Page last updated: 2024-12-10

sb 408124

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

Description

SB 408124: a hypocretin receptor type 1 (HcrtR1) antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4331799
CHEMBL ID1334465
CHEBI ID92941
SCHEMBL ID1586538
MeSH IDM0537803

Synonyms (56)

Synonym
HY-70068
HMS3268O20
1-(6,8-difluoro-2-methylquinolin-4-yl)-3-(4-dimethylaminophenyl)urea
sb408124
gtpl1704
sb 408124
NCGC00025330-01 ,
NCGC00025330-02
sb-408124 ,
CHEMBL1334465 ,
1-(6,8-difluoro-2-methylquinolin-4-yl)-3-[4-(dimethylamino)phenyl]urea
3-(6,8-difluoro-2-methylquinolin-4-yl)-1-[4-(dimethylamino)phenyl]urea
n-(6,8-difluoro-2-methyl-4-quinolinyl)-n'-[4-(dimethylamino)phenyl]urea
BCPP000072
288150-92-5
CS-0350
S1545
BRD-K53913732-001-01-8
bdbm50423648
smr004702996
MLS006011236
SCHEMBL1586538
c19h18f2n4o
1-(6,8-difluoro-2-methylquinolin-4-yl)-3-(4-(dimethylamino)phenyl)urea
AC-31977
AKOS024456881
DTXSID20402022
mfcd06411575
EX-A329
SR-01000597520-1
sr-01000597520
CHEBI:92941
HMS3655A03
AS-73125
sb-408124, >=98% (hplc), solid
J-017278
SW219651-1
FT-0709881
288150-92-5 (free base)
HMS3676P06
nvn ,
1-[6,8-bis(fluoranyl)-2-methyl-quinolin-4-yl]-3-[4-(dimethylamino)phenyl]urea
BCP02343
HMS3412P06
Q7388912
SB19534
urea, n-(6,8-difluoro-2-methyl-4-quinolinyl)-n'-[4-(dimethylamino)phenyl]-
HMS3884O19
HMS3748K15
CCG-268112
A876610
c3yt74c744 ,
1-(6,8-difluoro-2-methyl-quinolin-4-yl)-3-(4-dimethylamino-phenyl)-urea
urea, n-(6,8-difluoro-2-methyl-4-quinolinyl)-n-(4-(dimethylamino)phenyl)-
n-(6,8-difluoro-2-methyl-4-quinolinyl)-n-(4-(dimethylamino)phenyl)urea
1-(6,8-difluoro-2-methyl-4-quinolyl)-3-(4-dimethylaminophenyl)urea

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
quinolinesA class of aromatic heterocyclic compounds each of which contains a benzene ring ortho fused to carbons 2 and 3 of a pyridine ring.
organohalogen compoundA compound containing at least one carbon-halogen bond (where X is a halogen atom).
[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 (42)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency19.95260.003245.467312,589.2998AID2517
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency14.34840.004023.8416100.0000AID485290
Chain A, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.18380.177814.390939.8107AID2147
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
phosphopantetheinyl transferaseBacillus subtilisPotency31.62280.141337.9142100.0000AID1490
TDP1 proteinHomo sapiens (human)Potency11.88560.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency3.54810.180013.557439.8107AID1460
regulator of G-protein signaling 4Homo sapiens (human)Potency0.59730.531815.435837.6858AID504845
EWS/FLI fusion proteinHomo sapiens (human)Potency27.95830.001310.157742.8575AID1259255; AID1259256
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.62280.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency15.84890.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency6.30960.00636.904339.8107AID883
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency17.78280.354828.065989.1251AID504847
mitogen-activated protein kinase 1Homo sapiens (human)Potency15.84890.039816.784239.8107AID995
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency10.00000.00798.23321,122.0200AID2551
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency6.30960.031610.279239.8107AID884; AID885
lethal factor (plasmid)Bacillus anthracis str. A2012Potency15.84890.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency6.30960.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency23.73591.000010.475628.1838AID1457; AID901
GABA theta subunitRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
[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)
Orexin receptor type 1Homo sapiens (human)Ki0.02360.00030.28763.1623AID1582239; AID765089
Orexin receptor type 2Homo sapiens (human)Ki1.09970.00020.37713.7810AID1582240; AID765090
D(1A) dopamine receptorHomo sapiens (human)Ki1.78000.00010.836310.0000AID765085
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.32000.00030.769310.0000AID765084
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki1.40500.00030.26715.0700AID765090
[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)
Orexin receptor type 1Homo sapiens (human)Kd0.02690.00510.01600.0269AID347747
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (95)

