Compounds > 5-(ethylsulfonyl)-2-(naphthalen-2-yl)benzo(d)oxazole
Page last updated: 2024-11-13

5-(ethylsulfonyl)-2-(naphthalen-2-yl)benzo(d)oxazole

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

Description

ezutromid: a utrophin upregulator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25109292
CHEMBL ID1773683
SCHEMBL ID732212
MeSH IDM0559611

Synonyms (38)

Synonym
CHEMBL1773683
smt c1100
smtc-1100
ezutromid
smt-c1100
bmn-195
bmn 195
5-(ethylsulfonyl)-2-(naphthalen-2-yl)benzo(d)oxazole
unii-645r07lf0d
945531-77-1
ezutromid [inn]
5-ethylsulfonyl-nbo
benzoxazole, 5-(ethylsulfonyl)-2-(2-naphthalenyl)-
645r07lf0d ,
SCHEMBL732212
5-(ethanesulfonyl)-2-(naphthalen-2-yl)-1,3-benzoxazole
ezutromid [who-dd]
bmn195
AC-30950
5-(ethylsulfonyl)-2-(naphthalen-2-yl)benzo[d]oxazole
DTXSID30241525
HY-17614
CS-5710
AKOS030527030
gtpl11110
DB12888
BCP18328
F20702
EX-A2333
vox-c1100
5-ethylsulfonyl-2-naphthalen-2-yl-1,3-benzoxazole
smtc 1100
smtc1100
SB19603
bmn-195; smt c1100
Q27263708
A901653
bdbm50519636

