Page last updated: 2024-12-08

razaxaban

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

razaxaban: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID204102
CHEMBL ID206335
SCHEMBL ID677372
MeSH IDM0484106

Synonyms (26)

Synonym
IK8 ,
1Z6E ,
chembl206335 ,
razaxaban
1-(3-aminobenzisoxazol-5-yl)-3-trifluoromethyl-n-[2-fluoro-4-[(2-dimethylaminomethyl)imidazol-1-yl]phenyl]-1h-pyrazole-5-carboxyamide hydrochloride salt
bdbm12676
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-benzisoxazol-5-yl)-n-(4-{2-[(dimethylamino)methyl]-1h-imidazol-1-yl}-2-fluorophenyl)-3-(trifluoromethyl) -1h-pyrazole-5-carboxamide
bms-5613
3k2509846l ,
218298-21-6
1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-n-(2-fluoro-4-((2'-dimethylaminomethyl)imidazol-1-yl)phenyl)-1h-pyrazole-5-carboxyamide hydrochloride
razaxaban [inn]
unii-3k2509846l
AKOS016008770
1-(3-amino-1,2-benzisoxazol-5-yl)-n-(4-(2-((dimethylamino)methyl)-1h-imidazol-1-yl)-2-fluorophenyl)-3-(trifluoromethyl)-1h-pyrazole-5-carboxamide
1h-pyrazole-5-carboxamide, 1-(3-amino-1,2-benzisoxazol-5-yl)-n-(4-(2-((dimethylamino)methyl)-1h-imidazol-1-yl)-2-fluorophenyl)-3-(trifluoromethyl)-
SCHEMBL677372
2-(3-amino-1,2-benzoxazol-5-yl)-n-[4-[2-[(dimethylamino)methyl]imidazol-1-yl]-2-fluorophenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
1-(3-amino-1,2-benzisoxazol-5-yl)-n-(4-{2-[(dimethylamino)methyl]-1h-imidazol-1-yl}-2-fluorophenyl)-3-(trifluoromethyl)
-1h-pyrazole-5-carboxamide
BCP24153
bms 561389;dpc 906
Q27257381
DTXSID40870249
ofjrnbwsfxehsa-uhfffaoysa-n

Research Excerpts

Overview

Razaxaban is a selective, potent, and orally bioavailable inhibitor of coagulation factor Xa.

ExcerptReferenceRelevance
"Razaxaban is a selective, potent, and orally bioavailable inhibitor of coagulation factor Xa. "( Reductive isoxazole ring opening of the anticoagulant razaxaban is the major metabolic clearance pathway in rats and dogs.
Bonacorsi, SJ; Chen, SY; He, K; Knabb, RM; Lam, PY; Lecureux, L; Patrone, LM; Quan, M; Raghavan, N; Skiles, GL; Zhang, D; Zhang, H, 2008
)
2.04

Pharmacokinetics

A small number of indoline fXa inhibitors were profiled in a dog pharmacokinetic model. One of them demonstrated pharmacokinetics parameters similar to that of clinical candidate razaxaban.

ExcerptReferenceRelevance
" A small number of indoline fXa inhibitors were profiled in a dog pharmacokinetic model, one of which demonstrated pharmacokinetic parameters similar to that of clinical candidate razaxaban."( Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
Bai, S; Ellis, CD; He, K; He, MY; Jacobson, IC; Knabb, RM; Lam, PY; Luettgen, JM; Quan, ML; Rossi, KA; Varnes, JG; Wacker, DA; Wexler, RR, 2007
)
0.53
" Optimization by conversion from a P1 aminobenzisoxazole to a P1 p-methoxyphenyl residue, replacing the 3-trifluoromethylpyrazole with a 3-amidopyrazole, and employing a pyridone P4 group provided a fXa inhibitor with a potency and pharmacokinetic profile equivalent to that of razaxaban and improved selectivity over thrombin."( Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Bai, S; Galemo, RA; He, K; Knabb, RM; Lam, PY; Luettgen, JM; Orwat, MJ; Pinto, DJ; Theroff, JP; Varnes, JG; Wacker, DA; Wells, B; Wexler, RR, 2008
)
0.52

Compound-Compound Interactions

ExcerptReferenceRelevance
" Low-dose razaxaban was useful in combination with sub-optimal doses of aspirin and/or clopidogrel for the prevention of occlusive arterial thrombosis without excessive bleeding."( Razaxaban, a direct factor Xa inhibitor, in combination with aspirin and/or clopidogrel improves low-dose antithrombotic activity without enhancing bleeding liability in rabbits.
Crain, EJ; Knabb, RM; Lam, PY; Quan, ML; Watson, CA; Wexler, RR; Wong, PC, 2007
)
2.18

Bioavailability

Razaxaban is a selective, potent, and orally bioavailable inhibitor of coagulation factor Xa.

ExcerptReferenceRelevance
" These efforts culminated in 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide (11d), a potent, selective, and orally bioavailable inhibitor of factor Xa."( Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
Alexander, RS; Bai, S; Clark, CG; Ellis, CD; Han, Q; He, MY; Knabb, RM; Lam, PY; Li, R; Luettgen, JM; Pinto, DJ; Quan, ML; Sun, JH; Teleha, CA; Wexler, RR; Wong, PC, 2005
)
0.52
"We have previously reported on a series of aminobenzisoxazoles as potent, selective, and orally bioavailable factor Xa inhibitors, which culminated in the discovery of razaxaban."( Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
Bai, S; Fevig, JM; Han, Q; Knabb, RM; Lam, PY; Luettgen, JM; Quan, ML; Wexler, RR; Wong, PC, 2006
)
0.53
" Many of these compounds are potent, selective, and orally bioavailable inhibitors of coagulation factor Xa."( Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.
Bai, SA; Buriak, J; Cacciola, J; Fevig, JM; Knabb, RM; Lam, PY; Luettgen, JM; Rossi, KA; Wexler, RR; Wong, PC, 2006
)
0.33
"7x10(7) M-1 s-1) in vitro, selective (>1000-fold over other proteases), efficacious in the AVShunt thrombosis model, and orally bioavailable inhibitor of blood coagulation factor Xa."( 1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
Alexander, RS; Amparo, E; Bai, S; Ellis, C; Galemmo, RA; Han, Q; He, K; He, MY; Kettner, C; Knabb, RM; Lam, PY; Luettgen, JM; Mersinger, L; Orwat, MJ; Pinto, DJ; Quan, ML; Rendina, AR; Rossi, KA; Smallwood, A; Wells, B; Wexler, RR; Wong, PC, 2006
)
0.33
"Razaxaban is a selective, potent, and orally bioavailable inhibitor of coagulation factor Xa."( Reductive isoxazole ring opening of the anticoagulant razaxaban is the major metabolic clearance pathway in rats and dogs.
Bonacorsi, SJ; Chen, SY; He, K; Knabb, RM; Lam, PY; Lecureux, L; Patrone, LM; Quan, M; Raghavan, N; Skiles, GL; Zhang, D; Zhang, H, 2008
)
2.04
" A set of compounds obtained from optimization of the R group and the C-3 substituent were orally bioavailable in dogs."( Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
He, K; King, SR; Knabb, RM; Lam, PY; Luettgen, JM; Qiao, JX; Rendina, AR; Wexler, RR; Wong, PC; Xin, B, 2009
)
0.35

Dosage Studied

ExcerptRelevanceReference
"A multitier approach was successful in identifying a solid dosage form that minimizes the pH-dependent absorption of this drug candidate."( Formulation of solid dosage forms to overcome gastric pH interaction of the factor Xa inhibitor, BMS-561389.
Badawy, SI; Gray, DB; Hussain, MA; Schuster, AE; Sun, D; Zhao, F, 2006
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (18)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Coagulation factor XHomo sapiens (human)Ki0.00020.00020.00020.0002AID977610
Coagulation factor XOryctolagus cuniculus (rabbit)Ki0.00020.00010.00020.0002AID263278; AID302366
ProthrombinHomo sapiens (human)Ki4.83220.00000.78469.0000AID1796932; AID1796936; AID263264; AID269921; AID276527; AID310308; AID313678; AID343881; AID458312
Coagulation factor IXHomo sapiens (human)Ki6.66940.00022.35479.0000AID1796932; AID1796936; AID263267; AID269931; AID276531; AID313687
Coagulation factor XHomo sapiens (human)Ki3.22680.00000.47089.0000AID1796932; AID1796935; AID1796936; AID1796951; AID263261; AID269919; AID276519; AID302353; AID312549; AID313675; AID343864; AID396701; AID458311; AID527394
PlasminogenHomo sapiens (human)Ki8.65000.01701.15604.4000AID263269; AID269933; AID276533; AID313690
Urokinase-type plasminogen activatorHomo sapiens (human)Ki7.65000.01702.62687.0000AID263272; AID276534
Tissue-type plasminogen activatorHomo sapiens (human)Ki17.65000.01703.71968.6000AID263270; AID269935; AID276535; AID313691
Cationic trypsinBos taurus (cattle)Ki7.04000.00001.07539.0000AID1796932; AID1796936
Plasma kallikreinHomo sapiens (human)Ki6.70000.00023.34749.6000AID1796932; AID313679
Vitamin K-dependent protein CHomo sapiens (human)Ki11.15001.80002.10002.4000AID269930; AID313686
Trypsin-1Homo sapiens (human)Ki6.97140.00001.76768.9000AID263265; AID269928; AID276529; AID312550; AID313679; AID343866; AID458313
Trypsin-2Homo sapiens (human)Ki6.97140.00430.94873.2900AID263265; AID269928; AID276529; AID312550; AID313679; AID343866; AID458313
Coagulation factor VIIHomo sapiens (human)Ki6.93150.00021.55669.0000AID1796932; AID1796936; AID263268; AID269932; AID276532
Chymotrypsinogen BHomo sapiens (human)Ki5.40000.32004.41008.5000AID263273; AID269934
Trypsin-3Homo sapiens (human)Ki6.97140.00430.94873.2900AID263265; AID269928; AID276529; AID312550; AID313679; AID343866; AID458313
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (100)

Processvia Protein(s)Taxonomy
positive regulation of protein phosphorylationProthrombinHomo sapiens (human)
proteolysisProthrombinHomo sapiens (human)
acute-phase responseProthrombinHomo sapiens (human)
cell surface receptor signaling pathwayProthrombinHomo sapiens (human)
G protein-coupled receptor signaling pathwayProthrombinHomo sapiens (human)
blood coagulationProthrombinHomo sapiens (human)
positive regulation of cell population proliferationProthrombinHomo sapiens (human)
regulation of cell shapeProthrombinHomo sapiens (human)
response to woundingProthrombinHomo sapiens (human)
negative regulation of platelet activationProthrombinHomo sapiens (human)
platelet activationProthrombinHomo sapiens (human)
regulation of blood coagulationProthrombinHomo sapiens (human)
positive regulation of blood coagulationProthrombinHomo sapiens (human)
positive regulation of cell growthProthrombinHomo sapiens (human)
positive regulation of insulin secretionProthrombinHomo sapiens (human)
positive regulation of collagen biosynthetic processProthrombinHomo sapiens (human)
fibrinolysisProthrombinHomo sapiens (human)
negative regulation of proteolysisProthrombinHomo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATProthrombinHomo sapiens (human)
negative regulation of astrocyte differentiationProthrombinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolProthrombinHomo sapiens (human)
regulation of cytosolic calcium ion concentrationProthrombinHomo sapiens (human)
cytolysis by host of symbiont cellsProthrombinHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionProthrombinHomo sapiens (human)
negative regulation of fibrinolysisProthrombinHomo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptideProthrombinHomo sapiens (human)
neutrophil-mediated killing of gram-negative bacteriumProthrombinHomo sapiens (human)
positive regulation of lipid kinase activityProthrombinHomo sapiens (human)
negative regulation of cytokine production involved in inflammatory responseProthrombinHomo sapiens (human)
positive regulation of protein localization to nucleusProthrombinHomo sapiens (human)
positive regulation of phospholipase C-activating G protein-coupled receptor signaling pathwayProthrombinHomo sapiens (human)
ligand-gated ion channel signaling pathwayProthrombinHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processProthrombinHomo sapiens (human)
proteolysisCoagulation factor IXHomo sapiens (human)
blood coagulationCoagulation factor IXHomo sapiens (human)
zymogen activationCoagulation factor IXHomo sapiens (human)
proteolysisCoagulation factor XHomo sapiens (human)
blood coagulationCoagulation factor XHomo sapiens (human)
positive regulation of cell migrationCoagulation factor XHomo sapiens (human)
positive regulation of TOR signalingCoagulation factor XHomo sapiens (human)
proteolysisPlasminogenHomo sapiens (human)
blood coagulationPlasminogenHomo sapiens (human)
negative regulation of cell population proliferationPlasminogenHomo sapiens (human)
negative regulation of cell-substrate adhesionPlasminogenHomo sapiens (human)
extracellular matrix disassemblyPlasminogenHomo sapiens (human)
tissue regenerationPlasminogenHomo sapiens (human)
fibrinolysisPlasminogenHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationPlasminogenHomo sapiens (human)
myoblast differentiationPlasminogenHomo sapiens (human)
muscle cell cellular homeostasisPlasminogenHomo sapiens (human)
tissue remodelingPlasminogenHomo sapiens (human)
biological process involved in interaction with symbiontPlasminogenHomo sapiens (human)
negative regulation of fibrinolysisPlasminogenHomo sapiens (human)
positive regulation of fibrinolysisPlasminogenHomo sapiens (human)
trophoblast giant cell differentiationPlasminogenHomo sapiens (human)
labyrinthine layer blood vessel developmentPlasminogenHomo sapiens (human)
mononuclear cell migrationPlasminogenHomo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmissionPlasminogenHomo sapiens (human)
negative regulation of cell-cell adhesion mediated by cadherinPlasminogenHomo sapiens (human)
positive regulation of cell migrationUrokinase-type plasminogen activatorHomo sapiens (human)
response to hypoxiaUrokinase-type plasminogen activatorHomo sapiens (human)
proteolysisUrokinase-type plasminogen activatorHomo sapiens (human)
chemotaxisUrokinase-type plasminogen activatorHomo sapiens (human)
signal transductionUrokinase-type plasminogen activatorHomo sapiens (human)
blood coagulationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of signaling receptor activityUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of plasminogen activationUrokinase-type plasminogen activatorHomo sapiens (human)
negative regulation of plasminogen activationUrokinase-type plasminogen activatorHomo sapiens (human)
smooth muscle cell migrationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of smooth muscle cell migrationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of cell adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
plasminogen activationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of cell adhesion mediated by integrinUrokinase-type plasminogen activatorHomo sapiens (human)
urokinase plasminogen activator signaling pathwayUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of cell population proliferationUrokinase-type plasminogen activatorHomo sapiens (human)
fibrinolysisUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of fibrinolysisUrokinase-type plasminogen activatorHomo sapiens (human)
negative regulation of fibrinolysisUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of wound healingUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of smooth muscle cell-matrix adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
response to hypoxiaTissue-type plasminogen activatorHomo sapiens (human)
proteolysisTissue-type plasminogen activatorHomo sapiens (human)
blood coagulationTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of plasminogen activationTissue-type plasminogen activatorHomo sapiens (human)
plasminogen activationTissue-type plasminogen activatorHomo sapiens (human)
protein modification processTissue-type plasminogen activatorHomo sapiens (human)
fibrinolysisTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of proteolysisTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of fibrinolysisTissue-type plasminogen activatorHomo sapiens (human)
prevention of polyspermyTissue-type plasminogen activatorHomo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmissionTissue-type plasminogen activatorHomo sapiens (human)
platelet-derived growth factor receptor signaling pathwayTissue-type plasminogen activatorHomo sapiens (human)
smooth muscle cell migrationTissue-type plasminogen activatorHomo sapiens (human)
proteolysisCationic trypsinBos taurus (cattle)
digestionCationic trypsinBos taurus (cattle)
blood coagulationCoagulation factor XIHomo sapiens (human)
plasminogen activationCoagulation factor XIHomo sapiens (human)
positive regulation of fibrinolysisCoagulation factor XIHomo sapiens (human)
Factor XII activationPlasma kallikreinHomo sapiens (human)
proteolysisPlasma kallikreinHomo sapiens (human)
blood coagulationPlasma kallikreinHomo sapiens (human)
zymogen activationPlasma kallikreinHomo sapiens (human)
plasminogen activationPlasma kallikreinHomo sapiens (human)
fibrinolysisPlasma kallikreinHomo sapiens (human)
positive regulation of fibrinolysisPlasma kallikreinHomo sapiens (human)
proteolysisVitamin K-dependent protein CHomo sapiens (human)
blood coagulationVitamin K-dependent protein CHomo sapiens (human)
negative regulation of blood coagulationVitamin K-dependent protein CHomo sapiens (human)
negative regulation of apoptotic processVitamin K-dependent protein CHomo sapiens (human)
negative regulation of inflammatory responseVitamin K-dependent protein CHomo sapiens (human)
negative regulation of coagulationVitamin K-dependent protein CHomo sapiens (human)
positive regulation of establishment of endothelial barrierVitamin K-dependent protein CHomo sapiens (human)
digestionTrypsin-1Homo sapiens (human)
extracellular matrix disassemblyTrypsin-1Homo sapiens (human)
proteolysisTrypsin-1Homo sapiens (human)
proteolysisTrypsin-2Homo sapiens (human)
digestionTrypsin-2Homo sapiens (human)
antimicrobial humoral responseTrypsin-2Homo sapiens (human)
extracellular matrix disassemblyTrypsin-2Homo sapiens (human)
positive regulation of cell growthTrypsin-2Homo sapiens (human)
collagen catabolic processTrypsin-2Homo sapiens (human)
positive regulation of cell adhesionTrypsin-2Homo sapiens (human)
response to hypoxiaCoagulation factor VIIHomo sapiens (human)
positive regulation of leukocyte chemotaxisCoagulation factor VIIHomo sapiens (human)
blood coagulationCoagulation factor VIIHomo sapiens (human)
circadian rhythmCoagulation factor VIIHomo sapiens (human)
response to carbon dioxideCoagulation factor VIIHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor signaling pathwayCoagulation factor VIIHomo sapiens (human)
protein processingCoagulation factor VIIHomo sapiens (human)
positive regulation of blood coagulationCoagulation factor VIIHomo sapiens (human)
positive regulation of cell migrationCoagulation factor VIIHomo sapiens (human)
animal organ regenerationCoagulation factor VIIHomo sapiens (human)
positive regulation of TOR signalingCoagulation factor VIIHomo sapiens (human)
response to estradiolCoagulation factor VIIHomo sapiens (human)
response to vitamin KCoagulation factor VIIHomo sapiens (human)
response to genisteinCoagulation factor VIIHomo sapiens (human)
response to estrogenCoagulation factor VIIHomo sapiens (human)
positive regulation of positive chemotaxisCoagulation factor VIIHomo sapiens (human)
response to growth hormoneCoagulation factor VIIHomo sapiens (human)
response to cholesterolCoagulation factor VIIHomo sapiens (human)
response to thyroxineCoagulation factor VIIHomo sapiens (human)
response to Thyroid stimulating hormoneCoagulation factor VIIHomo sapiens (human)
response to 2,3,7,8-tetrachlorodibenzodioxineCoagulation factor VIIHomo sapiens (human)
response to astaxanthinCoagulation factor VIIHomo sapiens (human)
response to thyrotropin-releasing hormoneCoagulation factor VIIHomo sapiens (human)
response to vitamin KCoagulation factor VHomo sapiens (human)
blood coagulationCoagulation factor VHomo sapiens (human)
blood circulationCoagulation factor VHomo sapiens (human)
digestionChymotrypsinogen BHomo sapiens (human)
proteolysisChymotrypsinogen BHomo sapiens (human)
proteolysisTrypsin-3Homo sapiens (human)
digestionTrypsin-3Homo sapiens (human)
antimicrobial humoral responseTrypsin-3Homo sapiens (human)
zymogen activationTrypsin-3Homo sapiens (human)
endothelial cell migrationTrypsin-3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
lipopolysaccharide bindingProthrombinHomo sapiens (human)
serine-type endopeptidase activityProthrombinHomo sapiens (human)
signaling receptor bindingProthrombinHomo sapiens (human)
calcium ion bindingProthrombinHomo sapiens (human)
protein bindingProthrombinHomo sapiens (human)
growth factor activityProthrombinHomo sapiens (human)
heparin bindingProthrombinHomo sapiens (human)
thrombospondin receptor activityProthrombinHomo sapiens (human)
endopeptidase activityCoagulation factor IXHomo sapiens (human)
serine-type endopeptidase activityCoagulation factor IXHomo sapiens (human)
calcium ion bindingCoagulation factor IXHomo sapiens (human)
protein bindingCoagulation factor IXHomo sapiens (human)
metal ion bindingCoagulation factor IXHomo sapiens (human)
serine-type endopeptidase activityCoagulation factor XHomo sapiens (human)
calcium ion bindingCoagulation factor XHomo sapiens (human)
protein bindingCoagulation factor XHomo sapiens (human)
phospholipid bindingCoagulation factor XHomo sapiens (human)
protease bindingPlasminogenHomo sapiens (human)
endopeptidase activityPlasminogenHomo sapiens (human)
serine-type endopeptidase activityPlasminogenHomo sapiens (human)
signaling receptor bindingPlasminogenHomo sapiens (human)
protein bindingPlasminogenHomo sapiens (human)
serine-type peptidase activityPlasminogenHomo sapiens (human)
enzyme bindingPlasminogenHomo sapiens (human)
kinase bindingPlasminogenHomo sapiens (human)
protein domain specific bindingPlasminogenHomo sapiens (human)
apolipoprotein bindingPlasminogenHomo sapiens (human)
protein-folding chaperone bindingPlasminogenHomo sapiens (human)
protein antigen bindingPlasminogenHomo sapiens (human)
serine-type endopeptidase activityUrokinase-type plasminogen activatorHomo sapiens (human)
protein bindingUrokinase-type plasminogen activatorHomo sapiens (human)
serine-type endopeptidase activityTissue-type plasminogen activatorHomo sapiens (human)
signaling receptor bindingTissue-type plasminogen activatorHomo sapiens (human)
protein bindingTissue-type plasminogen activatorHomo sapiens (human)
phosphoprotein bindingTissue-type plasminogen activatorHomo sapiens (human)
endopeptidase activityCationic trypsinBos taurus (cattle)
serine-type endopeptidase activityCationic trypsinBos taurus (cattle)
protein bindingCationic trypsinBos taurus (cattle)
metal ion bindingCationic trypsinBos taurus (cattle)
serpin family protein bindingCationic trypsinBos taurus (cattle)
serine-type endopeptidase activityCoagulation factor XIHomo sapiens (human)
protein bindingCoagulation factor XIHomo sapiens (human)
heparin bindingCoagulation factor XIHomo sapiens (human)
serine-type aminopeptidase activityCoagulation factor XIHomo sapiens (human)
serine-type endopeptidase activityPlasma kallikreinHomo sapiens (human)
protein bindingPlasma kallikreinHomo sapiens (human)
serine-type endopeptidase activityVitamin K-dependent protein CHomo sapiens (human)
calcium ion bindingVitamin K-dependent protein CHomo sapiens (human)
protein bindingVitamin K-dependent protein CHomo sapiens (human)
serine-type endopeptidase activityTrypsin-1Homo sapiens (human)
metal ion bindingTrypsin-1Homo sapiens (human)
metalloendopeptidase activityTrypsin-2Homo sapiens (human)
serine-type endopeptidase activityTrypsin-2Homo sapiens (human)
calcium ion bindingTrypsin-2Homo sapiens (human)
protein bindingTrypsin-2Homo sapiens (human)
serine-type peptidase activityTrypsin-2Homo sapiens (human)
serine-type endopeptidase activityCoagulation factor VIIHomo sapiens (human)
signaling receptor bindingCoagulation factor VIIHomo sapiens (human)
calcium ion bindingCoagulation factor VIIHomo sapiens (human)
protein bindingCoagulation factor VIIHomo sapiens (human)
serine-type peptidase activityCoagulation factor VIIHomo sapiens (human)
copper ion bindingCoagulation factor VHomo sapiens (human)
protein bindingCoagulation factor VHomo sapiens (human)
serine-type endopeptidase activityChymotrypsinogen BHomo sapiens (human)
serine-type endopeptidase activityTrypsin-3Homo sapiens (human)
calcium ion bindingTrypsin-3Homo sapiens (human)
protein bindingTrypsin-3Homo sapiens (human)
serine-type peptidase activityTrypsin-3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (34)

