Page last updated: 2024-12-11
l-454,560
Description
Research Excerpts
Clinical Trials
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Description
L-454,560: Phosphodiesterase Inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9853498 |
| CHEMBL ID | 372575 |
| SCHEMBL ID | 4027148 |
| MeSH ID | M0494134 |
Synonyms (21)
| Synonym |
|---|
| l-454560 |
| CHEMBL372575 , |
| SCHEMBL4027148 |
| bdbm50174022 |
| 8-(3-(2-(3-methyl-1,2,4-oxadiazol-5-yl)-2-(4-(methylsulfonyl)phenyl)vinyl)phenyl)-6-(2-(methylsulfonyl)propan-2-yl)quinoline |
| (e)-8-(3-(2-(3-methyl-1,2,4-oxadiazol-5-yl)-2-(4-(methylsulfonyl)phenyl)vinyl)phenyl)-6-(2-(methylsulfonyl)propan-2-yl)quinoline |
| g6gso9sdnj , |
| unii-g6gso9sdnj |
| quinoline, 6-(1-methyl-1-(methylsulfonyl)ethyl)-8-(3-((1e)-2-(3-methyl-1,2,4-oxadiazol-5-yl)-2-(4-(methylsulfonyl)phenyl)ethenyl)phenyl)- |
| mk-0359 |
| 346629-30-9 |
| 6-(1-methanesulfonyl-1-methyl-ethyl)-8-{3-[(e)-2-(4-methanesulfonyl-phenyl)-2-(3-methyl-[1,2,4]oxadiazol-5-yl)-vinyl]-phenyl}-quinoline |
| l 454560 |
| l-454,560 |
| 3-methyl-5-[(e)-1-(4-methylsulfonylphenyl)-2-[3-[6-(2-methylsulfonylpropan-2-yl)quinolin-8-yl]phenyl]ethenyl]-1,2,4-oxadiazole |
| mk0359 |
| gtpl9852 |
| (e)-3-methyl-5-(1-(4-(methylsulfonyl)phenyl)-2-(3-(6-(2-(methylsulfonyl)propan-2-yl)quinolin-8-yl)phenyl)vinyl)-1,2,4-oxadiazole |
| 6-(1-methanesulfonyl-1-methyl-ethyl)-8-(3-[(e)-2-(4-methanesulfonyl-phenyl)-2-(3-methyl-[1,2,4]oxadiazol-5-yl)-vinyl]-phenyl)-quinoline |
| Q27278833 |
| AKOS040753082 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (6)
Inhibition Measurements
Biological Processes (65)
Molecular Functions (39)
Ceullar Components (25)
Bioassays (79)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID605277 | Ratio of drug level in brain of lister rat to IC50 for PDE4 activity | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID605282 | Cognitive enhancing effect in Lister rat assessed as change in escape latency pretreated 30 mins before sample phase by water maze delayed matching to position test | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID502802 | Inhibition of human PDE4C | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18 | The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. |
| AID314159 | Inhibition of CYP2C9 | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors. |
| AID314160 | Inhibition of PDE4 expressed in SF9 cells | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors. |
| AID388724 | Inhibition of late-phase antigen-induced bronchoconstriction in ascaris-sensitive sheep at 0.5 mg/kg, iv daily for 4 days and antigen challenged after 2 hrs post dose on 4th day | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID257464 | Cmax in rat at 20 mg/kg, po | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID257459 | Emetic threshold as plasma concentration in squirrel monkeys after 10 mg/kg oral dose | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID388720 | Bioavailability in orally and iv dosed dog | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID257447 | Inhibitory activity against PDE4B | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID388718 | Cmax in po dosed squirrel monkey assessed after first episode of emesis | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID314168 | Inhibition of ovalbumin-induced bronchoconstriction in guinea pig at 30 ug/kg, ip | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors. |
| AID257454 | Inhibition of early-phase antigen induced bronchoconstriction in Ascaris sensitive sheep at 0.5 mg/kg/day, iv | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID388717 | Half life in orally and iv dosed Squirrel monkey | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID447673 | Inhibition of human PDE4 | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors. |
| AID605284 | Drug level in brain of Lister rat during conditional taste aversion test | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID605280 | Ratio IC50 for PDE4 activity in human whole blood to IC50 for PDE4 | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID605108 | Inhibition of PDE4D | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID314158 | Inhibition of LPS-stimulated TNFalpha release in squirrel monkey whole blood | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors. |
| AID502803 | Inhibition of human PDE4D | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18 | The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. |
| AID447674 | Antiinflammatory activity in human whole blood assessed as inhibition of LPS-induced TNFalpha production treated 15 mins before LPS challenge by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors. |
| AID363105 | Inhibition of TNFalpha release in human whole blood | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease. |
| AID502804 | Ratio of IC50 for human PDE4B to IC50 for human PDE4D | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18 | The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. |
| AID605106 | Inhibition of PDE4A | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID388713 | Inhibition of LPS-induced TNFalpha production in Squirrel monkey whole blood | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID447849 | Therapeutic window, ratio of Cmax in squirrel monkey at 10 mg/kg to IC50 for inhibition of LPS-induced TNFalpha production in squirrel monkey whole blood | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors. |
| AID605275 | Drug level in brain of Lister rat during novel object recognition test | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID314165 | Cmax in squirrel monkey at 10 mg/kg | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors. |
| AID257455 | Inhibition of late-phase antigen induced bronchoconstriction in Ascaris sensitive sheep at 0.5 mg/kg/day, iv | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID388714 | Inhibition of CYP2C9 | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID388712 | Displacement of [35S]MK-499 from human ERG expressed in HEK293 cells | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID388723 | Inhibition of ovalbumin-induced bronchoconstriction in conscious guinea pig at 0.03 mg/kg, ip administered 30 mins before ovalbumin challenge | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID388715 | Half life in orally and iv dosed rat | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID257446 | Inhibitory activity against PDE4A | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID447845 | Cmax in squirrel monkey at 10 mg/kg | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors. |
| AID605216 | Induction of adverse effect in Lister rat assessed as induction of malaise by conditional taste aversion test | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID605109 | Inhibition of PDE4 activity in human whole blood assessed as inhibition of LPS-induced TNF-alpha release | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID388719 | Bioavailability in orally and iv dosed rat | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID632293 | Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells at 10 uM | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness. |
| AID257467 | Inhibition of ovalbumin-induced bronchoconstriction in guinea pig at 0.03 mg/kg, ip | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID605274 | Drug level in plasma of Lister rat during novel object recognition test | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID447844 | Antiinflammatory activity in squirrel monkey whole blood assessed as inhibition of LPS-induced TNFalpha production treated 15 mins before LPS challenge by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors. |
| AID632292 | Antitrypanosomal activity against blood stream Trypanosoma brucei brucei 427 after 48 hrs by Alamar blue assay | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness. |
| AID314167 | Therapeutic index, ratio of plasma concentration causing emesis to IC50 for inhibition of LPS-stimulated TNFalpha release in squirrel monkey whole blood | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors. |
| AID257465 | Oral bioavailability in rat at 20 mg/kg, po | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID257466 | Tmax in rat at 20 mg/kg, po | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID605276 | Ratio of drug level in brain to plasma of Lister rat Drug level in plasma of Lister rat during novel object recognition test relative to untreated control | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID257462 | Inhibition of LPS-induced TNFalpha production in squirrel monkey whole blood | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID447676 | Clearance in iv dosed rat | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors. |
| AID447672 | Inhibition of human CYP2C9 | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors. |
| AID388711 | Inhibition of LPS-induced TNFalpha production in human whole blood | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID388710 | Intrinsic inhibition of GST-fused human PDE4A expressed in SF9 cells | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID314161 | Inhibition of LPS-stimulated TNFalpha release in human whole blood | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors. |
| AID447671 | Toxicity in iv dosed squirrel monkey assessed as occurrence of emesis at plasma concentration of 3.8 uM | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors. |
| AID502801 | Inhibition of human PDE4B | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18 | The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. |
| AID632291 | Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB2 expressed in baculovirus infected insect Sf21 cells | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness. |
| AID388716 | Half life in orally and iv dosed dog | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID257449 | Inhibitory activity against PDE4D | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID605215 | Cognitive enhancing effect in Lister rat assessed as recognition of novel object at 0.1 mg/kg, po pretreated 90 mins before sample phase by novel object recognition test | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID605278 | Ratio of drug level in plasma of lister rat during conditional taste aversion test to IC50 for PDE4 activity in rat whole blood | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID363352 | Inhibition of CYP2C9 | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease. |
| AID257463 | Ratio of emesis threshold plasma concentration over inhibition of LPS-induced TNFalpha production in squirrel monkey whole blood | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID363081 | Inhibition of PDE4 | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease. |
| AID447843 | Bronchodilator effect in guinea pig assessed as inhibition of ovalbumin-induced bronchoconstriction at 30 ug/kg, ip | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors. |
| AID447675 | Bioavailability in iv dosed rat | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors. |
| AID605283 | Drug level in plasma of Lister rat during conditional taste aversion test | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID605111 | Competitive inhibition of CYP2C9 | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID632290 | Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness. |
| AID605107 | Inhibition of PDE4B | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID257450 | Inhibition of LPS-induced TNFalpha production in human whole blood | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID257448 | Inhibitory activity against PDE4C | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. |
| AID388722 | Ratio of emesis Cmax in Squirrel monkey at 10 mg/kg, po to IC50 for LPS-induced TNFalpha production in Squirrel monkey whole blood | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID502800 | Inhibition of human PDE4A | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18 | The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. |
| AID388721 | Bioavailability in orally and iv dosed Squirrel monkey | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. |
| AID605110 | Inhibition of PDE4 activity in rat whole blood assessed as inhibition of LPS-induced TNF-alpha release | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. |
| AID1345239 | Human phosphodiesterase 4D (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs)) | 2007 | Biochemical pharmacology, Jun-15, Volume: 73, Issue:12 | L-454,560, a potent and selective PDE4 inhibitor with in vivo efficacy in animal models of asthma and cognition. |
| AID1345234 | Human phosphodiesterase 4B (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs)) | 2007 | Biochemical pharmacology, Jun-15, Volume: 73, Issue:12 | L-454,560, a potent and selective PDE4 inhibitor with in vivo efficacy in animal models of asthma and cognition. |
| AID1345281 | Human phosphodiesterase 4C (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs)) | 2007 | Biochemical pharmacology, Jun-15, Volume: 73, Issue:12 | L-454,560, a potent and selective PDE4 inhibitor with in vivo efficacy in animal models of asthma and cognition. |
| AID1345251 | Human phosphodiesterase 4A (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs)) | 2007 | Biochemical pharmacology, Jun-15, Volume: 73, Issue:12 | L-454,560, a potent and selective PDE4 inhibitor with in vivo efficacy in animal models of asthma and cognition. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (10)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 7 (70.00) | 29.6817 |
| 2010's | 3 (30.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 11.85
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (11.85) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (10.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 9 (90.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||