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Adverse events (AEs) were monitored throughout the study."( Safety, Tolerability, and Pharmacokinetics of SMT C1100, a 2-Arylbenzoxazole Utrophin Modulator, following Single- and Multiple-Dose Administration to Pediatric Patients with Duchenne Muscular Dystrophy.
Davies, K; Hughes, I; Layton, G; Muntoni, F; Ricotti, V; Robinson, N; Roper, H; Spinty, S; Tejura, B; Tinsley, J, 2016)		0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
UtrophinHomo sapiens (human)EC50 (µMol)0.52570.11000.52571.2800AID1580310; AID1580311; AID1660788
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
positive regulation of cell-matrix adhesionUtrophinHomo sapiens (human)
muscle contractionUtrophinHomo sapiens (human)
muscle organ developmentUtrophinHomo sapiens (human)
regulation of sodium ion transmembrane transporter activityUtrophinHomo sapiens (human)
synaptic signalingUtrophinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
actin bindingUtrophinHomo sapiens (human)
integrin bindingUtrophinHomo sapiens (human)
protein bindingUtrophinHomo sapiens (human)
zinc ion bindingUtrophinHomo sapiens (human)
vinculin bindingUtrophinHomo sapiens (human)
protein kinase bindingUtrophinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
contractile ringUtrophinHomo sapiens (human)
nucleoplasmUtrophinHomo sapiens (human)
cytoplasmUtrophinHomo sapiens (human)
cytoskeletonUtrophinHomo sapiens (human)
plasma membraneUtrophinHomo sapiens (human)
membraneUtrophinHomo sapiens (human)
filopodiumUtrophinHomo sapiens (human)
filopodium membraneUtrophinHomo sapiens (human)
neuromuscular junctionUtrophinHomo sapiens (human)
sarcolemmaUtrophinHomo sapiens (human)
postsynaptic membraneUtrophinHomo sapiens (human)
extracellular exosomeUtrophinHomo sapiens (human)
dystrophin-associated glycoprotein complexUtrophinHomo sapiens (human)
protein-containing complexUtrophinHomo sapiens (human)
plasma membraneUtrophinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (100)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1580270Drug metabolism assessed as human CYP1A2-mediated metabolism by measuring DHD3 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580308Induction of CYP2E1 enzymes in minipig assessed as increase in 11-hydroxylase activity at 500 mg/kg/day, po for 39 weeks relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1660808Stability in human hepatocytes assessed as half life after 60 mins2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1580269Drug metabolism assessed as human CYP1A1-mediated metabolism by measuring DHD3 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580253Drug metabolism in beta-naphthoflavone/phenobarbital-induced rat liver S9 fraction assessed as compound-D2 formation at 100 ug/ml in presence of NADPH measured after 4 hrs by UV-Vis spectroscopy2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580291Induction of CYP1A2 in rat hepatocytes at 0.1 to 10 uM incubated for 48 hrs2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1660788Modulation of human utrophinA expressed in mouse H2K cells assessed as upregulation of utrophin production after 24 hrs by luciferase reporter gene assay2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1782742Upregulation of utrophin gene expression in DMD disease mouse model myoblasts expressing H2K-mdx utrnA-firefly luciferase assessed as fold increase in utrophin mRNA at 3 uM by qRT-PCR analysis relative to control2021European journal of medicinal chemistry, Aug-05, Volume: 220Discovery and mechanism of action studies of 4,6-diphenylpyrimidine-2-carbohydrazides as utrophin modulators for the treatment of Duchenne muscular dystrophy.
AID1580276Drug metabolism assessed as human CYP3A4-mediated metabolism by measuring DHD3 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580302Induction of CYP2B enzymes in minipig assessed as increase in PROD enzyme activity at 500 mg/kg/day, po for 39 weeks relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580282Drug metabolism in human liver microsomes assessed as formation of DHD1 in presence of CYP2D6 inhibitor Quinidine relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID596512Activation of UTRN promoter in mouse H2K cells assessed as upregulation of UTRN production at 10 uM after 72 hrs by RT-PCR analysis2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of Duchenne muscular dystrophy.
AID1580314Permeability at pH 7.4 by PAMPA2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580299Effect on microsomal protein concentrations in rat at 2000 mg/kg/day, po for 28 days2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580327Drug metabolism assessed as human UGT-mediated metabolism by measuring half life for DHD3 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1660796Plasma protein binding in human2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1580281Drug metabolism in human liver microsomes assessed as formation of DHD3 in presence of CYP1A inhibitor alpha-naphthoflavone relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580312Lipophilicity, logD of the compound at pH 7.42020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580259Drug metabolism assessed as human CYP1A2-mediated metabolism by measuring half life2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580287Drug metabolism in rat plasma assessed as isomeric dihydrodiol formation at 2000 mg/kg, po measured after 24 hrs2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580286Drug metabolism in rat plasma assessed as dihydrodiol formation at 2000 mg/kg, po measured after 24 hrs2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID596518Cmax in CD1 mouse at 50 mg/kg, ip2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of Duchenne muscular dystrophy.
AID596514Half life in mouse liver microsomes2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of Duchenne muscular dystrophy.
AID1580316Protein binding in human plasma assessed as bound fraction2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID596523Aqueous solubility of the compound by turbidimetry2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of Duchenne muscular dystrophy.
AID1580261Drug metabolism assessed as human CYP2C8-mediated metabolism by measuring half life2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580292Induction of CYP1A2 in human hepatocytes at 0.1 to 10 uM incubated for 48 hrs2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580307Induction of CYP3A enzymes in minipig assessed as increase in testosterone hydroxylase activity at 500 mg/kg/day, po for 39 weeks relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1660807Stability in mouse hepatocytes assessed as half life after 60 mins2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1580267Drug metabolism assessed as human CYP2B6-mediated metabolism by measuring DHD1 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1782744Upregulation of AhR gene expression in DMD disease mouse model myoblasts expressing H2K-mdx utrnA-firefly luciferase assessed as fold increase in AhR mRNA at 3 uM by qRT-PCR analysis relative to control2021European journal of medicinal chemistry, Aug-05, Volume: 220Discovery and mechanism of action studies of 4,6-diphenylpyrimidine-2-carbohydrazides as utrophin modulators for the treatment of Duchenne muscular dystrophy.
AID1580268Drug metabolism assessed as human CYP2D6-mediated metabolism by measuring DHD1 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580306Induction of CYP2B enzymes in male minipig assessed as increase in PROD enzyme activity at 500 mg/kg/day, po for 39 weeks relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580266Drug metabolism assessed as human CYP1A2-mediated metabolism by measuring DHD1 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580290Induction of CYP1A1 in rat hepatocytes at 0.1 to 10 uM incubated for 48 hrs2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580313Kinetic aqueous solubility of the compound2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580339Substrate activity at OATP1B1 (unknown origin)2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580311Activation of human utrophin-1 in iDMD cells by HTRF assay2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580264Drug metabolism assessed as human CYP2D6-mediated metabolism by measuring half life2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580277Intrinsic clearance in human liver microsomes in presence of CYP1A inhibitor alpha-naphthoflavone2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580320Half life in human liver S9 fraction2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580297Effect on microsomal protein concentrations in minipig at 500 mg/kg/day, po for 39 weeks2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580317Half life in mouse liver S9 fraction2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580273Drug metabolism assessed as human CYP2C9-mediated metabolism by measuring DHD3 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580322Intrinsic clearance in mouse liver S9 fraction2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580301Induction of CYP1A1/2 enzymes in minipig assessed as increase in EROD enzyme activity at 500 mg/kg/day, po for 39 weeks relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580243Drug level in rat plasma at 2000 mg/kg, po measured after 24 hrs2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580305Induction of CYP1A1/2 enzymes in male minipig assessed as increase in EROD enzyme activity at 500 mg/kg/day, po for 39 weeks relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580271Drug metabolism assessed as human CYP2B6-mediated metabolism by measuring DHD3 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580272Drug metabolism assessed as human CYP2C8-mediated metabolism by measuring DHD3 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580326Drug metabolism assessed as human UGT-mediated metabolism by measuring half life for DHD1 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1660799Intrinsic clearance in human liver microsomes2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1580285Drug metabolism in rat plasma assessed as isomeric dihydrodiol formation at 2000 mg/kg, po dosed for 28 days2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID596509Activation of UTRN promoter in mouse H2K cells assessed as upregulation of UTRN production after 48 hrs by luciferase reporter linked assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of Duchenne muscular dystrophy.
AID1580309Induction of CYP4A enzymes in minipig assessed as increase in 12-hydroxylase activity at 500 mg/kg/day, po for 39 weeks relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580304Induction of CYP2B enzymes in female minipig assessed as increase in PROD enzyme activity at 500 mg/kg/day, po for 39 weeks relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580296Induction of CYP1A1/2 enzymes in rat assessed as increase in EROD enzyme activity per nanomole of P450 at 2000 mg/kg/day, po for 28 days relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580298Effect on total cytochrome P450 content in minipig at 500 mg/kg/day, po for 39 weeks2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580294Induction of CYP1A1/2 enzymes in rat assessed as increase in EROD enzyme activity per milligram of protein at 2000 mg/kg/day, po for 28 days relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580244Drug metabolism in rat plasma assessed as dihydrodiol formation at 2000 mg/kg, po dosed for 28 days2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580278Intrinsic clearance in human liver microsomes in presence of CYP2B6 inhibitor Ticlopidine2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580293Inhibition of CYP1A2 in human liver microsomes2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1660844Drug metabolism in mouse hepatocytes assessed as compound racemization after 60 mins2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1580303Induction of CYP1A1/2 enzymes in female minipig assessed as increase in EROD enzyme activity at 500 mg/kg/day, po for 39 weeks relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1660795Plasma protein binding in mouse2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1580280Intrinsic clearance in human liver microsomes2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580310Activation of human utrophin-1 in mouse mdx myoblasts by H2K-mdx utrnA-luc assay2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580295Induction of CYP1A1/2 enzymes in rat assessed as increase in EROD enzyme activity per gram of liver at 2000 mg/kg/day, po for 28 days relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580336Substrate activity at BCRP (unknown origin)2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID596515Half life in human liver microsomes2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of Duchenne muscular dystrophy.
AID1580275Drug metabolism assessed as human CYP2D6-mediated metabolism by measuring DHD3 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1660789Solubility of compound by turbidimetric assay2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1580263Drug metabolism assessed as human CYP2C19-mediated metabolism by measuring half life2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580262Drug metabolism assessed as human CYP2C9-mediated metabolism by measuring half life2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580283Drug metabolism in human liver microsomes assessed as formation of DHD3 in presence of CYP2D6 inhibitor Quinidine relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580274Drug metabolism assessed as human CYP2C19-mediated metabolism by measuring DHD3 formation2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580258Drug metabolism assessed as human CYP1A1-mediated metabolism by measuring half life2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580245Drug metabolism in in human liver microsomes assessed as metabolite retention time incubation for 45 mins2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580289Drug metabolism in rat plasma assessed as formation of O-glucuronide conjugate of aromatized diol at 2000 mg/kg, po dosed for 28 days2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580338Substrate activity at MDR4 (unknown origin)2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580242Drug metabolism in human liver microsomes assessed as formation of DHD1 in presence of CYP1A inhibitor alpha-naphthoflavone relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580252Drug metabolism in beta-naphthoflavone/phenobarbital-induced rat liver S9 fraction assessed as compound-D1 formation at 100 ug/ml in presence of NADPH measured after 4 hrs by UV-Vis spectroscopy2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580340Substrate activity at OATP1B3 (unknown origin)2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1660805Intrinsic clearance in mouse hepatocytes after 60 mins2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1580265Drug metabolism assessed as human CYP3A4-mediated metabolism by measuring half life2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID596521AUC in CD1 mouse at 50 mg/kg, ip2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of Duchenne muscular dystrophy.
AID1580324Intrinsic clearance in human liver S9 fraction2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580260Drug metabolism assessed as human CYP2B6-mediated metabolism by measuring half life2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID596516Tmax in CD1 mouse at 50 mg/kg, ip2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of Duchenne muscular dystrophy.
AID1580315Protein binding in mouse plasma assessed as bound fraction2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1660806Intrinsic clearance in human hepatocytes after 60 mins2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1660800Microsomal stability in human liver microsomes assessed as half life2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1580300Effect on total cytochrome P450 content in rat at 2000 mg/kg/day, po for 28 days2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580279Intrinsic clearance in human liver microsomes in presence of CYP2D6 inhibitor Quinidine2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1660798Microsomal stability in mouse liver microsomes assessed as half life2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1660845Drug metabolism in human hepatocytes assessed as compound racemization after 60 mins2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1660797Intrinsic clearance in mouse liver microsomes2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
2-Arylbenzo[
AID1580337Substrate activity at MDR1 (unknown origin)2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
AID1580288Drug metabolism in rat plasma assessed as formation of glucuronide conjugate of dihydrodiol at 2000 mg/kg, po dosed for 28 days2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (40.00)24.3611
2020's6 (60.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.98

