Page last updated: 2024-12-11

bms 740808

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Description

1-(3-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-6-(2'-(3-hydroxy-N-pyrrolidinyl)methyl-(1,1')-biphen-4-yl)-1,4,5,6-tetrahydropyrazolo-(3,4-c)-pyridin-7-one: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6914623
CHEMBL ID378093
SCHEMBL ID8360280
MeSH IDM0501488

Synonyms (28)

Synonym
bms-740808 ,
1-(3-amino-1,2-benzisoxazol-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
5qc ,
2FZZ ,
1-(3-amino-1,2-benzoxazol-5-yl)-6-[4-(2-{[(3r)-3-hydroxypyrrolidin-1-yl]methyl}phenyl)phenyl]-3-(trifluoromethyl)-1h,4h,5h,6h,7h-pyrazolo[3,4-c]pyridin-7-one
bdbm12693
CHEMBL378093
1-(3-amino-1,2-benzoxazol-5-yl)-6-[4-[2-[[(3r)-3-hydroxypyrrolidin-1-yl]methyl]phenyl]phenyl]-3-(trifluoromethyl)-4,5-dihydropyrazolo[3,4-c]pyridin-7-one
BCP9000430
bms740808
bms 740808
BCPP000326
280118-23-2
BCP0726000241
unii-ldd74e663f
1-(3-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-6-(2'-(3-hydroxy-n-pyrrolidinyl)methyl-(1,1')-biphen-4-yl)-1,4,5,6-tetrahydropyrazolo-(3,4-c)-pyridin-7-one
ldd74e663f ,
7h-pyrazolo(3,4-c)pyridin-7-one, 1-(3-amino-1,2-benzisoxazol-5-yl)-1,4,5,6-tetrahydro-6-(2'-(((3r)-3-hydroxy-1-pyrrolidinyl)methyl)(1,1'-biphenyl)-4-yl)-3-(trifluoromethyl)-
1-(3-amino-1,2-benz(d)isoxazol-5-yl)-3-trifluoromethyl-6-(4-(2-(((3r)-3-hydroxy-1-pyrrolidinyl)methyl)phenyl)phenyl)-1,4,5,6-tetrahydro-7h-pyrazolo(3,4-c)pyridin-7-one
SCHEMBL8360280
J-503094
1-(3-amino-1,2-benz[d]isoxazol-5-yl)-3-trifluoromethyl-6-[4-[2-[[(3r)-3-hydroxy-1-pyrrolidinyl]methyl]phenyl]phenyl]-1,4,5,6-tetrahy dro-7h-pyrazolo[3,4-c]pyridin-7-one
DTXSID40182293
dfriqjhmgzbfom-jochjyfzsa-n
BCP23400
Q27282933
(r)-1-(3-aminobenzo[d]isoxazol-5-yl)-6-(2'-((3-hydroxypyrrolidin-1-yl)methyl)-[1,1'-biphenyl]-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7h-pyrazolo[3,4-c]pyridin-7-one
AKOS040750833

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" 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
)
0.35

Bioavailability

ExcerptReferenceRelevance
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (14)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Coagulation factor XHomo sapiens (human)Ki0.00000.00000.00000.0000AID977610
Coagulation factor XOryctolagus cuniculus (rabbit)Ki0.00010.00010.00020.0002AID302366
ProthrombinHomo sapiens (human)Ki0.03500.00000.78469.0000AID269921; AID313678
Coagulation factor IXHomo sapiens (human)Ki2.80000.00022.35479.0000AID269931
Coagulation factor XHomo sapiens (human)Ki0.00000.00000.47089.0000AID1796935; AID1796939; AID269919; AID276519; AID302353; AID313675; AID527394
PlasminogenHomo sapiens (human)Ki2.80000.01701.15604.4000AID269933
Tissue-type plasminogen activatorHomo sapiens (human)Ki2.80000.01703.71968.6000AID269935
Plasma kallikreinHomo sapiens (human)Ki2.80000.00023.34749.6000AID313679
Vitamin K-dependent protein CHomo sapiens (human)Ki2.80001.80002.10002.4000AID269930
Trypsin-1Homo sapiens (human)Ki2.80000.00001.76768.9000AID269928; AID313679
Trypsin-2Homo sapiens (human)Ki2.80000.00430.94873.2900AID269928; AID313679
Coagulation factor VIIHomo sapiens (human)Ki2.80000.00021.55669.0000AID269932
Chymotrypsinogen BHomo sapiens (human)Ki2.80000.32004.41008.5000AID269934
Trypsin-3Homo sapiens (human)Ki2.80000.00430.94873.2900AID269928; AID313679
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (87)

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)
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)
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)
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 (21)

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 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)
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)
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 (24)

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)
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)
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 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 (44)

Assay IDTitleYearJournalArticle
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.
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
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.
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.
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
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
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.
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
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.
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
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.
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
AID276520Anticoagulant activity in human plasma assessed as clotting PT value2006Bioorganic & 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.
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
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
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
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
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.
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
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
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.
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
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
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.
AID269936Protein binding in plasma by equilibrium dialysis 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
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
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
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
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.
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
AID527394Inhibition of factor 10a2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Factor Xa inhibitors: next-generation antithrombotic agents.
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
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
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
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
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
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
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
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
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.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2006Bioorganic & 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
AID1811Experimentally measured binding affinity data derived from PDB2006Bioorganic & 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
AID1796939Enzyme Assay and Determination of the Inhibition Constants. from Article 10.1016/j.bmcl.2006.08.027: \\Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.\\2006Bioorganic & 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.
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
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (80.00)29.6817
2010's1 (20.00)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: 12.56

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]