Assay ID | Title | Year | Journal | Article |
AID280895 | Half life in Sprague-Dawley rat at 1 mg/kg, iv and 2.5 mg/kg, po | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID455020 | Inhibition of human factor 10a by fluorescence assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs. |
AID578331 | Inhibition of factor 10a activity measured using bis-(CBZ-glycylglycly)-L-arginine amide fluorogenic substrate | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs. |
AID280888 | Selectivity for factor Xa over thrombin by fluorogenic assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID527422 | Anticoagulant activity in human platelet assessed as concentration required to 1.5 times activated partial prothrombin time | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
AID280897 | Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv and 2.5 mg/kg, po | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID307347 | Plasma clearance in Sprague-Dawley rat | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID280898 | Oral bioavailability in Sprague-Dawley rat at 1 mg/kg, iv and 2.5 mg/kg, po | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID280896 | Plasma clearance in Sprague-Dawley rat at 1 mg/kg, iv and 2.5 mg/kg, po | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID578332 | Anticoagulant activity in human plasma assessed as concentration required to 1.5 prothrombin time | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs. |
AID280902 | Oral bioavailability in Beagle dog at 1 mg/kg, iv and 2.5 mg/kg, po | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID527408 | Half life in dog | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
AID307350 | Half life in Beagle dog | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID280900 | Plasma clearance in Beagle dog at 1 mg/kg, iv and 2.5 mg/kg, po | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID280887 | Binding to human serum albumin in HPLC assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID280885 | Inhibition of human factor Xa by fluorescence assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID280899 | Half life in Beagle dog at 1 mg/kg, iv and 2.5 mg/kg, po | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID306764 | Inhibition of thrombin by fluorogenic assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Sulfonamide-related conformational effects and their importance in structure-based design. |
AID527412 | Oral bioavailability in rat | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
AID307337 | Inhibition of factor 10a by fluorogenic assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID280901 | Volume of distribution at steady state in Beagle dog at 1 mg/kg, iv and 2.5 mg/kg, po | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID307339 | Anticoagulant potency in plasma assessed as drug concentration required to increase 1.5 times the prothrombin time | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID455021 | Anticoagulant activity in human plasma assessed as concentration required to increase the prothrombin based clotting time by 1.5 | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs. |
AID280889 | Selectivity for factor Xa over tissue factor/factor VIIa by fluorogenic assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID527413 | Half life in rat | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
AID307351 | Plasma clearance in Beagle dog | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID307343 | Inhibition of trypsin by fluorogenic assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID307338 | Inhibition of thrombin by fluorogenic assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID307349 | Oral bioavailability in Sprague-Dawley rat | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID307348 | Volume of distribution in Sprague-Dawley rat | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID527394 | Inhibition of factor 10a | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
AID307344 | Inhibition of kallikrein by fluorogenic assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID307353 | Oral bioavailability in Beagle dog | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID307342 | Inhibition of plasmin by fluorogenic assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID280890 | Selectivity for factor Xa over factor XIIa | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID280891 | Selectivity for factor Xa over activated protein C by fluorogenic assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID280894 | Selectivity for factor Xa over kallikrein by fluorogenic assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID280892 | Selectivity for factor Xa over plasmin by fluorogenic assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID280886 | Lipophilicity, log D at pH 7.4 | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID280893 | Selectivity for factor Xa over trypsin by fluorogenic assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID307341 | Inhibition of activated protein C by fluorogenic assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID527407 | Oral bioavailability in dog | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
| Factor Xa inhibitors: next-generation antithrombotic agents. |
AID307352 | Volume of distribution in Beagle dog | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID307346 | Half life in Sprague-Dawley rat | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID307345 | Inhibition of tissue plasminogen activator by fluorogenic assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID307340 | Anticoagulant potency in plasma assessed as drug concentration required to increase 1.5 times the activated partial thromboplastin time | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
AID1797640 | In Vitro Assay for Inhibition of Factor Xa from Article 10.1021/jm060870c: \\Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides.\\ | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Selective and dual action orally active inhibitors of thrombin and factor Xa. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |