and diminishes binding to cell surface annexin 2, whereas selectively abolishing tissue factor promotes the annexin 2/factor Xa interaction
Manually annotated by BRENDA team
-
enzyme associated with thrombi is enzymatically active
Manually annotated by BRENDA team
additional information
-
factor Xa binds to cell surfaces
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
-
the enzyme is involved in the blood coagulation cascade, overview
physiological function
additional information
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
FA10_HUMAN
488
1
54732
Swiss-Prot
Secretory Pathway (Reliability: 1)
PDB
SCOP
CATH
UNIPROT
ORGANISM
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
-
and monomer. Dimer is about 1000000fold less active toward prothrombin than the monomer. Dimerization results in substantial change in tertiary or quarternary strucutre with a concomitant decrease in alpha-helix
homodimer
-
-
monomer
-
and dimer. Dimer is about 1000000fold less active toward prothrombin than the monomer. Dimerization results in substantial change in tertiary or quarternary strucutre with a concomitant decrease in alpha-helix
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
proteolytic modification
reorientation of the N-terminus of serine protease domain after proteolytic activation of factor X to factor Xa, cleavage of the activation peptide at the Arg194-Ile195 peptide bond
glycoprotein
-
-
proteolytic modification
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
20 ns of molecular dynamics and steered molecular dynamics simulations on open and closed conformation, based on crystal structure PBD entry 1C5M. Interchangeable conformational transition between open and closed form. The opening and closing dynamics of the FXa subsites involve potential mechanistic roles of residues Glu97, Lys96, and aromatic-aromatic interactions of various aromatic residues His57, Tyr60, Phe94, Tyr99, Phe194, and Trp215
chymotrypsin treated factor Xa, i.e. des-Gla(1-44), lacking the Gla domain, free or complexed with inhibitor BIBT0871, 3 mg/ml protein in 10 mM Tris-HCl, pH 7.5, 20 mM sodium chloride, 2 mM calcium chloride, equilibrated against 20% PEG 4000, 0.1 M malate/imidazole, 0.1 M sodium acetate, pH 6.0, some days, X-ray diffraction structure determination and analysis at 1.9-3.0 A, cocrystallization of factor Xa complexed with thrombin and inhibitor BIBR1109
complex between the enzyme from which the residues 1-44 of the light chain have been removed and the inhibitor (2RS)-(3'-amidino-3-biphenyl)-5-(4-pyridylamino)pentanoic acid
purified chymotrypsin treated enzyme lacking the first 45 amino acid residues, i.e. des(1-45)FXa, complexed with inhibitor, 8 mg/ml protein in 5 mM MES-NaOH, pH 6.0, 5 mM CaCl2, 0.001 mM inhibitor RPR128515, 0.003 ml mixed with equal volume of reservoir solution containing 18-20% PEG 600, 50 mM MES-NaOH, pH 5.7, hanging drop vapour diffusion method, 19°C, a few days, X-ray duffraction structure determination and analysis at 2.1 A resolution of crystals soaked in mother liquor containing 1-1.5 mM inhibitor and 5-10% dimethylformamide
purified factor Xa, 8 mg/ml, in MES-NaOH, pH 6.0, 5 mM CaCl2, 0.001 mM inhibitor RPR128515, hanging drop vapour diffusion method, equal volume of 0.003 ml of protein and reservoir solution, the latter containing 18-20% PEG 600, 50 mM MES-NaOH, pH 5.7, 19°C, a few days, seeding cycles are necessary to improve size and shape of the crystals, X-ray diffraction structure determination and analysis at 2.1 A resolution
purified factor Xa, cleaved to des-Gla-factor Xa via limited proteolysis with chymotrypsin, is crystallized in complex with inhibitors 3-chloro-N-(4-chloro-2-([(4-chlorophenyl)-amino]carbonyl)phenyl)-4-[(4-methyl-1-piperazinyl)methyl]-2-thiophenecarboxamide and 3-chloro-N-(4-chloro-2-([(5-chloro-2-pyridinyl)amino]carbonyl)-6-methoxyphenyl)-4-([(4,5-dihydro-2-oxazolyl)methylamino]methyl)-2-thiophenecarboxamide, within 2-4 weeks in 15-21% PEG 1500 and 10 mM CaCl2, or from 0.1 M imidazole/malate, pH 5.5, 0.5 M sodium acetate, pH 5.0, 24% PEG 3350, and 5 mM CaCl2, X-ray diffraction structure determination and analysis at 2.1-25 A
in complex with inhibitor 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 to 2.0 A resolution. The molecule adopts an extended binding mode with the para-methoxyphenyl group located in the S1 pocket and the alpha-CH2-N-pyrrolidinyl phenylcyclopropyl group occupying the S4 pocket
-
in complex with inhibitor 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, to 2.1 A resolution
-
method for quantifying the contributions to the free energy of binding due to the ligand evacuating energetically unfavorable and entropically structured solvent for the set of congeneric pairs. The expulsion of active-site water strongly impacts protein-ligand binding affinities in two ways. Hydrophobic ligand groups that displace water from energetically unfavorable hydrophobically enclosed environments contribute enthalpically since the water molecules will make more favorable interactions in the bulk fluid. Ligand groups that displace entropically structured solvent contribute even when the solvent interacts favorably with the protein since well-designed ligands will recapture the protein-water interaction energy
-
molecular modeling of complex with inhibitor [5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol. The imidazo[1,2-a]pyridine ring is deeply buried inside the hydrophobic S4 site and makes hydrophobic contacts with the aromatic rings of Tyr99, Phe174, and Trp215 without the salt bridge with any amino acid residue in this site. The imidazo[1,2-a]pyridine ring extends across the face of the Phe174 phenyl ring with a favorable pi-pi stacking interaction
-
purified chymotrypsin-treated enzyme, i.e. des-Gla-factor Xa, complexed with inhibitor (R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamide, 20°C, hanging drop vapour diffusion technique, from 0.1 M MES-OH, pH 5.8, 10 mM CaCl2, 18% PEG 6000, 10 mM inhibitor, enlarged by seeding, X-ray diffraction structure determination and analysis at 2.22 A resolution
-
structure of factor Xa in complex with PD0313052
-
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
G114R
simulation of the exchange of residues, conserved residue in the EGF2 domain sulfide loop, disruptive salt bridge interaction or blockage of interaction with factors VIIIa/IXa
G323S
simulation of the exchange of residues, mutation disrupts a highly conserved beta-sheet structure
N57T
simulation of the exchange of residues, loss of interaction with Cys81 with structural implications
P343S
simulation of the exchange of residues, conserved residue involved in a suface beta-sheet, affects intrinsic folding
R326C
simulation of the exchange of residues, surface residue, involved in protein-protein interactions, interaction with Gln376 located in the S1-binding site
T318M
simulation of the exchange of residues, surface residue involved in a side-chain hydrogen bond with Glu341 which is lost in the mutant, leads to clinical effect
V298M
simulation of the exchange of residues, unfolding occurs due to space limitation
D322N/S419A
-
no proteolytic activity
D70K
-
mutation of E2FXa mutant, loss of ability to bind Ca2+, activity is retained
E14D
-
E14 is posttranslationally carboxylated in wild-type enzyme. Heparin activated inhibition of mutant enzyme by antithrombin with and without Ca2+ is enhanced compared to wild-type recombinant FXa
E16D
-
E16 is posttranslationally carboxylated in wild-type enzyme. Heparin activated inhibition of mutant enzyme by antithrombin is not activated by Ca2+
E19D
-
E19 is posttranslationally carboxylated in wild-type enzyme. Heparin activated inhibition of mutant enzyme by antithrombin is the same as wild-type recombinant FXa
E217A
-
affinity for interaction with Na+ is impaired. 3-4fold decrease in activity towards both natural and synthetic substrates. Presence of factor Va restores most of the catalytic defect with substrate prothrombin
E217Q
-
affinity for interaction with Na+ is impaired. Presence of factor Va restores most of the catalytic defect with substrate prothrombin
E26D
-
E26 is posttranslationally carboxylated in wild-type enzyme. Heparin activated inhibition of mutant enzyme by antithrombin is not activated by Ca2+
E29D
-
E29D is posttranslationally carboxylated in wild-type enzyme. Heparin activated inhibition by antithrombin with and without Ca2+ is enhanced compared to wild-type recombinant FXa
E80K
-
mutation of E2FXa mutant, loss of ability to bind Ca2+, activity is retained
F174A
-
the mutant has about wild type activity
F174N
-
site-directed mutagenesis, reduced binding of inhibitor trimethylphenylammonium
G11V
-
naturally occuring mutation of factor Xa within the omega-loop of the gamma-carboxyglutamic-rich domain of the ature enzyme, leading to enzyme deficiency and a bleeding phenotype, overview. The mutant factor Xa activity is below 1% of wild-type activity, activation with RVV-X is 4fold less effective in the patient's plasma than in healthy plasma. The patient's phenotype appears to be due to a very low rate of FXG11V activation by TF/FVIIa and FVIIIa/FIXa complexes rather than to FXaG11V activity within prothrombinase, overview
I16L
-
mutation disrupts activation process of the factor X zymogen with alteration of active site function and impairment of Na+ and factor Va binding. Irreversible stabilization with L-Glu-Gly-L-Arg-chloromethyl ketone fully rescues factor Va binding. The Km value for prothrombin conversion for the mutant assembled into prothrombinase is unaltered, whereas the kcat is reduced 3- to 4fold
K147A
-
site-directed mutagenesis, reduced Km, reduced kcat compared to the wild-type enzyme for the synthetic substrate and for prothrombin as a substrate
L224A
-
affinity for interaction with Na+ is impaired
R143A
-
site-directed mutagenesis, reduced Km, reduced kcat compared to the wild-type enzyme for the synthetic substrate and for prothrombin as a substrate
R150A
R154A
-
site-directed mutagenesis, increased Km, increased kcat for the synthetic substrate, and reduced Km and kcat for prothrombin as a substrate compared to the wild-type enzyme
R221A
-
affinity for interaction with Na+ is impaired
S195A
-
catalytically inactive mutant, that still binds to inhibitor antithrombin with the same velocity as the wild-type enzyme
V17A
-
mutation disrupts activation process of the factor X zymogen with alteration of active site function and impairment of Na+ and factor Va binding. The Km value for prothrombin conversion for the mutant assembled into prothrombinase is unaltered, whereas the kcat is reduced 3- to 4fold
Y225P
-
mutation of the GDFXa mutant, exchange of the Na+ binding site residue results in 2fold decreased stimulation by Na+ in presence or absence of Ca2+
Y99A
-
the enzyme shows strongly reduced activity compared to the wild type enzyme
Y99A/F174A
-
the enzyme shows severely reduced activity compared to the wild type enzyme
Y99T
-
site-directed mutagenesis, 25fold reduced binding of inhibitor trimethylphenylammonium
additional information
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
native and recombinant wild-type, and mutant constructs expressed in 293 ells
-
native factor X from plasma
-
native wild-type from plasma
-
recombinant and inactive factor Xa(Asp322Asn,Ser419Ala)
-
recombinant facgtor X from BHK-21 cells
-
recombinant wild-type and mutant zymogens from expression in HEK293 cells, to homogeneity
-
recombinant wild-type inactive factor X and mutant proteins
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expression by the RSV-PL4 expression/purification vector system of wild-type inactive factor X, mutant inactive factor X lacking the 4-carboxyglutamic acid-domain, Y225P mutant of factor X, factor X E2FX mutant lacking both Gla-domain and EGF1-domain, as well as of mutants D70K and E80K of mutant E2FX, expression in human 293 cells
-
expression in BHK-21 cells
-
expression in HEK-293 cell
-
expression of wild-type and mutant zymogens in HEK293 cells, the enzyme is expressed with an introduced cleavage site for for furin-like processing enzymes which is required for expression of the enzyme and for processing of the zymgen to the mature enzyme
-
expression of wild-type enzyme, enzyme lacking the Gla- and the EGF-like domains, of the isolated Gla-domain, the EGF-like domain, and a construct comprising both, expression in human 293 cells
-
inactive factor Xa(Asp322Asn,Ser419Ala), expression in Chinese hamster ovary cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
activated protein C proteolytically inactivates factor Va through proteolytic cleavage and thereby downregulates prothrombinase. Factor Xa protects 17.3fold and prothrombin protects 5.8fold the inactivation of factor Va, while protein S increases the inactivation. Factor Xa and prothrombin together are highly protective, both with and without protein S. R506Q mutation of factor Va is only mildly prothrombotic, even though it profoundly affects the kinetics of inactivation of isolated FVa by activated protein C
-
sphingolipids, including lysosulfatide and some of its analogs like N-acetyl sulfatide, psychosine, gluco-psychosine, lyso-sphingomyelin or sulfatide, may down-regulate enzyme activity without inhibiting the enzyme's active site. Lysosulfatide is an anticoagulant lipid that inhibits the enzyme when it is bound to either phospholipids or to factor Va
-
the gene expression of factor X in retinal pigment epithelial cells is decreased by blood serum, activated factor X, thrombin, transforming growth factor beta1, and platelet-derived growth factor
-
the gene expression of factor X in retinal pigment epithelial cells is increased by hypoxia and prostaglandin E2
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pharmacology
enyme is a potential target for development of antithrombotics, structure-based drug design approach usig the crystal structure of the enzyme-inhibitor complex
analysis
-
development of an assay for the monitoring of anticoagulants inhibiting factor Xa and/or factor IIa. Assay is based on the addition of factor Xa and snake venom RVV-V, i.e. Russell viper venom factor V activator specifically activating factor V and phospholipids to platelet-poor plasma. Assay shows an almost linear dose-response and high sensitivity for unfractionated heparin, low molecular weight heparins, r-hirudin, and argatroban
drug development
medicine
pharmacology
synthesis
-
enzyme is a target for design of specific inhibitors
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Franssen, J.; Salemink, I.; Willems, G.M.; Wun, T.C.; Hemker, H.C.; Lindhout, T.
Prothrombinase is protected from inactivation by tissue factor pathway inhibitor: competition between prothrombin and inhibitor
Biochem. J.
323
33-37
1997
Homo sapiens
Manually annotated by BRENDA team
Kamata, K.; Kawamoto, H.; Honma, T.; Iwama, T.; Kim, S.H.
Structural basis for chemical inhibition of human blood coagulation factor Xa
Proc. Natl. Acad. Sci. USA
95
6630-6635
1998
Homo sapiens (P00742), Homo sapiens
Manually annotated by BRENDA team
Mao, S.S.; Przysiecki, C.T.; Krueger, J.A.; Cooper, C.M.; Lewis, S.D.; Joyce, J.; Lellis, C.; Garsky, V.M.; Sardana, M.; Shafer, J.A.
Selective inhibition of factor Xa in the prothrombinase complex by the carboxyl-terminal domain of antistasin
J. Biol. Chem.
273
30086-30091
1998
Homo sapiens
Manually annotated by BRENDA team
Waxman, L.; Smith, D.E.; Arcuri, K.E.; Vlasuk, G.P.
Tick anticoagulant peptide (TAP) is a novel inhibitor of blood coagulation factor Xa [published erratum appears in Science 1990 Jun 22;248(4962):1473
Science
248
593-596
1990
Homo sapiens
Manually annotated by BRENDA team
Sinha, U.; Hancock, T.E.; Lin, P.H.; Hollenbach, S.; Wolf, D.L.
Expression, purification, and characterization of inactive human coagulation factor Xa (Asn322Ala419)
Protein Expr. Purif.
3
518-524
1992
Homo sapiens
Manually annotated by BRENDA team
Scarborough, R.M.
Coagulation factor Xa: the prothrombinase complex as an emerging therapeutic target for small molecule inhibitors
J. Enzyme Inhib.
14
15-25
1998
Homo sapiens
Manually annotated by BRENDA team
Liang, A.M.; Light, D.R.; Kochanny, M.; Rumennik, G.; Trinh, L.; Lentz, D.; Post, J.; Morser, J.; Snider, M.
Discovery and characterization of a potent and selective non-amidine inhibitor of human factor Xa
Biochem. Pharmacol.
65
1407-1418
2003
Homo sapiens
Manually annotated by BRENDA team
Rezaie, A.R.; He, X.
Sodium binding site of factor Xa: role of sodium in the prothrombinase complex
Biochemistry
39
1817-1825
2000
Homo sapiens
Manually annotated by BRENDA team
Monnaie, D.; Arosio, D.; Griffon, N.; Rose, T.; Rezaie, A.R.; Di Cera, E.
Identification of a binding site for quaternary amines in factor Xa
Biochemistry
39
5349-5354
2000
Homo sapiens
Manually annotated by BRENDA team
Kalafatis, M.; Beck, D.O.
Identification of a binding site for blood coagulation factor Xa on the heavy chain of factor Va. Amino acid residues 323-331 of factor V represent an interactive site for activated factor X
Biochemistry
41
12715-12728
2002
Homo sapiens
Manually annotated by BRENDA team
Adler, M.; Kochanny, M.J.; Ye, B.; Rumennik, G.; Light, D.R.; Biancalana, S.; Whitlow, M.
Crystal structures of two potent nonamidine inhibitors bound to factor Xa
Biochemistry
41
15514-15523
2002
Homo sapiens (P00742)
Manually annotated by BRENDA team
Manithody, C.; Yang, L.; Rezaie, A.R.
Role of basic residues of the autolysis loop in the catalytic function of factor Xa
Biochemistry
41
6780-6788
2002
Homo sapiens
Manually annotated by BRENDA team
Banerjee, M.; Drummond, D.C.; Srivastava, A.; Daleke, D.; Lentz, B.R.
Specificity of soluble phospholipid binding sites on human factor Xa
Biochemistry
41
7751-7762
2002
Homo sapiens
Manually annotated by BRENDA team
Banerjee, M.; Majumder, R.; Weinreb, G.; Wang, J.; Lentz, B.R.
role of procoagulant lipids in human prothrombin activation. 2. Soluble phosphatidylserine upregulates and directs factor Xa to appropriate peptide bonds in prothrombin
Biochemistry
41
950-957
2002
Homo sapiens
Manually annotated by BRENDA team
O'Brien, L.A.; Stafford, A.R.; Fredenburgh, J.C.; Weitz, J.I.
Glycosaminoglycans bind factor Xa in a Ca2+-dependent fashion and modulate its catalytic activity
Biochemistry
42
13091-13098
2003
Homo sapiens
Manually annotated by BRENDA team
Studelska, D.R.; McDowell, L.M.; Adler, M.; O'Connor, R.D.; Mehta, A.K.; Guilford, W.J.; Dallas, J.L.; Arnaiz, D.; Light, D.R.; Schaefer, J.
Conformation of a bound inhibitor of blood coagulant factor Xa
Biochemistry
42
7942-7949
2003
Homo sapiens (P00742), Homo sapiens
Manually annotated by BRENDA team
Rezaie, A.R.; Yang, L.
Probing the molecular basis of factor Xa specificity by mutagenesis of the serpin, antithrombin
Biochim. Biophys. Acta
1528
167-176
2001
Homo sapiens
Manually annotated by BRENDA team
Mueller, M.M.; Sperl, S.; Sturzebecher, J.; Bode, W.; Moroder, L.
(R)-3-amidinophenylalanine-derived inhibitors of factor Xa with a novel active-site binding mode
Biol. Chem.
383
1185-1191
2002
Bos taurus, Homo sapiens
Manually annotated by BRENDA team
Venkateswarlu, D.; Perera, L.; Darden, T.; Pedersen, L.G.
Structure and dynamics of zymogen human blood coagulation factor X
Biophys. J.
82
1190-1206
2002
Homo sapiens (P00742), Homo sapiens
Manually annotated by BRENDA team
Nishida, H.; Miyazaki, Y.; Kitamura, Y.; Ohashi, M.; Matsusue, T.; Okamoto, A.; Hosaka, Y.; Ohnishi, S.; Mochizuki, H.
Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitor
Chem. Pharm. Bull.
49
1237-1244
2001
Homo sapiens
Manually annotated by BRENDA team
Oliva, M.L.V.; Andrade, S.A.; Juliano, M.A.; Sallai, R.C.; Torquato, R.J.; Sampaio, M.U.; Pott, V.J.; Sampaio, C.A.M.
Kinetic characterization of factor Xa binding using a quenched fluorescent substrate based on the reactive site of factor Xa inhibitor from Bauhinia ungulata seeds
Curr. Med. Chem.
10
1085-1093
2003
Homo sapiens
Manually annotated by BRENDA team
Leadley, R.J., Jr.; Chi, L.; Porcari, A.R.
Non-hemostatic activity of coagulation factor Xa: potential implications for various diseases
Curr. Opin. Pharmacol.
1
169-175
2001
Oryctolagus cuniculus, Homo sapiens, Rattus norvegicus, Sus scrofa
Manually annotated by BRENDA team
Gould, W.R.; Leadley, R.J.
Recent advances in the discovery and development of direct coagulation factor Xa inhibitors
Curr. Pharm. Des.
9
2337-2347
2003
Homo sapiens
Manually annotated by BRENDA team
Leadley, R.J., Jr.
Coagulation factor Xa inhibition: biological background and rationale
Curr. Top. Med. Chem.
1
151-159
2001
Canis lupus familiaris, Homo sapiens
Manually annotated by BRENDA team
Heran, C.; Morgan, S.; Kasiewski, C.; Bostwick, J.; Bentley, R.; Klein, S.; Chu, V.; Brown, K.; Colussi, D.; Czekaj, M.; Perrone, M.; Leadley, R.
Antithrombotic efficacy of RPR208566, a novel factor Xa inhibitor, in a rat model of carotid artery thrombosis
Eur. J. Pharmacol.
389
201-207
2000
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Hayashi, M.; Matsuo, A.; Nakamoto, H.; Aisaka, K.
Antithrombotic effects of a synthetic inhibitor of activated factor X, JTV-803, in animals
Eur. J. Pharmacol.
412
61-66
2001
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Srivastava, A.; Wang, J.; Majumder, R.; Rezaie, A.R.; Stenflo, J.; Esmon, C.T.; Lentz, B.R.
Localization of phosphatidylserine binding sites to structural domains of factor Xa
J. Biol. Chem.
277
1855-1863
2002
Bos taurus, Homo sapiens
Manually annotated by BRENDA team
Bianchini, E.P.; Louvain, V.B.; Marque, P.E.; Juliano, M.A.; Juliano, L.; Le Bonniec, B.F.
Mapping of the catalytic groove preferences of factor Xa reveals an inadequate selectivity for its macromolecule substrates
J. Biol. Chem.
277
20527-20534
2002
Homo sapiens
Manually annotated by BRENDA team
Buddai, S.K.; Toulokhonova, L.; Bergum, P.W.; Vlasuk, G.P.; Krishnaswamy, S.
Nematode anticoagulant protein c2 reveals a site on factor Xa that is important for macromolecular substrate binding to human prothrombinase
J. Biol. Chem.
277
26689-26698
2002
Homo sapiens
Manually annotated by BRENDA team
Harrison, L.M.; Nerlinger, A.; Bungiro, R.D.; Cordova, J.L.; Kuzmic, P.; Cappello, M.
Molecular characterization of Ancylostoma inhibitors of coagulation factor Xa. Hookworm anticoagulant activity in vitro predicts parasite bloodfeeding in vivo
J. Biol. Chem.
277
6223-6229
2002
Homo sapiens
Manually annotated by BRENDA team
Kalafatis, M.; Beck, D.O.; Mann, K.G.
Structural requirements for expression of factor Va activity
J. Biol. Chem.
278
33550-33561
2003
Homo sapiens
Manually annotated by BRENDA team
Brufatto, N.; Nesheim, M.E.
Analysis of the kinetics of prothrombin activation and evidence that two equilibrating forms of prothrombinase are involved in the process
J. Biol. Chem.
278
6755-6764
2003
Homo sapiens
Manually annotated by BRENDA team
Maignan, S.; Guilloteau, J.P.; Pouzieux, S.; Choi-Sledeski, Y.M.; Becker, M.R.; Klein, S.I.; Ewing, W.R.; Pauls, H.W.; Spada, A.P.; Mikol, V.
Crystal structures of human factor Xa complexed with potent inhibitors
J. Med. Chem.
43
3226-3232
2000
Homo sapiens (P00742), Homo sapiens
Manually annotated by BRENDA team
Verner, E.; Katz, B.A.; Spencer, J.R.; Allen, D.; Hataye, J.; Hruzewicz, W.; Hui, H.C.; Kolesnikov, A.; Li, Y.; Luong, C.; Martelli, A.; Radika, K.; Rai, R.; She, M.; Shrader, W.; Sprengeler, P.A.; Trapp, S.; Wang, J.; Young, W.B.; Mackman, R.L.
Development of serine protease inhibitors displaying a multicentered short 2.3 ANG hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa
J. Med. Chem.
44
2753-2771
2001
Homo sapiens
Manually annotated by BRENDA team
Pinto, D.J.; Orwat, M.J.; Wang, S.; Fevig, J.M.; Quan, M.L.; Amparo, E.; Cacciola, J.; Rossi, K.A.; Alexander, R.S.; Smallwood, A.M.; Luettgen, J.M.; Liang, L.; Aungst, B.J.; Wright, M.R.; Knabb, R.M.; Wong, P.C.; Wexler, R.R.; Lam, P.Y.
Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4 -yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa
J. Med. Chem.
44
566-578
2001
Homo sapiens
Manually annotated by BRENDA team
Choi-Sledeski, Y.M.; Kearney, R.; Poli, G.; Pauls, H.; Gardner, C.; Gong, Y.; Becker, M.; Davis, R.; Spada, A.; Liang, G.; Chu, V.; Brown, K.; Collussi, D.; Leadley, R.Jr.; Rebello, S.; Moxey, P.; Morgan, S.; Bentley, R.; Kasiewski, C.; Maignan, S.; Guilloteau, J.P.; Mikol, V.
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand
J. Med. Chem.
46
681-684
2003
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Li, Y.; Spencer, F.A.; Ball, S.; Becker, R.C.
Inhibition of platelet-dependent prothrombinase activity and thrombin generation by glycoprotein IIb/IIIa receptor-directed antagonists: potential contributing mechanism of benefit in acute coronary syndromes
J. Thromb. Thrombolysis
10
69-76
2000
Homo sapiens
Manually annotated by BRENDA team
Lorentsen, R.H.; Moller, C.H.; Etzerodt, M.; Thogersen, H.C.; Holtet, T.L.
Substrate turnover and inhibitor binding as selection parameters in directed evolution of blood coagulation factor Xa
Org. Biomol. Chem.
1
1657-1663
2003
Homo sapiens
Manually annotated by BRENDA team
Nar, H.; Bauer, M.; Schmid, A.; Stassen, J.M.; Wienen, W.; Priepke, H.W.M.; Kauffmann, I.K.; Ries, U.J.; Hauel, N.H.
Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors
Structure
9
29-37
2001
Homo sapiens (P00742), Homo sapiens
Manually annotated by BRENDA team
Chu, V.; Brown, K.; Colussi, D.; Gao, J.; Bostwick, J.; Kasiewski, C.; Bentley, R.; Morgan, S.; Guertin, K.; Pauls, H.W.; Gong, Y.; Zulli, A.; Perrone, M.H.; Dunwiddie, C.T.; Leadley, R.J.
Pharmacological characterization of a novel factor Xa inhibitor, FXV673
Thromb. Res.
103
309-324
2001
Canis lupus familiaris, Oryctolagus cuniculus, Homo sapiens
Manually annotated by BRENDA team
Chu, V.; Brown, K.; Colussi, D.; Choi, Y.M.; Green, D.; Pauls, H.W.; Spada, A.P.; Perrone, M.H.; Leadley, R.J.; Dunwiddie, C.T.
In vitro characterization of a novel factor Xa inhibitor, RPR 130737
Thromb. Res.
99
71-82
2000
Homo sapiens
Manually annotated by BRENDA team
Gould, W.R.; Cladera, E.; Harris, M.S.; Zhang, E.; Narasimhan, L.; Thorn, J.M.; Leadley, R.J.
Co-crystal structure and inhibition of factor Xa by PD0313052 identifies structurally stabilized active site residues of factor Xa and prothrombinase
Biochemistry
44
9280-9289
2005
Homo sapiens
Manually annotated by BRENDA team
Bianchini, E.P.; Pike, R.N.; Le Bonniec, B.F.
The elusive role of the potential factor X cation-binding exosite-1 in substrate and inhibitor interactions
J. Biol. Chem.
279
3671-3679
2004
Homo sapiens
Manually annotated by BRENDA team
Orcutt, S.J.; Krishnaswamy, S.
Binding of substrate in two conformations to human prothrombinase drives consecutive cleavage at two sites in prothrombin
J. Biol. Chem.
279
54927-54936
2004
Homo sapiens
Manually annotated by BRENDA team
Willardsen, J.A.; Dudley, D.A.; Cody, W.L.; Chi, L.; McClanahan, T.B.; Mertz, T.E.; Potoczak, R.E.; Narasimhan, L.S.; Holland, D.R.; Rapundalo, S.T.; Edmunds, J.J.
Design, synthesis, and biological activity of potent and selective inhibitors of blood coagulation factor Xa
J. Med. Chem.
47
4089-4099
2004
Homo sapiens
Manually annotated by BRENDA team
Whinna, H.C.; Lesesky, E.B.; Monroe, D.M.; High, K.A.; Larson, P.J.; Church, F.C.
Role of the gamma-carboxyglutamic acid domain of activated factor X in the presence of calcium during inhibition by antithrombin-heparin
J. Thromb. Haemost.
2
1127-1134
2004
Homo sapiens
Manually annotated by BRENDA team
Ieko, M.; Tarumi, T.; Takeda, M.; Naito, S.; Nakabayashi, T.; Koike, T.
Synthetic selective inhibitors of coagulation factor Xa strongly inhibit thrombin generation without affecting initial thrombin forming time necessary for platelet activation in hemostasis
J. Thromb. Haemost.
2
612-618
2004
Homo sapiens
Manually annotated by BRENDA team
Tanaka, M.; Arai, H.; Liu, N.; Nogaki, F.; Nomura, K.; Kasuno, K.; Oida, E.; Kita, T.; Ono, T.
Role of coagulation factor Xa and protease-activated receptor 2 in human mesangial cell proliferation
Kidney Int.
67
2123-2133
2005
Homo sapiens
Manually annotated by BRENDA team
Dennis, M.W.; Downey, C.; Brufatto, N.; Nesheim, M.E.; Stevenson, K.; Toh, C.H.
Prothrombinase enhancement through quantitative and qualitative changes affecting very low density lipoprotein in complex with C-reactive protein
Thromb. Haemost.
91
522-530
2004
Homo sapiens
Manually annotated by BRENDA team
Daubie, V.; Cauwenberghs, S.; Senden, N.H.; Pochet, R.; Lindhout, T.; Buurman, W.A.; Heemskerk, J.W.
Factor Xa and thrombin evoke additive calcium and proinflammatory responses in endothelial cells subjected to coagulation
Biochim. Biophys. Acta
1763
860-869
2006
Bos taurus, Homo sapiens
Manually annotated by BRENDA team
Fevig, J.M.; Cacciola, J.; Buriak, J.; Rossi, K.A.; Knabb, R.M.; Luettgen, J.M.; Wong, P.C.; Bai, S.A.; Wexler, R.R.; Lam, P.Y.
Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa
Bioorg. Med. Chem. Lett.
16
3755-3760
2006
Homo sapiens
Manually annotated by BRENDA team
Pinto, D.J.; Galemmo, R.A.; Quan, M.L.; Orwat, M.J.; Clark, C.; Li, R.; Wells, B.; Woerner, F.; Alexander, R.S.; Rossi, K.A.; Smallwood, A.; Wong, P.C.; Luettgen, J.M.; Rendina, A.R.; Knabb, R.M.; He, K.; Wexler, R.R.; Lam, P.Y.
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties
Bioorg. Med. Chem. Lett.
16
5584-5589
2006
Homo sapiens
Manually annotated by BRENDA team
Nagata, T.; Yoshino, T.; Haginoya, N.; Yoshikawa, K.; Isobe, Y.; Furugohri, T.; Kanno, H.
Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors
Bioorg. Med. Chem. Lett.
17
4683-4688
2007
Homo sapiens
Manually annotated by BRENDA team
Smallheer, J.M.; Wang, S.; Laws, M.L.; Nakajima, S.; Hu, Z.; Han, W.; Jacobson, I.; Luettgen, J.M.; Rossi, K.A.; Rendina, A.R.; Knabb, R.M.; Wexler, R.R.; Lam, P.Y.; Quan, M.L.
Sulfonamidolactam inhibitors of coagulation factor Xa
Bioorg. Med. Chem. Lett.
18
2428-2433
2008
Homo sapiens
Manually annotated by BRENDA team
Silva, F.P.; Antunes, O.A.; de Alencastro, R.B.; De Simone, S.G.
The Na+ binding channel of human coagulation proteases: Novel insights on the structure and allosteric modulation revealed by molecular surface analysis
Biophys. Chem.
119
282-294
2006
Homo sapiens
Manually annotated by BRENDA team
Panteleev, M.A.; Ovanesov, M.V.; Kireev, D.A.; Shibeko, A.M.; Sinauridze, E.I.; Ananyeva, N.M.; Butylin, A.A.; Saenko, E.L.; Ataullakhanov, F.I.
Spatial propagation and localization of blood coagulation are regulated by intrinsic and protein C pathways, respectively
Biophys. J.
90
1489-1500
2006
Homo sapiens
Manually annotated by BRENDA team
Khrenov, A.V.; Ananyeva, N.M.; Saenko, E.L.
Role of the B domain in proteolytic inactivation of activated coagulation factor VIII by activated protein C and activated factor X
Blood Coagul. Fibrinolysis
17
379-388
2006
Homo sapiens
Manually annotated by BRENDA team
Faure, G.; Gowda, V.T.; Maroun, R.C.
Characterization of a human coagulation factor Xa-binding site on Viperidae snake venom phospholipases A2 by affinity binding studies and molecular bioinformatics
BMC Struct. Biol.
7
82
2007
Homo sapiens (P00742), Homo sapiens
Manually annotated by BRENDA team
Borensztajn, K.S.; Bijlsma, M.F.; Groot, A.P.; Brueggemann, L.W.; Versteeg, H.H.; Reitsma, P.H.; Peppelenbosch, M.P.; Spek, C.A.
Coagulation factor Xa drives tumor cells into apoptosis through BH3-only protein Bim up-regulation
Exp. Cell Res.
313
2622-2633
2007
Homo sapiens
Manually annotated by BRENDA team
Norstrom, E.A.; Tran, S.; Steen, M.; Dahlbaeck, B.
Effects of factor Xa and protein S on the individual activated protein C-mediated cleavages of coagulation factor Va
J. Biol. Chem.
281
31486-31494
2006
Homo sapiens
Manually annotated by BRENDA team
Izaguirre, G.; Swanson, R.; Raja, S.M.; Rezaie, A.R.; Olson, S.T.
Mechanism by which exosites promote the inhibition of blood coagulation proteases by heparin-activated antithrombin
J. Biol. Chem.
282
33609-33622
2007
Homo sapiens
Manually annotated by BRENDA team
Gould, W.R.; McClanahan, T.B.; Welch, K.M.; Baxi, S.M.; Saiya-Cork, K.; Chi, L.; Johnson, T.R.; Leadley, R.J.
Inhibitors of blood coagulation factors Xa and IIa synergize to reduce thrombus weight and thrombin generation in vivo and in vitro
J. Thromb. Haemost.
4
834-841
2006
Homo sapiens
Manually annotated by BRENDA team
Calatzis, A.; Peetz, D.; Haas, S.; Spannagl, M.; Rudin, K.; Wilmer, M.
Prothrombinase-induced clotting time assay for determination of the anticoagulant effects of unfractionated and low-molecular-weight heparins, fondaparinux, and thrombin inhibitors
Am. J. Clin. Pathol.
130
446-454
2008
Homo sapiens
Manually annotated by BRENDA team
Fiore, M.M.; Mackie, I.J.
Dual effect of platelet factor 4 on the activities of factor Xa
Biochem. Biophys. Res. Commun.
379
1072-1075
2009
Homo sapiens
Manually annotated by BRENDA team
Yang, L.; Manithody, C.; Qureshi, S.H.; Rezaie, A.R.
Factor Va alters the conformation of the Na+-binding loop of factor Xa in the prothrombinase complex
Biochemistry
47
5976-5985
2008
Homo sapiens
Manually annotated by BRENDA team
Barhoover, M.A.; Orban, T.; Beck, D.O.; Bukys, M.A.; Kalafatis, M.
Contribution of amino acid region 334-335 from factor Va heavy chain to the catalytic efficiency of prothrombinase
Biochemistry
47
6840-6850
2008
Homo sapiens
Manually annotated by BRENDA team
Hirbawi, J.; Bukys, M.A.; Barhoover, M.A.; Erdogan, E.; Kalafatis, M.
Role of the acidic hirudin-like COOH-terminal amino acid region of factor Va heavy chain in the enhanced function of prothrombinase
Biochemistry
47
7963-7974
2008
Homo sapiens
Manually annotated by BRENDA team
Sun, W.; Eriksson, A.S.; Schedin-Weiss, S.
Heparin enhances the inhibition of factor Xa by protein C inhibitor in the presence but not in the absence of Ca2+
Biochemistry
48
1094-1098
2009
Homo sapiens
Manually annotated by BRENDA team
Joo, S.S.; Won, T.J.; Kim, J.S.; Yoo, Y.M.; Tak, E.S.; Park, S.Y.; Park, H.Y.; Hwang, K.W.; Park, S.C.; Lee, D.I.
Inhibition of coagulation activation and inflammation by a novel Factor Xa inhibitor synthesized from the earthworm Eisenia andrei
Biol. Pharm. Bull.
32
253-258
2009
Homo sapiens
Manually annotated by BRENDA team
Qiao, J.X.; Cheney, D.L.; Alexander, R.S.; Smallwood, A.M.; King, S.R.; He, K.; Rendina, A.R.; Luettgen, J.M.; Knabb, R.M.; Wexler, R.R.; Lam, P.Y.
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa
Bioorg. Med. Chem. Lett.
18
4118-4123
2008
Homo sapiens
Manually annotated by BRENDA team
Nagata, T.; Nagamochi, M.; Kobayashi, S.; Komoriya, S.; Yoshino, T.; Kanno, H.
Stereoselective synthesis and biological evaluation of 3,4-diaminocyclohexanecarboxylic acid derivatives as factor Xa inhibitors
Bioorg. Med. Chem. Lett.
18
4587-4592
2008
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Qiao, J.X.; King, S.R.; He, K.; Wong, P.C.; Rendina, A.R.; Luettgen, J.M.; Xin, B.; Knabb, R.M.; Wexler, R.R.; Lam, P.Y.
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties
Bioorg. Med. Chem. Lett.
19
462-468
2009
Homo sapiens
Manually annotated by BRENDA team
Imaeda, Y.; Kawamoto, T.; Tobisu, M.; Konishi, N.; Hiroe, K.; Kawamura, M.; Tanaka, T.; Kubo, K.
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors
Bioorg. Med. Chem.
16
3125-3140
2008
Macaca fascicularis, Homo sapiens
Manually annotated by BRENDA team
Nagata, T.; Yoshino, T.; Haginoya, N.; Yoshikawa, K.; Nagamochi, M.; Kobayashi, S.; Komoriya, S.; Yokomizo, A.; Muto, R.; Yamaguchi, M.; Osanai, K.; Suzuki, M.; Kanno, H.
Discovery of 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: a novel, potent and orally active direct inhibitor of factor Xa
Bioorg. Med. Chem.
17
1193-1206
2009
Homo sapiens
Manually annotated by BRENDA team
Chattopadhyay, R.; Iacob, R.; Sen, S.; Majumder, R.; Tomer, K.B.; Lentz, B.R.
Functional and structural characterization of factor Xa dimer in solution
Biophys. J.
96
974-986
2009
Homo sapiens
Manually annotated by BRENDA team
Singh, N.; Briggs, J.M.
Molecular dynamics simulations of Factor Xa: insight into conformational transition of its binding subsites
Biopolymers
89
1104-1113
2008
Homo sapiens (P00742), Homo sapiens
Manually annotated by BRENDA team
Coggin, M.H.; Srapionian, R.M.; Brecher, A.S.; Galoyan, A.A.
Comparative effects of atrial polypeptide and neurohormone C on the interaction of factor Xa with antithrombin III
Blood Coagul. Fibrinolysis
19
645-651
2008
Homo sapiens
Manually annotated by BRENDA team
Majumder, R.; Quinn-Allen, M.A.; Kane, W.H.; Lentz, B.R.
A phosphatidylserine binding site in factor Va C1 domain regulates both assembly and activity of the prothrombinase complex
Blood
112
2795-2802
2008
Homo sapiens
Manually annotated by BRENDA team
Noguchi, T.; Tanaka, N.; Nishimata, T.; Goto, R.; Hayakawa, M.; Sugidachi, A.; Ogawa, T.; Asai, F.; Fujimoto, K.
Cinnamyl derivatives: synthesis and factor Xa (FXa) inhibitory activities
Chem. Pharm. Bull.
56
758-770
2008
Homo sapiens
Manually annotated by BRENDA team
Noguchi, T.; Tanaka, N.; Nishimata, T.; Goto, R.; Hayakawa, M.; Sugidachi, A.; Ogawa, T.; Niitsu, Y.; Asai, F.; Ishizuka, T.; Fujimoto, K.
Discovery of R-142086 as a factor Xa (FXa) inhibitor: syntheses and structure-activity relationships of cinnamyl derivatives
Chem. Pharm. Bull.
57
22-33
2009
Canis lupus familiaris, Homo sapiens
Manually annotated by BRENDA team
Bhattacharjee, G.; Ahamed, J.; Pawlinski, R.; Liu, C.; Mackman, N.; Ruf, W.; Edgington, T.S.
Factor Xa binding to annexin 2 mediates signal transduction via protease-activated receptor 1
Circ. Res.
102
457-464
2008
Homo sapiens
Manually annotated by BRENDA team
Abel, R.; Young, T.; Farid, R.; Berne, B.J.; Friesner, R.A.
Role of the active-site solvent in the thermodynamics of factor Xa ligand binding
J. Am. Chem. Soc.
130
2817-2831
2008
Homo sapiens
Manually annotated by BRENDA team
Hsu, H.J.; Tsai, K.C.; Sun, Y.K.; Chang, H.J.; Huang, Y.J.; Yu, H.M.; Lin, C.H.; Mao, S.S.; Yang, A.S.
Factor Xa active site substrate specificity with substrate phage display and computational molecular modeling
J. Biol. Chem.
283
12343-12353
2008
Bos taurus, Homo sapiens
Manually annotated by BRENDA team
Toso, R.; Zhu, H.; Camire, R.M.
The conformational switch from the factor X zymogen to protease state mediates exosite expression and prothrombinase assembly
J. Biol. Chem.
283
18627-18635
2008
Homo sapiens
Manually annotated by BRENDA team
Steen, M.; Tran, S.; Autin, L.; Villoutreix, B.O.; Tholander, A.L.; Dahlbaeck, B.
Mapping of the factor Xa binding site on factor Va by site-directed mutagenesis
J. Biol. Chem.
283
20805-20812
2008
Homo sapiens
Manually annotated by BRENDA team
Huang, X.; Swanson, R.; Broze, G.J.; Olson, S.T.
Kinetic characterization of the protein Z-dependent protease inhibitor reaction with blood coagulation factor Xa
J. Biol. Chem.
283
29770-29783
2008
Homo sapiens
Manually annotated by BRENDA team
Kamath, P.; Krishnaswamy, S.
Fate of membrane-bound reactants and products during the activation of human prothrombin by prothrombinase
J. Biol. Chem.
283
30164-30173
2008
Homo sapiens
Manually annotated by BRENDA team
Yegneswaran, S.; Hackeng, T.M.; Dawson, P.E.; Griffin, J.H.
The thrombin-sensitive region of protein S mediates phospholipid-dependent interaction with factor Xa
J. Biol. Chem.
283
33046-33052
2008
Homo sapiens
Manually annotated by BRENDA team
Izaguirre, G.; Rezaie, A.R.; Olson, S.T.
Engineering functional antithrombin exosites in alpha1-proteinase inhibitor that specifically promote the inhibition of factor Xa and factor IXa
J. Biol. Chem.
284
1550-1558
2009
Homo sapiens
Manually annotated by BRENDA team
Abboud, M.A.; Needle, S.J.; Burns-Kurtis, C.L.; Valocik, R.E.; Koster, P.F.; Amour, A.J.; Chan, C.; Brown, D.; Chaudry, L.; Zhou, P.; Patikis, A.; Patel, C.; Pateman, A.J.; Young, R.J.; Watson, N.S.; Toomey, J.R.
Antithrombotic potential of GW813893: a novel, orally active, active-site directed factor Xa inhibitor
J. Cardiovasc. Pharmacol.
52
66-71
2008
Oryctolagus cuniculus, Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Rohde, G.
Determination of rivaroxaban - a novel, oral, direct Factor Xa inhibitor - in human plasma by high-performance liquid chromatography-tandem mass spectrometry
J. Chromatogr. B
872
43-50
2008
Homo sapiens
Manually annotated by BRENDA team
Imaeda, Y.; Kuroita, T.; Sakamoto, H.; Kawamoto, T.; Tobisu, M.; Konishi, N.; Hiroe, K.; Kawamura, M.; Tanaka, T.; Kubo, K.
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors
J. Med. Chem.
51
3422-3436
2008
Macaca fascicularis, Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Furugohri, T.; Isobe, K.; Honda, Y.; Kamisato-Matsumoto, C.; Sugiyama, N.; Nagahara, T.; Morishima, Y.; Shibano, T.
DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles
J. Thromb. Haemost.
6
1542-1549
2008
Oryctolagus cuniculus, Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Mueller, J.; Freitag, D.; Mayer, G.; Poetzsch, B.
Anticoagulant characteristics of HD1-22, a bivalent aptamer that specifically inhibits thrombin and prothrombinase
J. Thromb. Haemost.
6
2105-2112
2008
Homo sapiens
Manually annotated by BRENDA team
Wong, P.C.; Crain, E.J.; Xin, B.; Wexler, R.R.; Lam, P.Y.; Pinto, D.J.; Luettgen, J.M.; Knabb, R.M.
Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies
J. Thromb. Haemost.
6
820-829
2008
Canis lupus familiaris, Oryctolagus cuniculus, Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Turpie, A.G.; Bauer, K.A.; Davidson, B.L.; Fisher, W.D.; Gent, M.; Huo, M.H.; Sinha, U.; Gretler, D.D.; Gretler, D.D.
A randomized evaluation of betrixaban, an oral factor Xa inhibitor, for prevention of thromboembolic events after total knee replacement (EXPERT)
Thromb. Haemost.
101
68-76
2009
Homo sapiens
Manually annotated by BRENDA team
Bukys, M.A.; Orban, T.; Kim, P.Y.; Nesheim, M.E.; Kalafatis, M.
The interaction of fragment 1 of prothrombin with the membrane surface is a prerequisite for optimum expression of factor Va cofactor activity within prothrombinase
Thromb. Haemost.
99
511-522
2008
Homo sapiens
Manually annotated by BRENDA team
Borensztajn, K.; Bijlsma, M.F.; Reitsma, P.H.; Peppelenbosch, M.P.; Spek, C.A.
Coagulation Factor Xa inhibits cancer cell migration via protease-activated receptor-1 activation
Thromb. Res.
124
219-225
2009
Homo sapiens
Manually annotated by BRENDA team
Rauch, U.
Rivaroxaban - once daily, oral, direct factor Xa inhibition compared with vitamin K antagonism for prevention of stroke and embolism trial in atrial fibrillation: rationale and design of the ROCKET AF study
Am. Heart J.
159
340-347.e1
2010
Homo sapiens
Manually annotated by BRENDA team
Batista, I.F.; Ramos, O.H.; Ventura, J.S.; Junqueira-de-Azevedo, I.L.; Ho, P.L.; Chudzinski-Tavassi, A.M.
A new factor Xa inhibitor from Amblyomma cajennense with a unique domain composition
Arch. Biochem. Biophys.
493
151-156
2010
Homo sapiens
Manually annotated by BRENDA team
Perzborn, E.; Roehrig, S.; Straub, A.; Kubitza, D.; Mueck, W.; Laux, V.
Rivaroxaban: a new oral factor Xa inhibitor
Arterioscler. Thromb. Vasc. Biol.
30
376-381
2010
Homo sapiens
Manually annotated by BRENDA team
Quan, M.L.; Pinto, D.J.; Rossi, K.A.; Sheriff, S.; Alexander, R.S.; Amparo, E.; Kish, K.; Knabb, R.M.; Luettgen, J.M.; Morin, P.; Smallwood, A.; Woerner, F.J.; Wexler, R.R.
Phenyltriazolinones as potent factor Xa inhibitors
Bioorg. Med. Chem. Lett.
20
1373-1377
2010
Homo sapiens
Manually annotated by BRENDA team
Zhao, X.; Sun, P.; Zhou, Y.; Liu, Y.; Zhang, H.; Mueck, W.; Kubitza, D.; Bauer, R.J.; Zhang, H.; Cui, Y.
Safety, pharmacokinetics and pharmacodynamics of single/multiple doses of the oral, direct factor Xa inhibitor rivaroxaban in healthy Chinese subjects
Br. J. Clin. Pharmacol.
68
77-88
2009
Homo sapiens
Manually annotated by BRENDA team
Zikria, J.C.; Ansell, J.
Oral anticoagulation with factor Xa and thrombin inhibitors: on the threshold of change
Curr. Opin. Hematol.
16
347-356
2009
Homo sapiens
Manually annotated by BRENDA team
Lang, D.; Freudenberger, C.; Weinz, C.
In vitro metabolism of rivaroxaban, an oral, direct factor Xa inhibitor, in liver microsomes and hepatocytes of rats, dogs, and humans
Drug Metab. Dispos.
37
1046-1055
2009
Canis lupus familiaris, Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Weinz, C.; Schwarz, T.; Kubitza, D.; Mueck, W.; Lang, D.
Metabolism and excretion of rivaroxaban, an oral, direct factor Xa inhibitor, in rats, dogs, and humans
Drug Metab. Dispos.
37
1056-1064
2009
Canis lupus familiaris, Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Wang, L.; Zhang, D.; Raghavan, N.; Yao, M.; Ma, L.; Frost, C.E.; Frost, C.A.; Maxwell, B.D.; Chen, S.Y.; He, K.; Goosen, T.C.; Humphreys, W.G.; Grossman, S.J.
In vitro assessment of metabolic drug-drug interaction potential of apixaban through cytochrome P450 phenotyping, inhibition, and induction studies
Drug Metab. Dispos.
38
448-458
2010
Homo sapiens
Manually annotated by BRENDA team
de Candia, M.; Lopopolo, G.; Altomare, C.
Novel factor Xa inhibitors: a patent review
Expert Opin. Ther. Pat.
19
1535-1580
2009
Homo sapiens
Manually annotated by BRENDA team
Gan, W.; Deng, L.; Yang, C.; He, Q.; Hu, J.; Yin, H.; Jin, X.; Lu, C.; Wu, Y.; Peng, L.
An anticoagulant peptide from the human hookworm, Ancylostoma duodenale that inhibits coagulation factors Xa and XIa
FEBS Lett.
583
1976-1980
2009
Homo sapiens
Manually annotated by BRENDA team
Gettins, P.G.; Olson, S.T.
Activation of antithrombin as a factor IXa and Xa inhibitor involves mitigation of repression rather than positive enhancement
FEBS Lett.
583
3397-3400
2009
Homo sapiens
Manually annotated by BRENDA team
Perzborn, E.
Factor Xa inhibitors - new anticoagulants for secondary haemostasis
Hamostaseologie
29
260-267
2009
Homo sapiens
Manually annotated by BRENDA team
Imberti, D.; DallAsta, C.; Pierfranceschi, M.G.
Oral factor Xa inhibitors for thromboprophylaxis in major orthopedic surgery: a review
Intern. Emerg. Med.
4
471-477
2009
Homo sapiens
Manually annotated by BRENDA team
Bradford, H.N.; Micucci, J.A.; Krishnaswamy, S.
Regulated cleavage of prothrombin by prothrombinase: repositioning a cleavage site reveals the unique kinetic behavior of the action of prothrombinase on its compound substrate
J. Biol. Chem.
285
328-338
2010
Homo sapiens
Manually annotated by BRENDA team
Buddai, S.K.; Layzer, J.M.; Lu, G.; Rusconi, C.P.; Sullenger, B.A.; Monroe, D.M.; Krishnaswamy, S.
An anticoagulant RNA aptamer that inhibits proteinase-cofactor interactions within prothrombinase
J. Biol. Chem.
285
5212-5223
2010
Homo sapiens
Manually annotated by BRENDA team
Gomes, A.M.; Kozlowski, E.O.; Pomin, V.H.; de Barros, C.M.; Zaganeli, J.L.; Pavao, M.S.
Unique extracellular matrix heparan sulfate from the bivalve Nodipecten nodosus (Linnaeus, 1758) safely inhibits arterial thrombosis after photochemically induced endothelial lesion
J. Biol. Chem.
285
7312-7323
2010
Homo sapiens
Manually annotated by BRENDA team
Steffel, J.; Luescher, T.F.
Novel anticoagulants in clinical development: focus on factor Xa and direct thrombin inhibitors
J. Cardiovasc. Med.
10
616-623
2009
Homo sapiens
Manually annotated by BRENDA team
de Candia, M.; Liantonio, F.; Carotti, A.; De Cristofaro, R.; Altomare, C.
Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: inhibitors of factor Xa and platelet aggregation
J. Med. Chem.
52
1018-1028
2009
Homo sapiens
Manually annotated by BRENDA team
Chandrasekaran, V.; Lee, C.J.; Lin, P.; Duke, R.E.; Pedersen, L.G.
A computational modeling and molecular dynamics study of the Michaelis complex of human protein Z-dependent protease inhibitor (ZPI) and factor Xa (FXa)
J. Mol. Model.
15
897-911
2009
Homo sapiens
Manually annotated by BRENDA team
Veyrat-Follet, C.; Vivier, N.; Trellu, M.; Dubruc, C.; Sanderink, G.J.
The pharmacokinetics of idraparinux, a long-acting indirect factor Xa inhibitor: population pharmacokinetic analysis from phase III clinical trials
J. Thromb. Haemost.
7
559-565
2009
Homo sapiens
Manually annotated by BRENDA team
Roser-Jones, C.; Becker, R.C.
Apixaban: an emerging oral factor Xa inhibitor
J. Thromb. Thrombolysis
29
141-146
2010
Homo sapiens
Manually annotated by BRENDA team
Chafa, O.; Tagzirt, M.; Tapon-Bretaudiere, J.; Reghis, A.; Fischer, A.M.; LeBonniec, B.F.
Characterization of a homozygous Gly11Val mutation in the Gla domain of coagulation factor X
Thromb. Res.
124
144-148
2009
Homo sapiens
Manually annotated by BRENDA team
Borensztajn, K.; Peppelenbosch, M.P.; Spek, C.A.
Coagulation Factor Xa inhibits cancer cell migration via LIMK1-mediated cofilin inactivation
Thromb. Res.
125
e323-e328
2010
Homo sapiens
Manually annotated by BRENDA team
Fadeeva, O.A.; Panteleev, M.A.; Karamzin, S.S.; Balandina, A.N.; Smirnov, I.V.; Ataullakhanov, F.I.
Thromboplastin immobilized on polystyrene surface exhibits kinetic characteristics close to those for the native protein and activates in vitro blood coagulation similarly to thromboplastin on fibroblasts
Biochemistry (Moscow)
75
734-743
2010
Homo sapiens
Manually annotated by BRENDA team
Hirbawi, J.; Vaughn, J.L.; Bukys, M.A.; Vos, H.L.; Kalafatis, M.
Contribution of amino acid region 659-663 of Factor Va heavy chain to the activity of factor Xa within prothrombinase
Biochemistry
49
8520-8534
2010
Homo sapiens
Manually annotated by BRENDA team
Young, R.J.; Adams, C.; Blows, M.; Brown, D.; Burns-Kurtis, C.L.; Chan, C.; Chaudry, L.; Convery, M.A.; Davies, D.E.; Exall, A.M.; Foster, G.; Harling, J.D.; Hortense, E.; Irvine, S.; Irving, W.R.; Jackson, S.; Kleanthous, S.; Pateman, A.J.; Patikis, A.N.; Roethka, T.J.; Senger, S.; Stelman, G.J.; Toomey, J.R.
