Page last updated: 2024-12-09

6-Chlorobenzo[d]isoxazol-3-ol

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID2781852
CHEMBL ID445990
CHEBI ID194636
SCHEMBL ID481926

Synonyms (41)

Synonym
chembl445990 ,
6-chloro-1,2-benzoxazol-3-ol
cbio
bdbm23174
MLS000850688
smr000456705
6-chlorobenzo[d]isoxazol-3-ol
SR-01000641124-1
CHEBI:194636
6-chloro-1,2-benzoxazol-3-one
61977-29-5
A833514
CCG-1741
AKOS006230032
6-chloro-1,2-benzisoxazol-3-ol
HMS2790M22
FT-0621064
1,2-benzisoxazol-3(2h)-one,6-chloro-
6-chlorobenzo(d)isoxazol-3-ol
3-hydroxy-6-chloro-benzisoxazole
SJAPSPJRTQCDNO-UHFFFAOYSA-N
GEO-03212
6-chloro-3-hydroxy-1,2-benzisoxazole
SCHEMBL481926
TS-02303
6-chloro-1,2-benzisoxazol-3(2h)-one
1,2-benzisoxazol-3(2h)-one, 6-chloro-
DTXSID70381878
mfcd00125033
6-chlorobenzo[d]isoxazol-3-ol, aldrichcpr
cbio, >=95% (hplc)
bdbm50170230
6-chlorobenzo[d]isoxazol-3(2h)-one
CS-0063922
HMS3741O11
6-chloro-3-hydroxybenzisoxazole
SY104108
6-chlorobenzisoxazol-3(2h)-one
6-chloro-benzo[d]isoxazol-3-ol
EN300-318802
PD129399

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" We identified novel DAO inhibitors, in particular, acid 1, which demonstrated moderate potency for DAO in vitro and ex vivo, and raised plasma d-serine levels after dosing ip to rats."( The discovery of fused pyrrole carboxylic acids as novel, potent D-amino acid oxidase (DAO) inhibitors.
Abeywickrema, P; Almond, S; Brandon, N; Byrne, N; Campbell, A; Hutson, PH; Jacobson, M; Jones, B; Munshi, S; Pascarella, D; Pike, A; Prasad, GS; Sachs, N; Sakatis, M; Sardana, V; Sparey, T; Venkatraman, S; Young, MB, 2008
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzisoxazoleCompounds based on a fused 1,2-oxazole and benzene bicyclic ring skeleton.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency3.54810.003245.467312,589.2998AID2517
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
D-amino-acid oxidaseRattus norvegicus (Norway rat)IC50 (µMol)0.09000.00400.25890.8550AID1300692
D-amino-acid oxidaseSus scrofa (pig)IC50 (µMol)0.18800.18802.047810.0000AID1798301; AID404688
D-amino-acid oxidaseHomo sapiens (human)IC50 (µMol)0.16530.00401.119910.0000AID1300693; AID1389531; AID408637; AID619910
5-hydroxytryptamine receptor 1BOryctolagus cuniculus (rabbit)IC50 (µMol)0.18800.00060.09430.1880AID404688
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)10.00000.00091.901410.0000AID619916
D-aspartate oxidaseHomo sapiens (human)IC50 (µMol)5.00000.00400.39370.8550AID408638
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
D-amino-acid oxidaseSus scrofa (pig)Kd0.87000.15002.81006.3000AID1389535
D-amino-acid oxidaseHomo sapiens (human)Kd0.01500.00311.72789.0000AID619912; AID619913; AID619914
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (36)

Processvia Protein(s)Taxonomy
proline catabolic processD-amino-acid oxidaseHomo sapiens (human)
digestionD-amino-acid oxidaseHomo sapiens (human)
D-amino acid catabolic processD-amino-acid oxidaseHomo sapiens (human)
D-serine catabolic processD-amino-acid oxidaseHomo sapiens (human)
dopamine biosynthetic processD-amino-acid oxidaseHomo sapiens (human)
D-alanine catabolic processD-amino-acid oxidaseHomo sapiens (human)
D-serine metabolic processD-amino-acid oxidaseHomo sapiens (human)
neutrophil-mediated killing of gram-negative bacteriumD-amino-acid oxidaseHomo sapiens (human)
D-amino acid catabolic processD-aspartate oxidase Bos taurus (cattle)
nervous system processD-aspartate oxidase Bos taurus (cattle)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inseminationD-aspartate oxidaseHomo sapiens (human)
grooming behaviorD-aspartate oxidaseHomo sapiens (human)
regulation of cell communicationD-aspartate oxidaseHomo sapiens (human)
D-amino acid catabolic processD-aspartate oxidaseHomo sapiens (human)
hormone metabolic processD-aspartate oxidaseHomo sapiens (human)
nervous system processD-aspartate oxidaseHomo sapiens (human)
aspartate catabolic processD-aspartate oxidaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
D-amino-acid oxidase activityD-amino-acid oxidaseHomo sapiens (human)
protein bindingD-amino-acid oxidaseHomo sapiens (human)
identical protein bindingD-amino-acid oxidaseHomo sapiens (human)
FAD bindingD-amino-acid oxidaseHomo sapiens (human)
D-aspartate oxidase activityD-aspartate oxidase Bos taurus (cattle)
D-glutamate oxidase activityD-aspartate oxidase Bos taurus (cattle)
FAD bindingD-aspartate oxidase Bos taurus (cattle)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingD-aspartate oxidaseHomo sapiens (human)
D-aspartate oxidase activityD-aspartate oxidaseHomo sapiens (human)
D-glutamate oxidase activityD-aspartate oxidaseHomo sapiens (human)
FAD bindingD-aspartate oxidaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
mitochondrial outer membraneD-amino-acid oxidaseHomo sapiens (human)
extracellular regionD-amino-acid oxidaseHomo sapiens (human)
cytoplasmD-amino-acid oxidaseHomo sapiens (human)
peroxisomal matrixD-amino-acid oxidaseHomo sapiens (human)
cytosolD-amino-acid oxidaseHomo sapiens (human)
cell projectionD-amino-acid oxidaseHomo sapiens (human)
presynaptic active zoneD-amino-acid oxidaseHomo sapiens (human)
cytoplasmD-amino-acid oxidaseHomo sapiens (human)
peroxisomal matrixD-aspartate oxidase Bos taurus (cattle)
cytosolD-aspartate oxidase Bos taurus (cattle)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
peroxisomeD-aspartate oxidaseHomo sapiens (human)
peroxisomeD-aspartate oxidaseHomo sapiens (human)
peroxisomal matrixD-aspartate oxidaseHomo sapiens (human)
cytosolD-aspartate oxidaseHomo sapiens (human)
cytoplasmD-aspartate oxidaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (62)

Assay IDTitleYearJournalArticle
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID619988AUC (0 to last) in Swiss mouse brain at 10 mg/kg, po2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID620008Volume of distribution in Swiss mouse plasma at 1 mg/kg, iv2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619923Kinetic solubility of the compound in 0.01 M phosphate buffered saline at pH 7.4 assessed as maximum solubility after 2 hrs2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619986AUC (0 to last) in Wistar rat brain at 10 mg/kg, po2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619984Cmax in Swiss mouse brain at 10 mg/kg, po2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619994Oral bioavailability (0 to last) in Wistar rat plasma at 10 mg/kg2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID408638Inhibition of human DDO2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
The discovery of fused pyrrole carboxylic acids as novel, potent D-amino acid oxidase (DAO) inhibitors.
AID619917Binding affinity to human recombinant DAAO assessed as drug-enzyme complex half life2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID1300693Inhibition of human recombinant DAAO using D-alanine as substrate assessed as pyruvate production incubated for 60 mins by microplate reader analysis2016European journal of medicinal chemistry, Jul-19, Volume: 117Discovery and analgesic evaluation of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione as a novel potent d-amino acid oxidase inhibitor.
AID619992Ratio of drug level (0 to last) in brain to plasma in Swiss mouse at 10 mg/kg, po2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID1389531Inhibition of human DAAO using D-KYN as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by FP-6300-based fluorescence spectrometry2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Discovery of isatin and 1H-indazol-3-ol derivatives as d-amino acid oxidase (DAAO) inhibitors.
AID620004Terminal half life in Swiss mouse brain at 10 mg/kg, po2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID620006Volume of distribution in Wistar rat plasma at 1 mg/kg, iv2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID1300691Inhibition of DAAO in porcine kidney homogenate using D-alanine as substrate assessed as pyruvate production incubated for 5 mins by microplate reader analysis2016European journal of medicinal chemistry, Jul-19, Volume: 117Discovery and analgesic evaluation of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione as a novel potent d-amino acid oxidase inhibitor.
AID1171400Drug metabolism in mouse liver microsomes assessed as glucuronidation of compound measured as compound remaining after 60 mins by LC/MS analysis2014ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
Structure-Metabolism Relationships in the Glucuronidation of d-Amino Acid Oxidase Inhibitors.
AID620002Terminal half life in Wistar rat brain at 10 mg/kg, po2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID371730Dissociation constant, pKa of the compound2009Journal 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.
AID404690Increase in D-serine level in Sprague-Dawley rat prefrontal cortex at 30 mg/kg, po coadministered with D-serine2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Synthesis and biological evaluation of D-amino acid oxidase inhibitors.
AID1389535Binding affinity to pig kidney DAAO by ITC method2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Discovery of isatin and 1H-indazol-3-ol derivatives as d-amino acid oxidase (DAAO) inhibitors.
AID404688Inhibition of pig D-amino acid oxidase2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Synthesis and biological evaluation of D-amino acid oxidase inhibitors.
AID620082Plasma clearance in Swiss mouse plasma at 1 mg/kg, iv2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID404689Increase in D-serine level in Sprague-Dawley rat plasma at 30 mg/kg, po coadministered with D-serine2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Synthesis and biological evaluation of D-amino acid oxidase inhibitors.
AID619922Kinetic solubility of the compound in 0.01 M phosphate buffered saline at pH 7.4 assessed as minimum solubility after 2 hrs2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID620000Tmax in Swiss mouse brain at 10 mg/kg, po2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID404691Increase in D-serine level in Sprague-Dawley rat prefrontal cortex at 30 mg/kg, po2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Synthesis and biological evaluation of D-amino acid oxidase inhibitors.
AID408637Inhibition of human DAO2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
The discovery of fused pyrrole carboxylic acids as novel, potent D-amino acid oxidase (DAO) inhibitors.
AID619912Binding affinity to human recombinant DAAO by isothermal titration calorimeter analysis2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619982Cmax in Wistar rat brain at 10 mg/kg, po2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619924Apparent permeability across apical to basolateral side in human Caco2 cells by LC-MS/MS analysis2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619915Inhibition of bovine recombinant DASPO expressed in Escherichia coli preincubated for 15 mins by fluorescence assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID620010Plasma clearance in Wistar rat plasma at 1 mg/kg, iv2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619980Intrinsic clearance in human liver microsomes2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619998Tmax in Wistar rat brain at 10 mg/kg, po2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619990Ratio of drug level (0 to last) in brain to plasma in Wistar rat at 10 mg/kg, po2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619914Binding affinity to human recombinant DAAO by steady state study scintillation proximity assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619910Inhibition of human recombinant DAAO expressed in Escherichia coli assessed as H2O2 production from D-serine degradation after 30 mins by fluorescence assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619919Octanol-water partition coefficient, log P of the neutral compound by pH-metric method2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID1300692Inhibition of rat spinal DAAO using D-alanine as substrate assessed as pyruvate production incubated for 60 mins by microplate reader analysis2016European journal of medicinal chemistry, Jul-19, Volume: 117Discovery and analgesic evaluation of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione as a novel potent d-amino acid oxidase inhibitor.
AID619913Binding affinity to human recombinant DAAO by kinetic study scintillation proximity assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619918Dissociation constant, pKa of the compound by dip probe absorption spectroscopy technique2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619916Inhibition of human ERG expressed in HEK293 cells by whole cell voltage patch clamp technique2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619921Thermodynamic solubility of the compound in phosphate buffer at pH 7.4 after 24 hrs by HPLC analysis2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619996Oral bioavailability (0 to last) in Swiss mouse plasma at 10 mg/kg2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID1171397Drug metabolism in mouse liver microsomes assessed as glucuronidation of compound measured as compound remaining after 30 mins by LC/MS analysis2014ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
Structure-Metabolism Relationships in the Glucuronidation of d-Amino Acid Oxidase Inhibitors.
AID619925Apparent permeability from apical to basolateral side of MDCK cells expressing MDR1 by LC-MS/MS analysis2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID619979Efflux ratio of permeability from apical to basolateral over basolateral to apical side in human Caco2 cells by LC-MS/MS analysis2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1798301In vitro D-Amino Acid Oxidase Assay from Article 10.1021/jm800200u: \\Synthesis and Biological Evaluation of d-Amino Acid Oxidase Inhibitors.\\2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Synthesis and biological evaluation of D-amino acid oxidase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (26.67)29.6817
2010's9 (60.00)24.3611
2020's2 (13.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.70

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.

MetricThis Compound (vs All)
Research Demand Index11.70 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index4.47 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.70)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]