Processvia Protein(s)Taxonomy
external side of plasma membraneProthrombinHomo sapiens (human)
collagen-containing extracellular matrixProthrombinHomo sapiens (human)
extracellular regionProthrombinHomo sapiens (human)
extracellular spaceProthrombinHomo sapiens (human)
endoplasmic reticulum lumenProthrombinHomo sapiens (human)
Golgi lumenProthrombinHomo sapiens (human)
plasma membraneProthrombinHomo sapiens (human)
extracellular exosomeProthrombinHomo sapiens (human)
blood microparticleProthrombinHomo sapiens (human)
collagen-containing extracellular matrixProthrombinHomo sapiens (human)
extracellular spaceProthrombinHomo sapiens (human)
extracellular regionCoagulation factor IXHomo sapiens (human)
extracellular spaceCoagulation factor IXHomo sapiens (human)
endoplasmic reticulum lumenCoagulation factor IXHomo sapiens (human)
Golgi lumenCoagulation factor IXHomo sapiens (human)
plasma membraneCoagulation factor IXHomo sapiens (human)
collagen-containing extracellular matrixCoagulation factor IXHomo sapiens (human)
extracellular exosomeCoagulation factor IXHomo sapiens (human)
extracellular spaceCoagulation factor IXHomo sapiens (human)
extracellular regionCoagulation factor XHomo sapiens (human)
endoplasmic reticulum lumenCoagulation factor XHomo sapiens (human)
Golgi lumenCoagulation factor XHomo sapiens (human)
plasma membraneCoagulation factor XHomo sapiens (human)
external side of plasma membraneCoagulation factor XHomo sapiens (human)
extracellular spaceCoagulation factor XHomo sapiens (human)
extracellular regionPlasminogenHomo sapiens (human)
extracellular spacePlasminogenHomo sapiens (human)
plasma membranePlasminogenHomo sapiens (human)
external side of plasma membranePlasminogenHomo sapiens (human)
cell surfacePlasminogenHomo sapiens (human)
platelet alpha granule lumenPlasminogenHomo sapiens (human)
collagen-containing extracellular matrixPlasminogenHomo sapiens (human)
extracellular exosomePlasminogenHomo sapiens (human)
blood microparticlePlasminogenHomo sapiens (human)
Schaffer collateral - CA1 synapsePlasminogenHomo sapiens (human)
glutamatergic synapsePlasminogenHomo sapiens (human)
extracellular spacePlasminogenHomo sapiens (human)
extracellular regionUrokinase-type plasminogen activatorHomo sapiens (human)
extracellular spaceUrokinase-type plasminogen activatorHomo sapiens (human)
plasma membraneUrokinase-type plasminogen activatorHomo sapiens (human)
focal adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
external side of plasma membraneUrokinase-type plasminogen activatorHomo sapiens (human)
cell surfaceUrokinase-type plasminogen activatorHomo sapiens (human)
specific granule membraneUrokinase-type plasminogen activatorHomo sapiens (human)
extracellular exosomeUrokinase-type plasminogen activatorHomo sapiens (human)
tertiary granule membraneUrokinase-type plasminogen activatorHomo sapiens (human)
serine protease inhibitor complexUrokinase-type plasminogen activatorHomo sapiens (human)
protein complex involved in cell-matrix adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
serine-type endopeptidase complexUrokinase-type plasminogen activatorHomo sapiens (human)
extracellular spaceUrokinase-type plasminogen activatorHomo sapiens (human)
collagen-containing extracellular matrixTissue-type plasminogen activatorHomo sapiens (human)
extracellular regionTissue-type plasminogen activatorHomo sapiens (human)
cytoplasmTissue-type plasminogen activatorHomo sapiens (human)
cell surfaceTissue-type plasminogen activatorHomo sapiens (human)
secretory granuleTissue-type plasminogen activatorHomo sapiens (human)
apical part of cellTissue-type plasminogen activatorHomo sapiens (human)
extracellular exosomeTissue-type plasminogen activatorHomo sapiens (human)
serine protease inhibitor complexTissue-type plasminogen activatorHomo sapiens (human)
Schaffer collateral - CA1 synapseTissue-type plasminogen activatorHomo sapiens (human)
glutamatergic synapseTissue-type plasminogen activatorHomo sapiens (human)
extracellular spaceTissue-type plasminogen activatorHomo sapiens (human)
serine protease inhibitor complexCationic trypsinBos taurus (cattle)
extracellular regionCoagulation factor XIHomo sapiens (human)
extracellular spaceCoagulation factor XIHomo sapiens (human)
plasma membraneCoagulation factor XIHomo sapiens (human)
membraneCoagulation factor XIHomo sapiens (human)
extracellular exosomeCoagulation factor XIHomo sapiens (human)
extracellular regionPlasma kallikreinHomo sapiens (human)
extracellular spacePlasma kallikreinHomo sapiens (human)
plasma membranePlasma kallikreinHomo sapiens (human)
extracellular exosomePlasma kallikreinHomo sapiens (human)
extracellular regionVitamin K-dependent protein CHomo sapiens (human)
endoplasmic reticulumVitamin K-dependent protein CHomo sapiens (human)
endoplasmic reticulum lumenVitamin K-dependent protein CHomo sapiens (human)
Golgi apparatusVitamin K-dependent protein CHomo sapiens (human)
Golgi lumenVitamin K-dependent protein CHomo sapiens (human)
extracellular spaceVitamin K-dependent protein CHomo sapiens (human)
extracellular regionTrypsin-1Homo sapiens (human)
collagen-containing extracellular matrixTrypsin-1Homo sapiens (human)
blood microparticleTrypsin-1Homo sapiens (human)
extracellular spaceTrypsin-1Homo sapiens (human)
extracellular regionTrypsin-2Homo sapiens (human)
extracellular spaceTrypsin-2Homo sapiens (human)
extracellular matrixTrypsin-2Homo sapiens (human)
azurophil granule lumenTrypsin-2Homo sapiens (human)
extracellular spaceTrypsin-2Homo sapiens (human)
extracellular regionCoagulation factor VIIHomo sapiens (human)
endoplasmic reticulum lumenCoagulation factor VIIHomo sapiens (human)
Golgi lumenCoagulation factor VIIHomo sapiens (human)
plasma membraneCoagulation factor VIIHomo sapiens (human)
vesicleCoagulation factor VIIHomo sapiens (human)
collagen-containing extracellular matrixCoagulation factor VIIHomo sapiens (human)
serine-type peptidase complexCoagulation factor VIIHomo sapiens (human)
extracellular spaceCoagulation factor VIIHomo sapiens (human)
extracellular regionCoagulation factor VHomo sapiens (human)
extracellular spaceCoagulation factor VHomo sapiens (human)
endoplasmic reticulum lumenCoagulation factor VHomo sapiens (human)
plasma membraneCoagulation factor VHomo sapiens (human)
membraneCoagulation factor VHomo sapiens (human)
COPII-coated ER to Golgi transport vesicleCoagulation factor VHomo sapiens (human)
platelet alpha granule lumenCoagulation factor VHomo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartment membraneCoagulation factor VHomo sapiens (human)
extracellular vesicleCoagulation factor VHomo sapiens (human)
platelet alpha granuleCoagulation factor VHomo sapiens (human)
extracellular regionChymotrypsinogen BHomo sapiens (human)
extracellular regionTrypsin-3Homo sapiens (human)
extracellular spaceTrypsin-3Homo sapiens (human)
tertiary granule lumenTrypsin-3Homo sapiens (human)
extracellular spaceTrypsin-3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (131)

Assay IDTitleYearJournalArticle
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
AID1811Experimentally measured binding affinity data derived from PDB2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
AID313682Half life in dog at 0.2 mg/kg, po2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID269929Binding affinity to human plasma kallikrein2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID269923Clearance in dog2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID312547Inhibition of human alpha thrombin2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID313689Inhibition of human chymotrypsin2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID458311Inhibition of human factor 10a2010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Phenyltriazolinones as potent factor Xa inhibitors.
AID276523Volume of distribution in dog2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID263274Clearance in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID313687Inhibition of human factor 9a2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID527428Antithrombotic activity in rabbit arteriovenous-shunt thrombosis model measured per hr2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Factor Xa inhibitors: next-generation antithrombotic agents.
AID269930Binding affinity to human APC2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID313684Volume of distribution at steady state in dog at 0.5 mg/kg, iv2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID269922Apparent permeability in Caco-2 cells2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID263263Anticoagulant activity in human plasma by aPTT assay2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263261Binding affinity to human factor 10a2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID396708Oral bioavailability in dog at 0.2 mg/kg2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID310311Apparent permeability across Caco-2 cells2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID310308Inhibition of human thrombin2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID302367Antithrombotic potency in rabbit arteriovenous shunt thrombosis model2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Discovery of 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 (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation fa
AID312552Metabolic stability in human liver microsomes after 10 mins2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID458314Anticoagulant activity in rabbit plasma assessed as concentration required to double prothrombin time by aggregometer2010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Phenyltriazolinones as potent factor Xa inhibitors.
AID527410Volume of distribution at steady state in dog2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Factor Xa inhibitors: next-generation antithrombotic agents.
AID310312Clearance in dog at 0.5 mg/kg, iv and 0.2 mg/kg, po2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID343879Half life in dog at 0.2 mg/kg, po2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
AID302360Oral bioavailability in dog at 0.2 mg/kg, po2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Discovery of 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 (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation fa
AID313683Clearance in dog at 0.5 mg/kg, iv2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID269925Half life in orally dosed dog2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID313677Apparent permeability across human Caco-2 cells2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID263266Binding affinity to human aPC2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263272Binding affinity to human urokinase2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID396700Anticoagulant activity in human plasma assessed as drug level required to double prothrombin time2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID302365Protein binding in human serum by equilibrium dialysis2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Discovery of 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 (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation fa
AID276532Binding affinity to human factor VIIa2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID527411Antithrombotic activity in iv dosed rabbit assessed as restoration of integrated blood flow2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Factor Xa inhibitors: next-generation antithrombotic agents.
AID396709Anticoagulant activity in rabbit plasma assessed as drug level required to double prothrombin time2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID343877Clearance in dog at 0.5 mg/kg, iv2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
AID263279Anticoagulant activity in rabbit plasma by aPTT assay2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263262Permeability in Caco-2 cell2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID313690Inhibition of human plasmin2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID312553Apparent permeability across Caco-2 cells2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID276530Binding affinity to human APC2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID343865Anticoagulant activity in human plasma assessed as concentration required to double prothrombin time2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
AID263280Anticoagulant activity in rabbit plasma by PT assay2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263268Binding affinity to human factor 7a2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID276533Binding affinity to human plasmin2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID263273Binding affinity to human chymotrypsin2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263277Bioavailability in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID313691Inhibition of human tPA2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID276527Binding affinity to human thrombin2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID458312Inhibition of human factor 2a2010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Phenyltriazolinones as potent factor Xa inhibitors.
AID343878Volume of distribution at steady state in dog2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
AID276522Clearance in dog2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID269927Antithrombotic activity in rabbit arterio-venous shunt thrombosis model2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID276525Oral bioavailability in po dosed dog2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID269931Binding affinity to human f9a2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID302358Volume of distribution at steady state in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Discovery of 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 (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation fa
AID343864Inhibition of human factor 10a2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
AID313675Inhibition of human factor 10a2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID263269Binding affinity to human plasmin2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID343876Metabolic stability in human liver microsomes assessed as half life2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
AID310313Volume of distribution at steady state in dog at 0.5 mg/kg, iv and 0.2 mg/kg, po2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID396707Half life in dog at 0.2 mg/kg, po2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID313679Inhibition of human trypsin2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID312550Inhibition of human trypsin2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID269934Binding affinity to human chymotrypsin2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID527394Inhibition of factor 10a2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Factor Xa inhibitors: next-generation antithrombotic agents.
AID263276Half life in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID276524Half life in po dosed dog2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID313678Inhibition of human thrombin2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID313676Anticoagulant activity in human plasma assessed as concentration required to double prothrombin time2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID269920Anticoagulant activity in plasma by PT assay2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID302366Binding affinity to rabbit F10a2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Discovery of 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 (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation fa
AID312549Inhibition of human factor 10a2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID396701Binding affinity to human coagulation factor 10a2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID310314Half life in dog at 0.2 mg/kg, po2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID302357Clearance in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Discovery of 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 (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation fa
AID269932Binding affinity to human f7a2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID527407Oral bioavailability in dog2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Factor Xa inhibitors: next-generation antithrombotic agents.
AID396710Antithrombotic activity against iv dosed rabbit arterio-venous shunt model assessed as inhibition of thrombus formation2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID263264Binding affinity to human thrombin2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID396706Clearance in dog at 0.5 mg/kg, iv and 0.2 mg/kg, po2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID343867Inhibition of human factor 9a2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
AID263271Binding affinity to human plasma kallikrein2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID313688Inhibition of human factor 11a2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID276528Binding affinity to human chymotrypsin2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID312551Anticoagulant activity against human plasma assessed as concentration required to double activated partial thromboplastin time2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID269921Binding affinity to human F2a2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID527398Anticoagulant activity in human platelet assessed as concentration required to double activated partial prothrombin time2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Factor Xa inhibitors: next-generation antithrombotic agents.
AID396705Volume of distribution at steady state in dog at 0.5 mg/kg, iv and 0.2 mg/kg, po2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID313686Inhibition of human activated protein C2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID269919Binding affinity to human F10a2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID263281Antithrombotic activity in iv dosed rabbit arterio-venous shunt model2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263275Volume of distribution in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID458313Inhibition of human trypsin2010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Phenyltriazolinones as potent factor Xa inhibitors.
AID302353Binding affinity to human F10a2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Discovery of 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 (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation fa
AID269926Oral bioavailability in orally dosed dog2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID269924Volume of distribution in dog2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID276521Apparent permeability across Caco-2 cell membrane2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID302362Inhibition of thrombus formation in rabbit arteriovenous shunt thrombosis model2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Discovery of 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 (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation fa
AID343880Bioavailability in dog at 0.5 mg/kg, iv2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
AID527399Anticoagulant activity in human platelet assessed as concentration required to double prothrombin time2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Factor Xa inhibitors: next-generation antithrombotic agents.
AID269928Binding affinity to human trypsin2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID276531Binding affinity to human factor IXa2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID302363Half life in human liver microsomes2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Discovery of 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 (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation fa
AID263265Binding affinity to human trypsin2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID313685Inhibition of human plasma kallikrein2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID276534Binding affinity to human urokinase2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID269935Binding affinity to human tPA2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID276535Binding affinity to human tPA2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID343866Inhibition of human trypsin2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
AID396712Protein binding in rabbit plasma2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID263270Binding affinity to human tPA2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263282Protein binding in rabbit plasma2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID276519Binding affinity to human factor Xa2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID343881Inhibition of human thrombin2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
AID527409Clearance in dog2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Factor Xa inhibitors: next-generation antithrombotic agents.
AID269933Binding affinity to human plasmin2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID276526Inhibition of thrombus formation in rabbit AV shunt thrombosis model2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID313681Oral bioavailability in dog at 0.2 mg/kg2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID310315Oral bioavailability in dog at 0.2 mg/kg2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID396699Apparent permeability from apical to basolateral side of human Caco-2 cells2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID302359Half life in dog at 0.2 mg/kg, po2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Discovery of 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 (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation fa
AID263278Binding affinity to rabbit factor 10a2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID276529Binding affinity to human trypsin2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
AID263267Binding affinity to human factor 9a2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID1796932Enzyme Assay and Determination of the Inhibition Constants. from Article 10.1021/jm0497949: \\Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochlorid2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
AID1796936Enzyme Assay and Determination of the Inhibition Constants. from Article 10.1016/j.bmcl.2006.04.044: \\Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.\\2006Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14
Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.
AID1796935Enzyme Assay and Determination of the Inhibition Constants. from Article 10.1016/j.bmcl.2006.02.069: \\1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of bloo
AID1796951Enzyme Assay and Determination of the Inhibition Constants. from Article 10.1016/j.bmcl.2006.01.010: \\Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.\\2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's15 (75.00)29.6817
2010's5 (25.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.88

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index25.88 (24.57)
Research Supply Index3.04 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index29.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other19 (95.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]