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs
Bioorg. Med. Chem. Lett.
21
1582-1587
2011
Homo sapiens
Manually annotated by BRENDA team
Watson, N.S.; Adams, C.; Belton, D.; Brown, D.; Burns-Kurtis, C.L.; Chaudry, L.; Chan, C.; Convery, M.A.; Davies, D.E.; Exall, A.M.; Harling, J.D.; Irvine, S.; Irving, W.R.; Kleanthous, S.; McLay, I.M.; Pateman, A.J.; Patikis, A.N.; Roethke, T.J.; Senger, S.; Stelman, G.J.; Toomey, J.R.; West, R.I.; Whittaker, C.
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs
Bioorg. Med. Chem. Lett.
21
1588-1592
2011
Homo sapiens
Manually annotated by BRENDA team
Yoshikawa, K.; Yoshino, T.; Yokomizo, Y.; Uoto, K.; Naito, H.; Kawakami, K.; Mochizuki, A.; Nagata, T.; Suzuki, M.; Kanno, H.; Takemura, M.; Ohta, T.
Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors
Bioorg. Med. Chem. Lett.
21
2133-2140
2011
Homo sapiens
Manually annotated by BRENDA team
Lee, C.J.; Wu, S.; Eun, C.; Pedersen, L.G.
A revisit to the one form kinetic model of prothrombinase
Biophys. Chem.
149
28-33
2010
Homo sapiens
Manually annotated by BRENDA team
Kroh, H.K.; Panizzi, P.; Tchaikovski, S.; Baird, T.R.; Wei, N.; Krishnaswamy, S.; Tans, G.; Rosing, J.; Furie, B.; Furie, B.C.; Bock, P.E.
Active site-labeled prothrombin inhibits prothrombinase in vitro and thrombosis in vivo
J. Biol. Chem.
286
23345-23356
2011
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Pinto, D.; Smallheer, J.; Cheney, D.; Knabb, R.; Wexler, R.
Factor Xa inhibitors: Next-generation antithrombotic agents
J. Med. Chem.
53
6243-6274
2010
Homo sapiens
Manually annotated by BRENDA team
Al-Horani, R.A.; Liang, A.; Desai, U.R.
Designing nonsaccharide, allosteric activators of antithrombin for accelerated inhibition of factor Xa
J. Med. Chem.
54
6125-6138
2011
Homo sapiens
Manually annotated by BRENDA team
Kim, P.Y.; Nesheim, M.E.
Down regulation of prothrombinase by activated protein C during prothrombin activation
Thromb. Haemost.
104
61-70
2010
Homo sapiens
Manually annotated by BRENDA team
Koklic, T.; Majumder, R.; Lentz, B.R.
Ca2+ switches the effect of PS-containing membranes on Factor Xa from activating to inhibiting: implications for initiation of blood coagulation
Biochem. J.
462
591-601
2014
Homo sapiens
Manually annotated by BRENDA team
Griffiths, A.E.; Wintermute, J.; Newell-Caito, J.L.; Fay, P.J.
Residues flanking scissile bonds in Factor VIII modulate rates of cleavage and proteolytic activation catalyzed by Factor Xa
Biochemistry
52
8060-8068
2013
Homo sapiens
Manually annotated by BRENDA team
Ishihara, T.; Koga, Y.; Iwatsuki, Y.; Hirayama, F.
Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system
Bioorg. Med. Chem.
23
277-289
2015
Homo sapiens
Manually annotated by BRENDA team
Boehm, A.; Floesser, A.; Ermler, S.; Fender, A.C.; Lueth, A.; Kleuser, B.; Schroer, K.; Rauch, B.H.
Factor-Xa-induced mitogenesis and migration require sphingosine kinase activity and S1P formation in human vascular smooth muscle cells
Cardiovasc. Res.
99
505-513
2013
Homo sapiens
Manually annotated by BRENDA team
Bukowska, A.; Zacharias, I.; Weinert, S.; Skopp, K.; Hartmann, C.; Huth, C.; Goette, A.
Coagulation factor Xa induces an inflammatory signalling by activation of protease-activated receptors in human atrial tissue
Eur. J. Pharmacol.
718
114-123
2013
Homo sapiens
Manually annotated by BRENDA team
Hollborn, M.; Kohen, L.; Werschnik, C.; Tietz, L.; Wiedemann, P.; Bringmann, A.
Activated blood coagulation factor X (FXa) induces angiogenic growth factor expression in human retinal pigment epithelial cells
Invest. Ophthalmol. Vis. Sci.
53
5930-5939
2012
Homo sapiens
Manually annotated by BRENDA team
Nguyen, C.N.; Cruz, A.; Gilson, M.K.; Kurtzman, T.
Thermodynamics of Water in an Enzyme Active Site: Grid-based hydration analysis of coagulation factor Xa
J. Chem. Theory Comput.
10
2769-2780
2014
Homo sapiens
Manually annotated by BRENDA team
Al-Sallami, H.S.; Medlicott, N.J.
Investigation of an anti-activated factor X (anti-Xa) assay for the quantification of enoxaparin in human plasma
J. Pharm. Pharmacol.
67
209-214
2015
Homo sapiens
Manually annotated by BRENDA team
Henry, B.L.; Desai, U.R.
Sulfated low molecular weight lignins, allosteric inhibitors of coagulation proteinases via the heparin binding site, significantly alter the active site of thrombin and factor Xa compared to heparin
Thromb. Res.
134
1123-1129
2014
Homo sapiens
Manually annotated by BRENDA team
Koklic, T.; Chattopadhyay, R.; Majumder, R.; Lentz, B.R.
Factor Xa dimerization competes with prothrombinase complex formation on platelet-like membrane surfaces
Biochem. J.
467
37-46
2015
Bos taurus, Homo sapiens
Manually annotated by BRENDA team
Dhar, A.; Sadiq, F.; Anstee, Q.M.; Levene, A.P.; Goldin, R.D.; Thursz, M.R.
Thrombin and factor Xa link the coagulation system with liver fibrosis
BMC Gastroenterol.
18
60
2018
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Yang, J.; Su, G.; Ren, Y.; Chen, Y.
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors
Eur. J. Med. Chem.
101
41-51
2015
Homo sapiens
Manually annotated by BRENDA team
Ilin, I.; Lipets, E.; Sulimov, A.; Kutov, D.; Shikhaliev, K.; Potapov, A.; Krysin, M.; Zubkov, F.; Sapronova, L.; Ataullakhanov, F.; Sulimov, V.
New factor Xa inhibitors based on 1,2,3,4-tetrahydroquinoline developed by molecular modelling
J. Mol. Graph. Model.
89
215-224
2019
Homo sapiens (P00742)
Manually annotated by BRENDA team
Pryzdial, E.L.; Meixner, S.C.; Talbot, K.; Eltringham-Smith, L.J.; Baylis, J.R.; Lee, F.M.; Kastrup, C.J.; Sheffield, W.P.
Thrombolysis by chemically modified coagulation factor Xa
J. Thromb. Haemost.
14
1844-1854
2016
Homo sapiens
Manually annotated by BRENDA team
Verhoef, D.; Visscher, K.M.; Vosmeer, C.R.; Cheung, K.L.; Reitsma, P.H.; Geerke, D.P.; Bos, M.H.A.
Engineered factor Xa variants retain procoagulant activity independent of direct factor Xa inhibitors
Nat. Commun.
8
528
2017
Homo sapiens
Manually annotated by BRENDA team
Gera, O.; Bushi, D.; Ben Shimon, M.; Artan-Furman, A.; Harnof, S.; Maggio, N.; Dori, A.; Chapman, J.; Shavit-Stein, E.
Local regulation of thrombin activity by factor Xa in peripheral nerve Schwann cells
Neuroscience
371
445-454
2018
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Yegneswaran, S.; Banerjee, Y.; Fernandez, J.A.; Deguchi, H.; Griffin, J.H.
Lyso-sulfatide binds factor Xa and inhibits thrombin generation by the prothrombinase complex
PLoS ONE
10
e0135025
2015
Homo sapiens
Manually annotated by BRENDA team