| Assay ID | Title | Year | Journal | Article |
|---|
| AID368001 | Anticoagulant activity in rabbit plasma assessed as concentration required to double prothrombin time after 1min | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID362212 | Ratio of 2 fold prolongation of prothrombin time over 2 fold prolongation of activated partial thromboplastin time in human plasma | 2008 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 18, Issue:16
| Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination. |
| AID295782 | Anticoagulant activity in mouse plasma assessed as concentration required to double prothrombin time | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
| Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors. |
| AID367997 | Inhibition of human recombinant factor 7a/soluble tissue factor by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID367984 | Octanol-Japanese pharmacopoeia second fluid distribution coefficient, Log D after 30 mins by shake-flask method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID527401 | Half life in human | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
| AID211570 | Binding affinity against Thrombin. | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID322201 | Ex vivo anticoagulant potency in ICR mouse blood assessed as 1.1 times prolongation of prothrombin time at 30 mg/kg, po after 1 hr relative to control | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
| Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors. |
| AID368002 | Anticoagulant activity in human plasma assessed as concentration required to double activated partial thromboplastin time after 5 mins | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID50895 | Compound was tested for inhibition activity against factor Xa (FXa) | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors. |
| AID51487 | Inhibitory Activity against human Coagulation factor X | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16
| GRID/CPCA: a new computational tool to design selective ligands. |
| AID367980 | Anticoagulant activity in human plasma assessed as concentration required to double prothrombin time | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID322196 | Inhibition of human factor 10a | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
| Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors. |
| AID317183 | Ex vivo anticoagulant potency in ICR mouse blood at 100 mg/kg, po after 1 hr expressed as ratio of prothrombin time in drug treated animal to control | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
| Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors. |
| AID213267 | Binding affinity towards Thrombin. | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
| Design of benzamidine-type inhibitors of factor Xa. |
| AID367988 | Inhibition of human factor 10a by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID527400 | Oral bioavailability in human | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
| AID228228 | Inhibitory concentration against thrombin. | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors. |
| AID211034 | Compound was tested for inhibition activity against human thrombin (FIIa) | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors. |
| AID527402 | Clearance in human | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
| AID317179 | Inhibition of human factor 10a | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
| Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors. |
| AID190314 | Ex vivo anticoagulant activity was measured by calculating the Activated partial thromboplastin time (test/control) at 4 hr by dose of 100 mg/kg on oral administration in male Wistar rat | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
| Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors. |
| AID367990 | Inhibition of monkey factor 10a by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID367996 | Inhibition of human recombinant tissue plasminogen activator by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID527403 | Plasma protein binding in human | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
| AID211756 | Inhibitory Activity against Thrombin | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16
| GRID/CPCA: a new computational tool to design selective ligands. |
| AID113731 | Inhibitory concentration against mice | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID367999 | Anticoagulant activity in rat plasma assessed as concentration required to double prothrombin time after 1min | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID190312 | Ex vivo anticoagulant activity was measured by calculating the Activated partial thromboplastin time (test/control) at 1 hr by dose of 100 mg/kg on oral administration in male Wistar rat | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
| Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors. |
| 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. |
| AID210658 | In vitro evaluation for the concentration needed for inhibiting thrombin by 50% | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
| Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors. |
| AID367982 | Oral bioavailability in human | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID89212 | In vitro evaluation for the concentration needed to double the Plasma recalcification clotting time | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
| Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors. |
| AID215748 | Binding affinity against Trypsin | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID228991 | Compound was tested for the inhibition of serine protease factor Xa enzyme. | 1998 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
| Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa. |
| AID367991 | Inhibition of rabbit factor 10a by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID367981 | Ratio of concentration required to double prothrombin time to IC50 for human factor 10a | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID167467 | Inhibition of thrombosis in rabbits ( ED50 (sc) | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID317182 | Ex vivo anticoagulant potency in ICR mouse blood at 30 mg/kg, po after 1 hr expressed as ratio of prothrombin time in drug treated animal to control | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
| Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors. |
| AID527394 | Inhibition of factor 10a | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
| AID214858 | Binding affinity towards Trypsin. | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
| Design of benzamidine-type inhibitors of factor Xa. |
| AID527396 | Inhibition of thrombin | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
| AID190313 | Ex vivo anticoagulant activity was measured by calculating the Activated partial thromboplastin time (test/control) at 2 hr by dose of 100 mg/kg on oral administration in male Wistar rat | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
| Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors. |
| AID51844 | Binding affinity against Coagulation factor X | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID367998 | Anticoagulant activity in human plasma assessed as concentration required to double prothrombin time after 1min | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID52767 | Binding affinity against Chymotrypsinogen | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID367993 | Inhibition of human trypsin by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID322202 | Ex vivo anticoagulant potency in ICR mouse blood assessed as 1.4 times prolongation of prothrombin time at 100 mg/kg, po after 1 hr relative to control | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
| Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors. |
| AID295781 | Anticoagulant activity in human plasma assessed as concentration required to double prothrombin time | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
| Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors. |
| AID367994 | Inhibition of human chymotrypsin by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID295778 | Inhibition of human thrombin | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
| Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors. |
| AID51480 | In vitro evaluation for the concentration needed for inhibiting factor Xa by 50% | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
| Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors. |
| AID362000 | Inhibition of factor 10a in human plasma | 2008 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 18, Issue:16
| Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy. |
| 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. |
| AID367989 | Inhibition of rat factor 10a by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID190311 | Ex vivo anticoagulant activity was measured by calculating the Activated partial thromboplastin time (test/control) at 0.5 h by dose of 100 mg/kg on oral administration in male Wistar rat | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
| Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors. |
| AID295777 | Inhibition of human trypsin | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
| Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors. |
| AID295780 | Selectivity for human factor 10a over human thrombin | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
| Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors. |
| AID317180 | Anticoagulant potency in human plasma assessed as concentration required to double prothrombin time after 4 mins | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
| Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors. |
| AID167466 | Inhibition of thrombosis in rabbits ( ED50 (po) | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID362013 | Inhibition of human trypsin | 2008 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 18, Issue:16
| Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy. |
| AID322197 | Anticoagulant potency in human plasma assessed as concentration required to double prothrombin time | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
| Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors. |
| AID52158 | In vitro inhibition of human coagulation factor Xa (Xa) in a purified enzyme system. | 1999 | Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
| Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors. |
| AID295783 | Anticoagulant activity in ICR mouse plasma assessed as PT-prolongation at 100 mg/kg, po after 0.5 hrs relative to control | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
| Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors. |
| AID368003 | Anticoagulant activity in human plasma assessed as concentration required to double thrombin time after 1min | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID295776 | Inhibition of human factor 10a | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
| Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors. |
| AID51650 | Binding affinity towards Coagulation factor X | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
| Design of benzamidine-type inhibitors of factor Xa. |
| AID295779 | Selectivity for human factor 10a over human trypsin | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
| Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors. |
| AID367992 | Inhibition of human thrombin by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID317181 | Anticoagulant potency in mouse plasma assessed as concentration required to double prothrombin time after 4 mins | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
| Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors. |
| AID167465 | Inhibition of thrombosis in rabbits ( ED50 (iv) | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID367983 | Inhibition of human factor 10a | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID368000 | Anticoagulant activity in cynomolgus monkey plasma assessed as concentration required to double prothrombin time after 1 min | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID52164 | Inhibitory concentration against human Coagulation factor Xa (fXa) | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors. |
| AID362012 | Inhibition of human thrombin | 2008 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 18, Issue:16
| Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy. |
| AID367985 | AUC in monkey at 1 mg/kg, po by discrete dosing | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID367995 | Inhibition of human plasmin by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
| AID51333 | Binding affinity towards Coagulation factor X | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
| Design of benzamidine-type inhibitors of factor Xa. |
| AID228433 | Inhibitory concentration against bovine trypsin | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors. |
| AID215189 | Compound was tested for inhibition activity against bovine trypsin. | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors. |
| AID1797608 | Enzyme Inhibition Assay from Article 10.1107/s0907444999007350: \\Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin.\\ | 1999 | Acta crystallographica. Section D, Biological crystallography, Aug, Volume: 55, Issue:Pt 8
| Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 1996 | The Journal of biological chemistry, Nov-22, Volume: 271, Issue:47
| X-ray structure of active site-inhibited clotting factor Xa. Implications for drug design and substrate recognition. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 1996 | The Journal of biological chemistry, Nov-22, Volume: 271, Issue:47
| X-ray structure of active site-inhibited clotting factor Xa. Implications for drug design and substrate recognition. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |