Assay ID | Title | Year | Journal | Article |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID363103 | Displacement of [3H]rolipram from PDE4 by RBA | 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. |
AID158402 | Inhibition of recombinant human PDE4A expressed in Sf9 cells | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ). |
AID92879 | Inhibition of LPS-stimulated TNF-alpha production in human whole blood | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors. |
AID92877 | Inhibition of LPS-induced TNF-alpha formation in human whole blood. | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
| Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters. |
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. |
AID133070 | Percent inhibition of arachidonic acid (AA) formation, induced mouse ear edema after pretreatment at a concentration of 30 umol/kg (po) | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones. |
AID76934 | Inhibition of ozone-induced hyperactivity to histamine in guinea pigs on intraperitoneal dose | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors. |
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. |
AID58402 | Emetic effect in dogs at 1 mg/kg intravenous dose, 0 of 4 animals affected | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
| Novel cyclic compounds as potent phosphodiesterase 4 inhibitors. |
AID159796 | Inhibitory activity on human eosinophil phosphodiesterase 4. | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
| 7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase. |
AID157782 | Inhibition of human recombinant phosphodiesterase 4A | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors. |
AID214056 | Arbitary maximal response for cAMP elevation from baseline level was evaluated in Human U-937 cells | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
| 7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase. |
AID71921 | Emetic effect in ferrets | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor. |
AID205155 | Ascaris-induced bronchoconstriction in anesthetized squirrel monkey pretreated with 5 mg/kg intravenously for 30 min | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 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. |
AID76812 | Reduction of antigen-induced pulmonary eosinophilia in sensitized guinea pigs | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors. |
AID257451 | Inhibition of ovalbumin-induced bronchoconstriction in guinea pig at 1 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. |
AID158403 | Inhibition of recombinant human PDE4A expressed in Sf9 cells | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ). |
AID176364 | Reduction of IL-5 induced pleural eosinophilia in rats on oral dose | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors. |
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. |
AID158461 | Inhibition of Phosphodiesterase-4A (PDE4) | 2003 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
| Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors. |
AID92871 | Inhibitory concentration of compound against LPS- induced TNF-alpha production in whole human blood assay | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor. |
AID12308 | Half life of compound was determined in rat | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor. |
AID156050 | Inhibition of N-formyl-methionyl-leucyl-phenylalanine (fMLP)-stimulated production of reactive oxygen species (ROS) in human PMNL by 35% of control | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones. |
AID233957 | Ratio of ROS IC35/PDE4 IC50 was determined | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones. |
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. |
AID257456 | Emetic threshold as plasma concentration in ferrets after 30 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. |
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. |
AID76813 | Increased pulmonary inflation pressure causing bronchoconstriction in ovalbumin sensitized guinea pigs administered intraperitoneally 1 hr prior to antigen | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors. |
AID92729 | Ability to inhibit LPS-induced TNF-alpha formation in human whole blood (HWB) | 2003 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
| Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors. |
AID264627 | Inhibition of ovalbumin-induced bronchoconstriction in guinea pig at 1 mg/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10
| Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors. |
AID85467 | In vitro inhibition of PLS- induced TNF-alpha production in human whole blood (HWB) | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
| Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity. |
AID73324 | In vitro inhibitory activity was determined against human Phosphodiesterase 4 isoform using a construct representing the common region of spliced variants expressed as a GST-fusion protein in Sf 9 cells | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
| Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity. |
AID363104 | Inhibition of GST-tagged PDE4A | 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. |
AID133068 | Percent inhibition of arachidonic acid induced mouse ear edema after 30 uM/kg peroral pretreatment | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones. |
AID215249 | Inhibition of tumor necrosis factor alpha (TNF-alpha) release in murine endotoxemia model | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
| Novel cyclic compounds as potent phosphodiesterase 4 inhibitors. |
AID159651 | Displacement of [3H]rolipram binding to guinea pig brain membrane | 1998 | Bioorganic & medicinal chemistry letters, Jan-20, Volume: 8, Issue:2
| Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles. |
AID157777 | Inhibitory concentration against human PDE4A isoform using a construct representing the common region of spliced variants expressed as GST-fusion protein in Sf9 cells | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor. |
AID7751 | Half life of compound was determined in squirrel monkey | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 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. |
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. |
AID159935 | Inhibitory activity against phosphodiesterase 4 carried out in the cytosol of human neutrophils | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones. |
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. |
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. |
AID159632 | Inhibition of guinea pig macrophage Phosphodiesterase 4 | 1998 | Bioorganic & medicinal chemistry letters, Jan-20, Volume: 8, Issue:2
| Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles. |
AID159936 | Inhibitory concentration against phosphodiesterase 4 (PDE4) in cytosol of human neutrophils | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones. |
AID210151 | Inhibition of LPS-stimulated tumor necrosis factor-alpha release by human whole blood | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones. |
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. |
AID157778 | Inhibition of human Phosphodiesterase 4A isoform using construct representing the common region of spliced variants expressed as GST-fusion proteins in Sf9 cells. | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
| Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters. |
AID1345234 | Human phosphodiesterase 4B (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs)) | 1998 | Cell biochemistry and biophysics, , Volume: 29, Issue:1-2
| CDP840: a novel inhibitor of PDE-4. |
AID1345239 | Human phosphodiesterase 4D (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs)) | 1998 | Cell biochemistry and biophysics, , Volume: 29, Issue:1-2
| CDP840: a novel inhibitor of PDE-4. |
AID1345281 | Human phosphodiesterase 4C (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs)) | 1998 | Cell biochemistry and biophysics, , Volume: 29, Issue:1-2
| CDP840: a novel inhibitor of PDE-4. |
AID1345251 | Human phosphodiesterase 4A (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs)) | 1998 | Cell biochemistry and biophysics, , Volume: 29, Issue:1-2
| CDP840: a novel inhibitor of PDE-4. |
AID157782 | Inhibition of human recombinant phosphodiesterase 4A | 2002 | Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
| CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |