| Assay ID | Title | Year | Journal | Article |
|---|
| AID1171397 | Drug metabolism in mouse liver microsomes assessed as glucuronidation of compound measured as compound remaining after 30 mins by LC/MS analysis | 2014 | ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
| Structure-Metabolism Relationships in the Glucuronidation of d-Amino Acid Oxidase Inhibitors. |
| AID619911 | Inhibition of human DAAO | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID331025 | Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay | 2007 | The Journal of biological chemistry, Jun-22, Volume: 282, Issue:25
| Nicotinic acid receptor agonists differentially activate downstream effectors. |
| AID1171405 | Inhibition of human D-amino acid oxidase | 2014 | ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
| Structure-Metabolism Relationships in the Glucuronidation of d-Amino Acid Oxidase Inhibitors. |
| AID619916 | Inhibition of human ERG expressed in HEK293 cells by whole cell voltage patch clamp technique | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID1171400 | Drug metabolism in mouse liver microsomes assessed as glucuronidation of compound measured as compound remaining after 60 mins by LC/MS analysis | 2014 | ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
| Structure-Metabolism Relationships in the Glucuronidation of d-Amino Acid Oxidase Inhibitors. |
| AID619997 | Tmax in Wistar rat brain at 30 mg/kg, po | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID1917483 | Inhibition of porcine kidney DAAO using D-serine as substrate by Amplex red and horseradish peroxidase fluorescence assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Isatoic anhydrides as novel inhibitors of monoamine oxidase. |
| AID619923 | Kinetic solubility of the compound in 0.01 M phosphate buffered saline at pH 7.4 assessed as maximum solubility after 2 hrs | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID301343 | Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
| Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a. |
| AID619917 | Binding affinity to human recombinant DAAO assessed as drug-enzyme complex half life | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID331028 | Reduction of free fatty acid level in ip dosed C57/BL6 mouse plasma after 10 mins | 2007 | The Journal of biological chemistry, Jun-22, Volume: 282, Issue:25
| Nicotinic acid receptor agonists differentially activate downstream effectors. |
| AID331029 | Reduction of free fatty acid level in po dosed Sprague-Dawley rat plasma | 2007 | The Journal of biological chemistry, Jun-22, Volume: 282, Issue:25
| Nicotinic acid receptor agonists differentially activate downstream effectors. |
| AID619991 | Ratio of drug level (0 to last) in brain to plasma in Swiss mouse at 30 mg/kg, po | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID619921 | Thermodynamic solubility of the compound in phosphate buffer at pH 7.4 after 24 hrs by HPLC analysis | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID619912 | Binding affinity to human recombinant DAAO by isothermal titration calorimeter analysis | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID619915 | Inhibition of bovine recombinant DASPO expressed in Escherichia coli preincubated for 15 mins by fluorescence assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID1819261 | Binding affinity to Pseudomonas aeruginosa MurB assessed as change in melting temperature at 5 mM by differential scanning fluorimetry | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Inhibitors of Uridine Diphosphate- |
| AID301341 | Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
| Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a. |
| AID619983 | Cmax in Swiss mouse brain at 30 mg/kg, po | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID308653 | Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
| Agonist lead identification for the high affinity niacin receptor GPR109a. |
| AID331030 | Reduction of free fatty acid level in po dosed Sprague-Dawley rat plasma relative to baseline | 2007 | The Journal of biological chemistry, Jun-22, Volume: 282, Issue:25
| Nicotinic acid receptor agonists differentially activate downstream effectors. |
| AID619913 | Binding affinity to human recombinant DAAO by kinetic study scintillation proximity assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID620001 | Terminal half life in Wistar rat brain at 30 mg/kg, po | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID620009 | Plasma clearance in Wistar rat plasma at 10 mg/kg, iv | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID301348 | Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay in relative to niacin | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
| Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a. |
