| Assay ID | Title | Year | Journal | Article |
|---|
| AID8915 | Cmax in dog plasma after oral dose (1 mg/kg) | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
| Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates. |
| AID8904 | Bioavailability as Cmax in dogs at 5 mg/kg oral dose | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID228014 | in vitro anticoagulant potency (2x APTT) against rat plasma. | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| AID25885 | Half life was determined after oral administration at 1 mg/kg in dogs | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
| Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors. |
| AID187230 | Compound was evaluated for its anticoagulant and antithrombotic activity by measuring the final plasma concentration in rat plasma | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID24138 | Final plasma concentration after intravenous infusion at 5 ug/kg/min dose | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| AID183926 | Incidence of occlusion was determined in the rat ferric chloride arterial thrombosis model at 5 dose ug/kg/min after intravenous administration; 1/6 | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
| L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor. |
| AID215885 | Inhibitory constant evaluated against trypsin | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
| Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position. |
| AID1381624 | AUC in dog at 1 mg/kg, po | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | The selectivity and bioavailability improvement of novel oral anticoagulants: An overview. |
| AID159843 | Concentration needed to double the activated partial thromboplastin time in human plasma | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
| Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position. |
| AID227003 | Ratio of inhibitory constant evaluated against trypsin to that of thrombin (Factor IIa) | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
| Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position. |
| AID26783 | Partition coefficient (logP) | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID10089 | Compound was evaluated for half-life period in dogs at a dose of 5 mpk perorally | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID316643 | Half life in dog at 5 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles. |
| AID1381621 | Tmax in dog at 1 mg/kg, po | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | The selectivity and bioavailability improvement of novel oral anticoagulants: An overview. |
| AID1381639 | Inhibition of human thrombin assessed as release of p-nitroanilide from chromogenic substrate | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | The selectivity and bioavailability improvement of novel oral anticoagulants: An overview. |
| AID183798 | Incidence of occlusion was determined in the rat ferric chloride arterial thrombosis model at 1 dose ug/kg/min after intravenous administration; 5/6 | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
| L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor. |
| AID211179 | In vitro inhibitory constant against human thrombin (FIIa). | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
| Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. |
| AID89176 | Compound was evaluated for its anticoagulant and antithrombotic activity by measuring the clotting parameter in human plasma | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID8519 | Compound was evaluated for Clearance in dogs at a dose of 1 mpk intravenously | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID215539 | In vitro inhibitory constant against trypsin; Inactive | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
| Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. |
| AID26162 | Half-life in dogs at 1 mg/kg dose upon oral administration | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| AID14568 | Oral absorption kinetics (AUC) was determined after administration of compound orally at 1 mg/kg in dogs | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
| Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors. |
| AID188131 | Compound was evaluated for its anticoagulant and antithrombotic activity by measuring the occlusions in rat plasma | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID316644 | AUC in dog at 5 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles. |
| AID183925 | Incidence of occlusion was determined in the rat ferric chloride arterial thrombosis model at 3 dose ug/kg/min after intravenous administration; 2/6 | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
| L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor. |
| AID211005 | Binding affinity towards thrombin was evaluated | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
| L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor. |
| AID1381625 | Half life in dog at 1 mg/kg, po | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | The selectivity and bioavailability improvement of novel oral anticoagulants: An overview. |
| AID89394 | Compound was evaluated for its anticoagulant and antithrombotic activity by measuring the %protein binding in human plasma | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID316640 | Anticoagulant potency in human plasma assessed as concentration required to double activated partial thromboplastin time | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles. |
| AID189166 | Compound was evaluated for its anticoagulant and antithrombotic activity by measuring the %protein binding in rat plasma | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID215549 | Inhibitory activity against trypsin was determined | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| AID212081 | In vitro inhibitory activity against human Thrombin (FIIa) cleavage of the chromogenic substrate | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
| Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates. |
| AID213364 | Compound was evaluated to inhibit the trypsin enzyme | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID72493 | In vitro inhibitory constant against factor Xa (FXa). | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
| Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. |
| AID8328 | Compound was evaluated for area under curve (total concentration) in dogs at a dose of 1 mpk perorally | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID1381623 | Cmax in dog at 1 mg/kg, po | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | The selectivity and bioavailability improvement of novel oral anticoagulants: An overview. |
| AID215417 | Binding affinity towards trypsin was evaluated | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
| L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor. |
| AID24770 | time required for maximum concentration in dogs at 1 mg/kg dose upon oral administration | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| AID316648 | Half life in dog at 0.5 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles. |
| AID169110 | Compound was evaluated for its anticoagulant and antithrombotic activity by measuring the clotting parameter in rat plasma | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID316642 | Cmax in dog at 5 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles. |
| AID211201 | Inhibitory activity against thrombin (IIa) was determined | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| AID211602 | Inhibitory constant evaluated against thrombin (Factor IIa) | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
| Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position. |
| AID8329 | Compound was evaluated for area under curve (total concentration) in dogs at a dose of 5 mpk perorally | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID10694 | Area under curve(AUC) value of the compound | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| AID227293 | In vivo antithrombotic activity was measured after intravenous infusion (at 5 ug/kg/min) in rat FeCl3 arterial thrombosis model;1/6 | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| AID211030 | Compound was evaluated to inhibit the thrombin enzyme | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID183924 | Incidence of occlusion was determined in the rat ferric chloride arterial thrombosis model at 10 dose ug/kg/min after intravenous administration; 0/9 | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
| L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor. |
| AID8331 | In vivo area under curve was calculated by peroral administration at 1 mg/kg in fasted dog | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
| Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. |
| AID316639 | Inhibition of trypsin | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles. |
| AID316638 | Inhibition of thrombin | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles. |
| AID14257 | Maximum plasma concentration in dogs at 1 mg/kg dose upon oral administration | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| AID1381638 | Inhibition of human trypsin assessed as release of p-nitroanilide from chromogenic substrate | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | The selectivity and bioavailability improvement of novel oral anticoagulants: An overview. |
| AID316650 | Cmax in dog at 1 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles. |
| AID316651 | Half life in dog at 1 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles. |
| AID10319 | In vivo half life period was calculated at 1 mg/kg in dog | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
| Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. |
| AID14282 | Cmax in dog plasma after 1mg/kg oral dose | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
| Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors. |
| AID9700 | t1/2 in dog after oral dose (1 mg/kg) | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
| Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates. |
| AID196122 | In vivo antithrombotic activity was measured after intravenous infusion (at 10 ug/kg/min) in rat FeCl3 arterial thrombosis model; 0/9 | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| AID222611 | in vitro anticoagulant potency (2x APTT) against Human plasma. | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| AID8332 | AUC in dog after oral dose (1 mg/kg) | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
| Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates. |
| AID9899 | Bioavailability as Vdss in dogs at 1 mg/kg intravenous dose | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
| AID316647 | Cmax in dog at 0.5 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles. |
| AID24042 | Maximum time taken for oral absorption was determined after oral administration at 1 mg/kg in dogs | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
| Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors. |
| AID316649 | Selectivity for thrombin over trypsin | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles. |
| AID8912 | In vivo maximal concentration was calculated at 1 mg/kg in dog | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
| Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. |
| AID24137 | Final plasma concentration after intravenous infusion | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |