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] |