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

for references in articles please use BRENDA:EC3.4.21.6

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IUBMB Comments

A blood coagulation factor formed from the proenzyme factor X by limited proteolysis. Factor X is a glycoprotein composed of a heavy chain and a light chain, which are generated from a precursor protein by the excision of the tripeptide RKR and held together by one or more disulfide bonds. The activated factor Xa converts prothrombin to thrombin in the presence of factor Va, Ca2+ and phospholipids. Scutelarin (EC 3.4.21.60) has similar specificity, but does not require factor Va.

The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin

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
LITERATURE
COMMENTARY hide
Reversibility
r=reversible
ir=irreversible
?=not specified
prothrombin + H2O
thrombin + ?
show the reaction diagram
S-2765 + H2O
Z-D-Arg-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
Substrates: -
Products: -
?
SARS CoV-2 spike protein + H2O
?
show the reaction diagram
Substrates: -
Products: -
?
Z-D-Arg-Gly-Arg-4-nitroanilide + H2O
Z-D-Arg-Gly-Arg + 4-nitroaniline
show the reaction diagram
2-aminobenzoyl-VQFRILGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + ILGDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
Substrates: -
Products: -
?
2-aminobenzoyl-VQFRSAGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SAGDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
Substrates: -
Products: -
?
2-aminobenzoyl-VQFRSLEDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SLEDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
Substrates: -
Products: -
?
2-aminobenzoyl-VQFRSLTDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SLTDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
Substrates: -
Products: -
?
2-aminobenzoyl-VQFRSVGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SCGDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
Substrates: -
Products: -
?
2-aminobenzoyl-VQFRTLGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + TLGDQ-N-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
Substrates: -
Products: -
?
Abz-VMIAALPRTMFIQ-ED-dinitrophenyl + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
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
-
Substrates: I-1560
Products: -
?
D-cyclohexyl-Gly-L-Pro-L-Arg-4-nitroanilide + H2O
D-cyclohexyl-Gly-L-Pro-L-Arg + 4-nitroaniline
show the reaction diagram
-
Substrates: -
Products: -
?
D-hexahydrotyrosol-L-Ala-L-Arg-4-nitroanilide + H2O
D-hexahydrotyrosol-L-Ala-L-Arg + 4-nitroaniline
show the reaction diagram
-
Substrates: -
Products: -
?
D-Phe-Pip-Arg-4-nitroanilide + H2O
D-Phe-Pip-Arg + 4-nitroaniline
show the reaction diagram
-
Substrates: synthetic substrate S2238
Products: -
?
D-phenylalanyl-L-pipecolyl-L-arginine-4-nitroanilide + H2O
D-phenylalanyl-L-pipecolyl-L-arginine + 4-nitroaniline
show the reaction diagram
-
Substrates: -
Products: -
?
factor VIII + H2O
?
show the reaction diagram
-
Substrates: 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
Products: -
?
factor VIII + H2O
activated factor VIII + B domain
show the reaction diagram
FPR-prothrombin + H2O
meizothrombin
show the reaction diagram
-
Substrates: 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
Products: -
?
fragment 1.2:prethrombin-2 + H2O
thrombin
show the reaction diagram
-
Substrates: intermediate of prothrombin processing to thrombin, cleavage site is Arg320
Products: -
?
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
-
Substrates: -
Products: -
?
meizothrombin + H2O
thrombin
show the reaction diagram
-
Substrates: intermediate of prothrombin processing to thrombin, cleavage site is Arg271
Products: -
?
methoxycarbonyl-D-cyclohexylglycyl-Gly-L-Arg-4-nitroanilide + H2O
methoxycarbonyl-D-cyclohexylglycyl-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
-
Substrates: -
Products: -
?
methoxycarbonyl-D-cyclohexylglycyl-glycyl-L-ariginine-4-nitroanilide + H2O
methoxycarbonyl-D-cyclohexylglycyl-glycyl-L-ariginine + 4-nitroaniline
show the reaction diagram
-
Substrates: i.e. Spectrozyme fXa, SpfXa
Products: -
?
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide + H2O
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
-
Substrates: -
Products: -
?
N-2-benzyloxycarbonyl-D-arginyl-L-arginine-4-nitroanilide + H2O
N-2-benzyloxycarbonyl-D-arginyl-L-arginine + 4-nitroaniline
show the reaction diagram
-
Substrates: -
Products: -
?
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
-
Substrates: -
Products: -
?
N-benzoyl-Arg-4-nitroanilide + H2O
N-benzoyl-Arg + 4-nitroaniline
show the reaction diagram
-
Substrates: -
Products: -
?
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
-
Substrates: -
Products: -
?
prethrombin 1 + H2O
thrombin + ?
show the reaction diagram
-
Substrates: activation of prethrombin 1 is slow with cleavages at residues R320 and R271 occuring with similar rates
Products: -
?
Prethrombin 2 + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
prethrombin-1 + H2O
thrombin + ?
show the reaction diagram
-
Substrates: -
Products: -
?
prethrombin-2 + H2O
thrombin-2
show the reaction diagram
-
Substrates: smallest zymogen form of thrombin containing only the factor Xa cleavage site 2
Products: -
?
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
-
Substrates: 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
Products: -
?
prothrombin + H2O
thrombin + thrombin propeptide
show the reaction diagram
-
Substrates: -
Products: -
?
prothrombin + H2O
trhombin + ?
show the reaction diagram
-
Substrates: -
Products: -
?
ProTS195A + H2O
?
show the reaction diagram
-
Substrates: the mutant protein also acts as competitive inhibitor of prothrombin activation
Products: -
?
recombinant prothrombin R155A/R284A/R271A mutant rMZ-II + H2O
meizothrombin
show the reaction diagram
-
Substrates: cleavage site is Arg320
Products: 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
-
Substrates: labeled with fluorescein at Cys525, cleavage site is Arg320
Products: 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
-
Substrates: cleavage site is Arg271
Products: reaction intermediate in the reaction with wild-type prothrombin
?
recombinant prothrombin S525C mutant + H2O
thrombin
show the reaction diagram
-
Substrates: labeled with fluorescein at Cys525, cleavage sites are Arg271 and Arg320
Products: -
?
S-2765 + H2O
Z-D-Arg-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
-
Substrates: -
Products: -
?
S2222 + H2O
?
show the reaction diagram
S2238 + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
S2765 + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
tosyl-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
tosyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
Substrates: -
Products: -
?
tosyl-glycyl-prolyl-D-arginine-4-nitroanilide + H2O
tosyl-glycyl-prolyl-D-arginine + 4-nitroaniline
show the reaction diagram
-
Substrates: i.e. Chz-TH, synthetic chromogenic substrate
Products: -
?
Z-D-Arg-Gly-Arg-4-nitroanilide + H2O
Z-D-Arg-Gly-Arg + 4-nitroaniline
show the reaction diagram
-
Substrates: -
Products: -
?
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
LITERATURE
COMMENTARY hide
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
prothrombin + H2O
thrombin + ?
show the reaction diagram
Substrates: -
Products: -
?
activated factor VIII + H2O
factor VIII
show the reaction diagram
-
Substrates: proteolytic inactivation
Products: -
?
factor VIII + H2O
?
show the reaction diagram
-
Substrates: 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
Products: -
?
factor VIII + H2O
activated factor VIII + B domain
show the reaction diagram
-
Substrates: proteolytic activation by removal of the B domain
Products: -
?
protease-activated receptor 1 + H2O
activated protease-activated receptor 1 + ?
show the reaction diagram
-
Substrates: PAR-1 activation mediates activation of phospholipase C in endothelial cells
Products: -
?
protease-activated receptor 2 + H2O
activated protease-activated receptor 2 + ?
show the reaction diagram
-
Substrates: PAR-2 activation mediates activation of phospholipase C in endothelial cells
Products: -
?
prothrombin + H2O
thrombin + ?
show the reaction diagram
prothrombin + H2O
thrombin + propeptide of thrombin
show the reaction diagram
-
Substrates: proteolytic activation
Products: -
?
prothrombin + H2O
trhombin + ?
show the reaction diagram
-
Substrates: -
Products: -
?
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
(Z)-4,4,6-trimethyl-2-oxo-1-(4-oxo-2-thioxothiazolidin-5-ylidene)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-8-yl 2-methoxybenzoate
inhibits both factors Xa and Xia
(Z)-5-(6',6'-dimethyl-2'-oxo-5',6'-dihydrospiro[cyclohexane-1,4'-pyrrolo[3,2,1-ij]quinolin]-1'(2'H)-ylidene)-2-thioxothiazolidin-4-one
selective for factor Xa
(Z)-5-(6-(4-chlorophenyl)-8-fluoro-4,4,6-trimethyl-2-oxo-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)-2-thioxothiazolidin-4-one
selective for factor Xa
(Z)-5-(6-(4-chlorophenyl)-8-iodo-4,4,6-trimethyl-2-oxo-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)-2-thioxothiazolidin-4-one
inhibits both factors Xa and Xia
(Z)-5-(8-bromo-4,4,6-trimethyl-2-oxo-6-phenyl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)-2-thioxothiazolidin-4-one
inhibits both factors Xa and Xia
(Z)-5-(8-fluoro-4,4,6-trimethyl-2-oxo-6-phenyl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)-2-thioxothiazolidin-4-one
selective for factor Xa
2,2,4,7-tetramethyl-6-[2-(4-methylphenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]-1,2,3,4-tetrahydroquinoline
89% activity at 0.03 mM
2,6-dichloro-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-4-(4H-1,2,4-triazol-4-yl)benzamide
inhibits both factor IXa and Xa
2-chloro-6-methoxy-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-4-(4H-1,2,4-triazol-4-yl)benzamide
inhibits both factor IXa and Xa
2-chloro-6-methyl-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-4-(4H-1,2,4-triazol-4-yl)benzamide
inhibits both factor IXa and Xa
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
apixaban
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
eribaxaban
-
fondaparinux
does not inhibit FXa-mediated cleavage of SARS CoV-2 spike protein
heparin
inhibition via complex formation with and modulation of the activity of thrombin
letaxaban
methyl (Z)-2-(2-(2-((Z)-8-bromo-4,4,6-trimethyl-2-oxo-6-phenyl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)hydrazineyl)-4-oxothiazol-5(4H)-ylidene)acetate
inhibits both factors Xa and Xia
methyl (Z)-2-(2-(2-((Z)-8-bromo-6-(4-chlorophenyl)-4,4,6-trimethyl-2-oxo-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)hydrazineyl)-4-oxothiazol-5(4H)-ylidene)acetate
inhibits both factors Xa and Xia
methyl (Z)-2-(2-(2-((Z)-8-chloro-4,4,6-trimethyl-2-oxo-6-phenyl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)hydrazineyl)-4-oxothiazol-5(4H)-ylidene)acetate
inhibits both factors Xa and Xia
methyl (Z)-2-(2-(2-((Z)-8-chloro-6-(4-chlorophenyl)-4,4,6-trimethyl-2-oxo-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)hydrazineyl)-4-oxothiazol-5(4H)-ylidene)acetate
inhibits both factors Xa and Xia
methyl (Z)-2-(4-oxo-2-(2-((Z)-4,4,6-trimethyl-2-oxo-6-phenyl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)hydrazineyl)thiazol-5(4H)-ylidene)acetate
inhibits both factors Xa and Xia
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
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VGY-0224950
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VGY-0224963
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VGY-0224989
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VGY-0225108
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Viperidae snake venom group IIA secreted phospholipases A2
i.e. SVPLA2, different isoforms, overview, FXa strong-binding SVPLA2s CBc, MtxII, CbII and CBa2 inactivate factor Xa by direct binding and by interacting with FXa by the non-catalytic phospholipid-independent mechanism, identification of the potential FXa binding site, overview
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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
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(1R)-N2-(4-chlorophenyl)-N1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-1,3-dihydro-2H-isoindole-1,2-dicarboxamide
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(1R,2R)-N-(4-chlorophenyl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-hydroxycyclopentane-1,2-dicarboxamide
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(1R,2S)-N-(4-chlorophenyl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4,4-bis(hydroxymethyl)cyclopentane-1,2-dicarboxamide
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(1R,2S)-N-(5-chloropyridin-2-yl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]cyclopropane-1,2-dicarboxamide
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(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
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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
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(2R)-2-[(3-carbamimidoylphenyl)amino]-2-[2-(beta-L-glucopyranosyloxy)phenyl]-N-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]ethanamide
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(2R)-2-[(3-carbamimidoylphenyl)amino]-2-[2-(beta-L-glucopyranosyloxy)phenyl]-N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]-2-oxoethyl]ethanamide
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(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
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(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
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(2R)-N1-(5-chloropyridin-2-yl)-4-hydroxy-N2-[5-(3-oxomorpholin-4-yl)pyridin-2-yl]pyrrolidine-1,2-dicarboxamide
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(2R)-N1-(5-chloropyridin-2-yl)-N2-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)pyrrolidine-1,2-dicarboxamide
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(2R)-N1-(5-chloropyridin-2-yl)-N2-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-methoxypyrrolidine-1,2-dicarboxamide
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(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-hydroxypyrrolidine-1,2-dicarboxamide
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(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-methoxypyrrolidine-1,2-dicarboxamide
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(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
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(2R,4R)-N1-(4-chlorophenyl)-4-methoxy-N2-(3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)pyrrolidine-1,2-dicarboxamide
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(2R,4R)-N1-(5-chloropyridin-2-yl)-4-methoxy-N2-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidine-1,2-dicarboxamide
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(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
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(2S)-1-[(2R)-2-[3-chloro-5-(difluoromethoxy)phenyl]-2-hydroxyacetyl]-N-[4-(N'-methoxycarbamimidoyl)benzyl]azetidine-2-carboxamide
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(2S)-N-(2-[[2-(aminomethyl)-5-chlorobenzyl]amino]-2-oxoethyl)-2-[(benzylsulfonyl)amino]-4-(1-oxidopyridin-2-yl)butanamide
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(2S)-N-(4-carbamimidoylbenzyl)-1-[(2R)-2-[3-chloro-5-(difluoromethoxy)phenyl]-2-hydroxyacetyl]azetidine-2-carboxamide
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(2S,4S)-N1-(4-chlorophenyl)-N2-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-methoxypyrrolidine-1,2-dicarboxamide
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(3-[(5-chloropyridin-2-yl)carbamoyl]-4-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]phenoxy)acetic acid
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(3-[[(3-carbamimidoylphenyl)(2-[[4-(1-ethanimidoylpiperidin-4-yl)phenyl]amino]-2-oxoethyl)amino]methyl]phenoxy)acetic acid
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(3R)-N2-(4-chlorophenyl)-N3-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-3,4-dihydroisoquinoline-2,3(1H)-dicarboxamide
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(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
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(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
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(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
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(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
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(4S)-4-[[(5-chlorothiophen-2-yl)carbonyl]amino]-N-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-L-prolinamide
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(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
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(4S,5S)-3-(3-carbamimidoylphenyl)-5-(methoxymethyl)-N-(2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1,2-oxazole-4-carboxamide
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(5R)-N1-(5-chloropyridin-2-yl)-N5-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1H-pyrazole-1,5-dicarboxamide
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(5R,6R)-N-(4-chlorophenyl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]spiro[2.4]heptane-5,6-dicarboxamide
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(5S)-N1-(4-chlorophenyl)-N5-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-5-methyl-4,5-dihydro-1H-pyrazole-1,5-dicarboxamide
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(6R)-N7-(4-chlorophenyl)-N6-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-5,8-dihydro-1,7-naphthyridine-6,7(6H)-dicarboxamide
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(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
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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
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
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(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
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]ethenesulfonamide
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(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
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[1-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
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(E)-2-(5-chlorothiophen-2-yl)-N-[[(3R)-1-[[1-(pyridin-4-yl)piperidin-4-yl]carbonyl]pyrrolidin-3-yl]methyl]ethenesulfonamide
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(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid
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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
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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
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(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-fluorophenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
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(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-methylphenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
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(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]phenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
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potent anticoagulation activities in vitro and ex vivo
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamides
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([(2R)-2-(7-carbamimidoylnaphthalen-2-yl)-5-[(1-ethanimidoylpiperidin-4-yl)methyl]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
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([(3'-carbamimidoylbiphenyl-3-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
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([(7-carbamimidoylnaphthalen-2-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
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([2'-(butylsulfonyl)-4-[2-([[2-hydroxy-5-(N'-hydroxycarbamimidoyl)phenyl]sulfonyl]amino)ethyl]biphenyl-3-yl]oxy)acetic acid
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([2-[(E)-2-(5-carbamimidoyl-2-hydroxyphenyl)ethenyl]-5-[(1-ethanimidoylpiperidin-4-yl)oxy]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
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1,1'-(benzene-1,4-diyldimethanediyl)bis(N,N-diethylpiperidine-3-carboxamide)
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1,2-dicaproyl-sn-glycero-3-phospho-L-serine
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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
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slow binding inhibitor
1-(1-[(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2-hydroxypropanoyl]piperidin-4-yl)tetrahydropyrimidin-2(1H)-one
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1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[2,3-b]pyridin-2-ylsulfonyl)-piperazin-2-one
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1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[3,2-b]pyridin-2-ylsulfonyl)-piperazin-2-one
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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
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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
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1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[2-[(dimethylamino)methyl]pyridin-3-yl]-2-fluorophenyl)-7-fluoro-1H-indazole-3-carboxamide
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1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[2-[(dimethylamino)methyl]pyridin-3-yl]phenyl)-7-fluoro-1H-indazole-3-carboxamide
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1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[[3-(dimethylamino)propyl](pyridin-4-yl)amino]phenyl)-7-fluoro-1H-indazole-3-carboxamide
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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
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1-(3-amino-1,2-benzoxazol-5-yl)-7-fluoro-6-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-1H-indazole-3-carboxamide
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1-(3-amino-1,2-benzoxazol-5-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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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
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1-(3-amino-1,2-benzoxazol-5-yl)-N-[1-[2-(pyrrolidin-1-ylmethyl)phenyl]piperidin-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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1-(3-amino-1H-isoindol-5-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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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
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1-(3-carbamimidoylphenyl)-3-methyl-N-(2'-sulfamoylbiphenyl-4-yl)-1H-pyrazole-5-carboxamide
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1-(3-carbamoylphenyl)-N-[3-chloro-4-(2-thioxopyrrolidin-1-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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1-(3-carbamoylphenyl)-N-[4-(5-ethyl-2-imino-1,3,4-thiadiazol-3(2H)-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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1-(3-carbamoylphenyl)-N-[4-[(2Z)-2-(cyanoimino)imidazolidin-1-yl]phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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1-(3-[6-[4-(2-chloropyridin-4-yl)piperazin-1-yl]-7-fluoro-3-methyl-1H-indazol-1-yl]phenyl)methanamine
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1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
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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
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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
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1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt
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1-(3-[amino(imino)methyl]phenyl)-N-[2'-(fluoro)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
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1-(3-[amino(imino)methyl]phenyl)-N-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
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1-(3-[amino(imino)methyl]phenyl)-N-[2'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
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1-(3-[amino(imino)methyl]phenyl)-N-[[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
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1-(4-aminophthalazin-6-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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1-(4-aminoquinazolin-6-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
0.00235
(Z)-4,4,6-trimethyl-2-oxo-1-(4-oxo-2-thioxothiazolidin-5-ylidene)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-8-yl 2-methoxybenzoate
pH 8.0, temperature not specified in the publication
0.0026
(Z)-5-(6',6'-dimethyl-2'-oxo-5',6'-dihydrospiro[cyclohexane-1,4'-pyrrolo[3,2,1-ij]quinolin]-1'(2'H)-ylidene)-2-thioxothiazolidin-4-one
pH 8.0, temperature not specified in the publication
0.00285
(Z)-5-(6-(4-chlorophenyl)-8-fluoro-4,4,6-trimethyl-2-oxo-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)-2-thioxothiazolidin-4-one
pH 8.0, temperature not specified in the publication
0.00287
(Z)-5-(6-(4-chlorophenyl)-8-iodo-4,4,6-trimethyl-2-oxo-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)-2-thioxothiazolidin-4-one
pH 8.0, temperature not specified in the publication
0.00228
(Z)-5-(8-bromo-4,4,6-trimethyl-2-oxo-6-phenyl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)-2-thioxothiazolidin-4-one
pH 8.0, temperature not specified in the publication
0.0037
(Z)-5-(8-fluoro-4,4,6-trimethyl-2-oxo-6-phenyl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)-2-thioxothiazolidin-4-one
pH 8.0, temperature not specified in the publication
0.000000007
3-chloro-N-(4-chloro-2-([(5-chloro-2-pyridinyl)amino]carbonyl)-6-methoxyphenyl)-4-([(4,5-dihydro-2-oxazolyl)methylamino]methyl)-2-thiophenecarboxamide
-
0.000015
BIBM1015
pH 8.0, 37°C
0.00004
BIBR1109
pH 8.0, 37°C
0.000057
BIBT0871
pH 8.0, 37°C
0.00387
methyl (Z)-2-(2-(2-((Z)-8-bromo-4,4,6-trimethyl-2-oxo-6-phenyl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)hydrazineyl)-4-oxothiazol-5(4H)-ylidene)acetate
pH 8, temperature not specified in the publication
0.00361
methyl (Z)-2-(2-(2-((Z)-8-bromo-6-(4-chlorophenyl)-4,4,6-trimethyl-2-oxo-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)hydrazineyl)-4-oxothiazol-5(4H)-ylidene)acetate
pH 8, temperature not specified in the publication
0.00721
methyl (Z)-2-(2-(2-((Z)-8-chloro-4,4,6-trimethyl-2-oxo-6-phenyl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)hydrazineyl)-4-oxothiazol-5(4H)-ylidene)acetate
pH 8, temperature not specified in the publication
0.00459
methyl (Z)-2-(2-(2-((Z)-8-chloro-6-(4-chlorophenyl)-4,4,6-trimethyl-2-oxo-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)hydrazineyl)-4-oxothiazol-5(4H)-ylidene)acetate
pH 8, temperature not specified in the publication
0.01146
methyl (Z)-2-(4-oxo-2-(2-((Z)-4,4,6-trimethyl-2-oxo-6-phenyl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)hydrazineyl)thiazol-5(4H)-ylidene)acetate
pH 8, temperature not specified in the publication
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
0.000105
2,6-dichloro-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-4-(4H-1,2,4-triazol-4-yl)benzamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000245
2-chloro-6-methoxy-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-4-(4H-1,2,4-triazol-4-yl)benzamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000195
2-chloro-6-methyl-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-4-(4H-1,2,4-triazol-4-yl)benzamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00000008
apixaban
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.031
CFM-184
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000000315
DPC-423
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00000032
eribaxaban
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000035
letaxaban
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000007
rivaroxaban
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
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