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 Index11.98 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.98)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (20.00%)5.53%
Reviews1 (10.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational1 (10.00%)0.25%
Other6 (60.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
1,2-dihydroxy-1,2-dihydronaphthalene
1,2-dihydroxy-1,2-dihydronaphthalene: naphthalene metabolite; RN given refers to cpd without isomeric designation. 1,2-dihydronaphthalene-1,2-diol : A member of the class of naphthalenediols that is 1,2-dihydronaphthalene substituted by hydroxy groups at positions 1 and 2 respectively.		2.2510dihydronaphthalenes;
naphthalenediols		bacterial xenobiotic metabolite;
mouse metabolite
2-naphthol
2-naphthol: RN given refers to parent cpd. 2-naphthol : A naphthol carrying a hydroxy group at position 2.. naphthols : Any hydroxynaphthalene derivative that has a single hydroxy substituent.		2.2510naphtholantinematodal drug;
genotoxin;
human urinary metabolite;
human xenobiotic metabolite;
mouse metabolite;
radical scavenger
benzoxazoles
1,3-benzoxazole : A benzoxazole in which the benzene ring is fused to a 1,3-oxazole ring across positions 4 and 5.. benzoxazole : Compounds based on a fused 1,2- or 1,3-oxazole and benzene bicyclic ring skeleton.		7.5721,3-benzoxazoles;
mancude organic heterobicyclic parent
quinidine
Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.		2.2510cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		3.2110
ptc 124
[no description available]		3.2110oxadiazole;
ring assembly
ConditionIndicatedRelationship StrengthStudiesTrials
Becker Muscular Dystrophy
[description not available]		07.4582
Muscular Dystrophy, Duchenne
An X-linked recessive muscle disease caused by an inability to synthesize DYSTROPHIN, which is involved with maintaining the integrity of the sarcolemma. Muscle fibers undergo a process that features degeneration and regeneration. Clinical manifestations include proximal weakness in the first few years of life, pseudohypertrophy, cardiomyopathy (see MYOCARDIAL DISEASES), and an increased incidence of impaired mentation. Becker muscular dystrophy is a closely related condition featuring a later onset of disease (usually adolescence) and a slowly progressive course. (Adams et al., Principles of Neurology, 6th ed, p1415)		19.4582
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.0310