Assay ID | Title | Year | Journal | Article |
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. |
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 |
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. |
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. |
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 |
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 |
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. |
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 |
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. |
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 |
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. |
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 |
AID276520 | Anticoagulant activity in human plasma assessed as clotting PT value | 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. |
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 |
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 |
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 |
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 |
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. |
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 |
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 |
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. |
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 |
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 |
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. |
AID269936 | Protein binding in plasma by equilibrium dialysis 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 |
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 |
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 |
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 |
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. |
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 |
AID527394 | Inhibition of factor 10a | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 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 |
AID1811 | Experimentally measured binding affinity data derived from PDB | 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 |
AID1796939 | Enzyme Assay and Determination of the Inhibition Constants. from Article 10.1016/j.bmcl.2006.08.027: \\Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.\\ | 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. |
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 |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |