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 Source	ID
PubMed CID	204102
CHEMBL ID	206335
SCHEMBL ID	677372
MeSH ID	M0484106

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.

Excerpt	Reference	Relevance
"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.

Excerpt	Reference	Relevance
" 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

Excerpt	Reference	Relevance
" 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.

Excerpt	Reference	Relevance
" 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

Excerpt	Relevance	Reference
"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

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Coagulation factor X	Homo sapiens (human)	Ki	0.0002	0.0002	0.0002	0.0002	AID977610
Coagulation factor X	Oryctolagus cuniculus (rabbit)	Ki	0.0002	0.0001	0.0002	0.0002	AID263278; AID302366
Prothrombin	Homo sapiens (human)	Ki	4.8322	0.0000	0.7846	9.0000	AID1796932; AID1796936; AID263264; AID269921; AID276527; AID310308; AID313678; AID343881; AID458312
Coagulation factor IX	Homo sapiens (human)	Ki	6.6694	0.0002	2.3547	9.0000	AID1796932; AID1796936; AID263267; AID269931; AID276531; AID313687
Coagulation factor X	Homo sapiens (human)	Ki	3.2268	0.0000	0.4708	9.0000	AID1796932; AID1796935; AID1796936; AID1796951; AID263261; AID269919; AID276519; AID302353; AID312549; AID313675; AID343864; AID396701; AID458311; AID527394
Plasminogen	Homo sapiens (human)	Ki	8.6500	0.0170	1.1560	4.4000	AID263269; AID269933; AID276533; AID313690
Urokinase-type plasminogen activator	Homo sapiens (human)	Ki	7.6500	0.0170	2.6268	7.0000	AID263272; AID276534
Tissue-type plasminogen activator	Homo sapiens (human)	Ki	17.6500	0.0170	3.7196	8.6000	AID263270; AID269935; AID276535; AID313691
Cationic trypsin	Bos taurus (cattle)	Ki	7.0400	0.0000	1.0753	9.0000	AID1796932; AID1796936
Plasma kallikrein	Homo sapiens (human)	Ki	6.7000	0.0002	3.3474	9.6000	AID1796932; AID313679
Vitamin K-dependent protein C	Homo sapiens (human)	Ki	11.1500	1.8000	2.1000	2.4000	AID269930; AID313686
Trypsin-1	Homo sapiens (human)	Ki	6.9714	0.0000	1.7676	8.9000	AID263265; AID269928; AID276529; AID312550; AID313679; AID343866; AID458313
Trypsin-2	Homo sapiens (human)	Ki	6.9714	0.0043	0.9487	3.2900	AID263265; AID269928; AID276529; AID312550; AID313679; AID343866; AID458313
Coagulation factor VII	Homo sapiens (human)	Ki	6.9315	0.0002	1.5566	9.0000	AID1796932; AID1796936; AID263268; AID269932; AID276532
Chymotrypsinogen B	Homo sapiens (human)	Ki	5.4000	0.3200	4.4100	8.5000	AID263273; AID269934
Trypsin-3	Homo sapiens (human)	Ki	6.9714	0.0043	0.9487	3.2900	AID263265; 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)

Process	via Protein(s)	Taxonomy
positive regulation of protein phosphorylation	Prothrombin	Homo sapiens (human)
proteolysis	Prothrombin	Homo sapiens (human)
acute-phase response	Prothrombin	Homo sapiens (human)
cell surface receptor signaling pathway	Prothrombin	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Prothrombin	Homo sapiens (human)
blood coagulation	Prothrombin	Homo sapiens (human)
positive regulation of cell population proliferation	Prothrombin	Homo sapiens (human)
regulation of cell shape	Prothrombin	Homo sapiens (human)
response to wounding	Prothrombin	Homo sapiens (human)
negative regulation of platelet activation	Prothrombin	Homo sapiens (human)
platelet activation	Prothrombin	Homo sapiens (human)
regulation of blood coagulation	Prothrombin	Homo sapiens (human)
positive regulation of blood coagulation	Prothrombin	Homo sapiens (human)
positive regulation of cell growth	Prothrombin	Homo sapiens (human)
positive regulation of insulin secretion	Prothrombin	Homo sapiens (human)
positive regulation of collagen biosynthetic process	Prothrombin	Homo sapiens (human)
fibrinolysis	Prothrombin	Homo sapiens (human)
negative regulation of proteolysis	Prothrombin	Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STAT	Prothrombin	Homo sapiens (human)
negative regulation of astrocyte differentiation	Prothrombin	Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosol	Prothrombin	Homo sapiens (human)
regulation of cytosolic calcium ion concentration	Prothrombin	Homo sapiens (human)
cytolysis by host of symbiont cells	Prothrombin	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Prothrombin	Homo sapiens (human)
negative regulation of fibrinolysis	Prothrombin	Homo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptide	Prothrombin	Homo sapiens (human)
neutrophil-mediated killing of gram-negative bacterium	Prothrombin	Homo sapiens (human)
positive regulation of lipid kinase activity	Prothrombin	Homo sapiens (human)
negative regulation of cytokine production involved in inflammatory response	Prothrombin	Homo sapiens (human)
positive regulation of protein localization to nucleus	Prothrombin	Homo sapiens (human)
positive regulation of phospholipase C-activating G protein-coupled receptor signaling pathway	Prothrombin	Homo sapiens (human)
ligand-gated ion channel signaling pathway	Prothrombin	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Prothrombin	Homo sapiens (human)
proteolysis	Coagulation factor IX	Homo sapiens (human)
blood coagulation	Coagulation factor IX	Homo sapiens (human)
zymogen activation	Coagulation factor IX	Homo sapiens (human)
proteolysis	Coagulation factor X	Homo sapiens (human)
blood coagulation	Coagulation factor X	Homo sapiens (human)
positive regulation of cell migration	Coagulation factor X	Homo sapiens (human)
positive regulation of TOR signaling	Coagulation factor X	Homo sapiens (human)
proteolysis	Plasminogen	Homo sapiens (human)
blood coagulation	Plasminogen	Homo sapiens (human)
negative regulation of cell population proliferation	Plasminogen	Homo sapiens (human)
negative regulation of cell-substrate adhesion	Plasminogen	Homo sapiens (human)
extracellular matrix disassembly	Plasminogen	Homo sapiens (human)
tissue regeneration	Plasminogen	Homo sapiens (human)
fibrinolysis	Plasminogen	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	Plasminogen	Homo sapiens (human)
myoblast differentiation	Plasminogen	Homo sapiens (human)
muscle cell cellular homeostasis	Plasminogen	Homo sapiens (human)
tissue remodeling	Plasminogen	Homo sapiens (human)
biological process involved in interaction with symbiont	Plasminogen	Homo sapiens (human)
negative regulation of fibrinolysis	Plasminogen	Homo sapiens (human)
positive regulation of fibrinolysis	Plasminogen	Homo sapiens (human)
trophoblast giant cell differentiation	Plasminogen	Homo sapiens (human)
labyrinthine layer blood vessel development	Plasminogen	Homo sapiens (human)
mononuclear cell migration	Plasminogen	Homo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmission	Plasminogen	Homo sapiens (human)
negative regulation of cell-cell adhesion mediated by cadherin	Plasminogen	Homo sapiens (human)
positive regulation of cell migration	Urokinase-type plasminogen activator	Homo sapiens (human)
response to hypoxia	Urokinase-type plasminogen activator	Homo sapiens (human)
proteolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
chemotaxis	Urokinase-type plasminogen activator	Homo sapiens (human)
signal transduction	Urokinase-type plasminogen activator	Homo sapiens (human)
blood coagulation	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of signaling receptor activity	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of plasminogen activation	Urokinase-type plasminogen activator	Homo sapiens (human)
negative regulation of plasminogen activation	Urokinase-type plasminogen activator	Homo sapiens (human)
smooth muscle cell migration	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of smooth muscle cell migration	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of cell adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
plasminogen activation	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of cell adhesion mediated by integrin	Urokinase-type plasminogen activator	Homo sapiens (human)
urokinase plasminogen activator signaling pathway	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of cell population proliferation	Urokinase-type plasminogen activator	Homo sapiens (human)
fibrinolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of fibrinolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
negative regulation of fibrinolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of wound healing	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of smooth muscle cell-matrix adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
response to hypoxia	Tissue-type plasminogen activator	Homo sapiens (human)
proteolysis	Tissue-type plasminogen activator	Homo sapiens (human)
blood coagulation	Tissue-type plasminogen activator	Homo sapiens (human)
negative regulation of plasminogen activation	Tissue-type plasminogen activator	Homo sapiens (human)
plasminogen activation	Tissue-type plasminogen activator	Homo sapiens (human)
protein modification process	Tissue-type plasminogen activator	Homo sapiens (human)
fibrinolysis	Tissue-type plasminogen activator	Homo sapiens (human)
negative regulation of proteolysis	Tissue-type plasminogen activator	Homo sapiens (human)
negative regulation of fibrinolysis	Tissue-type plasminogen activator	Homo sapiens (human)
prevention of polyspermy	Tissue-type plasminogen activator	Homo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmission	Tissue-type plasminogen activator	Homo sapiens (human)
platelet-derived growth factor receptor signaling pathway	Tissue-type plasminogen activator	Homo sapiens (human)
smooth muscle cell migration	Tissue-type plasminogen activator	Homo sapiens (human)
proteolysis	Cationic trypsin	Bos taurus (cattle)
digestion	Cationic trypsin	Bos taurus (cattle)
blood coagulation	Coagulation factor XI	Homo sapiens (human)
plasminogen activation	Coagulation factor XI	Homo sapiens (human)
positive regulation of fibrinolysis	Coagulation factor XI	Homo sapiens (human)
Factor XII activation	Plasma kallikrein	Homo sapiens (human)
proteolysis	Plasma kallikrein	Homo sapiens (human)
blood coagulation	Plasma kallikrein	Homo sapiens (human)
zymogen activation	Plasma kallikrein	Homo sapiens (human)
plasminogen activation	Plasma kallikrein	Homo sapiens (human)
fibrinolysis	Plasma kallikrein	Homo sapiens (human)
positive regulation of fibrinolysis	Plasma kallikrein	Homo sapiens (human)
proteolysis	Vitamin K-dependent protein C	Homo sapiens (human)
blood coagulation	Vitamin K-dependent protein C	Homo sapiens (human)
negative regulation of blood coagulation	Vitamin K-dependent protein C	Homo sapiens (human)
negative regulation of apoptotic process	Vitamin K-dependent protein C	Homo sapiens (human)
negative regulation of inflammatory response	Vitamin K-dependent protein C	Homo sapiens (human)
negative regulation of coagulation	Vitamin K-dependent protein C	Homo sapiens (human)
positive regulation of establishment of endothelial barrier	Vitamin K-dependent protein C	Homo sapiens (human)
digestion	Trypsin-1	Homo sapiens (human)
extracellular matrix disassembly	Trypsin-1	Homo sapiens (human)
proteolysis	Trypsin-1	Homo sapiens (human)
proteolysis	Trypsin-2	Homo sapiens (human)
digestion	Trypsin-2	Homo sapiens (human)
antimicrobial humoral response	Trypsin-2	Homo sapiens (human)
extracellular matrix disassembly	Trypsin-2	Homo sapiens (human)
positive regulation of cell growth	Trypsin-2	Homo sapiens (human)
collagen catabolic process	Trypsin-2	Homo sapiens (human)
positive regulation of cell adhesion	Trypsin-2	Homo sapiens (human)
response to hypoxia	Coagulation factor VII	Homo sapiens (human)
positive regulation of leukocyte chemotaxis	Coagulation factor VII	Homo sapiens (human)
blood coagulation	Coagulation factor VII	Homo sapiens (human)
circadian rhythm	Coagulation factor VII	Homo sapiens (human)
response to carbon dioxide	Coagulation factor VII	Homo sapiens (human)
positive regulation of platelet-derived growth factor receptor signaling pathway	Coagulation factor VII	Homo sapiens (human)
protein processing	Coagulation factor VII	Homo sapiens (human)
positive regulation of blood coagulation	Coagulation factor VII	Homo sapiens (human)
positive regulation of cell migration	Coagulation factor VII	Homo sapiens (human)
animal organ regeneration	Coagulation factor VII	Homo sapiens (human)
positive regulation of TOR signaling	Coagulation factor VII	Homo sapiens (human)
response to estradiol	Coagulation factor VII	Homo sapiens (human)
response to vitamin K	Coagulation factor VII	Homo sapiens (human)
response to genistein	Coagulation factor VII	Homo sapiens (human)
response to estrogen	Coagulation factor VII	Homo sapiens (human)
positive regulation of positive chemotaxis	Coagulation factor VII	Homo sapiens (human)
response to growth hormone	Coagulation factor VII	Homo sapiens (human)
response to cholesterol	Coagulation factor VII	Homo sapiens (human)
response to thyroxine	Coagulation factor VII	Homo sapiens (human)
response to Thyroid stimulating hormone	Coagulation factor VII	Homo sapiens (human)
response to 2,3,7,8-tetrachlorodibenzodioxine	Coagulation factor VII	Homo sapiens (human)
response to astaxanthin	Coagulation factor VII	Homo sapiens (human)
response to thyrotropin-releasing hormone	Coagulation factor VII	Homo sapiens (human)
response to vitamin K	Coagulation factor V	Homo sapiens (human)
blood coagulation	Coagulation factor V	Homo sapiens (human)
blood circulation	Coagulation factor V	Homo sapiens (human)
digestion	Chymotrypsinogen B	Homo sapiens (human)
proteolysis	Chymotrypsinogen B	Homo sapiens (human)
proteolysis	Trypsin-3	Homo sapiens (human)
digestion	Trypsin-3	Homo sapiens (human)
antimicrobial humoral response	Trypsin-3	Homo sapiens (human)
zymogen activation	Trypsin-3	Homo sapiens (human)
endothelial cell migration	Trypsin-3	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Process	via Protein(s)	Taxonomy
lipopolysaccharide binding	Prothrombin	Homo sapiens (human)
serine-type endopeptidase activity	Prothrombin	Homo sapiens (human)
signaling receptor binding	Prothrombin	Homo sapiens (human)
calcium ion binding	Prothrombin	Homo sapiens (human)
protein binding	Prothrombin	Homo sapiens (human)
growth factor activity	Prothrombin	Homo sapiens (human)
heparin binding	Prothrombin	Homo sapiens (human)
thrombospondin receptor activity	Prothrombin	Homo sapiens (human)
endopeptidase activity	Coagulation factor IX	Homo sapiens (human)
serine-type endopeptidase activity	Coagulation factor IX	Homo sapiens (human)
calcium ion binding	Coagulation factor IX	Homo sapiens (human)
protein binding	Coagulation factor IX	Homo sapiens (human)
metal ion binding	Coagulation factor IX	Homo sapiens (human)
serine-type endopeptidase activity	Coagulation factor X	Homo sapiens (human)
calcium ion binding	Coagulation factor X	Homo sapiens (human)
protein binding	Coagulation factor X	Homo sapiens (human)
phospholipid binding	Coagulation factor X	Homo sapiens (human)
protease binding	Plasminogen	Homo sapiens (human)
endopeptidase activity	Plasminogen	Homo sapiens (human)
serine-type endopeptidase activity	Plasminogen	Homo sapiens (human)
signaling receptor binding	Plasminogen	Homo sapiens (human)
protein binding	Plasminogen	Homo sapiens (human)
serine-type peptidase activity	Plasminogen	Homo sapiens (human)
enzyme binding	Plasminogen	Homo sapiens (human)
kinase binding	Plasminogen	Homo sapiens (human)
protein domain specific binding	Plasminogen	Homo sapiens (human)
apolipoprotein binding	Plasminogen	Homo sapiens (human)
protein-folding chaperone binding	Plasminogen	Homo sapiens (human)
protein antigen binding	Plasminogen	Homo sapiens (human)
serine-type endopeptidase activity	Urokinase-type plasminogen activator	Homo sapiens (human)
protein binding	Urokinase-type plasminogen activator	Homo sapiens (human)
serine-type endopeptidase activity	Tissue-type plasminogen activator	Homo sapiens (human)
signaling receptor binding	Tissue-type plasminogen activator	Homo sapiens (human)
protein binding	Tissue-type plasminogen activator	Homo sapiens (human)
phosphoprotein binding	Tissue-type plasminogen activator	Homo sapiens (human)
endopeptidase activity	Cationic trypsin	Bos taurus (cattle)
serine-type endopeptidase activity	Cationic trypsin	Bos taurus (cattle)
protein binding	Cationic trypsin	Bos taurus (cattle)
metal ion binding	Cationic trypsin	Bos taurus (cattle)
serpin family protein binding	Cationic trypsin	Bos taurus (cattle)
serine-type endopeptidase activity	Coagulation factor XI	Homo sapiens (human)
protein binding	Coagulation factor XI	Homo sapiens (human)
heparin binding	Coagulation factor XI	Homo sapiens (human)
serine-type aminopeptidase activity	Coagulation factor XI	Homo sapiens (human)
serine-type endopeptidase activity	Plasma kallikrein	Homo sapiens (human)
protein binding	Plasma kallikrein	Homo sapiens (human)
serine-type endopeptidase activity	Vitamin K-dependent protein C	Homo sapiens (human)
calcium ion binding	Vitamin K-dependent protein C	Homo sapiens (human)
protein binding	Vitamin K-dependent protein C	Homo sapiens (human)
serine-type endopeptidase activity	Trypsin-1	Homo sapiens (human)
metal ion binding	Trypsin-1	Homo sapiens (human)
metalloendopeptidase activity	Trypsin-2	Homo sapiens (human)
serine-type endopeptidase activity	Trypsin-2	Homo sapiens (human)
calcium ion binding	Trypsin-2	Homo sapiens (human)
protein binding	Trypsin-2	Homo sapiens (human)
serine-type peptidase activity	Trypsin-2	Homo sapiens (human)
serine-type endopeptidase activity	Coagulation factor VII	Homo sapiens (human)
signaling receptor binding	Coagulation factor VII	Homo sapiens (human)
calcium ion binding	Coagulation factor VII	Homo sapiens (human)
protein binding	Coagulation factor VII	Homo sapiens (human)
serine-type peptidase activity	Coagulation factor VII	Homo sapiens (human)
copper ion binding	Coagulation factor V	Homo sapiens (human)
protein binding	Coagulation factor V	Homo sapiens (human)
serine-type endopeptidase activity	Chymotrypsinogen B	Homo sapiens (human)
serine-type endopeptidase activity	Trypsin-3	Homo sapiens (human)
calcium ion binding	Trypsin-3	Homo sapiens (human)
protein binding	Trypsin-3	Homo sapiens (human)
serine-type peptidase activity	Trypsin-3	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (34)

Process	via Protein(s)	Taxonomy
external side of plasma membrane	Prothrombin	Homo sapiens (human)
collagen-containing extracellular matrix	Prothrombin	Homo sapiens (human)
extracellular region	Prothrombin	Homo sapiens (human)
extracellular space	Prothrombin	Homo sapiens (human)
endoplasmic reticulum lumen	Prothrombin	Homo sapiens (human)
Golgi lumen	Prothrombin	Homo sapiens (human)
plasma membrane	Prothrombin	Homo sapiens (human)
extracellular exosome	Prothrombin	Homo sapiens (human)
blood microparticle	Prothrombin	Homo sapiens (human)
collagen-containing extracellular matrix	Prothrombin	Homo sapiens (human)
extracellular space	Prothrombin	Homo sapiens (human)
extracellular region	Coagulation factor IX	Homo sapiens (human)
extracellular space	Coagulation factor IX	Homo sapiens (human)
endoplasmic reticulum lumen	Coagulation factor IX	Homo sapiens (human)
Golgi lumen	Coagulation factor IX	Homo sapiens (human)
plasma membrane	Coagulation factor IX	Homo sapiens (human)
collagen-containing extracellular matrix	Coagulation factor IX	Homo sapiens (human)
extracellular exosome	Coagulation factor IX	Homo sapiens (human)
extracellular space	Coagulation factor IX	Homo sapiens (human)
extracellular region	Coagulation factor X	Homo sapiens (human)
endoplasmic reticulum lumen	Coagulation factor X	Homo sapiens (human)
Golgi lumen	Coagulation factor X	Homo sapiens (human)
plasma membrane	Coagulation factor X	Homo sapiens (human)
external side of plasma membrane	Coagulation factor X	Homo sapiens (human)
extracellular space	Coagulation factor X	Homo sapiens (human)
extracellular region	Plasminogen	Homo sapiens (human)
extracellular space	Plasminogen	Homo sapiens (human)
plasma membrane	Plasminogen	Homo sapiens (human)
external side of plasma membrane	Plasminogen	Homo sapiens (human)
cell surface	Plasminogen	Homo sapiens (human)
platelet alpha granule lumen	Plasminogen	Homo sapiens (human)
collagen-containing extracellular matrix	Plasminogen	Homo sapiens (human)
extracellular exosome	Plasminogen	Homo sapiens (human)
blood microparticle	Plasminogen	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Plasminogen	Homo sapiens (human)
glutamatergic synapse	Plasminogen	Homo sapiens (human)
extracellular space	Plasminogen	Homo sapiens (human)
extracellular region	Urokinase-type plasminogen activator	Homo sapiens (human)
extracellular space	Urokinase-type plasminogen activator	Homo sapiens (human)
plasma membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
focal adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
external side of plasma membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
cell surface	Urokinase-type plasminogen activator	Homo sapiens (human)
specific granule membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
extracellular exosome	Urokinase-type plasminogen activator	Homo sapiens (human)
tertiary granule membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
serine protease inhibitor complex	Urokinase-type plasminogen activator	Homo sapiens (human)
protein complex involved in cell-matrix adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
serine-type endopeptidase complex	Urokinase-type plasminogen activator	Homo sapiens (human)
extracellular space	Urokinase-type plasminogen activator	Homo sapiens (human)
collagen-containing extracellular matrix	Tissue-type plasminogen activator	Homo sapiens (human)
extracellular region	Tissue-type plasminogen activator	Homo sapiens (human)
cytoplasm	Tissue-type plasminogen activator	Homo sapiens (human)
cell surface	Tissue-type plasminogen activator	Homo sapiens (human)
secretory granule	Tissue-type plasminogen activator	Homo sapiens (human)
apical part of cell	Tissue-type plasminogen activator	Homo sapiens (human)
extracellular exosome	Tissue-type plasminogen activator	Homo sapiens (human)
serine protease inhibitor complex	Tissue-type plasminogen activator	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Tissue-type plasminogen activator	Homo sapiens (human)
glutamatergic synapse	Tissue-type plasminogen activator	Homo sapiens (human)
extracellular space	Tissue-type plasminogen activator	Homo sapiens (human)
serine protease inhibitor complex	Cationic trypsin	Bos taurus (cattle)
extracellular region	Coagulation factor XI	Homo sapiens (human)
extracellular space	Coagulation factor XI	Homo sapiens (human)
plasma membrane	Coagulation factor XI	Homo sapiens (human)
membrane	Coagulation factor XI	Homo sapiens (human)
extracellular exosome	Coagulation factor XI	Homo sapiens (human)
extracellular region	Plasma kallikrein	Homo sapiens (human)
extracellular space	Plasma kallikrein	Homo sapiens (human)
plasma membrane	Plasma kallikrein	Homo sapiens (human)
extracellular exosome	Plasma kallikrein	Homo sapiens (human)
extracellular region	Vitamin K-dependent protein C	Homo sapiens (human)
endoplasmic reticulum	Vitamin K-dependent protein C	Homo sapiens (human)
endoplasmic reticulum lumen	Vitamin K-dependent protein C	Homo sapiens (human)
Golgi apparatus	Vitamin K-dependent protein C	Homo sapiens (human)
Golgi lumen	Vitamin K-dependent protein C	Homo sapiens (human)
extracellular space	Vitamin K-dependent protein C	Homo sapiens (human)
extracellular region	Trypsin-1	Homo sapiens (human)
collagen-containing extracellular matrix	Trypsin-1	Homo sapiens (human)
blood microparticle	Trypsin-1	Homo sapiens (human)
extracellular space	Trypsin-1	Homo sapiens (human)
extracellular region	Trypsin-2	Homo sapiens (human)
extracellular space	Trypsin-2	Homo sapiens (human)
extracellular matrix	Trypsin-2	Homo sapiens (human)
azurophil granule lumen	Trypsin-2	Homo sapiens (human)
extracellular space	Trypsin-2	Homo sapiens (human)
extracellular region	Coagulation factor VII	Homo sapiens (human)
endoplasmic reticulum lumen	Coagulation factor VII	Homo sapiens (human)
Golgi lumen	Coagulation factor VII	Homo sapiens (human)
plasma membrane	Coagulation factor VII	Homo sapiens (human)
vesicle	Coagulation factor VII	Homo sapiens (human)
collagen-containing extracellular matrix	Coagulation factor VII	Homo sapiens (human)
serine-type peptidase complex	Coagulation factor VII	Homo sapiens (human)
extracellular space	Coagulation factor VII	Homo sapiens (human)
extracellular region	Coagulation factor V	Homo sapiens (human)
extracellular space	Coagulation factor V	Homo sapiens (human)
endoplasmic reticulum lumen	Coagulation factor V	Homo sapiens (human)
plasma membrane	Coagulation factor V	Homo sapiens (human)
membrane	Coagulation factor V	Homo sapiens (human)
COPII-coated ER to Golgi transport vesicle	Coagulation factor V	Homo sapiens (human)
platelet alpha granule lumen	Coagulation factor V	Homo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartment membrane	Coagulation factor V	Homo sapiens (human)
extracellular vesicle	Coagulation factor V	Homo sapiens (human)
platelet alpha granule	Coagulation factor V	Homo sapiens (human)
extracellular region	Chymotrypsinogen B	Homo sapiens (human)
extracellular region	Trypsin-3	Homo sapiens (human)
extracellular space	Trypsin-3	Homo sapiens (human)
tertiary granule lumen	Trypsin-3	Homo sapiens (human)
extracellular space	Trypsin-3	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (131)

Assay ID	Title	Year	Journal	Article
AID977610	Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB	2005	Journal 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.
AID1811	Experimentally measured binding affinity data derived from PDB	2005	Journal 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.
AID313682	Half life in dog at 0.2 mg/kg, po	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID269929	Binding affinity to human plasma kallikrein	2006	Bioorganic & 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
AID269923	Clearance in dog	2006	Bioorganic & 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
AID312547	Inhibition of human alpha thrombin	2008	Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2	7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID313689	Inhibition of human chymotrypsin	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID458311	Inhibition of human factor 10a	2010	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4	Phenyltriazolinones as potent factor Xa inhibitors.
AID276523	Volume of distribution in dog	2006	Bioorganic & 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.
AID263274	Clearance in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID313687	Inhibition of human factor 9a	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID527428	Antithrombotic activity in rabbit arteriovenous-shunt thrombosis model measured per hr	2010	Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17	Factor Xa inhibitors: next-generation antithrombotic agents.
AID269930	Binding affinity to human APC	2006	Bioorganic & 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
AID313684	Volume of distribution at steady state in dog at 0.5 mg/kg, iv	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID269922	Apparent permeability in Caco-2 cells	2006	Bioorganic & 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
AID263263	Anticoagulant activity in human plasma by aPTT assay	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263261	Binding affinity to human factor 10a	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID396708	Oral bioavailability in dog at 0.2 mg/kg	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID310311	Apparent permeability across Caco-2 cells	2007	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23	Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID310308	Inhibition of human thrombin	2007	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23	Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID302367	Antithrombotic potency in rabbit arteriovenous shunt thrombosis model	2007	Journal 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
AID312552	Metabolic stability in human liver microsomes after 10 mins	2008	Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2	7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID458314	Anticoagulant activity in rabbit plasma assessed as concentration required to double prothrombin time by aggregometer	2010	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4	Phenyltriazolinones as potent factor Xa inhibitors.
AID527410	Volume of distribution at steady state in dog	2010	Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17	Factor Xa inhibitors: next-generation antithrombotic agents.
AID310312	Clearance in dog at 0.5 mg/kg, iv and 0.2 mg/kg, po	2007	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23	Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID343879	Half life in dog at 0.2 mg/kg, po	2008	Bioorganic & 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.
AID302360	Oral bioavailability in dog at 0.2 mg/kg, po	2007	Journal 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
AID313683	Clearance in dog at 0.5 mg/kg, iv	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID269925	Half life in orally dosed dog	2006	Bioorganic & 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
AID313677	Apparent permeability across human Caco-2 cells	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID263266	Binding affinity to human aPC	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263272	Binding affinity to human urokinase	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID396700	Anticoagulant activity in human plasma assessed as drug level required to double prothrombin time	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID302365	Protein binding in human serum by equilibrium dialysis	2007	Journal 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
AID276532	Binding affinity to human factor VIIa	2006	Bioorganic & 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.
AID527411	Antithrombotic activity in iv dosed rabbit assessed as restoration of integrated blood flow	2010	Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17	Factor Xa inhibitors: next-generation antithrombotic agents.
AID396709	Anticoagulant activity in rabbit plasma assessed as drug level required to double prothrombin time	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID343877	Clearance in dog at 0.5 mg/kg, iv	2008	Bioorganic & 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.
AID263279	Anticoagulant activity in rabbit plasma by aPTT assay	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263262	Permeability in Caco-2 cell	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID313690	Inhibition of human plasmin	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID312553	Apparent permeability across Caco-2 cells	2008	Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2	7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID276530	Binding affinity to human APC	2006	Bioorganic & 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.
AID343865	Anticoagulant activity in human plasma assessed as concentration required to double prothrombin time	2008	Bioorganic & 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.
AID263280	Anticoagulant activity in rabbit plasma by PT assay	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263268	Binding affinity to human factor 7a	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID276533	Binding affinity to human plasmin	2006	Bioorganic & 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.
AID263273	Binding affinity to human chymotrypsin	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263277	Bioavailability in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID313691	Inhibition of human tPA	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID276527	Binding affinity to human thrombin	2006	Bioorganic & 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.
AID458312	Inhibition of human factor 2a	2010	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4	Phenyltriazolinones as potent factor Xa inhibitors.
AID343878	Volume of distribution at steady state in dog	2008	Bioorganic & 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.
AID276522	Clearance in dog	2006	Bioorganic & 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.
AID269927	Antithrombotic activity in rabbit arterio-venous shunt thrombosis model	2006	Bioorganic & 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
AID276525	Oral bioavailability in po dosed dog	2006	Bioorganic & 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.
AID269931	Binding affinity to human f9a	2006	Bioorganic & 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
AID302358	Volume of distribution at steady state in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po	2007	Journal 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
AID343864	Inhibition of human factor 10a	2008	Bioorganic & 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.
AID313675	Inhibition of human factor 10a	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID263269	Binding affinity to human plasmin	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID343876	Metabolic stability in human liver microsomes assessed as half life	2008	Bioorganic & 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.
AID310313	Volume of distribution at steady state in dog at 0.5 mg/kg, iv and 0.2 mg/kg, po	2007	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23	Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID396707	Half life in dog at 0.2 mg/kg, po	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID313679	Inhibition of human trypsin	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID312550	Inhibition of human trypsin	2008	Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2	7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID269934	Binding affinity to human chymotrypsin	2006	Bioorganic & 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
AID527394	Inhibition of factor 10a	2010	Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17	Factor Xa inhibitors: next-generation antithrombotic agents.
AID263276	Half life in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID276524	Half life in po dosed dog	2006	Bioorganic & 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.
AID313678	Inhibition of human thrombin	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID313676	Anticoagulant activity in human plasma assessed as concentration required to double prothrombin time	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID269920	Anticoagulant activity in plasma by PT assay	2006	Bioorganic & 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
AID302366	Binding affinity to rabbit F10a	2007	Journal 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
AID312549	Inhibition of human factor 10a	2008	Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2	7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID396701	Binding affinity to human coagulation factor 10a	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID310314	Half life in dog at 0.2 mg/kg, po	2007	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23	Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID302357	Clearance in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po	2007	Journal 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
AID269932	Binding affinity to human f7a	2006	Bioorganic & 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
AID527407	Oral bioavailability in dog	2010	Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17	Factor Xa inhibitors: next-generation antithrombotic agents.
AID396710	Antithrombotic activity against iv dosed rabbit arterio-venous shunt model assessed as inhibition of thrombus formation	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID263264	Binding affinity to human thrombin	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID396706	Clearance in dog at 0.5 mg/kg, iv and 0.2 mg/kg, po	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID343867	Inhibition of human factor 9a	2008	Bioorganic & 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.
AID263271	Binding affinity to human plasma kallikrein	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID313688	Inhibition of human factor 11a	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID276528	Binding affinity to human chymotrypsin	2006	Bioorganic & 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.
AID312551	Anticoagulant activity against human plasma assessed as concentration required to double activated partial thromboplastin time	2008	Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2	7-fluoroindazoles as potent and selective inhibitors of factor Xa.
AID269921	Binding affinity to human F2a	2006	Bioorganic & 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
AID527398	Anticoagulant activity in human platelet assessed as concentration required to double activated partial prothrombin time	2010	Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17	Factor Xa inhibitors: next-generation antithrombotic agents.
AID396705	Volume of distribution at steady state in dog at 0.5 mg/kg, iv and 0.2 mg/kg, po	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID313686	Inhibition of human activated protein C	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID269919	Binding affinity to human F10a	2006	Bioorganic & 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
AID263281	Antithrombotic activity in iv dosed rabbit arterio-venous shunt model	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263275	Volume of distribution in dog at 0.4 mg/kg, iv and 0.2 mg/kg, po	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID458313	Inhibition of human trypsin	2010	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4	Phenyltriazolinones as potent factor Xa inhibitors.
AID302353	Binding affinity to human F10a	2007	Journal 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
AID269926	Oral bioavailability in orally dosed dog	2006	Bioorganic & 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
AID269924	Volume of distribution in dog	2006	Bioorganic & 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
AID276521	Apparent permeability across Caco-2 cell membrane	2006	Bioorganic & 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.
AID302362	Inhibition of thrombus formation in rabbit arteriovenous shunt thrombosis model	2007	Journal 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
AID343880	Bioavailability in dog at 0.5 mg/kg, iv	2008	Bioorganic & 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.
AID527399	Anticoagulant activity in human platelet assessed as concentration required to double prothrombin time	2010	Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17	Factor Xa inhibitors: next-generation antithrombotic agents.
AID269928	Binding affinity to human trypsin	2006	Bioorganic & 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
AID276531	Binding affinity to human factor IXa	2006	Bioorganic & 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.
AID302363	Half life in human liver microsomes	2007	Journal 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
AID263265	Binding affinity to human trypsin	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID313685	Inhibition of human plasma kallikrein	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID276534	Binding affinity to human urokinase	2006	Bioorganic & 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.
AID269935	Binding affinity to human tPA	2006	Bioorganic & 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
AID276535	Binding affinity to human tPA	2006	Bioorganic & 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.
AID343866	Inhibition of human trypsin	2008	Bioorganic & 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.
AID396712	Protein binding in rabbit plasma	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID263270	Binding affinity to human tPA	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID263282	Protein binding in rabbit plasma	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID276519	Binding affinity to human factor Xa	2006	Bioorganic & 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.
AID343881	Inhibition of human thrombin	2008	Bioorganic & 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.
AID527409	Clearance in dog	2010	Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17	Factor Xa inhibitors: next-generation antithrombotic agents.
AID269933	Binding affinity to human plasmin	2006	Bioorganic & 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
AID276526	Inhibition of thrombus formation in rabbit AV shunt thrombosis model	2006	Bioorganic & 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.
AID313681	Oral bioavailability in dog at 0.2 mg/kg	2008	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
AID310315	Oral bioavailability in dog at 0.2 mg/kg	2007	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23	Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
AID396699	Apparent permeability from apical to basolateral side of human Caco-2 cells	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
AID302359	Half life in dog at 0.2 mg/kg, po	2007	Journal 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
AID263278	Binding affinity to rabbit factor 10a	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID276529	Binding affinity to human trypsin	2006	Bioorganic & 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.
AID263267	Binding affinity to human factor 9a	2006	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
AID1796932	Enzyme 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 hydrochlorid	2005	Journal 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.
AID1796936	Enzyme 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.\\	2006	Bioorganic & 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.
AID1796935	Enzyme 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]-pyridin	2006	Bioorganic & 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
AID1796951	Enzyme 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.\\	2006	Bioorganic & 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)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	15 (75.00)	29.6817
2010's	5 (25.00)	24.3611
2020's	0 (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.

Metric	This Compound (vs All)
Research Demand Index	25.88 (24.57)
Research Supply Index	3.04 (2.92)
Research Growth Index	4.25 (4.65)
Search Engine Demand Index	29.35 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (25.88)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	1 (5.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	19 (95.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
aspirin Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.	7.03	1	benzoic acids; phenyl acetates; salicylates	anticoagulant; antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; EC 1.1.1.188 (prostaglandin-F synthase) inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; plant activator; platelet aggregation inhibitor; prostaglandin antagonist; teratogenic agent
famotidine Famotidine: A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.	2.03	1	1,3-thiazoles; guanidines; sulfonamide	anti-ulcer drug; H2-receptor antagonist; P450 inhibitor
fidexaban Fidexaban: structure in first source	3.15	1
ticlopidine Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group.	2.03	1	monochlorobenzenes; thienopyridine	anticoagulant; fibrin modulating drug; hematologic agent; P2Y12 receptor antagonist; platelet aggregation inhibitor
alanine Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.	2.07	1	alanine zwitterion; alanine; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid	EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor; fundamental metabolite
n-vinyl-2-pyrrolidinone N-vinyl-2-pyrrolidinone: monomer of POVIDONE; structure given in first source	2.03	1	pyrrolidin-2-ones
thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.	2.05	1	mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound	non-polar solvent
isoxazoles Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.	3.65	9	isoxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
1,2-di(5-amidino-2-benzofuranyl)ethane 1,2-di(5-amidino-2-benzofuranyl)ethane: preferential inhibitor of bovine factor Xa; structure given in first source	3.15	1
clopidogrel Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks.	7.03	1	methyl ester; monochlorobenzenes; thienopyridine	anticoagulant; P2Y12 receptor antagonist; platelet aggregation inhibitor
dx 9065 [no description available]	3.15	1
tartaric acid tartaric acid: RN given refers to cpd with unspecified isomeric designation. D-tartaric acid : The D-enantiomer of tartaric acid.	2.04	1	tartaric acid	Escherichia coli metabolite
otamixaban otamixaban: structure in first source	3.15	1
bms 740808 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	4.23	5
ym 60828 YM 60828: YM-466 is the mesylate salt	3.15	1
pentagastrin Pentagastrin: A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid.	2.03	1	organic molecular entity
rivaroxaban Rivaroxaban: A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME.. rivaroxaban : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery.	3.56	2	aromatic amide; lactam; monocarboxylic acid amide; morpholines; organochlorine compound; oxazolidinone; thiophenes	anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor
pexacerfont [no description available]	2.07	1	pyrazolopyridine
dpc 423 [no description available]	3.83	3
gw 813893 [no description available]	3.15	1
ly517717 LY517717: an oral anticoagulant	3.15	1
apixaban [no description available]	4.24	5	aromatic ether; lactam; piperidones; pyrazolopyridine	anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor
betrixaban betrixaban: a highly potent, selective, and orally efficacious factor Xa inhibitor; structure in first source. betrixaban : A secondary carboxamide obtained by formal condensation of the carboxy group of 4-(N,N-dimethylcarbamimidoyl)benzoic acid with the amino group of 2-amino-N-(5-chloropyridin-2-yl)-5-methoxybenzamide. A synthetic anticoagulant compound that targets activated factor Xa in the coagulation cascade.	3.15	1	benzamides; guanidines; monochloropyridine; monomethoxybenzene; secondary carboxamide	anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor
edoxaban edoxaban : A monocarboxylic acid amide that is used (as its tosylate monohydrate) for the treatment of deep vein thrombosis and pulmonary embolism.	3.15	1	chloropyridine; monocarboxylic acid amide; tertiary amino compound; thiazolopyridine	anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor; platelet aggregation inhibitor
rpr 120844 [no description available]	3.15	1
brivanib [no description available]	2.07	1	aromatic ether; diether; fluoroindole; pyrrolotriazine; secondary alcohol	angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; drug metabolite; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; fibroblast growth factor receptor antagonist
pd 0348292 N-(4-chlorophenyl)-N-(2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidiine-1,2-dicarboxamide: structure in first source. eribaxaban : A member of the class of pyrrolidines that is (2R,4R)-N(1)-(p-chlorophenyl)-4-methoxypyrrolidine-1,2-dicarboxamide in which the nitrogen of the 2-carbamoyl group has been substituted by a 2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl group. It is a synthetic organic anticoagulant compound that targets activated factor Xa in the coagulation cascade.	3.15	1	monochlorobenzenes; monofluorobenzenes; pyridone; pyrrolidines; secondary carboxamide; ureas	anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor; serine protease inhibitor
thromboplastin Thromboplastin: Constituent composed of protein and phospholipid that is widely distributed in many tissues. It serves as a cofactor with factor VIIa to activate factor X in the extrinsic pathway of blood coagulation.	2.07	1

Condition	Relationship Strength	Studies
Blood Clot [description not available]	4.21	6
Thrombosis Formation and development of a thrombus or blood clot in the blood vessel.	4.21	6
Thromboembolism, Venous [description not available]	2.05	1
Venous Thromboembolism Obstruction of a vein or VEINS (embolism) by a blood clot (THROMBUS) in the blood stream.	2.05	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.03	1
Bleeding [description not available]	7.03	1
Hemorrhage Bleeding or escape of blood from a vessel.	2.03	1

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