| AID619981 | Cmax in Wistar rat brain at 30 mg/kg, po | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID1896384 | Inhibition of porcine kidney DAAO using D-serine as substrate assessed as H2O2 formation by amplex red and peroxidase-coupled continuous fluorescence spectrophotometric analysis | 2022 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 77 | The inhibition of monoamine oxidase by 2H-1,4-benzothiazin-3(4H)-ones. |
| AID619987 | AUC (0 to last) in Swiss mouse brain at 30 mg/kg, po | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID619918 | Dissociation constant, pKa of the compound by dip probe absorption spectroscopy technique | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID619985 | AUC (0 to last) in Wistar rat brain at 30 mg/kg, po | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID1655493 | Inhibition of RNase H activity of recombinant His-tagged HIV-1 group M subtype B reverse transcriptase p66/p51 expressed in Escherichia coli M15 using 18-nucleotide 3'-fluorescein-labeled RNA/5'-dabcyl-labeled DNA hybrid as substrate incubated for 1 hr | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Pyrrolyl Pyrazoles as Non-Diketo Acid Inhibitors of the HIV-1 Ribonuclease H Function of Reverse Transcriptase. |
| AID331026 | Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay relative to nicotinic acid | 2007 | The Journal of biological chemistry, Jun-22, Volume: 282, Issue:25
| Nicotinic acid receptor agonists differentially activate downstream effectors. |
| AID331027 | Inhibition of isoproterenol-induced lipolysis in human subcutaneous adipocytes after 5 hrs | 2007 | The Journal of biological chemistry, Jun-22, Volume: 282, Issue:25
| Nicotinic acid receptor agonists differentially activate downstream effectors. |
| AID619993 | Oral bioavailability (0 to last) in Wistar rat plasma at 30 mg/kg | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID619989 | Ratio of drug level (0 to last) in brain to plasma in Wistar rat at 30 mg/kg, po | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID1494470 | Inhibition of Rickettsia prowazekii N-terminal His6-tagged methionine aminopeptidase 1 expressed in Escherichia coli DLB3 Rosetta cells at 10 uM using Met-AMC as substrate preincubated for 1 hr followed by 30 mins incubation after substrate addition measu | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| The identification of inhibitory compounds of Rickettsia prowazekii methionine aminopeptidase for antibacterial applications. |
| AID620011 | Plasma clearance in Swiss mouse plasma at 10 mg/kg, iv | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID331033 | Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA | 2007 | The Journal of biological chemistry, Jun-22, Volume: 282, Issue:25
| Nicotinic acid receptor agonists differentially activate downstream effectors. |
| AID619995 | Oral bioavailability (0 to last) in Swiss mouse plasma at 30 mg/kg | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID301342 | Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level upto 50 uM by HTRF assay | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
| Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a. |
| AID331031 | Induction of flushing response in ip dosed C57/BL6 mouse | 2007 | The Journal of biological chemistry, Jun-22, Volume: 282, Issue:25
| Nicotinic acid receptor agonists differentially activate downstream effectors. |
| AID619914 | Binding affinity to human recombinant DAAO by steady state study scintillation proximity assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID1819260 | Binding affinity to Pseudomonas aeruginosa MurB assessed as change in melting temperature at 1 mM by differential scanning fluorimetry | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Discovery of Novel Inhibitors of Uridine Diphosphate- |
| AID620007 | Volume of distribution in Swiss mouse plasma at 10 mg/kg, iv | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID619910 | Inhibition of human recombinant DAAO expressed in Escherichia coli assessed as H2O2 production from D-serine degradation after 30 mins by fluorescence assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID619919 | Octanol-water partition coefficient, log P of the neutral compound by pH-metric method | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID619999 | Tmax in Swiss mouse brain at 30 mg/kg, po | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID308655 | Agonist activity at human cloned GPR109b receptor at 100 uM by forskolin-stimulated cAMP production test | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
| Agonist lead identification for the high affinity niacin receptor GPR109a. |
| AID620005 | Volume of distribution in Wistar rat plasma at 10 mg/kg, iv | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID371730 | Dissociation constant, pKa of the compound | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors. |
| AID620003 | Terminal half life in Swiss mouse brain at 30 mg/kg, po | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| AID619922 | Kinetic solubility of the compound in 0.01 M phosphate buffered saline at pH 7.4 assessed as minimum solubility after 2 hrs | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |