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Information on EC 3.4.21.6 - coagulation factor Xa
for references in articles please use BRENDA:EC3.4.21.6
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EC Tree 3 Hydrolases
3.4 Acting on peptide bonds (peptidases)
3.4.21 Serine endopeptidases
3.4.21.6 coagulation factor Xa
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 enzyme appears in viruses and cellular organisms
- 3.4.21.6
-
anticoagulant
- bleeding
- platelet
- heparin
- fibrinogen
- thrombosis
- pt
- venous
- antithrombin
- thromboembolism
- hemorrhage
- viii
-
antithrombotic
- fibrin
- rivaroxaban
- warfarin
-
hemostatic
- embolism
- stroke
-
intravascular
- apixaban
-
d-dimers
- coagulopathy
-
unfractionated
- thrombocytopenia
- fibrillation
- plasminogen
- atrial
-
fibrinolysis
-
transfusion
- hemophilia
- thrombus
-
lupus
-
chromogenic
- willebrand
-
hypercoagulable
- dabigatran
-
heparin-induced
- hematoma
- hirudin
-
haemostasis
-
antiphospholipid
-
antiplatelet
-
thrombin-antithrombin
- viper
-
amidolytic
-
k-dependent
- analysis
- rfviia
- pharmacology
- medicine
- thrombophilia
- synthesis
-
fibrinopeptide
- drug development
Reaction Schemes
showselective 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
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
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
factor X
factor Xa
fX
FXa
plasma thromboplastin
-
-
-
-
prothrombase
-
-
-
-
prothrombin activator
prothrombinase
Stuart factor
-
-
-
-
thrombokinase
-
-
-
-
thromboplastin
-
-
-
-
thromboplastin, plasma
-
-
-
-
Trocarin prothrombin activator
-
-
-
-
VAP
-
-
-
-
Virus activating protease
-
-
-
-
additional information
activated factor X
-
-
-
-
coagulation factor Xa
-
-
-
-
factor Xa
-
-
-
-
factor Xa
-
-
649797, 649955, 650111, 650170, 650179, 650193, 650336, 650463, 650846, 650914, 650933, 650938, 650939, 651189, 652253, 652262, 652278, 652349, 652447, 652728, 652731, 652755, 653979, 664120, 683178, 683235, 683252, 683629, 683823, 707025, 707279, 707307, 707693, 707903, 708249, 708321, 708322, 708509, 708634, 708815, 709156, 709211, 709434, 709578, 709726, 709729, 710601, 710607, 717234, 717253, 717336, 717381, 717829, 717968, 717974, 731276, 731308, 731484, 731588, 731756, 731958, 732376, 732937, 752707, 753093, 753480, 754515, 754844, 754909, 755098
FXa
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-
649955, 650164, 650846, 650933, 650939, 652262, 652731, 652755, 653979, 683235, 683241, 683243, 683250, 683295, 683443, 683629, 683823, 707279, 707903, 708451, 708505, 708634, 709434, 709578, 717335, 717339, 717381, 717829, 717968, 717974, 718415, 731276, 731308, 731484, 731588, 731756, 731958, 732229, 732937, 752707, 753093, 753480, 754844, 755098
prothrombinase
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-
-
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prothrombinase
-
-
enzyme complex consisting of factor Xa and factor Va, assembled in a calcium-dependent manner on the surface of phospholipid membranes
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additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
FXa belongs to the family of trypsin-like serine proteases
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
additional information
-
the enzyme belongs to the peptidase family S1, i.e. trypsin family
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
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.
-
-
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity, catalytic mechanism
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity, catalytic residues are Ser195 and His57, mechanism
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity, hydrolyzes two petide bonds in prothrombin having (Glu/Asp)-Gly-Arg-(Thr/Ile) as P3-P2-P1-P1' residues, glycine is not the best P2-residue, phenylalanine shows even higher activity at this position
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity, autolysis loop is formed by residues Arg143, Lys147, Arg150, and Arg154
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity, Ser89 is critical for enzyme activity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity, most selective P'2-position, less selective P'1-position, and non-selective P'3-position
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
scutelarin has similar specificity
-
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin
residues His57, Asp102, and Ser195 form the catalytic triad at the active site cleft between the two subdomains
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
ester hydrolysis
-
-
-
-
hydrolysis of peptide bond
-
-
endopeptidase
-
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CAS REGISTRY NUMBER
COMMENTARY
9002-05-5
-
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
2-aminobenzoyl-VQFRILGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + ILGDQ-N-(2,4-dinitrophenyl)ethylenediamine
-
Substrates: -
Products: -
Products: -
?
2-aminobenzoyl-VQFRSAGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SAGDQ-N-(2,4-dinitrophenyl)ethylenediamine
-
Substrates: -
Products: -
Products: -
?
2-aminobenzoyl-VQFRSLEDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SLEDQ-N-(2,4-dinitrophenyl)ethylenediamine
-
Substrates: -
Products: -
Products: -
?
2-aminobenzoyl-VQFRSLTDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SLTDQ-N-(2,4-dinitrophenyl)ethylenediamine
-
Substrates: -
Products: -
Products: -
?
2-aminobenzoyl-VQFRSVGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + SCGDQ-N-(2,4-dinitrophenyl)ethylenediamine
-
Substrates: -
Products: -
Products: -
?
2-aminobenzoyl-VQFRTLGDQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-VQFR + TLGDQ-N-(2,4-dinitrophenyl)ethylenediamine
-
Substrates: -
Products: -
Products: -
?
apomyoglobin + H2O
?
-
Substrates: maleylated sperm whale apomyoglobin. Hydrolysed at the Arg31-Leu32 bond
Products: -
Products: -
?
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
benzoyl-Ile-Glu(gamma-OR)-Gly-Arg-4-nitroanilide + H2O
benzoyl-Ile-Glu(gamma-OR)-Gly-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
benzoyl-Ile-Glu(piperidineamide)-Gly-Arg-p-nitroanilide + H2O
?
-
Substrates: -
Products: -
Products: -
?
benzoyl-Ile-Glu-(-H/OMe)-Gly-Arg-p-nitroanilide + H2O
?
-
Substrates: -
Products: -
Products: -
?
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
chymotrypsinogen + H2O
?
-
Substrates: maleylated and performate-oxidized bovine chymotrypsinogen A is hydrolyzed at the Arg230-Val231 bond and at the Arg15-Ile16 bond
Products: -
Products: -
?
D-cyclohexyl-Gly-L-Pro-L-Arg-4-nitroanilide + H2O
D-cyclohexyl-Gly-L-Pro-L-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
D-hexahydrotyrosol-L-Ala-L-Arg-4-nitroanilide + H2O
D-hexahydrotyrosol-L-Ala-L-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
D-hexahydrotyrosyl-L-alanyl-L-arginine-4-nitroanilide + H2O
D-hexahydrotyrosyl-L-alanyl-L-arginine + 4-nitroaniline
-
Substrates: synthetic chromogenic substrate
Products: -
Products: -
?
D-Phe-Pip-Arg-4-nitroanilide + H2O
D-Phe-Pip-Arg + 4-nitroaniline
-
Substrates: synthetic substrate S2238
Products: -
Products: -
?
D-phenylalanyl-L-pipecolyl-L-arginine-4-nitroanilide + H2O
D-phenylalanyl-L-pipecolyl-L-arginine + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
dimethylsulfonyl-D-norleucine-Gly-Arg-4-nitroanilide + H2O
dimethylsulfonyl-D-norleucine-Gly-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
factor VII + H2O
?
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Substrates: cleavage of two bonds, rapid cleavage of an Arg-Ile bond and slower cleavage of an Y-Gly bond
Products: -
Products: -
?
factor VIII + H2O
?
-
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: -
Products: -
?
FPR-prothrombin + H2O
meizothrombin
-
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: -
Products: -
?
FPR-prothrombin + H2O
meizothrombin + ?
-
Substrates: i.e. prothrombin specifically active site-labeled with D-Phe-Pro-Arg-CH2Cl and AF660-labeled, is cleaved by prothrombinase to intermediate meizothrombin, but the reaction is then directed to formation of a different FPR-prothrombin 2 intermediate product
Products: -
Products: -
?
fragment 1.2:prethrombin-2 + H2O
thrombin
-
Substrates: intermediate of prothrombin processing to thrombin, cleavage site is Arg320
Products: -
Products: -
?
meizothrombin + H2O
thrombin
-
Substrates: intermediate of prothrombin processing to thrombin, cleavage site is Arg271
Products: -
Products: -
?
methoxycarbonyl-D-cyclohexylglycyl-Gly-L-Arg-4-nitroanilide + H2O
methoxycarbonyl-D-cyclohexylglycyl-Gly-L-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
methoxycarbonyl-D-cyclohexylglycyl-glycyl-L-ariginine-4-nitroanilide + H2O
methoxycarbonyl-D-cyclohexylglycyl-glycyl-L-ariginine + 4-nitroaniline
-
Substrates: i.e. Spectrozyme fXa, SpfXa
Products: -
Products: -
?
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide + H2O
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
N-2-benzyloxycarbonyl-D-arginyl-L-arginine-4-nitroanilide + H2O
N-2-benzyloxycarbonyl-D-arginyl-L-arginine + 4-nitroaniline
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide + H2O
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine + 4-nitroaniline
N-alpha-benzyloxycarbonyl-Ile-Glu-Gly-Arg-7-amido-4-methylcoumarin + H2O
N-benzyloxycarbonyl-Ile-Glu-Gly-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
N-benzoyl-Arg-4-nitroanilide + H2O
N-benzoyl-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
N-benzoyl-Ile-Glu-Gly-Arg-4-nitroanilide + H2O
N-benzoyl-Ile-Glu-Gly-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
N6-CBZ-D-Lys-L-Pro-L-Arg-4-nitroanilide + H2O
N6-CBZ-D-Lys-L-Pro-L-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
Nalpha-benzyloxycarbonyl-L-Lys-4-nitrophenyl ester + H2O
Nalpha-benzyloxycarbonyl-L-Lys + 4-nitrophenol
-
Substrates: -
Products: -
Products: -
?
prethrombin 1 + H2O
thrombin + ?
-
Substrates: activation of prethrombin 1 is slow with cleavages at residues R320 and R271 occuring with similar rates
Products: -
Products: -
?
prethrombin-2 + H2O
thrombin-2
-
Substrates: smallest zymogen form of thrombin containing only the factor Xa cleavage site 2
Products: -
Products: -
?
prothrombin + H2O
thrombin + thrombin N-terminal fragment F12
-
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: -
Products: -
?
ProTS195A + H2O
?
-
Substrates: the mutant protein also acts as competitive inhibitor of prothrombin activation
Products: -
Products: -
?
recombinant prothrombin R155A/R284A/R271A mutant rMZ-II + H2O
meizothrombin
-
Substrates: cleavage site is Arg320
Products: reaction intermediate in the reaction with wild-type prothrombin
Products: reaction intermediate in the reaction with wild-type prothrombin
?
recombinant prothrombin R155A/R284A/R271A/S525C mutant rMZ-II-F + H2O
meizothrombin
-
Substrates: labeled with fluorescein at Cys525, cleavage site is Arg320
Products: reaction intermediate in the reaction with wild-type prothrombin
Products: reaction intermediate in the reaction with wild-type prothrombin
?
recombinant prothrombin R155A/R284A/R320A mutant rP2-II + H2O
fragment 1.2:prethrombin-2
-
Substrates: cleavage site is Arg271
Products: reaction intermediate in the reaction with wild-type prothrombin
Products: reaction intermediate in the reaction with wild-type prothrombin
?
recombinant prothrombin S525C mutant + H2O
thrombin
-
Substrates: labeled with fluorescein at Cys525, cleavage sites are Arg271 and Arg320
Products: -
Products: -
?
tosyl-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
tosyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
tosyl-glycyl-prolyl-D-arginine-4-nitroanilide + H2O
tosyl-glycyl-prolyl-D-arginine + 4-nitroaniline
-
Substrates: i.e. Chz-TH, synthetic chromogenic substrate
Products: -
Products: -
?
Trypsinogen + H2O
?
-
Substrates: maleylated performate-oxidized trypsinogen, slowly hydrolyzed at the Arg117-Val118 bond
Products: -
Products: -
?
activated factor VIII + H2O
factor VIII
-
Substrates: proteolytic inactivation
Products: -
Products: -
?
activated factor VIII + H2O
factor VIII
-
Substrates: inactivation by cleavage at Arg336 and Lys36 of domain A1, low activity
Products: -
Products: -
?
Arg-Gly-Arg-4-nitroanilide + H2O
Arg-Gly-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
Arg-Gly-Arg-4-nitroanilide + H2O
Arg-Gly-Arg + 4-nitroaniline
-
Substrates: synthetic substrate S2765
Products: -
Products: -
?
Arg-Gly-Arg-4-nitroanilide + H2O
Arg-Gly-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
Arg-Gly-Arg-4-nitroanilide + H2O
Arg-Gly-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
Arg-Gly-Arg-4-nitroanilide + H2O
Arg-Gly-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
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
-
Substrates: i.e. S2222, substrate is a 1:1 mixture of the 2 components
Products: -
Products: -
?
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
-
Substrates: mixed substrate
Products: -
Products: -
?
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
-
Substrates: mixed substrate S2222
Products: -
Products: -
?
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
-
Substrates: mixed substrate
Products: -
Products: -
?
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
-
Substrates: mixed substrate
Products: -
Products: -
?
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
-
Substrates: I-1560
Products: -
Products: -
?
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
-
Substrates: I-1560
Products: -
Products: -
?
factor VIII + H2O
activated factor VIII + B domain
-
Substrates: proteolytic activation by removal of the B domain
Products: -
Products: -
?
factor VIII + H2O
activated factor VIII + B domain
-
Substrates: activation by cleavage at Arg1689 and Arg1721 of domain A3
Products: -
Products: -
?
FS-2765 + H2O
?
-
Substrates: FS-2765 is a fluorescent peptidyl substrate, factor Xa
Products: -
Products: -
?
FS-2765 + H2O
?
-
Substrates: FS-2765 is a fluorescent peptidyl substrate, prothrombinase
Products: -
Products: -
?
L-Arg-Gly-Arg-4-nitroanilide + H2O
L-Arg-Gly-Arg + 4-nitroaniline
-
Substrates: chromogenic substrate
Products: -
Products: -
?
L-Arg-Gly-Arg-4-nitroanilide + H2O
L-Arg-Gly-Arg + 4-nitroaniline
-
Substrates: chromogenic synthetic substrate S2765
Products: -
Products: -
?
L-Arg-Gly-L-Arg-4-nitroanilide + H2O
L-Arg-Gly-L-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
L-Arg-Gly-L-Arg-4-nitroanilide + H2O
L-Arg-Gly-L-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
L-Arg-Gly-L-Arg-4-nitroanilide + H2O
L-Arg-Gly-L-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
L-Arg-Gly-L-Arg-4-nitroanilide + H2O
L-Arg-Gly-L-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
N-2-benzyloxycarbonyl-D-arginyl-L-arginine-4-nitroanilide + H2O
N-2-benzyloxycarbonyl-D-arginyl-L-arginine + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
N-2-benzyloxycarbonyl-D-arginyl-L-arginine-4-nitroanilide + H2O
N-2-benzyloxycarbonyl-D-arginyl-L-arginine + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide + H2O
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine + 4-nitroaniline
-
Substrates: i.e. S2765
Products: -
Products: -
?
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide + H2O
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine + 4-nitroaniline
-
Substrates: i.e. S-2765, synthetic chromogenic substrate
Products: -
Products: -
?
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide + H2O
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine + 4-nitroaniline
-
Substrates: i.e. S2765
Products: -
Products: -
?
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide + H2O
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine + 4-nitroaniline
-
Substrates: i.e. S-2765, synthetic fluorogenic substrate
Products: -
Products: -
?
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide + H2O
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine + 4-nitroaniline
-
Substrates: i.e. S-2765, synthetic chromogenic substrate
Products: -
Products: -
?
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide + H2O
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine + 4-nitroaniline
-
Substrates: i.e. Spectrozyme FXa, synthetic chromogenic substrate
Products: -
Products: -
?
protease-activated receptor 1 + H2O
activated protease-activated receptor 1 + ?
-
Substrates: PAR-1 activation mediates activation of phospholipase C in endothelial cells
Products: -
Products: -
?
protease-activated receptor 1 + H2O
activated protease-activated receptor 1 + ?
-
Substrates: -
Products: -
Products: -
?
protease-activated receptor 1 + H2O
activated protease-activated receptor 1 + ?
-
Substrates: PAR-1 activation mediates activation of phospholipase C in endothelial cells
Products: -
Products: -
?
protease-activated receptor 1 + H2O
activated protease-activated receptor 1 + ?
-
Substrates: -
Products: -
Products: -
?
protease-activated receptor 1 + H2O
activated protease-activated receptor 1 + ?
-
Substrates: -
Products: -
Products: -
?
protease-activated receptor 2 + H2O
activated protease-activated receptor 2 + ?
-
Substrates: PAR-2 activation mediates activation of phospholipase C in endothelial cells
Products: -
Products: -
?
protease-activated receptor 2 + H2O
activated protease-activated receptor 2 + ?
-
Substrates: -
Products: -
Products: -
?
protease-activated receptor 2 + H2O
activated protease-activated receptor 2 + ?
-
Substrates: PAR-2 activation mediates activation of phospholipase C in endothelial cells
Products: -
Products: -
?
protease-activated receptor 2 + H2O
activated protease-activated receptor 2 + ?
-
Substrates: -
Products: -
Products: -
?
protease-activated receptor 2 + H2O
activated protease-activated receptor 2 + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
?
-
Substrates: major role is the activation of prothrombin
Products: -
Products: -
?
prothrombin + H2O
?
-
Substrates: factor Xaalpha is predominantly responsible for thrombin generation. Slow conversion to factor Xabeta coordinates coagulation and the initiation of fibrinolysis at sites of thrombinase assembly
Products: -
Products: -
?
prothrombin + H2O
?
Substrates: gamma-carboxylation of prothrombin is required for cleavage
Products: -
Products: -
?
prothrombin + H2O
?
Substrates: gamma-carboxylation of prothrombin is required for cleavage
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: three major fragments are produced, one of these fragments is the 39000 Da alpha-thrombin
Products: three major fragments are produced, one of these fragments is the 39000 Da alpha-thrombin
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: thrombin and two activation fragments
Products: thrombin and two activation fragments
?
prothrombin + H2O
thrombin + ?
-
Substrates: cleaves first an Arg-Thr bond and then an Arg-Ile bond to form the two-chain enzyme
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: crucial step in blood coagulation process
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: a single type of exosite binding interaction drives affinity and binding specificity through the stepwise reactions necessary for the two cleavage reactions of prothrombin activation and product release
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: procoagulant activity
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: coupled assay method with measurement of thrombin activity against sythetic chromogenic substrate S2238
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: hydrolysis of Arg322-Ile323 produces meizothrombin as an intermediate, while hydrolysis of Arg273-Thr274 produces prethrombin 2-fragment 1.2
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: limited preference for the cleavage site, hydrolyzes two petide bonds in prothrombin having (Glu/Asp)-Gly-Arg-(Thr/Ile) as P3-P2-P1-P1' residues, glycine is not the best P2-residue, phenylalanine shows even higher activity at this position
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: the cleavage site 2 is preferred to cleavage site 1
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: wild-type II, cleavage sites are Arg271 and Arg320
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: acts within the prothrombinase complex
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme is involved in thrombotic complications of artherosclerosis and following diseases, overview
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme is responsible for the proteolysis of prothrombin to catalytically active thrombin
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme plays a key role in thrombosis and hemostasis by cleaving prothrombin to thrombin and thereby regulating the generation of this vital procoagulant enzyme, thrombus formation causes diseases like arterial restenosis, induces mitogenic signaling via binding to effector cell protease receptor-1, i.e. EPR-1, on cell surfaces, and via release of platelet-derived growth factor PDGF in aortic smooth-muscle cells
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: initial step in thrombus formation
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: key enzyme in coagulation cascade responsible for the generation of thrombin by limited proteolysis of its zymogen prothrombin
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: procoagulant activity
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: prothrombin activation requires proteolysis of 2 bonds and thus involves 2 possible activation pathways, parallel-sequential activation model
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: binding of substrate in two conformations to human prothrombinase drives consecutive cleavage at two sites in prothrombin
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: cleavage at Arg320 followed by cleavage at Arg271
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: the interaction of factor Xa with factor Va on membranes to form prothrombinase profoundly increases the rate of the proteolytic conversion of prothrombin to thrombin
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: cleavage at Arg320 followed by cleavage at Arg271. Enzyme activity and active site docking with wild-type prothrombin and cleavage site variants, in which the cleavage sequence Asp-Gly-Arg is replaced e.g. by Arg-Gly-Arg or Arg-Arg, overview. Product identification, overview
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: activation, interaction of factor Xa with factor Va promotes prothrombin activation
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: activation, a first cleavage of prothrombin by prothrombinase at Arg320 produces the active intermediate meizothrombin, while the second cleavage at Arg271 produces thrombin
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: prothrombinase cleaves prothrombin at two cleavage positions Arg-271-Thr-272 and Arg-320-Ile-321
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: the recombinantly expressed enzyme is inactive in Sf9 cells, activity can be restored by addition of phosphatidyl-L-serine, and further enhanced by addition of factor Va and Ca2+
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme plays a key role in thrombosis and hemostasis by cleaving prothrombin to thrombin and thereby regulating the generation of this vital procoagulant enzyme, thrombus formation causes diseases like arterial restenosis, induces mitogenic signaling via binding to effector cell protease receptor-1, i.e. EPR-1, on cell surfaces
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme plays a key role in thrombosis and hemostasis by cleaving prothrombin to thrombin and thereby regulating the generation of this vital procoagulant enzyme, thrombus formation causes diseases like arterial restenosis, induces mitogenic signaling via binding to effector cell protease receptor-1, i.e. EPR-1, on cell surfaces, and via release of platelet-derived growth factor PDGF in aortic smooth-muscle cells
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: initial step in thrombus formation
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme plays a key role in thrombosis and hemostasis by cleaving prothrombin to thrombin and thereby regulating the generation of this vital procoagulant enzyme, thrombus formation causes diseases like arterial restenosis, induces mitogenic signaling via binding to effector cell protease receptor-1, i.e. EPR-1, on cell surfaces
Products: -
Products: -
?
prothrombin + H2O
thrombin + propeptide of thrombin
-
Substrates: proteolytic activation
Products: -
Products: -
?
prothrombin + H2O
thrombin + propeptide of thrombin
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + propeptide of thrombin
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + propeptide of thrombin
-
Substrates: factor V is a cofactor for the prothrombin activation by factor Xa
Products: -
Products: -
?
prothrombin + H2O
trhombin + ?
-
Substrates: -
Products: -
Products: -
?
S-2765 + H2O
Z-D-Arg-Gly-L-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
S-2765 + H2O
Z-D-Arg-Gly-L-Arg + 4-nitroaniline
Substrates: -
Products: -
Products: -
?
S2222 + H2O
?
-
Substrates: chromogenic synthetic peptide substrate
Products: -
Products: -
?
S2222 + H2O
?
-
Substrates: chromogenic synthetic peptide substrate
Products: -
Products: -
?
S2238 + H2O
?
-
Substrates: chromogenic synthetic peptide substrate
Products: -
Products: -
?
Z-D-Arg-Gly-Arg-4-nitroanilide + H2O
Z-D-Arg-Gly-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
Z-D-Arg-Gly-Arg-4-nitroanilide + H2O
Z-D-Arg-Gly-Arg + 4-nitroaniline
Substrates: i.e S2765
Products: -
Products: -
?
Z-D-Arg-Gly-Arg-4-nitroanilide + H2O
Z-D-Arg-Gly-Arg + 4-nitroaniline
Substrates: i.e. S2765
Products: -
Products: -
?
Z-D-Arg-Gly-L-Arg-4-nitroanilide + H2O
Z-D-Arg-Gly-L-Arg + 4-nitroaniline
-
Substrates: i.e. S-2765
Products: -
Products: -
?
Z-D-Arg-Gly-L-Arg-4-nitroanilide + H2O
Z-D-Arg-Gly-L-Arg + 4-nitroaniline
-
Substrates: -
Products: -
Products: -
?
additional information
?
-
-
Substrates: substrate specificity study for the positions P'1, P'2, and P'3 with 57 substrates possesssing Gly-Pro-Arg at positions P1-P3, the P'2 position shows the highest selectivity, while the P'3 position is not selective at all, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: factor Xa and thrombin evoke additive calcium and proinflammatory responses in endothelial cells subjected to coagulation, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: selection of cleavage substrates by substrate phage display and construction of computational molecular models for enzyme-substrate complexes. Binding modes of substrates vary according to the substrate peptide sequence with at least three different substrate-enzyme recognition modes. Three binding modes corresponding to the aryl-binding site accommodating the P4, P3, and P2 side chains, respectively, are likely to account for the specificity of factor Xa toward substrate peptide sequences
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme is responsible for clot-associated procoagulant activity
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme possesses a macromolecular substrate binding site, exosite
Products: -
Products: -
?
additional information
?
-
-
Substrates: substrate specificity and catalytic efficiency, catalytic groove structure, activity with peptide substrate is virtually the same in presence or absence of complexed factor Va, indicating that the factor Va does not allosterically control the catalytic groove, catalytic efficacy of prothrombinase complex originates from exosite interactions with factor Va and/or prothrombin
Products: -
Products: -
?
additional information
?
-
-
Substrates: substrate specificity, no activity with a substrate containing the active site sequence of the Bauhinia variegata trypsin inhibitor BvTI
Products: -
Products: -
?
additional information
?
-
Substrates: enzyme is involved in the coagulation cascade
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme is involved in the coagulation cascade
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme link between cancer and thrombosis appears to be a bidirectional relationship, physiological role of factor Xa, involvement in inflammation and diseases, physiological interactions, regulation, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: properties of and indications for different enzyme inhibitors, overview, the enzyme is responsible for clot-associated procoagulant activity, enzyme inhibition lead to reduced platelet deposition and aggregation at thrombic sites
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme is regulated by sequential occupancy of a pair of linked lipid binding sites, each of which have different minimum ligand structural requirements to induce structural changes
Products: -
Products: -
?
additional information
?
-
-
Substrates: factor Xa can induce mesangial cell proliferation through the activation of extracellular regulated kinase via protease-activated receptor 2 in mesangial cells. Protease-activated receptor 2 may play a crucial role in the cell proliferation induced by factor Xa
Products: -
Products: -
?
additional information
?
-
-
Substrates: factor Xa inhibits the inhibition of the procoagulant function of activated factor V by activated protein C through proteolytic cleavages at Arg506, with a half-maximum inhibition of 2 nM, while the cleavage at Arg306, and Arg679 is not protected, protein S counteracted the inhibition by FXa of the Arg506 cleavage, whereas protein S and FXa yielded additive stimulatory effect of the cleavage at Arg306, activity with recombinant FVa Q306/Q679 and FVa Q506/Q679 variants, interaction analysis with 1.5-dansyl-Glu-Gly-Arg-inhibited factor Xa, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: PD0313052 and argatroban, inhibitors of blood coagulation factors Xa and IIa, synergize to reduce thrombus weight and thrombin generation in vivo and in vitro
Products: -
Products: -
?
additional information
?
-
-
Substrates: blood clot elongation is regulated by factor Xa formation by intrinsic tenase, i.e. factor VIIa and tissue factor complex, coagulation factors from plasma bind to tissue factor TF-expressing cells, become activated, dissociate, and diffuse into plasma to form enzymatic complexes on the membranes of activated platelets, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: factor Xa and thrombin evoke additive calcium and proinflammatory responses in endothelial cells subjected to coagulation, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: coagulation factor Xa is a serine protease that plays a crucial role during blood coagulation by converting prothrombin into thrombin, it drives tumor cells of epithelial, but not endothelial, origin into apoptosis through BH3-only protein Bim up-regulation, and enhances fibroblast survival, overview, signaling through protease-activated receptor 1, PAR-1, with rapid and transient desensitization of PAR-1 signaling, signaling pathway, overview
Products: -
Products: -
?
additional information
?
-
Substrates: different anticoagulant mechanisms, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: different anticoagulant mechanisms, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: structural basis for Na+ specificity of enzymes involved in the coagulation cascade, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: annexin 2 acts as a receptor for factor Xa on the cell surface. It facilitates factor Xa activation of receptor PAR-1 but does not enhance coagulant function of factor Xa. Overexpression of tissue factor abolishes annexin 2 dependence on factor Xa signaling and diminishes binding to cell surface annexin 2, whereas selectively abolishing tissue factor promotes the annexin 2/factor Xa interaction
Products: -
Products: -
?
additional information
?
-
-
Substrates: treatment with factor Xa markedly diminishes the migration of different cancer cell lines from breast, lung and colon. Factor Xa mediates inhibition of cancer cell migration specifically and dose dependently. It acts via protease-activated receptor-1 dependent signaling. The G protein alpha 1 pathway is not involved in signaling
Products: -
Products: -
?
additional information
?
-
-
Substrates: construction of computational molecular models for enzyme-substrate complexes. Binding modes of substrates vary according to the substrate peptide sequence with at least three different substrate-enzyme recognition modes. Three binding modes corresponding to the aryl-binding site accommodating the P4, P3, and P2 side chains, respectively, are likely to account for the specificity of factor Xa toward substrate peptide sequences
Products: -
Products: -
?
additional information
?
-
-
Substrates: coagulation factor Xa inhibits cancer cell migration via LIMK1-mediated cofilin inactivation through induction of myosin light chain phosphorylation and LIMK1 activation, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: effects of factor X on the respiratory function and asthmatic response in mice, factor X transcript levels and factor Xa activity are increased in lungs of asthmatic mice leading to a significant decrease in the thickness of the mucosal layer and in lung collagen deposition, factor Xa modulates airway remodeling, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme elicits a signaling response in C2C12 and NIH-3T3 fibroblast cells. ERK1/2 phosphorylation by factor Xa is dependent on protease-activated receptor PAR-2 cleavage and leads to fibroblast proliferation, migration, and differentiation into myofibroblasts
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme link between cancer and thrombosis appears to be a bidirectional relationship, physiological role of factor Xa, involvement in inflammation and diseases, physiological interactions, regulation, overview
Products: -
Products: -
?
additional information
?
-
Substrates: recombinant oscutarin cannot efficiently generate thrombin without additional protein cofactors
Products: -
Products: -
?
additional information
?
-
-
Substrates: recombinant oscutarin cannot efficiently generate thrombin without additional protein cofactors
Products: -
Products: -
?
additional information
?
-
Q56VR3; Q7SZN0
Substrates: the chromogenic assay does not distinguish between thrombin and meizothrombin
Products: -
Products: -
-
additional information
?
-
-
Substrates: enzyme link between cancer and thrombosis appears to be a bidirectional relationship, physiological role of factor Xa, involvement in inflammation and diseases, physiological interactions, regulation, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: roles of coagulation pathway and factor Xa in rat mesangioproliferative glomerulonephritis, initiation of the extrinsic coagulation pathway by activating coagulation factor X to factor Xa, factor Xa promote the proliferation of mesangial cells in culture, enzyme inhibitor DX-9065a treatment significantly ameliorated proteinuria in vivo in rats with a a significant reduction in the size of glomeruli, the total number of glomerular cells, and crescent formation, as well as abolishing phosphorylation of p44/42 MAP kinase on day 8, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme link between cancer and thrombosis appears to be a bidirectional relationship, physiological role of factor Xa, involvement in inflammation and diseases, physiological interactions, regulation, overview
Products: -
Products: -
?
additional information
?
-
Substrates: recombinant trocarin cannot efficiently generate thrombin without additional protein cofactors
Products: -
Products: -
?
additional information
?
-
-
Substrates: recombinant trocarin cannot efficiently generate thrombin without additional protein cofactors
Products: -
Products: -
?
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
activated factor VIII + H2O
factor VIII
-
Substrates: proteolytic inactivation
Products: -
Products: -
?
factor VIII + H2O
?
-
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: -
Products: -
?
factor VIII + H2O
activated factor VIII + B domain
-
Substrates: proteolytic activation by removal of the B domain
Products: -
Products: -
?
protease-activated receptor 1 + H2O
activated protease-activated receptor 1 + ?
-
Substrates: PAR-1 activation mediates activation of phospholipase C in endothelial cells
Products: -
Products: -
?
protease-activated receptor 1 + H2O
activated protease-activated receptor 1 + ?
-
Substrates: PAR-1 activation mediates activation of phospholipase C in endothelial cells
Products: -
Products: -
?
protease-activated receptor 1 + H2O
activated protease-activated receptor 1 + ?
-
Substrates: -
Products: -
Products: -
?
protease-activated receptor 2 + H2O
activated protease-activated receptor 2 + ?
-
Substrates: PAR-2 activation mediates activation of phospholipase C in endothelial cells
Products: -
Products: -
?
protease-activated receptor 2 + H2O
activated protease-activated receptor 2 + ?
-
Substrates: PAR-2 activation mediates activation of phospholipase C in endothelial cells
Products: -
Products: -
?
protease-activated receptor 2 + H2O
activated protease-activated receptor 2 + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
?
-
Substrates: major role is the activation of prothrombin
Products: -
Products: -
?
prothrombin + H2O
?
-
Substrates: factor Xaalpha is predominantly responsible for thrombin generation. Slow conversion to factor Xabeta coordinates coagulation and the initiation of fibrinolysis at sites of thrombinase assembly
Products: -
Products: -
?
prothrombin + H2O
?
Substrates: gamma-carboxylation of prothrombin is required for cleavage
Products: -
Products: -
?
prothrombin + H2O
?
Substrates: gamma-carboxylation of prothrombin is required for cleavage
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: crucial step in blood coagulation process
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: procoagulant activity
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: acts within the prothrombinase complex
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme is involved in thrombotic complications of artherosclerosis and following diseases, overview
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme is responsible for the proteolysis of prothrombin to catalytically active thrombin
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme plays a key role in thrombosis and hemostasis by cleaving prothrombin to thrombin and thereby regulating the generation of this vital procoagulant enzyme, thrombus formation causes diseases like arterial restenosis, induces mitogenic signaling via binding to effector cell protease receptor-1, i.e. EPR-1, on cell surfaces, and via release of platelet-derived growth factor PDGF in aortic smooth-muscle cells
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: initial step in thrombus formation
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: key enzyme in coagulation cascade responsible for the generation of thrombin by limited proteolysis of its zymogen prothrombin
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: procoagulant activity
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: prothrombin activation requires proteolysis of 2 bonds and thus involves 2 possible activation pathways, parallel-sequential activation model
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: cleavage at Arg320 followed by cleavage at Arg271
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: the interaction of factor Xa with factor Va on membranes to form prothrombinase profoundly increases the rate of the proteolytic conversion of prothrombin to thrombin
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: activation, interaction of factor Xa with factor Va promotes prothrombin activation
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: activation, a first cleavage of prothrombin by prothrombinase at Arg320 produces the active intermediate meizothrombin, while the second cleavage at Arg271 produces thrombin
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: prothrombinase cleaves prothrombin at two cleavage positions Arg-271-Thr-272 and Arg-320-Ile-321
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme plays a key role in thrombosis and hemostasis by cleaving prothrombin to thrombin and thereby regulating the generation of this vital procoagulant enzyme, thrombus formation causes diseases like arterial restenosis, induces mitogenic signaling via binding to effector cell protease receptor-1, i.e. EPR-1, on cell surfaces
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme plays a key role in thrombosis and hemostasis by cleaving prothrombin to thrombin and thereby regulating the generation of this vital procoagulant enzyme, thrombus formation causes diseases like arterial restenosis, induces mitogenic signaling via binding to effector cell protease receptor-1, i.e. EPR-1, on cell surfaces, and via release of platelet-derived growth factor PDGF in aortic smooth-muscle cells
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: initial step in thrombus formation
Products: -
Products: -
?
prothrombin + H2O
thrombin + ?
-
Substrates: enzyme plays a key role in thrombosis and hemostasis by cleaving prothrombin to thrombin and thereby regulating the generation of this vital procoagulant enzyme, thrombus formation causes diseases like arterial restenosis, induces mitogenic signaling via binding to effector cell protease receptor-1, i.e. EPR-1, on cell surfaces
Products: -
Products: -
?
prothrombin + H2O
thrombin + propeptide of thrombin
-
Substrates: proteolytic activation
Products: -
Products: -
?
prothrombin + H2O
thrombin + propeptide of thrombin
-
Substrates: -
Products: -
Products: -
?
prothrombin + H2O
trhombin + ?
-
Substrates: -
Products: -
Products: -
?
additional information
?
-
-
Substrates: factor Xa and thrombin evoke additive calcium and proinflammatory responses in endothelial cells subjected to coagulation, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme is responsible for clot-associated procoagulant activity
Products: -
Products: -
?
additional information
?
-
Substrates: enzyme is involved in the coagulation cascade
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme is involved in the coagulation cascade
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme link between cancer and thrombosis appears to be a bidirectional relationship, physiological role of factor Xa, involvement in inflammation and diseases, physiological interactions, regulation, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: properties of and indications for different enzyme inhibitors, overview, the enzyme is responsible for clot-associated procoagulant activity, enzyme inhibition lead to reduced platelet deposition and aggregation at thrombic sites
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme is regulated by sequential occupancy of a pair of linked lipid binding sites, each of which have different minimum ligand structural requirements to induce structural changes
Products: -
Products: -
?
additional information
?
-
-
Substrates: factor Xa can induce mesangial cell proliferation through the activation of extracellular regulated kinase via protease-activated receptor 2 in mesangial cells. Protease-activated receptor 2 may play a crucial role in the cell proliferation induced by factor Xa
Products: -
Products: -
?
additional information
?
-
-
Substrates: factor Xa inhibits the inhibition of the procoagulant function of activated factor V by activated protein C through proteolytic cleavages at Arg506, with a half-maximum inhibition of 2 nM, while the cleavage at Arg306, and Arg679 is not protected, protein S counteracted the inhibition by FXa of the Arg506 cleavage, whereas protein S and FXa yielded additive stimulatory effect of the cleavage at Arg306, activity with recombinant FVa Q306/Q679 and FVa Q506/Q679 variants, interaction analysis with 1.5-dansyl-Glu-Gly-Arg-inhibited factor Xa, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: PD0313052 and argatroban, inhibitors of blood coagulation factors Xa and IIa, synergize to reduce thrombus weight and thrombin generation in vivo and in vitro
Products: -
Products: -
?
additional information
?
-
-
Substrates: blood clot elongation is regulated by factor Xa formation by intrinsic tenase, i.e. factor VIIa and tissue factor complex, coagulation factors from plasma bind to tissue factor TF-expressing cells, become activated, dissociate, and diffuse into plasma to form enzymatic complexes on the membranes of activated platelets, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: factor Xa and thrombin evoke additive calcium and proinflammatory responses in endothelial cells subjected to coagulation, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: coagulation factor Xa is a serine protease that plays a crucial role during blood coagulation by converting prothrombin into thrombin, it drives tumor cells of epithelial, but not endothelial, origin into apoptosis through BH3-only protein Bim up-regulation, and enhances fibroblast survival, overview, signaling through protease-activated receptor 1, PAR-1, with rapid and transient desensitization of PAR-1 signaling, signaling pathway, overview
Products: -
Products: -
?
additional information
?
-
Substrates: different anticoagulant mechanisms, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: different anticoagulant mechanisms, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: annexin 2 acts as a receptor for factor Xa on the cell surface. It facilitates factor Xa activation of receptor PAR-1 but does not enhance coagulant function of factor Xa. Overexpression of tissue factor abolishes annexin 2 dependence on factor Xa signaling and diminishes binding to cell surface annexin 2, whereas selectively abolishing tissue factor promotes the annexin 2/factor Xa interaction
Products: -
Products: -
?
additional information
?
-
-
Substrates: treatment with factor Xa markedly diminishes the migration of different cancer cell lines from breast, lung and colon. Factor Xa mediates inhibition of cancer cell migration specifically and dose dependently. It acts via protease-activated receptor-1 dependent signaling. The G protein alpha 1 pathway is not involved in signaling
Products: -
Products: -
?
additional information
?
-
-
Substrates: coagulation factor Xa inhibits cancer cell migration via LIMK1-mediated cofilin inactivation through induction of myosin light chain phosphorylation and LIMK1 activation, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: effects of factor X on the respiratory function and asthmatic response in mice, factor X transcript levels and factor Xa activity are increased in lungs of asthmatic mice leading to a significant decrease in the thickness of the mucosal layer and in lung collagen deposition, factor Xa modulates airway remodeling, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme elicits a signaling response in C2C12 and NIH-3T3 fibroblast cells. ERK1/2 phosphorylation by factor Xa is dependent on protease-activated receptor PAR-2 cleavage and leads to fibroblast proliferation, migration, and differentiation into myofibroblasts
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme link between cancer and thrombosis appears to be a bidirectional relationship, physiological role of factor Xa, involvement in inflammation and diseases, physiological interactions, regulation, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme link between cancer and thrombosis appears to be a bidirectional relationship, physiological role of factor Xa, involvement in inflammation and diseases, physiological interactions, regulation, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: roles of coagulation pathway and factor Xa in rat mesangioproliferative glomerulonephritis, initiation of the extrinsic coagulation pathway by activating coagulation factor X to factor Xa, factor Xa promote the proliferation of mesangial cells in culture, enzyme inhibitor DX-9065a treatment significantly ameliorated proteinuria in vivo in rats with a a significant reduction in the size of glomeruli, the total number of glomerular cells, and crescent formation, as well as abolishing phosphorylation of p44/42 MAP kinase on day 8, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme link between cancer and thrombosis appears to be a bidirectional relationship, physiological role of factor Xa, involvement in inflammation and diseases, physiological interactions, regulation, overview
Products: -
Products: -
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
1,2-dicaproyl-sn-glycero-3-phospho-L-serine
-
i.e. C6PS, soluble phospholipid, 2 molecules per enzyme molecule, binding to 2 binding sites in sigmoidal fashion with active site labeled enzyme and in hyperbolic fashion with nonlabeled enzyme, binding induces conformaional changes of secondary structure, binding to the tighter of the 2 binding site triggers structural changes which lead to Ca2+-dependent dimer formation, model of sequential binding mechanism
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
Factor Va
-
binding site for factor Xa is located at amino acid residues 307-348 of the heavy chain, purified factor Va is not stable during rapid freezing and thawing
-
additional information
-
the intact enzyme and also of its Gla-domain and EGF-like domain interact with negatively charged phospholipids containing 25% phosphatidylserine and 75% phosphatidylcholine, kinetics
-
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+
-
additional information
recombinant trocarin cannot efficiently generate thrombin without additional protein cofactors
-
additional information
-
recombinant trocarin cannot efficiently generate thrombin without additional protein cofactors
-
additional information
recombinant oscutarin cannot efficiently generate thrombin without additional protein cofactors
-
additional information
-
recombinant oscutarin cannot efficiently generate thrombin without additional protein cofactors
-
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Ca2+
Na+
phosphatidyl-L-serine
-
best in lipid vesicles with up to 25% phosphatidyl-L-serine and at least 75% phosphocholine, absolutely required for activity as part of the prothrombinase complex
phosphocholine
-
best in lipid vesicles with up to 25% phosphatidyl-L-serine and at least 75% phosphocholine
Ca2+
-
factor Xa forms the prothrombin-converting complex with factor V, phospholipid and Ca2+
Ca2+
-
dependent on, cooperative binding, required of the intact enzyme and also of its Gla-domain and EGF-like domain to interact with negatively charged phospholipids containing 25% phosphatidylserine and 75% phosphatidylcholine, 3 Ca2+ per binding partner
Ca2+
-
required for binding of the EGF-like domains at the catalytic C-terminus and the N-terminus, the EGF-like domain are linked via Ca2+ to the Gla-domain of the enzyme, which itself does not need Ca2+ for binding of C6PS
Ca2+
-
required for binding of the EGF-like domains at the catalytic C-terminus and the N-terminus, the EGF-like domain are linked via Ca2+ to the Gla-domain of the enzyme, which itself does not need Ca2+ for binding of C6PS
Ca2+
-
the enzyme is sharply regulated by a Ca2+ switch centered at 1.16 mM, below which factor Xa is active and above which factor Xa forms inactive dimers on phosphatidylserine-exposing membranes
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
Na+
-
binding channel structure, topography and lipophilicity, and allosteric modulation of the enzyme activity, no aperture on the enzyme surface opposite to the S1 subsite entrance and lack of the three-residue insertion in loop 1, residues 183-189, as found in thrombin, modeling, overview
Na+
-
ionic interaction between residues E217 and K224 stabilizes the 220-loop of factor Xa for binding Na+
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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]prop-1-ene-1-sulfonamide
-
-
(1R)-N2-(4-chlorophenyl)-N1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-1,3-dihydro-2H-isoindole-1,2-dicarboxamide
-
-
(1R,2R)-N-(4-chlorophenyl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-hydroxycyclopentane-1,2-dicarboxamide
-
-
(1R,2S)-N-(4-chlorophenyl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4,4-bis(hydroxymethyl)cyclopentane-1,2-dicarboxamide
-
-
(1R,2S)-N-(5-chloropyridin-2-yl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]cyclopropane-1,2-dicarboxamide
-
-
(1S,3R,4S)-4-[(1H-indol-2-ylcarbonyl)amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
(2-[2-[(4-carbamimidoylbenzyl)amino]azetidin-1-yl]-1-cyclohexyl-2-oxoethoxy)carbamic acid
-
-
(2R)-2-[(3-carbamimidoylphenyl)amino]-2-[2-(beta-L-glucopyranosyloxy)phenyl]-N-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]ethanamide
-
-
(2R)-2-[(3-carbamimidoylphenyl)amino]-2-[2-(beta-L-glucopyranosyloxy)phenyl]-N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]-2-oxoethyl]ethanamide
-
-
(2R)-2-[(5-carbamimidoyl-2-hydroxyphenyl)amino]-2-[2-(beta-L-glucopyranosyloxy)phenyl]-N-[2-(4-methyl-1,4-diazepan-1-yl)-2-oxoethyl]ethanamide
-
-
(2R)-N1-(4-chlorophenyl)-N2-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2,3-dihydro-1H-pyrrolo[2,3-b]pyridine-1,2-dicarboxamide
-
-
(2R)-N1-(5-chloropyridin-2-yl)-4-hydroxy-N2-[5-(3-oxomorpholin-4-yl)pyridin-2-yl]pyrrolidine-1,2-dicarboxamide
-
-
(2R)-N1-(5-chloropyridin-2-yl)-N2-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)pyrrolidine-1,2-dicarboxamide
-
-
(2R)-N1-(5-chloropyridin-2-yl)-N2-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-methoxypyrrolidine-1,2-dicarboxamide
-
-
(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-hydroxypyrrolidine-1,2-dicarboxamide
-
-
(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-methoxypyrrolidine-1,2-dicarboxamide
-
-
(2R,3S)-N2-(5-chloropyridin-2-yl)-N1-(2,2-difluoroethyl)-N3-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-N1-methylcyclopropane-1,2,3-tricarboxamide
-
-
(2R,4R)-N1-(4-chlorophenyl)-4-methoxy-N2-(3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)pyrrolidine-1,2-dicarboxamide
-
-
(2R,4R)-N1-(5-chloropyridin-2-yl)-4-methoxy-N2-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidine-1,2-dicarboxamide
-
-
(2R,4S)-N1-(5-chloropyridin-2-yl)-4-(2,4-difluorophenyl)-4-hydroxy-N2-(2-oxo-2H-1,3'-bipyridin-6'-yl)pyrrolidine-1,2-dicarboxamide
-
-
(2RS)-(3'-amidino-3-biphenyl)-5-(4-pyridylamino)pentanoic acid
i.e. FX-2212, 50% inhibition by 272 nM
(2S)-1-[(2R)-2-[3-chloro-5-(difluoromethoxy)phenyl]-2-hydroxyacetyl]-N-[4-(N'-methoxycarbamimidoyl)benzyl]azetidine-2-carboxamide
-
-
(2S)-N-(2-[[2-(aminomethyl)-5-chlorobenzyl]amino]-2-oxoethyl)-2-[(benzylsulfonyl)amino]-4-(1-oxidopyridin-2-yl)butanamide
-
-
(2S)-N-(4-carbamimidoylbenzyl)-1-[(2R)-2-[3-chloro-5-(difluoromethoxy)phenyl]-2-hydroxyacetyl]azetidine-2-carboxamide
-
-
(2S,4S)-N1-(4-chlorophenyl)-N2-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-methoxypyrrolidine-1,2-dicarboxamide
-
-
(3-[(5-chloropyridin-2-yl)carbamoyl]-4-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]phenoxy)acetic acid
-
-
(3-[[(3-carbamimidoylphenyl)(2-[[4-(1-ethanimidoylpiperidin-4-yl)phenyl]amino]-2-oxoethyl)amino]methyl]phenoxy)acetic acid
-
-
(3R)-N2-(4-chlorophenyl)-N3-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-3,4-dihydroisoquinoline-2,3(1H)-dicarboxamide
-
-
(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
-
-
(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetic acid
-
-
(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)acetic acid
-
-
(4R)-4-[[(5-chlorothiophen-2-yl)carbonyl]amino]-N,N-dimethyl-1-[(3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)carbonyl]-L-prolinamide
-
-
(4S)-4-[[(5-chlorothiophen-2-yl)carbonyl]amino]-N-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-L-prolinamide
-
-
(4S)-N5-(4-chlorophenyl)-N4-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-1-methyl-4,6-dihydropyrrolo[3,4-c]pyrazole-4,5(1H)-dicarboxamide
-
-
(4S,5S)-3-(3-carbamimidoylphenyl)-5-(methoxymethyl)-N-(2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1,2-oxazole-4-carboxamide
-
-
(5R)-N1-(5-chloropyridin-2-yl)-N5-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1H-pyrazole-1,5-dicarboxamide
-
-
(5R,6R)-N-(4-chlorophenyl)-N'-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]spiro[2.4]heptane-5,6-dicarboxamide
-
-
(5S)-N1-(4-chlorophenyl)-N5-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-5-methyl-4,5-dihydro-1H-pyrazole-1,5-dicarboxamide
-
-
(6R)-N7-(4-chlorophenyl)-N6-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-5,8-dihydro-1,7-naphthyridine-6,7(6H)-dicarboxamide
-
-
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
(E)-2-(5-chlorothiophen-2-yl)-N-(1-[5-[2-(methylsulfonyl)phenyl]pyridin-2-yl]-2-oxopyrrolidin-3-yl)ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(6-fluoro-2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[1-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
-
(E)-2-(5-chlorothiophen-2-yl)-N-[[(3R)-1-[[1-(pyridin-4-yl)piperidin-4-yl]carbonyl]pyrrolidin-3-yl]methyl]ethenesulfonamide
-
-
(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
-
potent anticoagulation activities in vitro and ex vivo
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-chlorophenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
-
-
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-fluorophenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
-
-
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-methylphenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
-
-
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]phenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
-
potent anticoagulation activities in vitro and ex vivo
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-4-cyanobenzylpropionamide
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-4-hydroxyphenethylpropionamide
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-aryl-propionamides
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-benzylpropionamide
-
non-substrate-like binding mode
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-ethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-phenpropionyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-propionic acid phenethyl ester
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(2-chloro)-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(3-chloro)-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(4-amino)-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(4-tert-butyl)-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamide
-
-
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamides
-
-
(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
([(2R)-2-(7-carbamimidoylnaphthalen-2-yl)-5-[(1-ethanimidoylpiperidin-4-yl)methyl]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
-
-
([(3'-carbamimidoylbiphenyl-3-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
-
-
([(7-carbamimidoylnaphthalen-2-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
-
-
([2'-(butylsulfonyl)-4-[2-([[2-hydroxy-5-(N'-hydroxycarbamimidoyl)phenyl]sulfonyl]amino)ethyl]biphenyl-3-yl]oxy)acetic acid
-
-
([2-[(E)-2-(5-carbamimidoyl-2-hydroxyphenyl)ethenyl]-5-[(1-ethanimidoylpiperidin-4-yl)oxy]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
-
-
1,1'-(benzene-1,4-diyldimethanediyl)bis(N,N-diethylpiperidine-3-carboxamide)
-
-
1,2-dioleoyl-phosphatidylglycerol
-
in vesicles with 1,2-dioleoyl-phosphatidylglycerol, 18fold activation of enzyme activity with prothrombin
1-(1-[(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2-hydroxypropanoyl]piperidin-4-yl)tetrahydropyrimidin-2(1H)-one
-
-
1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[2,3-b]pyridin-2-ylsulfonyl)-piperazin-2-one
-
-
1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[3,2-b]pyridin-2-ylsulfonyl)-piperazin-2-one
-
-
1-(3-amino-1,2-benzisoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[2-[(dimethylamino)methyl]pyridin-3-yl]-2-fluorophenyl)-7-fluoro-1H-indazole-3-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[2-[(dimethylamino)methyl]pyridin-3-yl]phenyl)-7-fluoro-1H-indazole-3-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[[3-(dimethylamino)propyl](pyridin-4-yl)amino]phenyl)-7-fluoro-1H-indazole-3-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-5-methyl-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-7-fluoro-6-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-1H-indazole-3-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-N-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-amino-1,2-benzoxazol-5-yl)-N-[1-[2-(pyrrolidin-1-ylmethyl)phenyl]piperidin-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-amino-1H-isoindol-5-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-aminophenyl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(3-carbamimidoylphenyl)-3-methyl-N-(2'-sulfamoylbiphenyl-4-yl)-1H-pyrazole-5-carboxamide
-
-
1-(3-carbamoylphenyl)-N-[3-chloro-4-(2-thioxopyrrolidin-1-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-carbamoylphenyl)-N-[4-(5-ethyl-2-imino-1,3,4-thiadiazol-3(2H)-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-carbamoylphenyl)-N-[4-[(2Z)-2-(cyanoimino)imidazolidin-1-yl]phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(3-[6-[4-(2-chloropyridin-4-yl)piperazin-1-yl]-7-fluoro-3-methyl-1H-indazol-1-yl]phenyl)methanamine
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
i.e. SN429
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-4-bromo-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(fluoro)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-(3-[amino(imino)methyl]phenyl)-N-[[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-(4-aminophthalazin-6-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(4-aminoquinazolin-6-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-(4-methoxyphenyl)-3-(methylsulfonyl)-6-(4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
good factor Xa binding ability and good plasma anticoagulant activity
1-(4-methoxyphenyl)-4-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[3,4-d]pyridazin-7-one
-
-
1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(1H-tetrazol-1-ylmethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(2H-tetrazol-2-ylmethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
1-(4-methoxyphenyl)-6-(4-[1-[(methylamino)methyl]cyclopropyl]phenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
good factor Xa binding ability and good plasma anticoagulant activity
1-(4-methoxyphenyl)-6-(4-[1-[(methylamino)methyl]cyclopropyl]phenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-6-[4-(1-[[(1-methylethyl)amino]methyl]cyclopropyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(4-methoxyphenyl)-6-[4-(2-oxopiperidin-1-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(4-methoxyphenyl)-6-[4-[1-(morpholin-4-ylmethyl)cyclopropyl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(4-methoxyphenyl)-6-[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(4-methoxyphenyl)-7-oxo-6-(4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
good factor Xa binding ability and good plasma anticoagulant activity
1-(4-methoxyphenyl)-7-oxo-6-[1-[2-(pyrrolidin-1-ylmethyl)phenyl]piperidin-4-yl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1,3-oxazolidin-3-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[4-[(2-oxopiperidin-1-yl)oxy]phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
1-(4-methoxyphenyl)-7-oxo-6-[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
good factor Xa binding ability and good plasma anticoagulant activity
1-(4-methoxyphenyl)-7-[2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-6,7-dihydropyrazolo[3,4-c]azepin-8(1H)-one
-
-
1-(4-[1-[3-(aminomethyl)phenyl]-7-fluoro-3-methyl-1H-indazol-6-yl]-3-fluorophenyl)piperidin-2-one
-
-
1-(5-methoxypyridin-2-yl)-6-[4-[2-(methylsulfonyl)pyridin-1(2H)-yl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-(6-chloronaphthalen-2-yl)-N-[2'-[(dimethylamino)methyl]-3-fluorobiphenyl-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-palmitoyl-2-oleoyl-3-sn-phosphatidylcholine
-
in vesicles with 1,2-palmitoyl-2-oleoyl-3-sn-phosphatidylcholine, 18fold activation of enzyme activity with prothrombin
1-[(4-amino-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-piperazin-2-one
-
-
1-[(4-aminoquinazolin-7-yl)methyl]-4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]piperazin-2-one
-
-
1-[(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)methyl]cyclopropanecarboxylic acid
-
-
1-[(6-chloro-2-naphthyl)sulfonyl]-4-[(1-pyridin-4-ylpiperidin-4-yl)carbonyl]piperazine
-
-
1-[1-(3-amino-1,2-benzoxazol-5-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-2-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]phenyl)ethanone
-
-
1-[2-(aminomethyl)phenyl]-N-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-[2-([2-[(5-chloropyridin-2-yl)carbamoyl]-4-methoxyphenyl]carbamoyl)-5-(N,N-dimethylcarbamimidoyl)phenyl]piperidine-4-carboxylic acid
-
-
1-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide
-
-
1-[2-[(5-chlorothiophen-2-yl)amino]-2-oxoethyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]-D-prolinamide
-
-
1-[2-[(aminooxy)sulfinyl]phenyl]-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-[3-(5-amino-1,3,4-thiadiazol-2-yl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-[3-(5-amino-4H-1,2,4-triazol-3-yl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
1-[3-(aminomethyl)phenyl]-N-3-fluoro-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
i.e. DPC423, highly potent, selective, and orally bioavailable inhibitor
1-[3-(aminomethyl)phenyl]-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
i.e. DPC 423
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-[3-(aminomethyl)phenyl]-N-[4-(2-iminopyrrolidin-1-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
1-[3-[([1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methyl)sulfonyl]phenyl]pyridinium
-
-
1-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]urea
-
-
1-[3-[amino(imino)methyl]phenyl]-N-[2'-(aminosulfonyl)[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
1-[4-amino-3-[([1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methyl)sulfonyl]phenyl]pyridinium
-
-
1-[4-[1-(5-methoxypyridin-2-yl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]phenyl]-1,2-dihydropyridine-2-sulfonamide
-
-
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]-2-ethylpropan-2-ol
-
-
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]ethanol
-
-
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]propan-2-ol
-
-
1-[[2-(5-chlorothiophen-2-yl)-1,3-thiazol-5-yl]methyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]-D-prolinamide
-
-
1-[[4-([4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]phenyl]carbamoyl)phenyl]carbonoimidoyl]piperidine-4-carboxylic acid
-
-
1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide
-
-
10-[(5-chloro-1H-indol-2-yl)sulfonyl]-1'-(4,5-dihydro-1,3-oxazol-2-yl)-2-methyldihydro-1H-spiro[imidazo[5',1':2,3]imidazo[1,2-a]pyrazine-5,4'-piperidine]-3,8(2H,9H)-dione
-
-
1H-pyrrolo[3,2-c]pyridine-1-acetamide, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-
-
-
1H-pyrrolo[3,2-c]pyridine-1-acetic acid, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-
-
-
1H-pyrrolo[3,2-c]pyridine-1-acetic acid, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-, methyl ester
-
-
2,2,4,7-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-(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-(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-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-carbamimidoyl-2-hydroxyphenoxy)ethyl 4-(pyrrolidin-1-ylcarbonoimidoyl)benzoate
-
-
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
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
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-[[(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-chloro-2-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-N-[(3R,4S)-3-fluoro-1-(propan-2-yl)piperidin-4-yl]benzamide
-
-
3-chloro-2-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-N-[1-(propan-2-yl)piperidin-4-yl]benzamide
-
-
3-chloro-4-[3-[(4-chlorophenyl)amino]-3-oxopropyl]-5-([[5-(propan-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]carbonyl]amino)benzoic acid
-
-
3-chloro-N-(4-chloro-2-([(4-chlorophenyl)-amino]carbonyl)phenyl)-4-[(4-methyl-1-piperazinyl)methyl]-2-thiophenecarboxamide
binding structure and mechanism
3-chloro-N-(4-chloro-2-([(5-chloro-2-pyridinyl)amino]carbonyl)-6-methoxyphenyl)-4-([(4,5-dihydro-2-oxazolyl)methylamino]methyl)-2-thiophenecarboxamide
binding structure and mechanism, good bioavailability
3-chloro-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
-
3-chloro-N-[(1R,2S)-2-[[4-(2-oxopyridin-1(2H)-yl)benzoyl]amino]cyclohexyl]-1H-indole-6-carboxamide
-
-
3-chloro-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
3-chloro-N-[2-[(4-chlorophenyl)carbamoyl]-4-methylphenyl]-1-benzothiophene-2-carboxamide
-
-
3-chloro-N-[2-[(4-fluorophenyl)carbamoyl]-4-methylphenyl]-1-benzothiophene-2-carboxamide
-
-
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
highly potent and selective non-amidine inhibitor, reversibel inhibition, 5fold higher affinity for the free factor Xa than for the enzyme/substrate complex, inhibition mechanism, 19fold decreased inhibitory effect in presence of phospholipid
3-chloro-N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]-6-methoxyphenyl]-4-[[2-(methylamino)-1H-imidazol-1-yl]methyl]thiophene-2-carboxamide
-
-
3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]-N-(5-methyl-2-pyridyl)benzamide
-
-
3-hydroxy-4'-methoxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
-
-
3-hydroxy-4'-methoxy-4-methyl-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
-
-
3-hydroxy-4'-methyl-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
-
-
3-hydroxy-N-(5-methoxy-2-pyridyl)-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
-
-
3-methyl-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
3-methyl-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
-
3-[(4-methoxyphenyl)carbamoyl]-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]phenyl beta-D-glucopyranosiduronic acid
-
-
3-[(5-chloropyridin-2-yl)carbamoyl]-2-[[4-(1-methyl-2-oxo-1,2-dihydropyridin-3-yl)benzoyl]amino]phenyl b-D-glucopyranosiduronic acid
-
-
3-[6-(2'-dimethylaminomethyl-biphenyl-4-yl)-7-oxo-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridine-1-yl]-benzamide
-
the inhibitor shows good fXa potency, selectivity, in vivo efficacy and oral bioavailability
3-[6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
3-[7-fluoro-3-methyl-6-[4-(2-oxopiperidin-1-yl)phenyl]-1H-indazol-1-yl]benzenecarboximidamide
-
-
3-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl](methyl)amino]-2-oxopyrrolidin-1-yl]methyl]benzenecarboximidamide
-
-
3-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl]amino]-2-oxopyrrolidin-1-yl]methyl]benzenecarboximidamide
-
-
3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
-
-
3-{4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl}-4-hydroxybenzamidine
-
-
4'-chloro-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
-
-
4'-[1-(4-methoxyphenyl)-4-methyl-7-oxo-3-(trifluoromethyl)-1,7-dihydro-6H-pyrazolo[3,4-d]pyridazin-6-yl]biphenyl-2-sulfonamide
-
-
4'-[1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,7-dihydro-6H-pyrazolo[4,3-d]pyrimidin-6-yl]biphenyl-2-sulfonamide
-
-
4,4'-[(2-oxocycloheptane-1,3-diylidene)di(E)methylylidene]dibenzenecarboximidamide
-
-
4-(3-(aminoiminomethyl)phenyl)-1-(6-chloro-benzo[b]thiophene-2-sulfonyl)-piperazin-2-one
-
-
4-(4-(2-oxopyridin-1(2H)-yl)benzamido)-3-(3,4,5-trimethoxybenzamido)benzoic acid
-
-
4-(4-amino-quinazolin-7-ylmethyl)-1-(6-chloro-benzo[b]thiophene-2-sulfonyl)-piperazin-2-one
-
-
4-(4-[5-[([[(5-chlorothiophen-2-yl)carbonyl]oxy]amino)methyl]-2-oxo-1,3-oxazolidin-3-yl]phenyl)morpholin-3-one
-
-
4-(benzo[b]thien-2-ylsulfonyl)-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-([[(5-chlorothiophen-2-yl)carbonyl]amino]methyl)-3-fluoro-5-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]benzoic acid
-
-
4-acetamido-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-benzamide
-
-
4-bromo-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)benzamide
-
-
4-chloro-3-([[(4-chlorocyclopenta-1,3-dien-1-yl)carbonyl]amino]methyl)-N-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2,3-dihydro-1H-indole-1-carboxamide
-
-
4-chloro-N-[4-(2-[[2-fluoro-4-(2-oxopyrazin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-1,3-thiazol-2-yl]benzamide
-
-
4-chloro-N-[5-(2-oxo-2-[4-[2-oxo-2-(pyrrolidin-1-yl)ethyl]piperazin-1-yl]ethyl)-3H-pyrrol-2-yl]benzamide
-
-
4-hydroxy-3-[2-oxo-3-(S)-(5-pyridin-3-yl-thiophene-2-sulfonylamino)-pyrrolidin-1-ylmethyl]-benzamidine
-
i.e. RPR130737, highly specific inhibitor of factor Xa realtive to other serine proteases, reversible, fast binding, competitive active-site directed inhibitor
4-methoxy-N-[2-[([[1-(pyridin-4-yl)piperidin-4-yl]methyl]carbamoyl)amino]phenyl]benzamide
-
-
4-[(3-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(4'-chloro[1,1'-biphenyl]-4-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(5'-chloro[2,2'-bithiophen]-5-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazine-2-one
-
-
4-[(5-chloro-1H-indol-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
-
4-[(6-bromobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
-
4-[(6-chloro-2-naphthalenyl)sulfonyl]-1-[[1-(4-pyridinyl)-4-piperidinyl]-methyl]piperazinone
-
i.e. M55113, strong inhibitor, highly selective for factor Xa over trypsin and thrombin
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-imidazo[4,5-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-b]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(furo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(1-methyl-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(4,5-dihydro-4-oxo-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(5-oxido-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[[1-(2-hydroxyethyl)-1H-pyrrolo[3,2-c]pyridin-2-yl]methyl]-piperazin-2-one
-
-
4-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorothieno[3,2-b]pyridin-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-3-methoxy-5-[[1-(propan-2-yl)piperidin-4-yl]carbamoyl]benzoic acid
-
-
4-[3-[(4-chlorophenyl)amino]-3-oxopropyl]-3-([[5-(propan-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]carbonyl]amino)-5-(trifluoromethyl)benzoic acid
-
-
4-[[(1E)-2-(4-chlorophenyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[[(1E)-2-(5-chloro-2-thienyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[[(1E)-2-(5-chloro-4-methoxy-2-thienyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl]-1-(pyridin-4-yl)piperidine-4-carboxylic acid
-
-
4-[[(3-carbamimidoylphenyl)amino]methyl]-3-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzoic acid
-
-
4-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl](methyl)amino]-2-oxopyrrolidin-1-yl]methyl]thiophene-2-carboximidamide
-
-
4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
-
-
4-[[(E)-2-(5-chlorothiophen-2-yl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
-
4-[[2-(5-chloro-2-thienyl)ethyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate
5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)-2-methylimidazo[1,2-a]pyridine
-
-
5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridine
-
-
5-bromo-N-([(5S)-3-[4-(3-methylidenemorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-butyl-2-(3-carbamimidoyl-phenyl)-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
5-chloro-3-hydroxy-4'-methoxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzanilide
-
-
5-chloro-3-[(5-chloro-2-pyridyl)carbamoyl]-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]phenyl beta-D-glucopyranosiduronic acid
-
-
5-chloro-N-(1-oxo-2-[3-[(pyridin-4-ylamino)methyl]benzyl]-2,3-dihydro-1H-isoindol-4-yl)thiophene-2-carboxamide
-
-
5-chloro-N-(2-[[1-(propan-2-yl)piperidin-4-yl](1,3-thiazol-2-ylmethyl)sulfamoyl]ethyl)thiophene-2-carboxamide
-
-
5-chloro-N-(4-[2-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]-2-oxoethyl]-1,3-thiazol-2-yl)thiophene-2-carboxamide
-
-
5-chloro-N-(5-chloro-2-pyridyl)-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
-
-
5-chloro-N-(5-chloro-2-pyridyl)-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
-
AS1468240, potent inhibitor
5-chloro-N-(5-chloropyridin-2-yl)-2-([4-[(2-imino-1,3-oxazolidin-3-yl)methyl]benzoyl]amino)benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-([4-[(dimethylamino)methyl]benzoyl]amino)benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-([[trans-4-(3-oxomorpholin-4-yl)cyclohexyl]carbonyl]amino)benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-[(4-[[ethanimidoyl(methyl)amino]methyl]benzoyl)amino]benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)benzoyl]amino]-3-methoxybenzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-2-[[4-(piperidin-1-ylcarbonoimidoyl)benzoyl]amino]benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-3-hydroxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-3-methoxy-2-[[4-(2-oxopiperidin-1-yl)benzoyl]amino]benzamide
-
-
5-chloro-N-(5-chloropyridin-2-yl)-3-methoxy-2-[[4-(2-oxopyridin-1(2H)-yl)benzoyl]amino]benzamide
-
-
5-chloro-N-([(5R)-3-[4-(2-imino-1,3-oxazolidin-3-yl)phenyl]-4,5-dihydro-1,2-oxazol-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-2-imino-3-[4-(2-oxo-1,3-oxazolidin-3-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-2-imino-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-2-oxo-3-[4-(2-oxopyrrolidin-1-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-3-[2-fluoro-4-(3-oxomorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-3-[3-cyclopropyl-4-(5-oxo-1,4-oxazepan-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-3-[3-fluoro-4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-3-[3-fluoro-4-(thiomorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([(5S)-3-[4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([1-[2-(3-oxopiperazin-1-yl)-4-(2-oxopyridin-1(2H)-yl)phenyl]-1H-imidazol-4-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([1-[2-(methylamino)-4-(2-oxopyridin-1(2H)-yl)phenyl]-1H-1,2,3-triazol-4-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([1-[4-(2-imino-1,3-oxazolidin-3-yl)phenyl]-3-phenyl-1H-pyrazol-4-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([1-[4-(2-oxopyridin-1(2H)-yl)-2-(piperazin-1-yl)phenyl]-1H-1,2,3-triazol-4-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([1-[4-(2-oxopyridin-1(2H)-yl)phenyl]-1H-imidazol-4-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([3-[4-(3-oxomorpholin-4-yl)phenyl]-1,2,4-oxadiazol-5-yl]methyl)thiophene-2-carboxamide
-
-
5-chloro-N-([4-[6-fluoro-7-(methylamino)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl]phenyl]carbamoyl)thiophene-2-sulfonamide
-
-
5-chloro-N-[(1-[3-methyl-4-(3-oxomorpholin-4-yl)phenyl]-2-[[(methylsulfonyl)amino]methyl]-1H-imidazol-4-yl)methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1R,2S)-2-([4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]benzoyl]amino)cyclopentyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1R,2S)-2-[[4-(2-oxopyridin-1(2H)-yl)benzoyl]amino]cyclopentyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1R,4R)-4-[[2-fluoro-4-(2-oxopyrazin-1(2H)-yl)phenyl]carbamoyl]-2-(2-oxopropyl)cyclopentyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1R,4S)-2-ethoxy-4-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]carbamoyl]cyclopentyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1R,4S)-4-[[2-fluoro-4-(2-oxopyrazin-1(2H)-yl)phenyl]carbamoyl]-2-hydroxycyclopentyl]thiophene-2-carboxamide
-
-
5-chloro-N-[(1S,2S)-2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]carbamoyl]cyclohexyl]pyridine-2-carboxamide
-
-
5-chloro-N-[(2R)-3-methoxy-1-[[3-methyl-4-(3-oxomorpholin-4-yl)phenyl]amino]-1-oxopropan-2-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[(3R)-1-(3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)-5-oxopyrrolidin-3-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[(3R)-1-[2-fluoro-4-(3-oxomorpholin-4-yl)phenyl]-5-oxopyrrolidin-3-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[(3R,4R)-1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-4-methoxypyrrolidin-3-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[(3R,4S)-4-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]carbamoyl]-1-(methylsulfonyl)pyrrolidin-3-yl]pyridine-2-carboxamide
-
-
5-chloro-N-[(3S)-1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-4-methoxypyrrolidin-3-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[(3S,4S)-3-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]carbamoyl]-1-methylpiperidin-4-yl]pyridine-2-carboxamide
-
-
5-chloro-N-[1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-1H-1,2,4-triazol-3-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[1-oxo-2-[3-(3-oxomorpholin-4-yl)benzyl]-2,3-dihydro-1H-isoindol-4-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[1-[(3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)carbamoyl]cyclopropyl]thiophene-2-carboxamide
-
-
5-chloro-N-[2-[3-(2-imino-1,3-oxazolidin-3-yl)benzyl]-3-oxo-2,3-dihydro-1H-isoindol-4-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[3-oxo-2-[3-(3-oxomorpholin-4-yl)benzyl]-2,3-dihydro-1H-isoindol-4-yl]thiophene-2-carboxamide
-
-
5-chloro-N-[4-(dimethylamino)-2-[[4-(2-imino-1,3-oxazolidin-3-yl)phenyl]carbamoyl]-5-methylphenyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[(5R)-3-[4-[2-(furan-2-yl)-4,5-dihydro-1H-imidazol-1-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[(5S)-3-[2-fluoro-4-[3-(hydroxymethyl)-2-oxopyridin-1(2H)-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[(5S)-3-[4-[3-(hydroxymethyl)-2-oxopyridin-1(2H)-yl]-3-methylphenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[(5S)-3-[4-[3-[2-[(2-hydroxyethyl)amino]ethyl]-2-oxopyridin-1(2H)-yl]-3-(methoxymethyl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[(5S)-3-[4-[3-[2-[(trans-4-hydroxycyclohexyl)amino]ethoxy]-2-oxopyridin-1(2H)-yl]-3-methylphenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
-
-
5-chloro-N-[[3-(4-cyanophenyl)-4,5-dihydro-1,2-oxazol-5-yl]methyl]thiophene-2-carboxamide
-
-
5-ethynyl-N-(2-methyl-1-[[3-methyl-4-(3-oxomorpholin-4-yl)phenyl]amino]-1-oxopropan-2-yl)thiophene-2-carboxamide
-
-
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-(4-[1-[(dimethylamino)methyl]cyclopropyl]phenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]phenyl)-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-(4-[2-[(dimethylamino)methyl]cyclopenta-2,4-dien-1-yl]phenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-chloro-benzo[b]thiophene-2-sulfonic acid [2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)-pyrrolidin-3-yl]-amide
-
-
6-chloro-benzo[b]thiophene-2-sulfonic acid [2-oxo-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-pyrrolidin-3-yl]-amide
-
-
6-chloro-N-methyl-N-[(3S)-2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pyrrolidin-3-yl]-1-benzothiophene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-(6-fluoro-2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[(1R)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[(1S)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[(1S)-1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[2-fluoro-4-[(1S)-1-(methylamino)ethyl]phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-(2-fluoro-4-piperidin-1-ylphenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-(2-fluoro-4-pyridin-4-ylphenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]thieno[2,3-b]pyridine-2-sulfonamide
-
-
6-chloro-N-[1-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
-
6-chloro-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]thieno[2,3-b]pyridine-2-sulfonamide
-
-
6-[2'-(methylsulfonyl)biphenyl-4-yl]-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(aminooxy)sulfinyl]-3-fluorobiphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-4-methyl-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[3,4-d]pyridazin-7-one
-
-
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylic acid
-
-
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(3-nitrophenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-ethylphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(iminomethyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-5-methyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
6-[2-(4-chlorophenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]-2,2,4,7-tetramethyl-1,2,3,4-tetrahydroquinoline
16% activity at 0.005 mM; 35% activity at 0.03 mM; 63% activity at 0.001 mM; 67% activity at 0.03 mM; 76% activity at 0.005 mM; 8% activity at 0.005 mM; 82% activity at 0.03 mM; 85% activity at 0.005 mM; 87% activity at 0.03 mM; 94% activity at 0.03 mM
6-[3-fluoro-2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
6-[4-(1-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]cyclopropyl)phenyl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
6-[4-([(2S)-4-[(3-chloro-1H-indol-6-yl)sulfonyl]-2-methyl-6-oxopiperazin-1-yl]methyl)phenyl]-2-methylpyridazin-3(2H)-one
-
-
6-[4-([4-[(3-chloro-1H-indol-6-yl)sulfonyl]-3-hydroxypiperazin-1-yl]carbonyl)piperidin-1-yl]-2-methylpyridazin-3(2H)-one
-
-
6-[4-([4-[(5-chloro-1H-indol-2-yl)sulfonyl]-2-oxopiperazin-1-yl]methyl)phenyl]-2-[2-(dimethylamino)ethyl]pyridazin-3(2H)-one
-
-
7'-[(6-chloronaphthalen-2-yl)sulfonyl]-8a'-(hydroxymethyl)-1-(pyridin-4-yl)tetrahydro-5'H-spiro[piperidine-4,2'-[1,3]thiazolo[3,2-a]pyrazin]-5'-one
-
-
7-([7-[(1-ethanimidoylpiperidin-4-yl)oxy]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]methyl)naphthalene-2-carboximidamide
-
-
7-oxo-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
7-[(2R)-5-[(1-ethanimidoylpiperidin-4-yl)methyl]-1-(ethylsulfonyl)-2,3-dihydro-1H-indol-2-yl]naphthalene-2-carboximidamide
-
-
8-amino-N-[(1R)-2-oxo-1-phenyl-2-[4-(pyridin-4-yl)piperazin-1-yl]ethyl]naphthalene-2-carboxamide
-
-
8-amino-N-[(1R)-2-[4-[4-fluoro-2-(methylsulfonyl)phenyl]piperazin-1-yl]-2-oxo-1-phenylethyl]naphthalene-2-carboxamide
-
-
abciximab
-
glycoprotein IIb/IIIa receptor-antagonist, 3.8% inhibition at 0.140 mM in absence of heparin, 49% inhibition at 0.14 mM in presence of heparin 1 U/ml
-
AduNAP4
-
an anticoagulant peptide from the blood-feeding human hookworm, Ancylostoma duodenale, that consits of 104 amino acids including a predicted 23-residue signal peptide. Cloning and recombinant expression of His-tagged and thioredoxin-tagged in Escherichia coli strain BL21, GenBank ID EU552548. Exhibits mixed-type inhibition versus factor Xa
-
Alpha1-proteinase inhibitor
-
engineering of functional exosites in P1 Arg variant increases the association rate constant for the reactions with factors Xa and IXa, without affecting the inhibitor reactions with trypsin and thrombin. Mutation K222Y/L224E in alpha1-proteinase inhibitor increases the association rate constant 14fold
-
amblyomin-X
-
cloning of the inhibitor from the salivary glands of the tick Amblyomma cajennense, the transcript codes for a protein with unique structure containing an N-terminal Kunitz-type domain and a C-terminus, which acts as an inhibitor factor Xa, recombinant inhibitor expression in Escherichia coli, amblyomin-X structure-function relationships, molecular modelling, overview
-
Ancylostoma ceylanicum anticoagulant peptide 1
-
i.e. AcAP1, natural enzyme inhibitor from human specific hookworm, cloned and sequenced, GenBank accession number AF399710, purified, recombinant expression in Escherichia coli, possesses anticoagulant activity in vivo, specific inhibition of factor Xa, no inhibition of other proteases like thrombin, kallikrein, or coagulation factor XIIa, inhibition mechanism
-
Ancylostoma ceylanicum anticoagulant peptide 5
-
i.e. AcAP5, natural enzyme inhibitor from dog specific hookworm, also inhibits the human factor Xa, competitive to AcAP1
-
antithrombin mutant HAT/Proth-1
-
mutant of human antithrombin possessing factor Xa-cleavage site 1 from human thrombin, recombinant from expression in inhuman 293 cells, inactivation of factor Xa is 3-4fold more effective that with mutant HAT/Proth-2, increased inactivation by heparin and 300-500fold by pentasaccharide fragment of heparin
-
antithrombin mutant HAT/Proth-2
-
mutant of human antithrombin possessing factor Xa-cleavage site 2 from human thrombin, recombinant from expression in inhuman 293 cells, increased inactivation by heparin and 300-500fold by pentasaccharide fragment of heparin
-
AP'4
-
nonapeptide comprising amino acids 323-331 of factor Va, strong, inhibition of prothrombinase activity, noncompetitive with respect to prothrombin, inhibition mechanism
Aprotinin
-
95% inhibition of factor Xa and 2% inhibition of prothrombinase complex activity at 10 U/ml
atrial polypeptide
-
promotes factor Xa-antithrombin III complex formation when preincubated with antithrombin III, or when added within 1 min to factor Xa/antithrombin III mixtures. It promotes transformation of free factor Xaalpha into factor Xabeta
-
Bauhinia ungulata factor Xa inhibitor
-
i.e. BuXI, specific Kunitz-type inhibitor of factor Xa, methionine residues at the active site of the inhibitor are involved in the inhibition mechanism, oxidized protein does no longer inhibit factor Xa
-
BIBT0871
possesses a 1-methyl-benzimidazole scaffold placing the methyl substitutent into the S2-subsite, pyridinyl moiety interacts with F174, binding structure
coronary-dilatory hypothalamic neurohormone C
-
incubation with factor Xa and antithrombin III results in a decrease in total complex formation, a decrease in modified antithrombin III, a decrease in factor Xagamma and little change in the ratio of free factor Xaalpha to factor Xabeta. Neurohormone C retards the hydrolysis of the factor Xa/antithrombin III complexes which forms free factor Xa and modified antithrombin III
-
cycloheximide
-
61% inhibition at 0.01 mg/ml after 3 h, complete inhibition after 20 h
endogeneous polypeptide inhibitor
-
8.8fold purification of a 15 kDa polypeptide inhibitor from nymphs of camel tick Hyalomma dromedarii, with potent antocoagulant properties, specific for factor Xa compared to other serine proteases, binds 2 sites of factor Xa, uncompetitive, inhibits blood coagulation, 329 U/mg, complete inhibition by 2 inhibitor units
-
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
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
-
FPR-prothrombin
-
i.e. prothrombin specifically active site-labeled with D-Phe-Pro-Arg-CH2Cl, acts as a competitive inhibitor of prothrombin activation. The inhibitory effect of FPR-ProT increases with decreasing phospholipid concentration, with a 5fold decrease in the FPR-ProT concentration required for 50% inhibition at 0.002 mM phospholipid compared with that at 0.030 mM
-
fucoidan
-
brown algae sulfated polysaccharide from Fucus evanescens. Deacetylation of fucoidan does not alter its inhibitory capacities, while purification from protein and polyphenols reduces inhibitory effects. depolymerization of fucoidan increases inhibitory activity
HD1-22
-
bivalent fusion aptamer consisting of 15-base spanning DNA aptamer HD1 which specifically inhibits the procoagulant functions of thrombin, and aptamer HD22 which binds to exosite 2 of thrombin, interconnected by a poly-dA linker. Aptamer HD1-22 binds to (pro)exosite 1 of prothrombin and inhibits the prothrombinase activity nearly 2fold better than HD1. The anticoagulant activities of HD1-22 are fully reversed by addition of antidote-oligodeoxynucleotides
-
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
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
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-([[4-(1-oxidopyridin-4-yl)benzoyl]amino]oxy)butanoate
-
-
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate
methyl (3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetate
-
-
methyl (4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetate
-
-
methyl (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
methyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2-methylpropanoate
-
-
methyl 2-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)propanoate
-
-
methyl 2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzenesulfinate
-
-
methyl 3'-fluoro-4'-(3-[[(3-methoxyphenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-(3-[[(4-fluorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-(3-[[(4-methoxyphenyl)sulfonyl]amino]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-(3-[[(5-isoxazol-3-ylthiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-([[1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]carbonyl]amino)biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[2-oxo-3-[(phenylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[2-oxo-3-[(quinolin-3-ylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[2-oxo-3-[(quinolin-6-ylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[3-(4-methoxyphenoxy)-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[3-(iminomethyl)-1-(4-methoxyphenyl)-5,7-dioxo-1,4,5,7-tetrahydro-6H-pyrazolo[4,3-d]pyrimidin-6-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[3-([[4-(iminomethyl)phenyl]sulfonyl]methyl)-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[3-[(1H-indazol-6-ylsulfamoyl)methyl]-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3'-fluoro-4'-[3-[(4-methoxyphenyl)amino]-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
methyl 3-(3-carbamimidoylphenyl)-5-[(4-carbamimidoylphenyl)carbamoyl]-4,5-dihydro-1,2-oxazole-5-carboxylate
-
-
methyl 3-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2,2-dimethylpropanoate
-
-
methyl 3-[3-[amino(imino)methyl]phenyl]-5-[4-[amino(imino)methyl]phenyl]pentanoate
-
-
methyl 3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
-
-
methyl 4'-(3-[[(2,5-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(3,4-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(3,4-difluorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(3,5-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(3-chlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(4-chloro-6-methyl-1-benzothiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(4-chlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(4-ethylphenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(5-chlorothiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(diethylamino)ethyl](methyl)amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(dimethylamino)ethyl](methyl)amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(dimethylamino)ethyl]amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](3-hydroxypropyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl]amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl][2-(4-methylpiperazin-1-yl)-2-oxoethyl]amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-(3-[[(7-chloronaphthalen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-([[4-amino-3-(iminomethyl)-1-(4-methoxyphenyl)-1H-pyrazol-5-yl]carbonyl]amino)-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-[1-(2-amino-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[1-(2-carbamoyl-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[1-(2-carbamoylphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[1-[2-[(aminooxy)sulfinyl]-4-methoxyphenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[1-[2-[(aminooxy)sulfinyl]phenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[(2-hydroxyethyl)(methyl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[methyl(1-methylpiperidin-4-yl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4'-[3-[(cyclohexylsulfonyl)methyl]-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
methyl 4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
-
-
methyl 6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
methyl N-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]glycinate
-
-
methyl N-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycinate
-
-
methyl [3-(3-carbamimidoylphenyl)-4-[(2'-sulfamoylbiphenyl-4-yl)carbamoyl]-4,5-dihydro-1,2-oxazol-5-yl]acetate
-
-
methyl [3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]amidosulfite
-
-
N-(2,4-dichlorophenyl)-4-(2,2,4,7-tetramethyl-1,2,3,4-tetrahydroquinolin-6-yl)pyrimidin-2-amine
1% activity at 0.03 mM
N-(2-chlorophenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
11% inhibition at 0.00136 mM
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl](methyl)amino]ethyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl](methyl)amino]ethyl)-N,5-dimethyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]ethyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]ethyl)-N,5-dimethyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]phenyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-(3-chloro-4-methoxyphenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
39% inhibition at 0.00136 mM
N-(3-chlorophenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
76% inhibition at 0.00136 mM
N-(3-methoxyphenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
40% inhibition at 0.00136 mM
N-(3-[[4'-(trifluoromethyl)biphenyl-4-yl]methoxy]phenyl)piperidine-4-carboxamide
-
-
N-(4-carbamoyl-2-(3,4,5-trimethoxybenzamido)phenyl)-2-oxo-1-phenyl-1,2-di-hydropyridine-4-carboxamide
-
-
N-(4-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
-
N-(4-chlorophenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
complete inhibition at 0.00136 mM
N-(4-ethylphenyl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
15% inhibition at 0.00136 mM
N-(5-carbamoyl-2-(4-(2-oxopiperidin-1-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dichlorobenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dimethoxybenzamide
-
highly potent, selective, direct inhibitor
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-chlorobenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-fluorobenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-formamidobenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-methoxybenzamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-5-chlorothio-phene-2-carboxamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-6-chloronicotinamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)benzo[d]oxa-zole-6-carboxamide
-
-
N-(5-carbamoyl-2-(4-(2-oxopyrrolidin-1-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
-
N-(5-chloro-2-pyridyl)-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
-
-
N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide
-
-
N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]benzamide
-
-
N-(5-chloropyridin-2-yl)-3-hydroxy-2-[[4-(1-methyl-4-oxo-1,4-dihydropyridin-3-yl)benzoyl]amino]benzamide
-
-
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]ethanediamide
-
-
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
N-(5-chloropyridin-2-yl)-N'-[(3R,4S)-1-formyl-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]piperidin-4-yl]ethanediamide
-
-
N-(5-chloropyridin-2-yl)-N'-[4-(3-oxomorpholin-4-yl)phenyl]pyrazine-2,3-dicarboxamide
-
-
N-(5-chlorothiophen-2-yl)-N'-[(3R,4S)-1-formyl-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]piperidin-4-yl]ethanediamide
-
-
N-(6-methoxypyridin-3-yl)-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide
-
7% inhibition at 0.00136 mM
N-(benzylsulfonyl)-3-(1-carbamimidoylpiperidin-4-yl)-D-alanyl-N-[(2S)-5-carbamimidamido-1-hydroxypentan-2-yl]glycinamide
-
-
N-([1-[4-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-methoxy-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3-fluorophenyl]-1H-imidazol-2-yl]methyl)-2-methoxy-N,N-dimethyl-2-oxoethanaminium
-
-
N-([1-[4-(3-[[(6-chloronaphthalen-2-yl)sulfonyl]amino]-2-oxopiperidin-1-yl)-3-fluorophenyl]-1H-imidazol-2-yl]methyl)-2-methoxy-N,N-dimethyl-2-oxoethanaminium
-
-
N-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
N-[(1R,2S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2S,4R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2S,5S)-2-[(1H-indol-2-ylcarbonyl)amino]-5-(methylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
N-[(1R,2S,5S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
potent inhibition, promising anticoagulant activity and good oral bioavailability
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dipropylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
-
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-[(2-hydroxyethyl)(methyl)carbamoyl]cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
-
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-[(2-methoxyethyl)(methyl)carbamoyl]cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclobutyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cycloheptyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclooctyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(2-[[(4-carbamimidoylphenyl)amino]methyl]-1-methyl-1H-benzimidazol-5-yl)carbonyl]-N-pyridin-2-yl-b-alanine
-
-
N-[(2S)-1-[(2R)-2-[[2-(aminomethyl)-5-chlorobenzyl]carbamoyl]pyrrolidin-1-yl]-4-(1-oxidopyridin-2-yl)-1-oxobutan-2-yl]glycine
-
-
N-[(2S)-1-[(2R)-2-[[2-(aminomethyl)-5-chlorobenzyl]carbamoyl]pyrrolidin-1-yl]-4-(4-hydroxyphenyl)-1-oxobutan-2-yl]glycine
-
-
N-[(2S)-5-carbamimidamido-1-(2,3-dihydro-1,3-thiazol-2-yl)-1-oxopentan-2-yl]-2-[4-[(4-chlorophenyl)sulfonyl]-2-oxopiperazin-1-yl]acetamide
-
-
N-[(3aR,7aR)-2-[3-(2-amino-2-iminoethoxy)benzyl]-1,3-dioxooctahydro-1H-isoindol-4-yl]-5-chlorothiophene-2-carboxamide
-
-
N-[(3R,4S)-1-acetyl-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]piperidin-4-yl]-N'-(5-chloropyridin-2-yl)ethanediamide
-
-
N-[(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-1-methoxypiperidin-3-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-1-[(dimethylamino)oxy]piperidin-3-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[(3S)-1-(1-amino-2,3-dihydro-1H-inden-5-yl)-2-oxopyrrolidin-3-yl]-6-chloronaphthalene-2-sulfonamide
-
-
N-[(3S)-1-[(1,6-diaminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
-
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]-7-methoxynaphthalene-2-sulfonamide
-
-
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
-
N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
-
N-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]glycine
-
-
N-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycine
-
-
N-[1-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-(dimethylamino)-4-oxobutan-2-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
N-[2-([[4-(aminomethyl)cyclohexyl]methyl]amino)-2-oxo-1-phenylethyl]-3-carbamimidoylbenzamide
-
-
N-[2-([[4-(aminomethyl)cyclohexyl]methyl]amino)-2-oxoethyl]-3-carbamimidoylbenzamide
-
-
N-[2-[(4-methoxybenzoyl)amino]phenyl]-1-(pyridin-4-yl)piperidine-4-carboxamide
-
-
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-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',4',6'-trifluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
N-[3-[(3',4',5'-trifluorobiphenyl-4-yl)methoxy]phenyl]piperidine-4-carboxamide
-
-
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-(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-[2-(2-[[1-(2-fluorobenzoyl)piperidin-4-yl]oxy]phenyl)-2-oxoethyl]pyridin-3-yl]-4-methoxybenzamide
-
-
N1-(4-bromophenyl)-3-methoxy-N2-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)azetidine-1,2-dicarboxamide
-
-
N2,N2-dimethyl-N5-[[(2-methyl-1-benzofuran-5-yl)amino]([2-oxo-1-[2-oxo-2-(pyrrolidin-1-yl)ethyl]azepan-3-yl]amino)methylidene]pyridine-2,5-dicarboxamide
-
-
N2-(benzylsulfonyl)-D-arginyl-N-[(2S)-5-carbamimidamido-1-hydroxypentan-2-yl]glycinamide
-
-
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(1-methyl-4,5-dihydro-1H-imidazol-2-yl)phenyl]glycinamide
-
-
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]-D-norvalinamide
-
-
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]norvalinamide
-
-
N2-[(4-chlorophenyl)carbamoyl]-N2-(cyclopropylmethyl)-N-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]glycinamide
-
-
N2-[(4-chlorophenyl)carbamoyl]-N2-(cyclopropylmethyl)-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]glycinamide
-
-
N2-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
N2-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N2-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycinamide
-
-
N24R
-
peptide comprising amino acids 307-348 of the factor Va heavy chain, binds to membrane-bound factor Xa and inhibits its activity
-
N5-(5-chloropyridin-2-yl)-N4-[4-(2-imino-1,3-oxazolidin-3-yl)phenyl]-2-methyl-1,3-thiazole-4,5-dicarboxamide
-
-
Nalpha-4'-amidinobenzensulfonyl-glycyl-D,L-4-amimidinophenylalanine ethyl ester
-
-
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
-
platelet factor 4
-
upon preincubation with factor Xa and heparin, platelet factor 4 at about 250 nM decreases the kcat of peptide substrate S2765 hydrolysis about fivefold and that of prothrombin activation about 25fold. In the presence of saturating fVa, inhibition of factor Xa by platelet factor is abolished, while in the presence of limiting factor Va, platelet factor 4 alters the interaction of factor Xa with factor Va. High concentrations of platelet factor 4 restore factor Xa activity toward peptide S2765 and prothrombin, indicating a dual effect of platelet factor 4 on factor Xa activities. Heparin is required to promote the formation of an fXaPF4 complex
-
PMSF
-
complete inhibition of factor Xa and 5% inhibition of prothrombinase complex activity at 1 mM
propan-2-yl 4-[(3-chloro-1H-indol-6-yl)sulfonyl]-1-[[1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl]methyl]-6-oxopiperazine-2-carboxylate
-
-
protein inhibitor C
-
presence of heparin enhances inhibition up to 42fold in the presence of a physiological Ca2+ concentration. In the absence of Ca2+, no enhancement of inhibition is observed
-
protein 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
-
ProTS195A
-
the prothrombin mutant also does inhibit thrombin generation, but with a much smaller effect compared to that with FPR-ProT
-
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
-
RPR128515
compound contains a benzamidine moiety and surrogate of the basic group, binds in a canonical fashion typical for synthetic serine protease inhibitors, no direct hydrogen bonding with the carboxylate of Asp189 at the bottom of the S1 pocket, binding mode and inhibition mechanism; i.e. 3-[(3'-aminomethyl-biphenyl-4-carbonyl)-amino]-2-(3-carbamimidoyl-benzyl)-butyric acid methyl ester
RPR131247
compound contains a benzamidine moiety and surrogate of the basic group, binds in a canonical fashion typical for synthetic serine protease inhibitors, no direct hydrogen bonding with the carboxylate of Asp189 at the bottom of the S1 pocket, binding mode and inhibition mechanism
RPR132747
i.e. 3-[4-(6-chloro-benzo[b]thiophene-2-sulfonyl)-2-oxo-piperazin-1-ylmethyl]-benzamidine, non-peptide inhibitor based on a sulfonylpiperazinone scaffold
RPR200095
i.e. 4-[4-(6-chloro-benzo[b]thiophene-2-sulfonyl)-2-oxo-piperazin-1-ylmethyl]-benzamidine
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
SR90107A/ORG31540
-
synthetic pentasaccharide, selective, antithrombin-III dependent factor Xa inhibitor, inhibition of platelet and fibrin deposition onshunts in vivo, prevention of thrombosis
tert-butyl [(3S,4R)-1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-4-(trifluoromethyl)pyrrolidin-3-yl]carbamate
-
-
therostasin
-
highly specific, natural, tight-binding inhibitor, 5200fold purified from the rhynchobdellid leech Theromyzon tessulatum, DNA and amino acid sequence determination and analysis, protein of 8990 Da encoded by 825 bp, SwissProt accession number P82355, GenBank accession number AF239803, causes a 4fold increase in blood clotting velocity
-
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
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
Viperidae snake venom group IIA secreted phospholipases A2
i.e. SVPLA2, different isoforms, overview, FXa strong-binding SVPLA2s CBc, MtxII, CbII and CBa2 inactivate factor Xa by direct binding and by interacting with FXa by the non-catalytic phospholipid-independent mechanism, identification of the potential FXa binding site, overview
-
ZK-816042
CI-1031, 183305-24-0, amidine-imidazole inhibitor, inhibitor conformation and binding mode to the enzyme is investigated by NMR structure determination of the lyophilized enzyme-inhibitor complex formed in presence of stabilizing excipients
[2-([4-[(5S)-5-([[(5-chlorothiophen-2-yl)carbonyl]amino]methyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]amino)ethoxy]acetic acid
-
-
[4-[(5-chloro-1H-indol-2-yl)sulfonyl]piperazin-1-yl](5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)methanone
-
-
[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol
[[4-(2-[[(5-carbamimidoyl-2-hydroxyphenyl)sulfonyl]amino]ethyl)-2'-(methylsulfonyl)biphenyl-3-yl]oxy]acetic acid
-
-
(1S,3R,4S)-4-[(1H-indol-2-ylcarbonyl)amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
-
100% remaining rate after 5 min incubation with human liver microsomes
(1S,3R,4S)-4-[(1H-indol-2-ylcarbonyl)amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
-
less oral availability than compound N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, more metabolically stable
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
i.e. GW813893. More than 90fold selective over all enzymes tested, including thrombin, factor IXa, factor XIa, kallikrein, plasmin and several more
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
i.e. GW813893. Suppresses thrombotic activity correlating with the suppression of plasma-based clotting activity and the inhibition of plasma factor Xa activity. Inhibitor is orally active
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
i.e. GW813893. Suppresses thrombotic activity correlating with the suppression of plasma-based clotting activity and the inhibition of plasma factor Xa activity. Inhibitor is orally active
(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid
-
i.e. R-142086. Exhibits potent anti-factor Xa activity and anticoagulant activity when administered orally
(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid
-
potent anticoagulant activity, no mutagenic potential and high selectivity for factor Xa over trypsin
1,2-dicaproyl-sn-glycero-3-phospho-L-serine
-
i.e. C6PS, soluble phospholipid, inhibition of amidolytic activity of factor Xa in absence of Ca2+
1,2-dicaproyl-sn-glycero-3-phospho-L-serine
-
presence of 1,2-dicaproyl-sn-glycero-3-phospho-L-serine and 5 mM Ca2+ results in dimerization with concomitant decrease in kcat value. Binding of 1,2-dicaproyl-sn-glycero-3-phospho-L-serine exposes residues K351. K242, and K420
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
selective for factor Xa over thrombin, trypsin, plasmin, and tissue plasminogen activator
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
-
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
inhibitor shows bioavailability under both fasted and fed conditions
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
inhibitor shows bioavailability under both fasted and fed conditions and antithrombotic efficacy in a rat model of venous thrombosis after oral administration, without a significant increase in bleeding time
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
i.e. FXV673, highly specific fo factor Xa compared to other serine protesases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, inhibition of thrombus formation in vivo in the acute arterial and venous electrolytic injury canine model, no effect on platelet aggregation
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
i.e. FXV673, highly specific fo factor Xa compared to other serine proteases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, no effect on platelet aggregation
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
i.e. FXV673, highly specific fo factor Xa compared to other serine protesases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, no effect on platelet aggregation
4-aminobenzamidine
-
90% inhibition of factor Xa and 2% inhibition of prothrombinase complex activity at 1 mM
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate
-
i.e. JTV-803, strong, synthetic inhibitor highly specific for factor Xa compared to other serine proteases
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate
-
i.e. JTV-803, synthetic the enzyme in vitro and thrombus formation in rats in vivo
antistasin
-
naturally occurring inhibitor, anticoagulant isolated from Mexican leech Haementeria officinalis, slow, tight-binding, selective inhibitor protein
-
antistasin
-
the inhibitor exerts its inhibitory effect at a site removed from the active site of factor Xa
-
antithrombin
-
Arg150 of the autolysis loop is involved in specific interaction with the activated conformation of antithrombin
-
antithrombin
-
i.e. HAT, serpin, human, recombinant from expression in human 293 cells, inhibition is increased by heparin
-
antithrombin
-
inhibition is enhanced by heparin. Ca2+ increases about 3fold the inhibition rate of wild-type recombinant enzyme over that in presence of EDTA
-
antithrombin
-
human recombinant protein, competitive inhibition, heparin-activated antithrombin, interaction and inhibition mechanism involving inhibitor residues Tyr253, as well as Glu255, Glu237, and Arg399, and exosites generated via heparin binding, rapid kinetic studies, wild-type and mutant antithrombins, overview
-
antithrombin
-
allosteric activation of antithrombin as a factor IXa and Xa inhibitor requires binding of a high-affinity heparin pentasaccharide and involves mitigation of repression rather than positive enhancement, via a mechanism in which heparin activates antithrombin by mitigating an unfavorable surface interaction, by altering its nature, and by moving the attached proteinase away from the site of the unfavorable interaction through RCL expulsion, detailed overview
-
antithrombin
-
heparin and antithrombin-binding sulfated pentasaccharide DEFGH, and derivatives thereof, activate antithrombin, design of two tetra-sulfated N-arylacyl tetrahydroisoquinoline variants as potential nonsaccharide activators of antithrombin, binding affinities, kinetics, and binding sites, modeling, overview. Second-order rate constants of antithrombin inhibition of factor Xa in the presence and absence of the designed activators show antithrombin activation in the range of 8-80fold at pH 6.0
-
antithrombin III
-
AT3, a member of the serpin superfamily of protease inhibitors, X-ray crystal structure-based simulations of AT3/FXa, PDB code 2GD4, overview
-
antithrombin III
-
90% inhibition of factor Xa at 0.01 mg/ml in presence of heparin and 5% inhibition of prothrombinase complex activity at 1 U/ml
-
apixaban
-
inhibitor does not alter platelet aggregation to ADP, gamma-thrombin, and collagen
apixaban
-
an oral, direct, and highly selective factor Xa inhibitor in late-stage clinical development for the prevention and treatment of thromboembolic diseases. Evaluation of the metabolic drug-drug interaction potential of apixaban in vitro, overview. Apixaban shows a slow metabolic turnover in incubations of human liver microsomes with formation of O-demethylation and hydroxylation products as prominent in vitro metabolites
apixaban
-
i.e. BMS-562247, a small molecule able to inhibit in a selective and reversible manner the active site of both free and prothrombinase-bound factor Xa, requires oraladministration, bleeding rates of 0.69%
apixaban
-
a direct, oral applicable, selective factor Xa inhibitor and activated prothrombinase, reversible and potent inhibition of both free and cell bound factor Xa. It has low potential for drug-drug interactions and is predominantly eliminated through metabolic pathways and non-renal mechanisms
apixaban
-
study on use for prevention of arterial thrombosis in rabbit models of electrically induced carotid artery thrombosis and cuticle bleeding time. Addition of aspirin to apixaban significally reduces the thrombus weight with no significant increase in bleeding time. Addition of aspirin and apixaban to clopidogrel produces a further significant reduction in thrombus weight. Combination of clopidogrel and aspirin with apixaban produces a significant but moderate 2.1fold increase in bleeding time
apixaban
-
inhibitor does not alter platelet aggregation to ADP, gamma-thrombin, and collagen. In vivo, apixaban is effective in the prevention of experimental thrombosis at doses that preserve hemostasis
apixaban
-
i.e. BMS-562247 or 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5-dihydropyrazolo[5,4-c]pyridine-3-carboxamide. Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban. Oxidative metabolism of radiolabeled apixaban by liver microsomes is approximately 20times faster in rabbits than in rats or humans. Prominant metabolites are O-demethyl apixaban, O-demethyl apixaban glucuronide and O-demethyl apixaban sulfate, metabolic profiles, overview
Ca2+
-
presence of heparin enhances inhibition by protein inhibitor C up to 42fold in the presence of a physiological Ca2+ concentration. In the absence of Ca2+, no enhancement of inhibition is observed
Ca2+
-
the strength of the dimer interaction is strongly Ca2+-concentration-dependent, such that significant dimer forms in solution only at or above 5 mM Ca2+
CI-1031
-
i.e. ZK-807834, small molecule direct inhibitor of facor Xa, prevention of thrombosis when administered in vivo
diisopropylfluorophosphate
-
2.5 mM: 10% inhibition of factor Xa and 95% inhibition of prothrombinase complex activity, 10 mM: 90% inhibition of factor Xa and 95% inhibition of prothrombinase complex activity
DX-9065a
-
synthetic selective inhibitor of coagulation factor Xa strongly inhibits thrombin generation without affecting initial thrombin forming time necessary for platelet activation in hemostasis
DX-9065a
-
inhibits factor Xa increased thymidine incorporation in mesangial cells, inhibits activation of extracellular regulated kinase in mesangial cells
DX-9065a
-
i.e. (2S)-2[4-[[(3S)-1-acetimidoyl-3-pyrrolidinyl]oxy]phenyl]-3-(7-amidino-2-naphthyl) propanoic acid hydrochloride pentahydrate, a specific factor Xa inhibitor, DX-9065a treatment significantly ameliorated proteinuria in vivo in rats with a significant reduction in the size of glomeruli, the total number of glomerular cells, and crescent formation, as well as abolishing the phosphorylation of p44/42 MAP kinase on day 8
DX9065a
-
small, potent and selective direct inhibitor of fXa, prevents thrombosis in vivo
fondaparinux
does not inhibit FXa-mediated cleavage of SARS CoV-2 spike protein
fondaparinux
does not inhibit FXa-mediated cleavage of SARS CoV-2 spike protein
FXV673
-
small molecule direct inhibitor of facor Xa, prevention of thrombosis when administered in vivo
heparin
-
highly increases the inhibitory effects of glycoprotein IIb/IIIa receptor-antagonists
heparin
inhibition via complex formation with and modulation of the activity of thrombin
idraparinux
-
a synthetic pentasaccharide and long-acting, indirect, specific antithrombin-dependent factor Xa inhibitor, population pharmacokinetic modelling and analysis from phase III clinical trials, investigation in the treatment and prevention of thromboembolic events
LY517717
-
a direct factor Xa inhibitor, requires oraladministration, with an oral bioavailability of 25-82%. LY517717 is apparently primarily cleared via a gastrointestinal route
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate
-
i.e. RPR208566, highly specific
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate
-
i.e. RPR208566, inhibits thrombus formation in the rat artery model, highly specific
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
i.e. DU-176b. Presence prolongs the activated partial thromboplastin time, prothrombin time and thrombin time in plasma. It does not impair human platelet aggregation induced by ADP or thromboxane A2 receptor agonist U46619. Thrombin-induced platelet aggregation is inhibited with IC50 value of 2.9 microM
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
i.e. DU-176b. Dose-dependently inhibits thrombus formation in a rabbit thrombosis model
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
i.e. DU-176b dose-dependently inhibits thrombus formation in a rat thrombosis model. Bleeding time in rats is not significantly prolonged at an antithrombotic dose
N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
46% remaining rate after 5 min incubation with human liver microsomes
N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
higher oral availability than compounds (1S,3R,4S)-4-[(1H-indol-2-ylcarbonyl)amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid, N-[(1R,2S,5S)-2-[(1H-indol-2-ylcarbonyl)amino]-5-(methylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, less metabolically stable
N-[(1R,2S,5S)-2-[(1H-indol-2-ylcarbonyl)amino]-5-(methylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
63% remaining rate after 5 min incubation with human liver microsomes
N-[(1R,2S,5S)-2-[(1H-indol-2-ylcarbonyl)amino]-5-(methylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
less oral availability than compound N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, more metabolically stable
PD0313052
-
slow, tight-binding mechanism, factor Xa; slow, tight-binding mechanism, prothrombinase
PD0313052
-
i.e. [(2R, 6S)-2-(5-carbamimidoyl-2-hydroxy-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-quinoxaline-6-carboxylic acid]
protein Z-dependent protease inhibitor
-
inhibition by branched pathway acyl-intermediate trapping mechanism. Reaction proceeds by the initial assembly of a membrane-associated protein Z-protein Z-dependent protease inhibitor-factor Xa Michaelis complex followed by conversion to a stable protein Z-dependent protease inhibitor-factor Xa complex. Assembly of the Michaelis complex is rate-limiting. For every factor Xa molecule inhibited, two inhibitor molecules are cleaved. Protein Z dissociates from protein Z-dependent inhibitor once a stable complex with factor Xa is formed. It acts catalytically to accelerate the membrane-dependent protein Z-dependent protease-factor Xa reaction
-
protein Z-dependent protease inhibitor
-
ZPI, UniProt ID Q9UK55, a member of the serpin superfamily of protease inhibitors, ZPI can produce rapid inhibition of FXa in the presence of the not-essential cofactor protein Z, negatively charged phospholipids and Ca2+ ions, mechanism. Generation of a three-dimensional structural model of the Michaelis complex of human ZPI/FXa using homology modeling, protein-protein docking and molecular dynamics simulation methods, overview
-
rivaroxaban
-
i.e. 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide or BAY 597939, an oral, direct factor Xa inhibitor for the prevention and treatment of thromboembolic disorders, in vitro metabolism and pathways, detailed overview
rivaroxaban
-
sensitive and specific quantification in human plasma by high-performance liquid chromatography-tandem mass spectrometry. Concentrations between 0.5 and 500 micrograms per liter can be detected. Inter-assay precision is below 7.4% and inter-assay accuracy is between 96.3% and 102.9%
rivaroxaban
-
an oral direct factor Xa inhibitor, in advanced development as an alternative to warfarin for the prevention and treatment of thromboembolic disorders
rivaroxaban
-
i.e. 5-chloro-N-[[(2S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxaziolidin-5-yl]methyl]thiophene-2-carboxamide, an small molecule oral factor Xa inhibitor, binds factor Xa rapidly and reversibly, mode of binding, pharmacodynamics and pharmacokinetics, overview
rivaroxaban
-
an oral inhibitor, safety, pharmacokinetics and pharmacodynamics of single/multiple doses of the oral, direct factor Xa inhibitor rivaroxaban in healthy male Chinese individuals, overview
rivaroxaban
-
i.e. 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide or BAY 597939, an oral, direct factor Xa inhibitor for the prevention and treatment of thromboembolic disorders, in vitro metabolism and pathways, detailed overview
rivaroxaban
-
i.e. BAY 59-7939, requires oraladministration. It is absorbed in the gastrointestinal tract, is primarily excreted by the kidneys, and has a bioavailability of more than 80%, and bleeding rates of 4.3-10.2%
rivaroxaban
inhibits FXa-mediated cleavage of SARS CoV-2 spike protein and facilitates viral entry
rivaroxaban
inhibits FXa-mediated cleavage of SARS CoV-2 spike protein and facilitates viral entry
rivaroxaban
-
i.e. 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide or BAY 597939, an oral, direct factor Xa inhibitor for the prevention and treatment of thromboembolic disorders, in vitro metabolism and pathways, detailed overview
Soybean trypsin inhibitor
-
complete inhibition of factor Xa and 5% inhibition of prothrombinase complex activity at 0.01 mg/ml
-
TAK-442
-
potent factor Xa/prothrombinase inhibitor, acts synergistically with aspirin or clopidogrel in preventing arterial thrombosis and whole blood coagulation. TAK-442, aspirin, or clopidogrel alone have no significant effect on thrombus formation, whereas the combination of TAK-442 with aspirin and clopidogrel remarkably prolonge the time to thrombus formation without additional significant prolongation of bleeding time
tick anticoagulant peptide
-
inhibition is thermodynamically favored when the enzyme is assembled in the prothrombinase complex
-
tick anticoagulant peptide
-
i.e. TAP, 60 amino acid peptide, isolated from the tick Ornithodoros moubata, reversible, slow, tight-binding inhibitor, short-term inhibition of clot-associated procoagulant activity in vitro and in vivo
-
tick anticoagulant peptide
-
a slow, tight-binding specific inhibitor. The inhibitor is purified from extracts of Ornithodoros moubata
-
YM150
-
a direct inhibitor of factor Xa, requires oraladministration,bleeding rate is 11.8-23.5%
[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol
-
selective and orally bioavailable inhibitor
[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol
-
good oral bioavailability after oral administration at a dose of 3 mg/kg in fasted monkeys. Pharmakokinetics study
additional information
-
inhibition potential of overlapping peptides within the region of amino acids 307-348 of factor Va heavy chain
-
additional information
-
no inhibition by the Bauhinia variegata trypsin inhibitor BvTI
-
additional information
neutral groups such as chlorobenzohtiophene or chlorothiophene and basic groups such as benzamidine interact in the S1 pocket through the neutral group whereas the S4 pocket is occupied by the basic moiety
-
additional information
-
neutral groups such as chlorobenzohtiophene or chlorothiophene and basic groups such as benzamidine interact in the S1 pocket through the neutral group whereas the S4 pocket is occupied by the basic moiety
-
additional information
-
structure-activity relationship, development and synthesis of zinc-binding independent inhibitors, overview
-
additional information
-
inhibitory effect, oral bioavailability and pharmakokinetic profile of DPC423 derivatives, overview
-
additional information
binding mode of dual specific inhibitors, with a N-methyl-benzimidazole scaffold, of thrombin and factor Xa, overview
-
additional information
-
binding mode of dual specific inhibitors, with a N-methyl-benzimidazole scaffold, of thrombin and factor Xa, overview
-
additional information
-
potencies of inhibitor molecules and anticoagulant activities, overview
-
additional information
-
inhibitors of blood coagulation factors Xa and IIa, i.e. PD0313052 and argatroban, synergize to reduce thrombus weight and thrombin generation in vivo and in vitro
-
additional information
-
development of phenyltriazolinone inhibitors, X-ray structure analysis and binding structure, overview
-
additional information
-
rational design of small-molecule direct fXa inhibitors, synthesis, overview
-
additional information
-
clinical studies, efficacy and safety of factor Xa inhibitors, overview
-
additional information
-
factor Xa acts as anticoagulants, clinical studies, overview
-
additional information
-
synthesis of a series of benzyloxy anilides of nipecotic and isonipecotic acids, as inhibitors of ADP-induced platelet aggregation and the blood coagulation enzyme factor Xa
-
additional information
-
structure and property based design of factor Xa pyrrolidin-2-one inhibitors with aminoindane and phenylpyrrolidine P4 motifs, rational design, syntheses and evaluation, overview
-
additional information
-
evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs, overview
-
additional information
-
design, synthesis, and structure-activity relationship of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors
-
additional information
-
development of direct FXa inhibitors, overview. Selectivity is a significant issue in the development of factor Xa inhibitors, since several trypsin-like serine proteases play key regulatory roles in the coagulation cascade, among them FVIIa, FIXa, FXa, FXIa, and thrombin
-
additional information
-
sulfated low-molecular weight lignins CDSO3, FDSO3, SDSO3, and unfractionated heparin inhibit thrombin and factor Xa through allosteric disruption of the catalytic apparatus, specifically through the catalytic step
-
additional information
using structural alignment, molecular docking, and pharmacophore modeling, the selectivity of a ligand for FIXa over FXa may be defined quantitatively as a docking score of lower than -8.0 kcal/mol in the FIXa-grids and higher than -7.5 kcal/mol in the FXa-grids
-
additional information
-
benzamidine functionally is a common theme in most classes of inhibitors, with many of the most potent compounds requiring two basic functional groups to afford potent inhibition. Reliance on this structural feature may afford difficulty in obtaining inhibitors with acceptable oral absorption and with sufficiant duration of action to qualify as clinical candidates for oral anticoagulant trials
-
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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-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
1,2-dioleoyl-sn-glycero-3-phosphoethanolamine
-
activates prothrombinase activity after enzyme binding to membranes, binding to model membranes, binding of prothrombinase via factor Va, overview. 1,2-diphytanoyl-sn-glycero-3-phosphocholine deminishes activation by 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine
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+
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+
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
-
1,2-dicaproyl-sn-glycero-3-phospho-L-serine
-
i.e. C6PS, binding constants in presence of Ca2+
1,2-dicaproyl-sn-glycero-3-phospho-L-serine
-
the cofactor activity of factor Va is enhanced in presence of 1,2-dicaproyl-sn-glycero-3-phospho-L-serine. Both C1 and C2 domains of factor Va bind one molecule of 1,2-dicaproyl-sn-glycero-3-phospho-L-serine, with binding to the C1 domain regulating prothrombinase complex assembly
Ca2+
-
binding to the enzyme stabilizes the binding of Na+, required for prothrombinase complex formation
Factor V
-
factor Xa forms the prothrombin-converting complex with factor V, phospholipid and 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 V
Q56VR3; Q7SZN0
PEGylation labeling efficiency of diverse ptfV Cys mutant variants, overview
-
Factor Va
-
expression of factor Va with mutations in either the C1 domain, Y1956A/L1957A, the C2 domain, W2063A/W2064A, or both C domains, Y1956A/L1957A/W2063A/W2064A. Mutations in the C1 and C1-C2 domains of recombinant factor Va reduce the rate of activation of prothrombin to thrombin by factor Xa in the presence of 1,2-dicaproyl-sn-glycero-3-phospho-L-serine by 14000- to 15000fold relative to either wild-type or C2 mutant factor Va. The Kd values of factor Xa binding with factor Va wild-type, C2 mutant, C1 mutant, and C1-C2 mutant are 3, 4, 564, and 624 nM, respectively
-
Factor Va
-
the Na+ and factor Va binding sites are energetically linked. A cofactor function for factor Va in the prothrombinase complex involves inducing a conformational change in the 220-loop of factor Xa that appears to stabilize this loop in the Na+-bound conformation
-
Factor Va
-
kcat values of prothrombinase assembled with cofactor factor Va mutants D334K/Y335F or D334A/Y335A is reduced. Prothrombinase assembled with quadruple mutant molecules E323Y/E330Y/D334K/Y335F or E323Y/E330Y/D334A/Y335A displays a second-order rate constant up to 400fold lower than the value obtained with wild-type factor Va
-
Factor Va
-
interaction of factor Va with factor Xa on a membrane or cell surface in the presence of divalent metal ions and formation of the prothrombinase complex results in the reversal of the order of cleavage and a 300000fold increase in the catalytic efficiency of factor Xa for thrombin generation, structural contribution of the acidic COOH-terminal region of factor Va heavy chain to factor Xa activity within prothrombinase, overview. Functional properties and kinetics of different recombinant factor Va molecules, wild-type and mutants. Mutant factor VaDELTA659-663, factor Va5K, and factor V5A display 3.5, 11, and 24fold less clotting activity, respectively, than wild-type factor Va. Wild-type Va has a similar affinity for the factor Xa as its plasma counterpart
-
Factor Va
-
absolutely required for activity as part of the prothrombinase complex
-
Na+
-
bound by Tyr225 of the wild-type enzyme, stimulation of amidolytic activity cleaving small synthetic substrates, kinetics, temperature dependence of dissociation constants in absence and presence of Ca2+, mutant GDFXa Y225P is 2fold less stimulatable, can only partly be replaced by other monovalent cations
Phospholipid
-
factor Xa forms the prothrombin-converting complex with factor V, phospholipid and Ca2+
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
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
additional information
-
no activation of CA2+ responses by tissue factor TF or factor VIIa
-
additional information
-
specificity for phosphatidylserine analogues, bound to a pair of linked lipid binding sites involved in regulation of enzyme activity, binding structure and specificity of the 2 binding sites, cooperative and competitive binding
-
additional information
-
formation of the prothrombinase enzyme complex increases the factor Xa activity by 300000fold, the complex includes phospholipids, Ca2+, factor Xa and factor Va
-
additional information
-
prothrombinase enhancement through quantitative and qualitative changes affecting very low density lipoprotein in complex with C-reactive protein
-
additional information
-
no activation of CA2+ responses by tissue factor TF or factor VIIa
-
additional information
-
the presence of prothrombin-derived fragment 1 accelerates both the rate of cleavage at residues R320 of prethrombin 1 and thrombin formation by prothrombinase
-
additional information
-
factor Xa must bind to phosphatidylserine-containing membranes to produce thrombin at a physiologically significant rate
-
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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
-
0.061
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
0.0045
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
0.000071
ProTS195A
-
pH 7.7, 37°C, versus prothrombin, in absence of phospholipid
-
0.0965
benzoyl-Ile-Glu(piperidineamide)-Gly-Arg-p-nitroanilide
-
enzyme from which the residues 1-44 of the light chain have been removed by chymotryptic proteolysis
0.189
benzoyl-Ile-Glu-(-H/OMe)-Gly-Arg-p-nitroanilide
-
enzyme from which the residues 1-44 of the light chain have been removed by chymotryptic proteolysis
0.00058
fragment 1.2:prethrombin-2
-
pH 7.4, 22°C, in presence of 20 mM factor Va
-
0.072
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
native factor Xa, pH 7.5
0.089
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
recombinant factor Xa, pH 7.5
0.13
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
prothrombinase assembled with recombinant factor Xa, pH 7.5
0.17
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
prothrombinase assembled with native factor Xa, pH 7.5
0.29
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
prothrombinase assembled with mutant I16L, pH 7.5
0.49
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
prothrombinase assembled with mutant V17A, pH 7.5
1.15
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
mutant I16L, pH 7.5
1.38
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
mutant V17A, pH 7.5
0.042
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
pH 7.4, 23°C, in presence of 0.001 mM heparin
0.057
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
pH 7.4, 23°C, in absence of heparin
0.065
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant mutant R150A, 22°C
0.068
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant mutant R143A, 22°C
0.069
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant mutant K147A, 22°C
0.083
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant wild-type enzyme, 22°C
0.09
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
native wild-type enzyme, 22°C
0.122
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant mutant R154A, 22°C
0.0052
prethrombin-1
-
prothrombinase assembled with recombinant factor Xa, pH 7.5
-
0.00035
prothrombin
-
prothrombinase assembled with recombinant factor Xa, pH 7.5
-
0.00036
recombinant prothrombin R155A/R284A/R271A mutant rMZ-II
-
pH 7.4, 22°C, in presence of 20 mM factor Va
-
0.00045
recombinant prothrombin R155A/R284A/R271A mutant rMZ-II
-
pH 7.4, 22°C, in absence of factor Va
-
0.00039
recombinant prothrombin R155A/R284A/R320A mutant rP2-II
-
pH 7.4, 22°C, in presence of 20 mM factor Va
-
0.0005
recombinant prothrombin R155A/R284A/R320A mutant rP2-II
-
pH 7.4, 22°C, in absence of factor Va
-
0.097
tosyl-glycyl-prolyl-D-arginine-4-nitroanilide
-
pH 7.4, 23°C, in presence of 0.001 mM heparin
0.206
tosyl-glycyl-prolyl-D-arginine-4-nitroanilide
-
pH 7.4, 23°C, in absence of heparin
additional information
additional information
-
substrate specificity for amino acid residues at positions P3, P2, P1', P2', and P3', overview
-
additional information
additional information
-
kinetics, dissociation constants
-
additional information
additional information
-
binding kinetics of heparin and other glycosaminoglycans to the active site-blocked enzyme
-
additional information
additional information
-
kinetics of FVIIIa inactivation
-
additional information
additional information
FXa binding kinetic parameters and effect on prothrombinase activity of Viperidae SVPLA2 isoforms, overview
-
additional information
additional information
-
FXa binding kinetic parameters and effect on prothrombinase activity of Viperidae SVPLA2 isoforms, overview
-
additional information
additional information
-
kinetics with wild-type and mutant prothrombin substrates, overview
-
additional information
additional information
-
kinetics of prothrombinase, methematical analysis, overview
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
149
benzoyl-Ile-Glu(piperidineamide)-Gly-Arg-p-nitroanilide
-
enzyme from which the residues 1-44 of the light chain have been removed by chymotryptic proteolysis
140
benzoyl-Ile-Glu-(-H/OMe)-Gly-Arg-p-nitroanilide
-
enzyme from which the residues 1-44 of the light chain have been removed by chymotryptic proteolysis
33
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
prothrombinase assembled with mutant I16L, pH 7.5
72
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
prothrombinase assembled with native factor Xa, pH 7.5
91
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
prothrombinase assembled with mutant V17A, pH 7.5
140
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
native factor Xa, pH 7.5
140
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
prothrombinase assembled with recombinant factor Xa, pH 7.5
210
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide
-
recombinant factor Xa, pH 7.5
1.4
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant mutant R143A, 22°C
21
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant mutant R150A, 22°C
55
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant mutant K147A, 22°C
98.6
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant mutant R143A, 22°C
121
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
native wild-type enzyme, 22°C
126.5
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant wild-type enzyme, 22°C
127
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant wild-type enzyme, 22°C
144
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
pH 7.4, 23°C, in presence of 0.001 mM heparin
169
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
pH 7.4, 23°C, in absence of heparin
411
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide
-
recombinant mutant R154A, 22°C
17.5
prethrombin-1
-
prothrombinase assembled with recombinant factor Xa, pH 7.5
-
0.6
prothrombin
-
pH 7.4, 25°C, mutant enzyme E36Q/E37Q/E39Q, activated by factor Va
-
0.6
prothrombin
-
pH 7.4, 25°C, mutant enzyme E36K/E37K/E39K, activated by factor Va
-
7.3
prothrombin
-
pH 7.4, 25°C, mutant enzyme E74K/E76K/E77K, activated by factor Va
-
10.5
prothrombin
-
pH 7.4, 25°C, mutant enzyme E74Q, E76Q/E77Q, activated by factor Va
-
32.3
prothrombin
-
prothrombinase assembled with recombinant factor Xa, pH 7.5
-
0.0068
recombinant prothrombin R155A/R284A/R271A mutant rMZ-II
-
pH 7.4, 22°C, in absence of factor Va
-
110
recombinant prothrombin R155A/R284A/R271A mutant rMZ-II
-
pH 7.4, 22°C, in presence of 20 mM factor Va
-
0.324
recombinant prothrombin R155A/R284A/R320A mutant rP2-II
-
pH 7.4, 22°C, in absence of factor Va
-
114
recombinant prothrombin R155A/R284A/R320A mutant rP2-II
-
pH 7.4, 22°C, in presence of 20 mM factor Va
-
46
tosyl-glycyl-prolyl-D-arginine-4-nitroanilide
-
pH 7.4, 23°C, in presence of 0.001 mM heparin
79
tosyl-glycyl-prolyl-D-arginine-4-nitroanilide
-
pH 7.4, 23°C, in absence of heparin
additional information
additional information
-
kcat values of prothrombinase assembled with mutant cofactor factor Va D334K/Y335F or D334A/Y335A is reduced. Prothrombinase assembled with quadruple mutant molecules E323Y/E330Y/D334K/Y335F or E323Y/E330Y/D334A/Y335A displays a second-order rate constant up to 400fold lower than the value obtained with wild-type factor Va
-
additional information
prothrombin
-
and monomer. Dimer is about 1000000fold less active toward prothrombin than the monomer, mainly due to a substantial decrease in kcat. Dimerization results in substantial change in tertiary or quarternary structure with a concomitant decrease in alpha-helix
-
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Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000272
(2RS)-(3'-amidino-3-biphenyl)-5-(4-pyridylamino)pentanoic acid
i.e. FX-2212
0.0000017
(3-[[(3-carbamimidoylphenyl)(2-[[4-(1-ethanimidoylpiperidin-4-yl)phenyl]amino]-2-oxoethyl)amino]methyl]phenoxy)acetic acid
-
pH and temperature not specified in the publication
0.00000055
(4S,5S)-3-(3-carbamimidoylphenyl)-5-(methoxymethyl)-N-(2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1,2-oxazole-4-carboxamide
-
pH and temperature not specified in the publication
0.000004 - 0.0000097
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
0.0000003
(E)-2-(5-chlorothiophen-2-yl)-N-(1-[5-[2-(methylsulfonyl)phenyl]pyridin-2-yl]-2-oxopyrrolidin-3-yl)ethenesulfonamide
-
pH and temperature not specified in the publication
0.000001
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000006
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000013
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(6-fluoro-2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000002
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000015
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000006
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000008
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000001
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000005
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000003
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000006
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000002
(E)-2-(5-chlorothiophen-2-yl)-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.000004
(E)-2-(5-chlorothiophen-2-yl)-N-[1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000002
(E)-2-(5-chlorothiophen-2-yl)-N-[1-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.0000055
(E)-2-(5-chlorothiophen-2-yl)-N-[[(3R)-1-[[1-(pyridin-4-yl)piperidin-4-yl]carbonyl]pyrrolidin-3-yl]methyl]ethenesulfonamide
-
pH and temperature not specified in the publication
0.00054
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-4-cyanobenzylpropionamide
-
pH 8.0, 25°C
0.00017
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-4-hydroxyphenethylpropionamide
-
pH 8.0, 25°C
0.00022
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-benzylpropionamide
-
pH 8.0, 25°C
0.00034
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-ethyl-propionamide
-
pH 8.0, 25°C
0.000074
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamide
-
pH 8.0, 25°C
0.00049
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-phenpropionyl-propionamide
-
pH 8.0, 25°C
0.00023
(R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-propionic acid phenethyl ester
-
pH 8.0, 25°C
0.000074
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(2-chloro)-phenethyl-propionamide
-
pH 8.0, 25°C
0.000074
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(3-chloro)-phenethyl-propionamide
-
pH 8.0, 25°C
0.00095
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(4-amino)-phenethyl-propionamide
-
pH 8.0, 25°C
0.002
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-(4-tert-butyl)-phenethyl-propionamide
-
pH 8.0, 25°C
0.000025
(R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamides
-
pH 8.0, 25°C
0.00000076
(R)-6-(2'-((3-hydroxypyrrolidin-1-yl)methyl)-[1,1'-biphenyl]-4-yl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-5,6-dihydro-1H-pyrazolo[3,4-c]pyridin-7(4H)-one
-
-
0.00235
(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
0.0000013
([(7-carbamimidoylnaphthalen-2-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
-
pH and temperature not specified in the publication
0.0012
1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[2,3-b]pyridin-2-ylsulfonyl)-piperazin-2-one
-
above
0.0012
1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-4-(thieno[3,2-b]pyridin-2-ylsulfonyl)-piperazin-2-one
-
above
0.00000004
1-(3-amino-1,2-benzisoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.00000003
1-(3-amino-1,2-benzoxazol-5-yl)-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
pH and temperature not specified in the publication
0.0000044
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-[2-[(dimethylamino)methyl]pyridin-3-yl]-2-fluorophenyl)-7-fluoro-1H-indazole-3-carboxamide
-
pH and temperature not specified in the publication
0.00000017
1-(3-amino-1,2-benzoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-5-methyl-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
pH and temperature not specified in the publication
0.00000019
1-(3-amino-1,2-benzoxazol-5-yl)-N-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.000002
1-(3-aminophenyl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000013
1-(3-carbamimidoylphenyl)-3-methyl-N-(2'-sulfamoylbiphenyl-4-yl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.000000015
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
0.000000013
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00000016
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
0.00000029
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-4-bromo-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt
-
-
0.0000008
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt
-
-
0.00000046
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(fluoro)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.000000008
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00000004
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.0000013
1-(3-[amino(imino)methyl]phenyl)-N-[2'-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00000011
1-(4-methoxyphenyl)-3-(methylsulfonyl)-6-(4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000018
1-(4-methoxyphenyl)-4-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[3,4-d]pyridazin-7-one
-
-
0.0000014
1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(1H-tetrazol-1-ylmethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.0000029
1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(2H-tetrazol-2-ylmethyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.000000054
1-(4-methoxyphenyl)-6-(4-[1-[(methylamino)methyl]cyclopropyl]phenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000055
1-(4-methoxyphenyl)-6-(4-[1-[(methylamino)methyl]cyclopropyl]phenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.000000042
1-(4-methoxyphenyl)-6-[4-(1-[[(1-methylethyl)amino]methyl]cyclopropyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000064
1-(4-methoxyphenyl)-6-[4-[1-(morpholin-4-ylmethyl)cyclopropyl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000021
1-(4-methoxyphenyl)-6-[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.00000024
1-(4-methoxyphenyl)-7-oxo-6-(4-[1-[(2-oxopyrrolidin-1-yl)methyl]cyclopropyl]phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.0000011
1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
0.00000008
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
pH and temperature not specified in the publication
0.000000074
1-(4-methoxyphenyl)-7-oxo-6-[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.0000015
1-(6-chloronaphthalen-2-yl)-N-[2'-[(dimethylamino)methyl]-3-fluorobiphenyl-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.057
1-carbamimidoyl-N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-3-carboxamide
-
pH 8.0, 25°C
0.0338
1-carbamimidoyl-N-[3-[(4-fluorobenzyl)oxy]phenyl]piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00122
1-[(4-amino-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-piperazin-2-one
-
-
0.0000008
1-[(4-aminoquinazolin-7-yl)methyl]-4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]piperazin-2-one
-
pH and temperature not specified in the publication
0.00000097
1-[1-(3-amino-1,2-benzoxazol-5-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-2-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]phenyl)ethanone
-
pH and temperature not specified in the publication
0.00000091
1-[2-(aminomethyl)phenyl]-N-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.000001
1-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide
-
pH and temperature not specified in the publication
0.0000012
1-[2-[(aminooxy)sulfinyl]phenyl]-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.021
1-[3-(5-amino-1,3,4-thiadiazol-2-yl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
above
0.0049
1-[3-(5-amino-4H-1,2,4-triazol-3-yl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
0.0000004
1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000027
1-[3-(aminomethyl)phenyl]-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt
-
-
0.000000013
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-(2'-(methylsulfonyl))-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
0.00000015
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
-
0.00000015
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.0026
1-[3-[([1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methyl)sulfonyl]phenyl]pyridinium
-
-
0.000054
1-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]urea
-
-
0.000011
1-[3-[amino(imino)methyl]phenyl]-N-[2'-(aminosulfonyl)[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide
-
-
0.00026
1-[4-amino-3-[([1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methyl)sulfonyl]phenyl]pyridinium
-
-
0.000003
1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide
-
pH and temperature not specified in the publication
0.000008
1H-pyrrolo[3,2-c]pyridine-1-acetamide, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-
-
-
0.000154
1H-pyrrolo[3,2-c]pyridine-1-acetic acid, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-
-
-
0.000018
1H-pyrrolo[3,2-c]pyridine-1-acetic acid, 2-[[4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-2-oxo-1-piperazinyl]methyl]-, methyl ester
-
-
0.00057
2,2'-ethane-1,2-diylbis(1-benzofuran-5-carboximidamide)
-
pH and temperature not specified in the publication
0.0000005
2-(1-[(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2-hydroxypropanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
pH and temperature not specified in the publication
0.000002
2-(1-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
-
pH and temperature not specified in the publication
0.00021
2-(2-hydroxy-5-methylbiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.03
2-(2-hydroxyphenyl)3-methyl-3H-benzoimidazole-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
0.00000001
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-bromo-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.000000009
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-chloro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.00000002
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.000000005
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.000000007
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide
-
-
0.000000041
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide
-
-
0.000000008
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide
-
-
0.000000005
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide
-
below
0.000000005
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide
-
below
0.000000009
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide
-
-
0.00000001
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide
-
-
0.00021
2-(5-bromo-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.00034
2-(5-chloro-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.000014
2-(5-nitro-2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
-
pH 7.4, 22°C
0.00000027 - 0.00000141
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
0.0000065
2-cyano-1-(2-methyl-1-benzofuran-5-yl)-3-[2-oxo-1-[2-oxo-2-(pyrrolidin-1-yl)ethyl]azepan-3-yl]guanidine
-
pH and temperature not specified in the publication
0.0000027
2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
0.0000004
2-[6-[3-([[(E)-2-(5-chlorothiophen-2-yl)ethenyl]sulfonyl]amino)-2-oxopyrrolidin-1-yl]pyridin-3-yl]benzenesulfonamide
-
pH and temperature not specified in the publication
0.00000013
2-[N2-(benzylsulfonyl)-D-arginylglycyl-L-arginyl]-1,3-thiazole
-
pH and temperature not specified in the publication
0.0000115
2-[[4-(dimethylamino)benzoyl]amino]-N-(5-methoxypyridin-2-yl)-5-[(methylsulfonyl)amino]benzamide
-
pH and temperature not specified in the publication
0.0000235
3-(1-[5-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-pentyl]-2-oxo-1,2-dihydroquinolin-3-yl)-4-hydroxybenzamidine
-
-
0.0000189
3-(1-[5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl]-2-oxo-1,2,3,4-tetrahydro-3-quinolinyl)-4-hydroxybenzenecarboximidamide
-
-
0.0000129
3-(1-[5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl]-2-oxo-1,2,3,4-tetrahydro-3-quinolinyl)benzenecarboximidamide
-
-
0.0000021
3-(1H-imidazol-1-ylmethyl)-1-(4-methoxyphenyl)-5-methyl-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00000015
3-(3-carbamimidoyl-phenyl)-isoxazole-4-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.00000015
3-(3-carbamimidoylphenyl)-N-(2'-sulfamoylbiphenyl-4-yl)-1,2-oxazole-4-carboxamide
-
pH and temperature not specified in the publication
0.00000016
3-(4-(5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]pentyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-4-hydroxybenzenecarboximidamide
-
-
0.0000605
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl)-4-hydroxybenzamidine
-
-
0.0000008 - 0.000067
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-3-oxo-3,4-dihydroquinoxolin-2-yl)benzamidine
0.0000023
3-(4-[5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1-benzenecarboximidamide
-
-
0.000022
3-(aminomethyl)-6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.0000017
3-(iminomethyl)-1-(4-methoxyphenyl)-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00023
3-([(3S)-3-[(naphthalen-2-ylsulfonyl)amino]-2-oxopyrrolidin-1-yl]methyl)benzenecarboximidamide
-
pH and temperature not specified in the publication
0.000004
3-([4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]-2-oxopiperazin-1-yl]methyl)benzenecarboximidamide
-
pH and temperature not specified in the publication
0.039
3-([[3-(4-carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino)-4-(3,4-dihydroisoquinolin-2(1H)-yl)-4-oxobutanoic acid
-
pH and temperature not specified in the publication
0.000019
3-amino-2,3-dihydro-1,3-benzoxazol-5-yl [1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]methanesulfonate
-
-
0.000004
3-amino-4-chloro-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]benzamide
-
pH and temperature not specified in the publication
0.000002
3-amino-4-chloro-N-[(1R)-2-[4-[4-fluoro-2-(methylsulfonyl)phenyl]piperazin-1-yl]-2-oxo-1-phenylethyl]benzamide
-
pH and temperature not specified in the publication
0.25
3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.000000007
3-chloro-N-(4-chloro-2-([(5-chloro-2-pyridinyl)amino]carbonyl)-6-methoxyphenyl)-4-([(4,5-dihydro-2-oxazolyl)methylamino]methyl)-2-thiophenecarboxamide
-
0.0000007
3-chloro-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.00000076
3-chloro-N-[(1R,2S)-2-[[4-(2-oxopyridin-1(2H)-yl)benzoyl]amino]cyclohexyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.000002
3-chloro-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
3-chloro-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
3-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.0000003
3-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
3-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000015
3-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.0000008
3-chloro-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000002
3-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.00000032
3-chloro-N-[2-[(4-chlorophenyl)carbamoyl]-4-methylphenyl]-1-benzothiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.000011
3-chloro-N-[2-[(4-fluorophenyl)carbamoyl]-4-methylphenyl]-1-benzothiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.000015 - 0.000464
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
0.000000005
3-chloro-N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]-6-methoxyphenyl]-4-[[2-(methylamino)-1H-imidazol-1-yl]methyl]thiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.0000081
3-methyl-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000009
3-methyl-N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.00000072
3-[6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
0.00000018
3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
0.000022
3-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl](methyl)amino]-2-oxopyrrolidin-1-yl]methyl]benzenecarboximidamide
-
pH and temperature not specified in the publication
0.000047
3-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl]amino]-2-oxopyrrolidin-1-yl]methyl]benzenecarboximidamide
-
pH and temperature not specified in the publication
0.00061
4,4'-[(2-oxocycloheptane-1,3-diylidene)di(E)methylylidene]dibenzenecarboximidamide
-
pH and temperature not specified in the publication
0.0000013
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
-
-
0.0000024
4-hydroxy-3-[2-oxo-3-(S)-(5-pyridin-3-yl-thiophene-2-sulfonylamino)-pyrrolidin-1-ylmethyl]-benzamidine
-
pH 7.5, 22°C
0.0012
4-[(3-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.0012
4-[(4'-chloro[1,1'-biphenyl]-4-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000023
4-[(5'-chloro[2,2'-bithiophen]-5-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazine-2-one
-
-
0.0000019
4-[(5-chloro-1H-indol-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
pH and temperature not specified in the publication
0.000003
4-[(6-bromobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000004
4-[(6-chloro-1-benzothiophen-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
pH and temperature not specified in the publication
0.0012
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-imidazo[4,5-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000045
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0012
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-b]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000004
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
0.00122
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(furo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000003
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(1-methyl-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
-
0.00122
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(4,5-dihydro-4-oxo-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
above
0.000038
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[(5-oxido-1H-pyrrolo[3,2-c]pyridin-2-yl)methyl]-piperazin-2-one
-
-
0.000003
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-[[1-(2-hydroxyethyl)-1H-pyrrolo[3,2-c]pyridin-2-yl]methyl]-piperazin-2-one
-
-
0.000004
4-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0012
4-[(6-chlorothieno[3,2-b]pyridin-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000048
4-[[(1E)-2-(4-chlorophenyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0000011
4-[[(1E)-2-(5-chloro-2-thienyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0012
4-[[(1E)-2-(5-chloro-4-methoxy-2-thienyl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
above
0.000019
4-[[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl]-1-(pyridin-4-yl)piperidine-4-carboxylic acid
-
pH and temperature not specified in the publication
0.000007
4-[[(3S)-3-[[(7-methoxynaphthalen-2-yl)sulfonyl](methyl)amino]-2-oxopyrrolidin-1-yl]methyl]thiophene-2-carboximidamide
-
pH and temperature not specified in the publication
0.0000011
4-[[(E)-2-(5-chlorothiophen-2-yl)ethenyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one
-
pH and temperature not specified in the publication
0.000128
4-[[2-(5-chloro-2-thienyl)ethyl]sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000019
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate
-
-
0.00000006
5-butyl-2-(3-carbamimidoyl-phenyl)-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide
-
-
0.0000015
5-chloro-N-(5-chloropyridin-2-yl)-2-([4-[(2-imino-1,3-oxazolidin-3-yl)methyl]benzoyl]amino)benzamide
-
pH and temperature not specified in the publication
0.0000013
5-chloro-N-(5-chloropyridin-2-yl)-2-([4-[(dimethylamino)methyl]benzoyl]amino)benzamide
-
pH and temperature not specified in the publication
0.0000006
5-chloro-N-(5-chloropyridin-2-yl)-2-[(4-[[ethanimidoyl(methyl)amino]methyl]benzoyl)amino]benzamide
-
pH and temperature not specified in the publication
0.00000044
5-chloro-N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.0002
5-chloro-N-(5-chloropyridin-2-yl)-2-[[4-(piperidin-1-ylcarbonoimidoyl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.000000057
5-chloro-N-(5-chloropyridin-2-yl)-3-methoxy-2-[[4-(2-oxopiperidin-1-yl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.00000051
5-chloro-N-[(1R,2S)-2-([4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]benzoyl]amino)cyclopentyl]thiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.000003
5-chloro-N-[(3S)-1-(2-[[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]amino]-2-oxoethyl)-4-methoxypyrrolidin-3-yl]thiophene-2-carboxamide
-
pH and temperature not specified in the publication
0.0000015
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.00000084
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000000035
6-(4-[1-[(dimethylamino)methyl]cyclopropyl]phenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000002
6-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]phenyl)-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.000043
6-chloro-benzo[b]thiophene-2-sulfonic acid [2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)-pyrrolidin-3-yl]-amide
-
-
0.000096
6-chloro-benzo[b]thiophene-2-sulfonic acid [2-oxo-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-pyrrolidin-3-yl]-amide
-
-
0.000043
6-chloro-N-methyl-N-[(3S)-2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pyrrolidin-3-yl]-1-benzothiophene-2-sulfonamide
-
pH and temperature not specified in the publication
0.0000013
6-chloro-N-[(3S)-1-(5-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.0000008
6-chloro-N-[(3S)-1-(6-fluoro-2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000003
6-chloro-N-[(3S)-1-(7-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-1-[(1R)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000009
6-chloro-N-[(3S)-1-[(1S)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-1-[(1S)-1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000003
6-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000005
6-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-1-[2-fluoro-4-[(1S)-1-(methylamino)ethyl]phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000006
6-chloro-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000001
6-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.00001
6-chloro-N-[(3S)-2-oxo-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.0000008
6-chloro-N-[(3S)-2-oxo-1-(2,3,4,5-tetrahydro-1H-2-benzazepin-7-yl)pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000002
6-chloro-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000004
6-chloro-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000016
6-chloro-N-[1-(2-fluoro-4-piperidin-1-ylphenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.000028
6-chloro-N-[1-(2-fluoro-4-pyridin-4-ylphenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.0000024
6-chloro-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.0000006
6-chloro-N-[1-(4-[2-[(dimethylamino)methyl]-1H-imidazol-1-yl]-2-fluorophenyl)-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000006
6-chloro-N-[1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.00001
6-chloro-N-[1-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.00000011
6-chloro-N-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]naphthalene-2-sulfonamide
-
-
0.000000016
6-chloro-N-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]thieno[2,3-b]pyridine-2-sulfonamide
-
-
0.0000001
6-chloro-N-[1-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.00000005
6-chloro-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]thieno[2,3-b]pyridine-2-sulfonamide
-
-
0.0000022
6-[2'-(methylsulfonyl)biphenyl-4-yl]-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000012 - 0.0000017
6-[2'-[(aminooxy)sulfinyl]-3-fluorobiphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
0.0000028
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-4-methyl-3-(trifluoromethyl)-1,6-dihydro-7H-pyrazolo[3,4-d]pyridazin-7-one
-
-
0.0000018
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.000038
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylic acid
-
-
0.0000019
6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-1,4,5,6-tetrahydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00002
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(3-nitrophenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000026
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-ethylphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.00000035
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000011
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000012
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(iminomethyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000021
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.0000018
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(iminomethyl)-1-(4-methoxyphenyl)-5-methyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
-
-
0.00000074
6-[3-fluoro-2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.000000038
6-[4-(1-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]cyclopropyl)phenyl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
-
0.0000012
7'-[(6-chloronaphthalen-2-yl)sulfonyl]-8a'-(hydroxymethyl)-1-(pyridin-4-yl)tetrahydro-5'H-spiro[piperidine-4,2'-[1,3]thiazolo[3,2-a]pyrazin]-5'-one
-
pH and temperature not specified in the publication
0.000006
7-([7-[(1-ethanimidoylpiperidin-4-yl)oxy]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]methyl)naphthalene-2-carboximidamide
-
pH and temperature not specified in the publication
0.00000025
7-oxo-1-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
-
0.0001
8-amino-N-[(1R)-2-oxo-1-phenyl-2-[4-(pyridin-4-yl)piperazin-1-yl]ethyl]naphthalene-2-carboxamide
-
pH and temperature not specified in the publication
0.000003
8-amino-N-[(1R)-2-[4-[4-fluoro-2-(methylsulfonyl)phenyl]piperazin-1-yl]-2-oxo-1-phenylethyl]naphthalene-2-carboxamide
-
pH and temperature not specified in the publication
0.0000038
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
-
-
0.0000013
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate
-
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
0.00000082
methyl 2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzenesulfinate
-
-
0.0001
methyl 3'-fluoro-4'-(3-[[(3-methoxyphenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.0000445
methyl 3'-fluoro-4'-(3-[[(4-fluorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.000053
methyl 3'-fluoro-4'-(3-[[(4-methoxyphenyl)sulfonyl]amino]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.000026
methyl 3'-fluoro-4'-(3-[[(5-isoxazol-3-ylthiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)biphenyl-2-sulfinate
-
-
0.0000036
methyl 3'-fluoro-4'-([[1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]carbonyl]amino)biphenyl-2-sulfinate
-
-
0.00037
methyl 3'-fluoro-4'-[2-oxo-3-[(phenylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000028
methyl 3'-fluoro-4'-[2-oxo-3-[(quinolin-3-ylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000073
methyl 3'-fluoro-4'-[2-oxo-3-[(quinolin-6-ylsulfonyl)methyl]piperidin-1-yl]biphenyl-2-sulfinate
-
-
0.0002
methyl 3'-fluoro-4'-[3-(4-methoxyphenoxy)-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000003
methyl 3'-fluoro-4'-[3-(iminomethyl)-1-(4-methoxyphenyl)-5,7-dioxo-1,4,5,7-tetrahydro-6H-pyrazolo[4,3-d]pyrimidin-6-yl]biphenyl-2-sulfinate
-
-
0.00042
methyl 3'-fluoro-4'-[3-([[4-(iminomethyl)phenyl]sulfonyl]methyl)-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000019
methyl 3'-fluoro-4'-[3-[(1H-indazol-6-ylsulfamoyl)methyl]-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.00056
methyl 3'-fluoro-4'-[3-[(4-methoxyphenyl)amino]-2-oxopiperidin-1-yl]biphenyl-2-sulfinate
-
-
0.000094
methyl 3-(3-carbamimidoylphenyl)-5-[(4-carbamimidoylphenyl)carbamoyl]-4,5-dihydro-1,2-oxazole-5-carboxylate
-
pH and temperature not specified in the publication
0.0000034
methyl 3-[3-[amino(imino)methyl]phenyl]-5-[4-[amino(imino)methyl]phenyl]pentanoate
-
pH 8.0, 25°C
0.00065
methyl 4'-(3-[[(2,5-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000061
methyl 4'-(3-[[(3,4-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00027
methyl 4'-(3-[[(3,4-difluorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00073
methyl 4'-(3-[[(3,5-dichlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00038
methyl 4'-(3-[[(3-chlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00016
methyl 4'-(3-[[(4-chloro-6-methyl-1-benzothiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000023
methyl 4'-(3-[[(4-chlorophenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000078
methyl 4'-(3-[[(4-ethylphenyl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000053
methyl 4'-(3-[[(5-chlorothiophen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000011
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(diethylamino)ethyl](methyl)amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.00000084
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(dimethylamino)ethyl](methyl)amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000022
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-[[2-(dimethylamino)ethyl]amino]-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000023
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](3-hydroxypropyl)amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000022
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl]amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate2
-
-
0.00000071
methyl 4'-(3-[[(6-chloronaphthalen-2-yl)sulfonyl][2-(4-methylpiperazin-1-yl)-2-oxoethyl]amino]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.000018
methyl 4'-(3-[[(7-chloronaphthalen-2-yl)sulfonyl]methyl]-2-oxopiperidin-1-yl)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000084
methyl 4'-([[4-amino-3-(iminomethyl)-1-(4-methoxyphenyl)-1H-pyrazol-5-yl]carbonyl]amino)-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000002
methyl 4'-[1-(2-amino-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000018
methyl 4'-[1-(2-carbamoyl-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.000002
methyl 4'-[1-(2-carbamoylphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000018
methyl 4'-[1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000012
methyl 4'-[1-[2-[(aminooxy)sulfinyl]-4-methoxyphenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.00000074
methyl 4'-[1-[2-[(aminooxy)sulfinyl]phenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
-
0.0000027
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[(2-hydroxyethyl)(methyl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
0.00000043
methyl 4'-[3-([(6-chloronaphthalen-2-yl)sulfonyl][2-[methyl(1-methylpiperidin-4-yl)amino]-2-oxoethyl]amino)-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
0.0032
methyl 4'-[3-[(cyclohexylsulfonyl)methyl]-2-oxopiperidin-1-yl]-3'-fluorobiphenyl-2-sulfinate
-
-
0.0000028
methyl 6-[2'-[(aminooxy)sulfinyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxylate
-
-
0.00000088
methyl N-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]glycinate
-
-
0.000000043
methyl N-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycinate
-
-
0.0000063
methyl [3-(3-carbamimidoylphenyl)-4-[(2'-sulfamoylbiphenyl-4-yl)carbamoyl]-4,5-dihydro-1,2-oxazol-5-yl]acetate
-
pH and temperature not specified in the publication
0.000047
methyl [3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]amidosulfite
-
-
0.000057
N-(3-[[4'-(trifluoromethyl)biphenyl-4-yl]methoxy]phenyl)piperidine-4-carboxamide
-
pH 8.0, 25°C
0.00000012
N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide
-
pH and temperature not specified in the publication
0.000003
N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]benzamide
-
pH and temperature not specified in the publication
0.00000056
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]ethanediamide
-
pH and temperature not specified in the publication
0.000000561 - 0.000007
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
0.00000021
N-([1-[4-(3-[[(6-chloronaphthalen-2-yl)sulfonyl](2-methoxy-2-oxoethyl)amino]-2-oxopiperidin-1-yl)-3-fluorophenyl]-1H-imidazol-2-yl]methyl)-2-methoxy-N,N-dimethyl-2-oxoethanaminium
-
-
0.00000035
N-([1-[4-(3-[[(6-chloronaphthalen-2-yl)sulfonyl]amino]-2-oxopiperidin-1-yl)-3-fluorophenyl]-1H-imidazol-2-yl]methyl)-2-methoxy-N,N-dimethyl-2-oxoethanaminium
-
-
0.0009
N-1-adamantylaminocarbonyl-D,L-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.000074
N-1-adamantyloxycarbonyl-(R)-3-amidinophenylalanine-(2-phenyl)-1-ethylamide
-
pH 8.0, 25°C
0.00022
N-1-adamantyloxycarbonyl-(R)-D-3-amidinophenylalanine benzylamide
-
pH 8.0, 25°C
0.00039
N-1-adamantyloxycarbonyl-(R)-D-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.0046
N-1-adamantyloxycarbonyl-(R)-L-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.00062
N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.0017
N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine piperidine
-
pH 8.0, 25°C
0.0014
N-1-adamantyloxycarbonyl-D,L-4-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
1
N-1-adamantyloxycarbonyl-D,L-4-guanidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.0034
N-9-fluorenemethyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.000018
N-methyl-N-[(3S)-2-oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
pH and temperature not specified in the publication
0.016
N-tert-butyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester
-
pH 8.0, 25°C
0.000004
N-[(1R)-2-(1'-methyl-4,4'-bipiperidin-1-yl)-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
-
pH and temperature not specified in the publication
0.000016
N-[(1R)-2-(4-benzoylpiperidin-1-yl)-2-oxo-1-phenylethyl]-3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.002
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclobutyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0000113
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cycloheptyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000013
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclooctyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000086
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.1
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.01
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.00000285
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
-
pH 7.4
0.000265
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclobutyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000175
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cycloheptyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000041
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0014
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclooctyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000118
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000187
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0044
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.0032
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopentyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.00027
N-[(1S,2R)-2-[[(5-chloro-1H-indol-2-yl)sulfonyl]amino]cyclopropyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
-
-
0.000005
N-[(3S)-1-(1-amino-2,3-dihydro-1H-inden-5-yl)-2-oxopyrrolidin-3-yl]-6-chloronaphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000006
N-[(3S)-1-[(1,6-diaminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
pH and temperature not specified in the publication
0.00018
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]-7-methoxynaphthalene-2-sulfonamide
-
pH and temperature not specified in the publication
0.000022
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
-
pH and temperature not specified in the publication
0.0001
N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
pH and temperature not specified in the publication
0.000001
N-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[1-[3-fluoro-2'-(methoxysulfinyl)biphenyl-4-yl]-2-oxopiperidin-3-yl]glycine
-
-
0.00000013
N-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycine
-
-
0.00021
N-[2-([[4-(aminomethyl)cyclohexyl]methyl]amino)-2-oxo-1-phenylethyl]-3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.011
N-[2-([[4-(aminomethyl)cyclohexyl]methyl]amino)-2-oxoethyl]-3-carbamimidoylbenzamide
-
pH and temperature not specified in the publication
0.002
N-[3-(biphenyl-4-ylmethoxy)phenyl]-1-carbamimidoylpiperidine-3-carboxamide
-
pH 8.0, 25°C
0.0052
N-[3-(biphenyl-4-ylmethoxy)phenyl]-1-carbamimidoylpiperidine-4-carboxamide
-
pH 8.0, 25°C
0.0025
N-[3-(biphenyl-4-ylmethoxy)phenyl]piperidine-3-carboxamide
-
pH 8.0, 25°C
0.021
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
0.000088
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
-
-
0.0000007
N-[4-(N,N-dimethylcarbamimidoyl)-2-fluorophenyl]-1-(3-fluoronaphthalen-2-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
0.0000001
N-[4-chloro-2-[(5-chloropyridin-2-yl)carbamoyl]phenyl]-2'-[(dimethylamino)methyl]biphenyl-4-carboxamide
-
pH and temperature not specified in the publication
0.0000017
N2-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopiperidin-1-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.00000002
N2-[(6-chloronaphthalen-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.00000013
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N-[2-(dimethylamino)ethyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.00000037
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N2-[1-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-2-oxopiperidin-3-yl]-N-methylglycinamide
-
-
0.0000001
N2-[(6-chlorothieno[2,3-b]pyridin-2-yl)sulfonyl]-N2-[2-oxo-1-[4-(2-oxopyridin-1(2H)-yl)phenyl]piperidin-3-yl]glycinamide
-
-
0.0005
Nalpha-4'-amidinobenzensulfonyl-glycyl-D,L-4-amimidinophenylalanine ethyl ester
-
pH 8.0, 25°C
0.000098
ProTS195A
-
pH 7.7, 37°C, versus prothrombin, in absence of phospholipid
-
0.0000007
recombinant tick saliva anticoagulant protein
-
wild type enzyme, at pH 7.5 and 25°C
-
0.016
tert-butyl N-(3-carbamimidoylbenzoyl)-D-tyrosinate
-
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
0.000004
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
factor Xa, pH 7.5, 22°C
0.0000097
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
factor Xa assembled in prothrombinase complex, pH 7.5, 22°C
0.0000011
1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.0000011
1-(4-methoxyphenyl)-7-oxo-6-[2'-(pyrrolidin-1-ylmethyl)biphenyl-4-yl]-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
pH and temperature not specified in the publication
0.00000027
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
pH 7.5, 37°C
0.00000052
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
pH 7.5, 37°C
0.00000141
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester
-
pH 7.5, 37°C
0.0000008
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-3-oxo-3,4-dihydroquinoxolin-2-yl)benzamidine
-
-
0.000067
3-(4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-3-oxo-3,4-dihydroquinoxolin-2-yl)benzamidine
-
-
0.000015
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
pH 7.5, 22°C, factor Xa
0.000016
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
pH 7.5, 22°C, Gla-domainless factor Xa
0.000318
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
pH 7.5, 22°C, factor Xa in presence of 0.02 mM phospholipid vesicles containing 80% phosphocholine and 20% phosphatidylserine
0.000454
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
pH 7.5, 22°C, prothrombinase complex
0.000464
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide
-
pH 7.5, 22°C, Gla-domainless factor Xa in presence of 0.02 mM phospholipid vesicles containing 80% phosphocholine and 20% phosphatidylserine
0.00000018
3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
-
0.00000018
3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
pH and temperature not specified in the publication
0.000592
4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide)
-
pH 7.5, 22°C, factor Xa
0.000649
4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide)
-
pH 7.5, 22°C, factor Xa in presence of 0.02 mM phospholipid vesicles containing 80% phosphocholine and 20% phosphatidylserine
0.000004
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.000004
4-[(6-chlorobenzo[b]thien-2-yl)sulfonyl]-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-piperazin-2-one
-
-
0.0000012
6-[2'-[(aminooxy)sulfinyl]-3-fluorobiphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.0000017
6-[2'-[(aminooxy)sulfinyl]-3-fluorobiphenyl-4-yl]-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide
-
-
0.000057
FPR-prothrombin
-
pH 7.7, 37°C, versus prothrombin, in absence of phospholipid
-
0.00028
FPR-prothrombin
-
pH 7.7, 37°C, versus prothrombin, in presence of phospholipid at 0.025 mM
-
0.000000561
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
pH 7.4, 30°C
0.000000715
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
pH 7.4, 30°C
0.000007
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate
-
pH 7.4, 30°C
0.00000011
tissue factor pathway inhibitor
-
recombinant wild-type enzyme, 22°C
-
additional information
additional information
-
inactivation kinetics of wild-type and mutant antithrombins
-
additional information
additional information
-
Ki values for derivatives of (R)-2-(3-adamant-1-yl-oxycarbonylamino)-3-(3-carbimidoylphenyl)-N-aryl-propionamides and (R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-aryl-propionamides, overview
-
additional information
additional information
-
the Gla-domainless factor Xa shows a higher Ki in presence of phospholipids
-
additional information
additional information
-
rapid inhibition kinetic studies, wild-type and mutant antithrombins, overview
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0000075
(1S,3R,4S)-4-[(1H-indol-2-ylcarbonyl)amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.000018
(2R)-N1-(5-chloropyridin-2-yl)-N2-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)pyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00000032
(2R)-N1-(5-chloropyridin-2-yl)-N2-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]-4-methoxypyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00000038
(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-hydroxypyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00000016
(2R)-N1-(5-chloropyridin-2-yl)-N2-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-4-methoxypyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000001
(2R,4S)-N1-(5-chloropyridin-2-yl)-4-(2,4-difluorophenyl)-4-hydroxy-N2-(2-oxo-2H-1,3'-bipyridin-6'-yl)pyrrolidine-1,2-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000075
(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexanecarboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000025
(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000019
(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000008
(5R)-N1-(5-chloropyridin-2-yl)-N5-(3-fluoro-2'-sulfamoylbiphenyl-4-yl)-4,5-dihydro-1H-pyrazole-1,5-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000012
(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
37°C, pH 8.4
0.0000071
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000074
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-chlorophenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000037
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-fluorophenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.000005
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-methylphenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000064
(N-[4-[1-(acetimidoyl)piperidin-4-yloxy]phenyl]-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH 8.4, 37°C
0.0000039
([(2R)-2-(7-carbamimidoylnaphthalen-2-yl)-5-[(1-ethanimidoylpiperidin-4-yl)methyl]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000007
([(3'-carbamimidoylbiphenyl-3-yl)methyl][4-[(1-ethanimidoylpiperidin-4-yl)oxy]phenyl]sulfamoyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000044
([2-[(E)-2-(5-carbamimidoyl-2-hydroxyphenyl)ethenyl]-5-[(1-ethanimidoylpiperidin-4-yl)oxy]-2,3-dihydro-1H-indol-1-yl]sulfonyl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.045
1,1'-(benzene-1,4-diyldimethanediyl)bis(N,N-diethylpiperidine-3-carboxamide)
Homo sapiens
-
pH 8.0, 25°C
0.0000035
1-(1-[(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2-hydroxypropanoyl]piperidin-4-yl)tetrahydropyrimidin-2(1H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.0000027
1-[(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)methyl]cyclopropanecarboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000022
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]-2-ethylpropan-2-ol
Homo sapiens
-
pH 8.3, 37°C
0.00002
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]ethanol
Homo sapiens
-
pH 8.3, 37°C
0.000018
1-[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]propan-2-ol
Homo sapiens
-
pH 8.3, 37°C
0.000105
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
0.0000048
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
0.000245
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
0.000003
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
0.031
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
0.0000018
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
0.00000032
eribaxaban
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
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
0.0000035
letaxaban
Homo sapiens
pH not specified in the publication, 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
0.0000286
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.0000065
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dichlorobenzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.0000171
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dimethoxybenzamide
Homo sapiens
-
at pH 6.0 and 25°C
0.000016
N-(5-chloro-2-pyridyl)-3-hydroxy-2-[[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino]benzamide
Homo sapiens
-
at pH 8.4 and 37°C
0.00000083
N-(benzylsulfonyl)-3-(1-carbamimidoylpiperidin-4-yl)-D-alanyl-N-[(2S)-5-carbamimidamido-1-hydroxypentan-2-yl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
N-[(1R,2R)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
N-[(1R,2S)-2-[(1H-indol-2-ylcarbonyl)amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH 7.4, 22°C
0.0000028
N-[(1R,2S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
N-[(1R,2S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000051
N-[(1R,2S,5S)-2-[(1H-indol-2-ylcarbonyl)amino]-5-(methylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH 7.4, 22°C
0.0000023
N-[(1R,2S,5S)-2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000023
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.0000023
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dipropylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.0000025
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-[(2-hydroxyethyl)(methyl)carbamoyl]cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.0000022
N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-[(2-methoxyethyl)(methyl)carbamoyl]cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride
Homo sapiens
-
pH 7.4
0.000002
N-[(2S)-5-carbamimidamido-1-(2,3-dihydro-1,3-thiazol-2-yl)-1-oxopentan-2-yl]-2-[4-[(4-chlorophenyl)sulfonyl]-2-oxopiperazin-1-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00012
N-[(3aR,7aR)-2-[3-(2-amino-2-iminoethoxy)benzyl]-1,3-dioxooctahydro-1H-isoindol-4-yl]-5-chlorothiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000086
N-[(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-1-methoxypiperidin-3-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000084
N-[(3R,4S)-4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-1-[(dimethylamino)oxy]piperidin-3-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000047 - 0.00077
N-[1-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-(dimethylamino)-4-oxobutan-2-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
0.0000077
N-[2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)phenyl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
N2,N2-dimethyl-N5-[[(2-methyl-1-benzofuran-5-yl)amino]([2-oxo-1-[2-oxo-2-(pyrrolidin-1-yl)ethyl]azepan-3-yl]amino)methylidene]pyridine-2,5-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000015
N2-(benzylsulfonyl)-D-arginyl-N-[(2S)-5-carbamimidamido-1-hydroxypentan-2-yl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000056
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]-D-norvalinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000085
N2-[(4-chlorophenyl)carbamoyl]-N-[4-(3-oxomorpholin-4-yl)phenyl]norvalinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
N2-[(4-chlorophenyl)carbamoyl]-N2-(cyclopropylmethyl)-N-[2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
N2-[(4-chlorophenyl)carbamoyl]-N2-(cyclopropylmethyl)-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]glycinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
[5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol
Homo sapiens
-
pH 8.3, 37°C
0.00046
3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00061
3-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0002
4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0021
4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00000008
apixaban
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0001
methyl 3-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2,2-dimethylpropanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00012
methyl 3-(4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]phenoxy)-2,2-dimethylpropanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00007
methyl 4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.0012
methyl 4-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-3-[[(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]butanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.000047
N-[1-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-(dimethylamino)-4-oxobutan-2-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00077
N-[1-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-4-(dimethylamino)-4-oxobutan-2-yl]-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000007
rivaroxaban
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
measurement of Ca2+ responses, oscillatory response pattern, overview
additional information
-
measurement of Ca2+ responses, oscillatory response pattern, overview
additional information
-
rate of activation of native plasma-derived prothrombin in presence of prothrombinase assembled with different recombinant factor Va species, overview
additional information
-
coagulation activity of different, recombinant enzymes forms in presence of varying mixtures of phospholipids
additional information
-
platelet aggregation/Thrombus formation activity, overview
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.4
7.5
7.6
7.7
7.8
7.4
-
assay at
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
22
25
37
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
81416, 81417, 81418, 81419, 81420, 81421, 81422, 81425, 81428, 650446, 650463, 650585, 651123, 651531, 652253, 665514, 683178, 698745, 717848, 752707
-
-
brenda
native enzyme and enzyme from which the residues 1-44 of the light chain have been removed by chymotryptic proteolysis
-
-
brenda
-
650846, 650914, 650933, 650938, 650939, 651189, 651191, 652253, 652262, 652278, 652349, 652447, 652501
-
-
brenda
-
652728, 652731, 652755, 653059, 653400, 653979, 653986, 664120, 665556, 665598, 665972, 666179, 666180, 666200, 666962, 683178, 683235, 683241, 683243, 683250, 683252, 683259, 683295
-
-
brenda
-
683443, 683629, 683656, 683823, 695438, 696025, 696269, 696276, 696303, 696562, 696632, 696637, 696689, 696712, 696741, 696780
-
-
brenda
-
696928, 696937, 697301, 697304, 697353, 698471, 698745, 698769, 698777, 698820, 698822, 698841, 698900, 699091, 699159, 699432, 699861, 699865, 699866, 701285, 701294, 707025, 707279, 707307, 707693, 708249, 708321, 708322, 708323, 708451, 708505, 708509, 708634, 708815, 709137, 709147, 709156, 709211, 709434, 709578, 709726, 709729, 710601, 710607, 717234, 717253, 717335, 717336, 717339, 717381, 717829, 717968, 717974, 718415, 731276, 731308, 731484, 731588, 731756, 731958, 732229, 732376, 732937, 752707, 753093, 753480
-
-
brenda
chymotrypsin treated factor Xa, i.e. des-Gla(1-44), lacking the Gla domain
UniProt
brenda
enzyme from which the residues 1-44 of the light chain have been removed
UniProt
brenda
enzyme modified with [5-(dimethylamino)-1-naphthalenesulfonyl]glutamylglycylarginyl chloromethyl ketone
-
-
brenda
prothrombinase, enzyme complex consisting of factor Xa and factor Va, assembled in a calcium-dependent manner on the surface of phospholipid membranes
-
-
brenda
prothrombin activator pseutarin-C catalytic subunit and prothrombin activator pseutarin-C non-catalytic subunit; Australian eastern brown snake
Q56VR3; Q7SZN0
SwissProt
brenda
-
-
-
brenda
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
enzyme elicits a signaling response. ERK1/2 phosphorylation by factor Xa is dependent on protease-activated receptor PAR-2 cleavage and leads to fibroblast proliferation, migration, and differentiation into myofibroblasts
brenda
-
factor Xa is part of the prothrombinase complex formed by factor Xa, nonenzymatic cofacor Va and Ca2+ on the phospholipid surface of platelets or endothelial cells
brenda
-
annexin 2 acts as a receptor for factor Xa on the cell surface. It facilitates factor Xa activation of receptor PAR-1 but does not enhance coagulant function of factor Xa. Overexpression of tissue factor abolishes annexin 2 dependence on factor Xa signaling and diminishes binding to cell surface annexin 2, whereas selectively abolishing tissue factor promotes the annexin 2/factor Xa interaction
brenda
-
murine model of ovalbumin-induced asthma, factor X transcript levels and factor Xa activity are increased in lungs of asthmatic mice
brenda
-
enzyme elicits a signaling response. ERK1/2 phosphorylation by factor Xa is dependent on protease-activated receptor PAR-2 cleavage and leads to fibroblast proliferation, migration, and differentiation into myofibroblasts
brenda
additional information
-
factor Xa is part of the prothrombinase complex formed by factor Xa, nonenzymatic cofacor Va and Ca2+ on the phospholipid surface of platelets or endothelial cells
brenda
-
coagulation factors from plasma bind to tissue factor TF-expressing cells, e.g. lung fibroblast, become activated, dissociate, and diffuse into plasma to form enzymatic complexes on the membranes of activated platelets, overview
brenda
-
factor Xa and 5-dimethylaminonaphthalene-1-sulfonyl-(dansyl-)Glu-Gly-Arg factor Xa
brenda
-
-
698777, 701294, 701285, 696303, 699865, 696928, 699091, 696276, 696712, 710601, 710607, 717974, 717336, 717335, 717339
brenda
-
high expression level in bronchoalveolar lavage fluid macrophages from asthmatic mice
brenda
-
-
brenda
-
factor Xa is part of the prothrombinase complex formed by factor Xa, nonenzymatic cofacor Va and Ca2+ on the phospholipid surface of platelets or endothelial cells
brenda
-
enzyme associated with thrombi is enzymatically active
brenda
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
-
-
brenda
-
interaction of factor Xa with factor Va on membranes to form prothrombinase
brenda
Highest Expressing Human Cell Lines
Cell Line LinksPlease wait a moment until the data is sorted. This message will disappear when the data is sorted.
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
metabolism
physiological function
additional information
malfunction
-
enzyme inhibition is beneficial in prevention and treatment of thromboembolic disorders
malfunction
-
factor Xa deficiency is a rare inherited autosomal recessive trait, a patient harboring the mutation is affected by a severe bleeding diathesis
malfunction
-
enzyme inhibition by anticoagulants are recommended for numerous medical conditions, including the prevention and treatment of venous thromboembolism, stroke prevention in patients with atrial fibrillation, and secondary prevention in acute coronary syndromes
malfunction
-
enzyme inhibition reduces thioacetamide-induced murine liver fibrosis
metabolism
-
constituents of platelet membranes regulate the activity of the prothrombinase complex. Membranes containing phosphatidylcholine and phosphatidylethanolamine bind factor Va with high affinity in the absence of phosphatidylserine, specific protein-PE interactions appear to contribute to the effects of phosphatidylethanolamine
metabolism
Q56VR3; Q7SZN0
thrombin activates fV to fVa by cleavage at 3 sites, Arg709, Arg1018, and Arg1545, excising the B domain and unveiling the binding site of fXa. The heavy (A1-A2) and light (A3-C1-C2) chains of fVa remain noncovalently associated in the presence of divalent copper and calcium ions. fXa is activated from its zymogen precursor fX by the extrinsic or intrinsic Xase complexes and is composed of a light chain containing the membrane-anchoring gamma-carboxyglutamic acid (Gla) domain and 2 epidermal growth factor-like (EGF) domains, linked via disulfide bond to the heavy chain comprising the serine protease domain. The affinity of fXa for fVa is sufficiently low that prothrombinase can form only when both components are bound to the same membrane surface. Pseutarin C cleaves prothrombin when ptfXa is bound to ptfV and prothrombin can interact with ptfV
physiological function
-
factor Xa is a serine protease located at the confluence of the intrinsic and extrinsic pathways of the blood coagulation cascade, that catalyzes the conversion of prothrombin to thrombin via the prothrombinase complex, the enzyme is required for blood coagulation, overview
physiological function
-
factor Xa is part of the blood coagulation cascade
physiological function
-
factor Xa plays a role in blood coagulation. And FXa also plays a key role in cell migration, and is involved in a mechanism of PAR-1-mediated inhibition of migration via Rho and Src dependent pathways
physiological function
-
FXa plays a critical role in coagulation. Together with FVa and calcium ions on a phospholipid surface, FXa forms the prothrombinase complex, which is responsible for the conversion of prothrombin to thrombin, the final effector of coagulation. Regulation of thrombin generation is the primary physiologic function of FXa
physiological function
-
the final serine proteinase zymogen activation step of the blood coagulation pathway is the proteolytic activation of prothrombin to thrombin by prothrombinase. Prothrombinase consists of the proteinase, factor Xa, bound to its protein cofactor, factor Va, assembled in the presence of calcium on phospholipid membranes containing phosphatidylserine
physiological function
-
the final serine proteinase zymogen activation step of the blood coagulation pathway is the proteolytic activation of prothrombin to thrombin by prothrombinase. Prothrombinase consists of the proteinase, factor Xa, bound to its protein cofactor, factor Va, assembled in the presence of calcium on phospholipid membranes containing phosphatidylserine
physiological function
apart from the natural activation pathway, human prothrombin can also be activated by prothrombin activators in snake venoms. Trocarin depends on calcium and phospholipids as well as factor Va for activity and generation of thrombin
physiological function
apart from the natural activation pathway, human prothrombin can also be activated by prothrombin activators in snake venoms. Oscutarin depends on calcium and phospholipids but not on factor Va for activity and generation of thrombin
physiological function
-
the membrane-dependent interaction of factor Xa with factor Va forms prothrombinase and drives thrombin formation essential for hemostasis
physiological function
-
factor-Xa-induced mitogenesis and migration require sphingosine kinase activity and sphingosine-1-phosphate formation in human vascular smooth muscle cells. Factor Xa induces sphingosine kinase-1 expression and increases sphingosine-1-phosphate formation independent of thrombin, involving the activation of Rho A and protein kinase C signalling
physiological function
-
activated factor Xa is an important player in the coagulation cascade responsible for thrombin generation, which is activated during atrial fibrillation. Factor Xa induces an inflammatory signalling by activation of protease-activated receptors in human atrial tissue. FXa and tachyarrhythmia act synergistically to increase expression of protease-activated receptors and inflammatory mediators
physiological function
-
activated blood coagulation factor X (FXa) induces angiogenic growth factor expression in human retinal pigment epithelial (RPE) cells. FXa induced chemotaxis of RPE cells via activation of the p38 mitogen-activated protein kinase signal transduction pathway. FXa also induces expression of vascular endothelial growth factor, heparin-binding epidermal growth factor-like growth factor, and basic fibroblast growth factor, as well as release of these factors from RPE cells
physiological function
-
the enzyme induces inflammation by activating protease-activated receptor 1 and protease-activated receptor 2
physiological function
-
the enzyme promotes stellate cell contractility and activation
physiological function
Q56VR3; Q7SZN0
pseutarin C does not require membranes and is unable to cleave prothrombin unless ptfXa is bound to ptfV and prothrombin can interact with ptfV. Therefore, blocking the interaction of prothrombin with pseutarin C will result in no thrombin generation or prothrombin cleavage
additional information
-
factor Va is the non-enzymatic cofactor of prothrombinase, which comprises, along with FVa, the enzyme factor Xa, a negatively charged phospholipid surface, and calcium ions
additional information
-
the mechanism for the activation of prothrombin to thrombin by prothrombinase is achieved through two distinct intermediate pathways, overview
additional information
-
prothrombin specifically active site-labeled with D-Phe-Pro-Arg-CH2Cl shows altered activity in vitro and in vivo compared to the wild-type protein, overview
additional information
-
prothrombin specifically active site-labeled with D-Phe-Pro-Arg-CH2Cl shows altered activity in vitro and in vivo compared to the wild-type protein. [AF660]FPR-mouse ProT binds to fibroblast membranes in mouse plasma, overview
additional information
the enzyme is similar to human coagulation factor X
additional information
-
the enzyme is similar to human coagulation factor X
additional information
the enzyme is similar to human coagulation factor X
additional information
-
the enzyme is similar to human coagulation factor X
additional information
Q56VR3; Q7SZN0
based on the crystal structure of the prothrombinase complex from the venom of Australian eastern brown snake, pseutarin C, an initial prothrombin docking mode is modeled, which involves an interaction with discrete portions of the A1 and A2 domains of fV and the loop connecting the 2 domains, known as the a1-loop. The proposed interface is analyzed by site-directed PEGylation and by swapping the a1-loop in pseutarin C with that of human fV and fVIII and measuring the effect on rate and pathway of thrombin generation. PEGylation of residues within our proposed binding site greatly reduces the rate of thrombin generation, without affecting the pathway, whereas those outside the proposed interface have no effect. PEGylation of residues within the a1-loop also reduces the rate of thrombin generation. The sequence of the a1-loop plays a critical role in prothrombin binding and in the presentation of Arg320 for initial cleavage. Mapping the prothrombin-binding site of pseutarin C by site-directed PEGylation, overview. PEGylation of residues within the proposed binding site greatly reduces the rate of thrombin generation, without affecting the pathway, whereas those outside the proposed interface have no effect. PEGylation of residues within the a1-loop also reduces the rate of thrombin generation. Important role of the a1-loop and R320 in the initial interaction with prothrombin
Show AA Sequence and Transmembrane Helices (717 entries)
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PDB
SCOP
CATH
UNIPROT
ORGANISM
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
114000
-
enzyme in presence of 5 mM Ca2+ and 0.4 mM 1,2-dicaproyl-sn-glycero-3-phospho-L-serine, native PAGE
45000
47000
-
enzyme in absence of Ca2+ and 1,2-dicaproyl-sn-glycero-3-phospho-L-serine, native PAGE
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SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
dimer
homodimer
monomer
additional information
dimer
-
and monomer. Dimer is about 1000000fold less active toward prothrombin than the monomer. Dimerization results in substantial change in tertiary or quarternary strucutre with a concomitant decrease in alpha-helix
monomer
-
and dimer. Dimer is about 1000000fold less active toward prothrombin than the monomer. Dimerization results in substantial change in tertiary or quarternary strucutre with a concomitant decrease in alpha-helix
additional information
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the intact enzyme contains a Gla-domain and a N-terminal EGF-like domain, amino acid residues 1-86, as well as a C-terminal EGF-like domain, amino acid residues 154-183
additional information
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factor Xa is part of the prothrombinase complex with Ca2+, phospholipids and factor Va, binding of 1,2-dicaproyl-sn-glycero-3-phospho-L-serine to the second binding site in presence of Ca2+ leads to dimerization
additional information
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enzyme is part of the prothrombinase enzyme complex including also factor Va, phospholipids and Ca2+
additional information
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enzyme is part of the prothrombinase enzyme complex including also factor Va, phospholipids and Ca2+
additional information
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Ca2+, factor Xa and factor Va are part of the prothrombinase enzyme complex
additional information
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factor Xa is part of the prothrombinase complex formed by factor Xa, nonenzymatic cofacor Va and Ca2+ on the phospholipid surface of platelets or endothelial cells
additional information
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enzyme is complexed in the prothrombinase complex with factor Va, Ca2+, and phospholipids
additional information
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enzyme is complexed in the prothrombinase complex with factor Va, Ca2+, and phospholipids or membrane, respectively
additional information
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factor Xa is part of the prothrombinase complex with Ca2+, phospholipids and factor Va
additional information
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factor Xa is part of the prothrombinase complex with Ca2+, phospholipids and factor Va
additional information
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factor Xa is part of the prothrombinase complex with Ca2+, phospholipids and factor Va
additional information
schematic representation and modeling of the structure of the two peptide chains of factor X, amino acid sequence, enzyme possesses an activation peptide, a catalytic serine protease domain, a GF2 domain, and a EGF1 domain, overview
additional information
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schematic representation and modeling of the structure of the two peptide chains of factor X, amino acid sequence, enzyme possesses an activation peptide, a catalytic serine protease domain, a GF2 domain, and a EGF1 domain, overview
additional information
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the enzyme is part of the prothrombinase complex also including phospholipid and factor Va
additional information
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factor Xa is part of the prothrombinase complex also including e.g. factor Va
additional information
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formation of the prothrombinase enzyme complex increases the factor Xa activity by 300000fold, the complex includes phospholipids, Ca2+, factor Xa and factor Va
additional information
FXa circulates as light and the heavy chains connected by a single disulfide linkage in plasma
additional information
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FXa circulates as light and the heavy chains connected by a single disulfide linkage in plasma
additional information
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membrane-bound factor Xa binds to protein S, a non-enzymatic cofactor of activated protein C. Binding involves the thrombin-sensitive region of protein S
additional information
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the C-terminal region of factor Va heavy chain is crucial for coordinated prothrombin activation by prothrombinase, an enzyme complex consisting of factor Xa and factor Va
additional information
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the catalytic domain which consists of two similar antiparallel beta-barrel folds that together form the catalytic triad and substrate binding site
additional information
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three-dimensional model structure of the prothrombinase/prothrombin complex obtained from solvent equilibration molecular dynamics simulations for factor Xa/factor Va, docking, structure, and mechanism analysis, model comparisons, overview
additional information
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factor Xa is part of the prothrombinase complex with Ca2+, phospholipids and factor Va
additional information
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enzyme is part of the prothrombinase enzyme complex including also factor Va, phospholipids and Ca2+
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POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
no modification
-
analysis for hexoses, amino sugars and neuraminic acids is negative
proteolytic modification
proteolytic modification
-
a protein present in Russell's viper venom specifically cleaves a specific peptide bond, resulting in the release of a glycopeptide of MW 11000 Da from the amino terminal end of the heavy chain
proteolytic modification
-
autoproteolytic conversion of factor Xaalpha to factor Xabeta by excision of a 4000 Da fragment, beta-peptide
proteolytic modification
-
the zymogen factor X is converted to its actively enzymatic form by incubation with Russell's viper venom
proteolytic modification
-
processing and activation of the recombinant wild-type and mutant zymogens to mature enzymes by Russell's viper venom
proteolytic modification
-
the factor X is activated to factor Xa by Russell's viper venom
proteolytic modification
-
processing of factor X to factor Xa can be performed with Russell's viper venom at pH 8.3
proteolytic modification
-
processing of factor X to factor Xa can be performed with Russell's viper venom
proteolytic modification
-
processing and activation of the recombinant wild-type and mutant zymogens to mature enzymes by Russell's viper venom at 37°C and pH 7.4
proteolytic modification
reorientation of the N-terminus of serine protease domain after proteolytic activation of factor X to factor Xa, cleavage of the activation peptide at the Arg194-Ile195 peptide bond
proteolytic modification
-
activation of factor X and GDFX to factor Xa and GDFXa, respectively, by Russel's viper venom and human antithrombin
proteolytic modification
-
factor Xa formation is catalyzed by the intrinsic tenase, i.e. factor VIIa and tissue factor complex, via proteolytic cleavage, analysis of roles of extrinsic and intrinsic tenases in fX activation, and roles of extrinsic tenase and fXIa in fIX activation during clot formation in a reaction-diffusion system, computational simulations, overview
proteolytic modification
-
the factor X is activated to factor Xa by Russell's viper venom
proteolytic modification
-
factor X is converted into its active form, factor Xa, in response to the factor VIIa-tissue factor, i.e. thromboplastin, complex, overview. Kinetics of immobilized tissue factor binding to factor VIIa compared to non-immobilzed one, overview. Immobilization of the tissue factor on the surface has no qualitative effect on the kinetics of tissue factor interaction with factor VIIa and does not affect the activation activity of factor Xa and the coagulation cascade
proteolytic modification
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activation of the zymogen factor X to factor Xa by proteolytic cleavage initiates the extrinsic coagulation pathway, overview
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CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
20 ns of molecular dynamics and steered molecular dynamics simulations on open and closed conformation, based on crystal structure PBD entry 1C5M. Interchangeable conformational transition between open and closed form. The opening and closing dynamics of the FXa subsites involve potential mechanistic roles of residues Glu97, Lys96, and aromatic-aromatic interactions of various aromatic residues His57, Tyr60, Phe94, Tyr99, Phe194, and Trp215
chymotrypsin treated factor Xa, i.e. des-Gla(1-44), lacking the Gla domain, free or complexed with inhibitor BIBT0871, 3 mg/ml protein in 10 mM Tris-HCl, pH 7.5, 20 mM sodium chloride, 2 mM calcium chloride, equilibrated against 20% PEG 4000, 0.1 M malate/imidazole, 0.1 M sodium acetate, pH 6.0, some days, X-ray diffraction structure determination and analysis at 1.9-3.0 A, cocrystallization of factor Xa complexed with thrombin and inhibitor BIBR1109
complex between the enzyme from which the residues 1-44 of the light chain have been removed and the inhibitor (2RS)-(3'-amidino-3-biphenyl)-5-(4-pyridylamino)pentanoic acid
in complex with inhibitor 1-(4-methoxyphenyl)-6-[4-[1-(pyrrolidin-1-ylmethyl)cyclopropyl]phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one to 2.0 A resolution. The molecule adopts an extended binding mode with the para-methoxyphenyl group located in the S1 pocket and the alpha-CH2-N-pyrrolidinyl phenylcyclopropyl group occupying the S4 pocket
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in complex with inhibitor N-[(1R,2S,5S)-2-[[(5-chloroindol-2-yl)carbonyl]amino]-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride, to 2.1 A resolution
-
method for quantifying the contributions to the free energy of binding due to the ligand evacuating energetically unfavorable and entropically structured solvent for the set of congeneric pairs. The expulsion of active-site water strongly impacts protein-ligand binding affinities in two ways. Hydrophobic ligand groups that displace water from energetically unfavorable hydrophobically enclosed environments contribute enthalpically since the water molecules will make more favorable interactions in the bulk fluid. Ligand groups that displace entropically structured solvent contribute even when the solvent interacts favorably with the protein since well-designed ligands will recapture the protein-water interaction energy
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molecular modeling of complex with inhibitor [5-(4-[3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl]piperazin-1-yl)imidazo[1,2-a]pyridin-2-yl]methanol. The imidazo[1,2-a]pyridine ring is deeply buried inside the hydrophobic S4 site and makes hydrophobic contacts with the aromatic rings of Tyr99, Phe174, and Trp215 without the salt bridge with any amino acid residue in this site. The imidazo[1,2-a]pyridine ring extends across the face of the Phe174 phenyl ring with a favorable pi-pi stacking interaction
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purified chymotrypsin treated enzyme lacking the first 45 amino acid residues, i.e. des(1-45)FXa, complexed with inhibitor, 8 mg/ml protein in 5 mM MES-NaOH, pH 6.0, 5 mM CaCl2, 0.001 mM inhibitor RPR128515, 0.003 ml mixed with equal volume of reservoir solution containing 18-20% PEG 600, 50 mM MES-NaOH, pH 5.7, hanging drop vapour diffusion method, 19°C, a few days, X-ray duffraction structure determination and analysis at 2.1 A resolution of crystals soaked in mother liquor containing 1-1.5 mM inhibitor and 5-10% dimethylformamide
purified chymotrypsin-treated enzyme, i.e. des-Gla-factor Xa, complexed with inhibitor (R)-2-(3-adamant-1-yl-ureido)-3-(3-carbimidoylphenyl)-N-phenethyl-propionamide, 20°C, hanging drop vapour diffusion technique, from 0.1 M MES-OH, pH 5.8, 10 mM CaCl2, 18% PEG 6000, 10 mM inhibitor, enlarged by seeding, X-ray diffraction structure determination and analysis at 2.22 A resolution
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purified factor Xa, 8 mg/ml, in MES-NaOH, pH 6.0, 5 mM CaCl2, 0.001 mM inhibitor RPR128515, hanging drop vapour diffusion method, equal volume of 0.003 ml of protein and reservoir solution, the latter containing 18-20% PEG 600, 50 mM MES-NaOH, pH 5.7, 19°C, a few days, seeding cycles are necessary to improve size and shape of the crystals, X-ray diffraction structure determination and analysis at 2.1 A resolution
purified factor Xa, cleaved to des-Gla-factor Xa via limited proteolysis with chymotrypsin, is crystallized in complex with inhibitors 3-chloro-N-(4-chloro-2-([(4-chlorophenyl)-amino]carbonyl)phenyl)-4-[(4-methyl-1-piperazinyl)methyl]-2-thiophenecarboxamide and 3-chloro-N-(4-chloro-2-([(5-chloro-2-pyridinyl)amino]carbonyl)-6-methoxyphenyl)-4-([(4,5-dihydro-2-oxazolyl)methylamino]methyl)-2-thiophenecarboxamide, within 2-4 weeks in 15-21% PEG 1500 and 10 mM CaCl2, or from 0.1 M imidazole/malate, pH 5.5, 0.5 M sodium acetate, pH 5.0, 24% PEG 3350, and 5 mM CaCl2, X-ray diffraction structure determination and analysis at 2.1-25 A
analysis of the crystal structure of the prothrombinase complex from the venom of the Australian eastern brown snake, pseutarin C
Q56VR3; Q7SZN0
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PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
D70K
-
mutation of E2FXa mutant, loss of ability to bind Ca2+, activity is retained
E14D
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E14 is posttranslationally carboxylated in wild-type enzyme. Heparin activated inhibition of mutant enzyme by antithrombin with and without Ca2+ is enhanced compared to wild-type recombinant FXa
E16D
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E16 is posttranslationally carboxylated in wild-type enzyme. Heparin activated inhibition of mutant enzyme by antithrombin is not activated by Ca2+
E19D
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E19 is posttranslationally carboxylated in wild-type enzyme. Heparin activated inhibition of mutant enzyme by antithrombin is the same as wild-type recombinant FXa
E217A
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affinity for interaction with Na+ is impaired. 3-4fold decrease in activity towards both natural and synthetic substrates. Presence of factor Va restores most of the catalytic defect with substrate prothrombin
E217Q
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affinity for interaction with Na+ is impaired. Presence of factor Va restores most of the catalytic defect with substrate prothrombin
E26D
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E26 is posttranslationally carboxylated in wild-type enzyme. Heparin activated inhibition of mutant enzyme by antithrombin is not activated by Ca2+
E29D
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E29D is posttranslationally carboxylated in wild-type enzyme. Heparin activated inhibition by antithrombin with and without Ca2+ is enhanced compared to wild-type recombinant FXa
E80K
-
mutation of E2FXa mutant, loss of ability to bind Ca2+, activity is retained
F174N
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site-directed mutagenesis, reduced binding of inhibitor trimethylphenylammonium
G114R
simulation of the exchange of residues, conserved residue in the EGF2 domain sulfide loop, disruptive salt bridge interaction or blockage of interaction with factors VIIIa/IXa
G11V
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naturally occuring mutation of factor Xa within the omega-loop of the gamma-carboxyglutamic-rich domain of the ature enzyme, leading to enzyme deficiency and a bleeding phenotype, overview. The mutant factor Xa activity is below 1% of wild-type activity, activation with RVV-X is 4fold less effective in the patient's plasma than in healthy plasma. The patient's phenotype appears to be due to a very low rate of FXG11V activation by TF/FVIIa and FVIIIa/FIXa complexes rather than to FXaG11V activity within prothrombinase, overview
G323S
simulation of the exchange of residues, mutation disrupts a highly conserved beta-sheet structure
I16L
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mutation disrupts activation process of the factor X zymogen with alteration of active site function and impairment of Na+ and factor Va binding. Irreversible stabilization with L-Glu-Gly-L-Arg-chloromethyl ketone fully rescues factor Va binding. The Km value for prothrombin conversion for the mutant assembled into prothrombinase is unaltered, whereas the kcat is reduced 3- to 4fold
K147A
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site-directed mutagenesis, reduced Km, reduced kcat compared to the wild-type enzyme for the synthetic substrate and for prothrombin as a substrate
N57T
simulation of the exchange of residues, loss of interaction with Cys81 with structural implications
P343S
simulation of the exchange of residues, conserved residue involved in a suface beta-sheet, affects intrinsic folding
R143A
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site-directed mutagenesis, reduced Km, reduced kcat compared to the wild-type enzyme for the synthetic substrate and for prothrombin as a substrate
R150A
R154A
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site-directed mutagenesis, increased Km, increased kcat for the synthetic substrate, and reduced Km and kcat for prothrombin as a substrate compared to the wild-type enzyme
R326C
simulation of the exchange of residues, surface residue, involved in protein-protein interactions, interaction with Gln376 located in the S1-binding site
S195A
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catalytically inactive mutant, that still binds to inhibitor antithrombin with the same velocity as the wild-type enzyme
T318M
simulation of the exchange of residues, surface residue involved in a side-chain hydrogen bond with Glu341 which is lost in the mutant, leads to clinical effect
V17A
-
mutation disrupts activation process of the factor X zymogen with alteration of active site function and impairment of Na+ and factor Va binding. The Km value for prothrombin conversion for the mutant assembled into prothrombinase is unaltered, whereas the kcat is reduced 3- to 4fold
V298M
simulation of the exchange of residues, unfolding occurs due to space limitation
Y225P
-
mutation of the GDFXa mutant, exchange of the Na+ binding site residue results in 2fold decreased stimulation by Na+ in presence or absence of Ca2+
Y99A
-
the enzyme shows strongly reduced activity compared to the wild type enzyme
Y99A/F174A
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the enzyme shows severely reduced activity compared to the wild type enzyme
Y99T
-
site-directed mutagenesis, 25fold reduced binding of inhibitor trimethylphenylammonium
S135A
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site-directed mutagenesis, unaltered activity compared to the wild-type enzyme
S425A
-
site-directed mutagenesis, unaltered activity compared to the wild-type enzyme
additional information
R150A
-
site-directed mutagenesis, reduced Km, reduced kcat compared to the wild-type enzyme for the synthetic substrate and for prothrombin as a substrate
R150A
-
modification of the complementary exosite residue that interacts with the antithrombin exosite. Mutant shows a marked attenuation of the exosite-dependent enhancement of the alpha1-proteinase inhibitor reaction
additional information
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the enzyme from which the residues 1-44 of the light chain have been removed by chymotryptic proteolysis is indistinguishable from the native enzyme in its activity on benzoyl-Ile-Glu-Gly-Arg-p-nitroanilide, on prothrombin alone, and on prothrombin plus factor Va
additional information
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construction of factor Xa-trypsin hybrids, display on phage for selection of a mutant with domain architecture of trypsin and specificity of factor Xa
additional information
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mutant GDFXa shows reduced ability to differentiate between the metal ions bound and reduced amidolyic activity
additional information
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mutation of factor Va in the prothrombinase enzyme complex consisting of factor Xa and factor Va. The C-terminal region of factor Va heavy chain is crucial for coordinated prothrombin activation by prothrombinase
additional information
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expression of several differently truncated enzymes reveal that residues 285-335 are critical for prothrombinase activity, a truncated enzyme lacking these residues is catalytically inactive
additional information
Q56VR3; Q7SZN0
mutation of selected residues on the A1, A2, and A3 domains of ptfV to Cys for modification with a large polyethylene glycol (PEG) moiety to sterically interfere with docking. Residues in the a1-loop are also swapped with those of hfV and the unrelated fVIII to assess the role of a1-loop composition and length in prothrombin binding and processing. PEGylation at residues 134 and 168 has no effect on thrombin generation, whereas PEGylation at 276 and 302 slows thrombin generation by 7fold and 12.6fold, respectively
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GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
Ca2+ stabilizes. At 4°C, in absence of CaCl2, the activity of factor Xa decreases to 20% of the initial level after 4.5 months in 0.05 M Tris-HCl, 0.1 M NaCl, pH 7.5, in presence of 5 mM CaCl2 the enzyme remains fully active
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STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
4°C, in absence of CaCl2, the activity of factor Xa decreases to 20% of the initial level after 4.5 months in 0.05 M Tris-HCl, 0.1 M NaCl, pH 7.5, in presence of 5 mM CaCl2 the enzyme remains fully active
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PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
native and recombinant wild-type, and mutant constructs expressed in 293 ells
native factor X from plasma
recombinant wild-type and mutant zymogens from expression in HEK293 cells, to homogeneity
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CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
DNA and amino acid sequence determination and analysis, sequence comparison, transient recombinant expression in COS-7 cells, the enzyme is secreted
expression by the RSV-PL4 expression/purification vector system of wild-type inactive factor X, mutant inactive factor X lacking the 4-carboxyglutamic acid-domain, Y225P mutant of factor X, factor X E2FX mutant lacking both Gla-domain and EGF1-domain, as well as of mutants D70K and E80K of mutant E2FX, expression in human 293 cells
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expression of wild-type and mutant zymogens in HEK293 cells, the enzyme is expressed with an introduced cleavage site for for furin-like processing enzymes which is required for expression of the enzyme and for processing of the zymgen to the mature enzyme
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expression of wild-type enzyme, enzyme lacking the Gla- and the EGF-like domains, of the isolated Gla-domain, the EGF-like domain, and a construct comprising both, expression in human 293 cells
gene fgl2, expression of the full sized, His-tagged enzyme in Spodoptera frugiperda Sf9 cells via transfection with baculovirus, expression of truncated enzyme forms and enzyme mutants in CHO-K1 cells
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inactive factor Xa(Asp322Asn,Ser419Ala), expression in Chinese hamster ovary cells
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transient recombinant expression in COS-7 cells, the enzyme is secreted
expression of wild-type enzyme, enzyme lacking the Gla- and the EGF-like domains, of the isolated Gla-domain, the EGF-like domain, and a construct comprising both, expression in human 293 cells
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expression of wild-type enzyme, enzyme lacking the Gla- and the EGF-like domains, of the isolated Gla-domain, the EGF-like domain, and a construct comprising both, expression in human 293 cells
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
activated protein C proteolytically inactivates factor Va through proteolytic cleavage and thereby downregulates prothrombinase. Factor Xa protects 17.3fold and prothrombin protects 5.8fold the inactivation of factor Va, while protein S increases the inactivation. Factor Xa and prothrombin together are highly protective, both with and without protein S. R506Q mutation of factor Va is only mildly prothrombotic, even though it profoundly affects the kinetics of inactivation of isolated FVa by activated protein C
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enzyme protein levels increase 1 h after injury of the peripheral nerve and then decrease significantly at 1 and 2 days following injury
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sphingolipids, including lysosulfatide and some of its analogs like N-acetyl sulfatide, psychosine, gluco-psychosine, lyso-sphingomyelin or sulfatide, may down-regulate enzyme activity without inhibiting the enzyme's active site. Lysosulfatide is an anticoagulant lipid that inhibits the enzyme when it is bound to either phospholipids or to factor Va
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the gene expression of factor X in retinal pigment epithelial cells is decreased by blood serum, activated factor X, thrombin, transforming growth factor beta1, and platelet-derived growth factor
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the gene expression of factor X in retinal pigment epithelial cells is increased by hypoxia and prostaglandin E2
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APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
analysis
-
development of an assay for the monitoring of anticoagulants inhibiting factor Xa and/or factor IIa. Assay is based on the addition of factor Xa and snake venom RVV-V, i.e. Russell viper venom factor V activator specifically activating factor V and phospholipids to platelet-poor plasma. Assay shows an almost linear dose-response and high sensitivity for unfractionated heparin, low molecular weight heparins, r-hirudin, and argatroban
drug development
medicine
pharmacology
synthesis
drug development
-
structure-based drug design of small molecule factor Xa inhibitors. fXa inhibitors, the so-called xabans, are attractive options that can overcome limitations, e.g. bleeding, of the current oral antithrombotic therapy, he rational design of small-molecule direct fXa inhibitors, overview
drug development
-
oral factor Xa inhibitors are a promising alternative to current anticoagulants
drug development
-
the enzyme is a target for drug development in prevention and treatment of thromboembolic disorders, overview
drug development
-
factor Xa is a target for development of anticoagulant therapeutics, drug development and clinical trials. overview
medicine
-
glycoprotein IIb/IIIa receptor antagonists in combination with heparin might contribute to improved therapy of acute coronary syndromes abd during percutaneous coronary interventions
medicine
-
enzyme is a target for discovery, design of direct inhibitors and development of antithrombotic agents, overview
medicine
-
enzyme inhibition by anticoagulants are recommended for numerous medical conditions, including the prevention and treatment of venous thromboembolism, stroke prevention in patients with atrial fibrillation, and secondary prevention in acute coronary syndromes
medicine
-
FXa is an attractive and potentially specific target for anticoagulant agents
medicine
FXa cleaves SARS CoV-2 spike protein protein, preventing its binding to ACE2, and blocking viral entry and infection. FXa is less effective against variants carrying the D614G mutation
medicine
exogenous FXa inhibits while FXa knockout promotes SARSCoV-2 infection in the K18-hACE2 mouse model. Inhibitor rivaroxaban abrogates FXa-mediated protection of K18-hACE2 mice from wild-type SARS-CoV-2 infection
pharmacology
enyme is a potential target for development of antithrombotics, structure-based drug design approach usig the crystal structure of the enzyme-inhibitor complex
pharmacology
-
the enzyme is a target for development of antithrombotic drug therapy mechanism
pharmacology
-
enzyme is a major target for new therapeutics in prevention of blood coagulation
pharmacology
-
factor Xa is a therapeutic target for development of potent and selective direct enzyme inhibitors as antithrombotic compounds for the improved therapy of ischemic heart disease and cerebrovascular disease, no bleeding effect, only modest change in markers of systemic anticoagulation, use of animal models, overview
pharmacology
-
enzyme is a target for discovery, design of direct inhibitors and development of antithrombotic agents, overview
pharmacology
-
the enzyme is a target for development of antithrombotic drug therapy mechanism
pharmacology
-
sensitive and specific quantification of inhibitor rivaroxaban in human plasma by high-performance liquid chromatography-tandem mass spectrometry. Concentrations between 0.5 and 500 micrograms per liter can be detected. Inter-assay precision is below 7.4% and inter-assay accuracy is between 96.3% and 102.9%
pharmacology
-
treatment of patients undergoing elective total knee replacement post-operatively with betrixaban or enoxiparin for 10-14 days to prevent thromboembolism. Betrixaban shows a dose- and concentration-dependent effect on inhibition of thrombin generation and anti-factor Xa levels. Betrixaban demonstrates antithrombotic activity and is well tolerated in knee replacement patients
pharmacology
-
presence of inhibitor 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 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
pharmacology
-
inhibitor 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 dose-dependently inhibits thrombus formation in a rat thrombosis model. Bleeding time in rats is not significantly prolonged at an antithrombotic dose
pharmacology
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inhibitor 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 dose-dependently inhibits thrombus formation in a rabbit thrombosis model
pharmacology
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study on use of apixaban for prevention of arterial thrombosis in rabbit models of electrically induced carotid artery thrombosis and cuticle bleeding time. Addition of aspirin to apixaban significally reduces the thrombus weight with no significant increase in bleeding time. Addition of aspirin and apixaban to clopidogrel produces a further significant reduction in thrombus weight. Combination of clopidogrel and aspirin with apixaban produces a significant but moderate 2.1fold increase in bleeding time
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Release 2026.1 (March 2026)
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