Processvia Protein(s)Taxonomy
neuropeptide signaling pathwayOrexin receptor type 1Homo sapiens (human)
chemical synaptic transmissionOrexin receptor type 1Homo sapiens (human)
feeding behaviorOrexin receptor type 1Homo sapiens (human)
regulation of cytosolic calcium ion concentrationOrexin receptor type 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeOrexin receptor type 1Homo sapiens (human)
cellular response to hormone stimulusOrexin receptor type 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayOrexin receptor type 2Homo sapiens (human)
neuropeptide signaling pathwayOrexin receptor type 2Homo sapiens (human)
chemical synaptic transmissionOrexin receptor type 2Homo sapiens (human)
feeding behaviorOrexin receptor type 2Homo sapiens (human)
regulation of circadian sleep/wake cycle, wakefulnessOrexin receptor type 2Homo sapiens (human)
circadian sleep/wake cycle processOrexin receptor type 2Homo sapiens (human)
locomotionOrexin receptor type 2Homo sapiens (human)
regulation of cytosolic calcium ion concentrationOrexin receptor type 2Homo sapiens (human)
cellular response to hormone stimulusOrexin receptor type 2Homo sapiens (human)
temperature homeostasisD(1A) dopamine receptorHomo sapiens (human)
conditioned taste aversionD(1A) dopamine receptorHomo sapiens (human)
behavioral fear responseD(1A) dopamine receptorHomo sapiens (human)
regulation of protein phosphorylationD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1A) dopamine receptorHomo sapiens (human)
response to amphetamineD(1A) dopamine receptorHomo sapiens (human)
protein import into nucleusD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
synapse assemblyD(1A) dopamine receptorHomo sapiens (human)
memoryD(1A) dopamine receptorHomo sapiens (human)
mating behaviorD(1A) dopamine receptorHomo sapiens (human)
grooming behaviorD(1A) dopamine receptorHomo sapiens (human)
adult walking behaviorD(1A) dopamine receptorHomo sapiens (human)
visual learningD(1A) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(1A) dopamine receptorHomo sapiens (human)
astrocyte developmentD(1A) dopamine receptorHomo sapiens (human)
dopamine transportD(1A) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1A) dopamine receptorHomo sapiens (human)
neuronal action potentialD(1A) dopamine receptorHomo sapiens (human)
dentate gyrus developmentD(1A) dopamine receptorHomo sapiens (human)
striatum developmentD(1A) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of cell migrationD(1A) dopamine receptorHomo sapiens (human)
peristalsisD(1A) dopamine receptorHomo sapiens (human)
operant conditioningD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
vasodilationD(1A) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
maternal behaviorD(1A) dopamine receptorHomo sapiens (human)
positive regulation of potassium ion transportD(1A) dopamine receptorHomo sapiens (human)
glucose importD(1A) dopamine receptorHomo sapiens (human)
habituationD(1A) dopamine receptorHomo sapiens (human)
sensitizationD(1A) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(1A) dopamine receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(1A) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic potentiationD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1A) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1A) dopamine receptorHomo sapiens (human)
modification of postsynaptic structureD(1A) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of neuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityOrexin receptor type 1Homo sapiens (human)
protein bindingOrexin receptor type 1Homo sapiens (human)
orexin receptor activityOrexin receptor type 1Homo sapiens (human)
peptide hormone bindingOrexin receptor type 1Homo sapiens (human)
peptide bindingOrexin receptor type 1Homo sapiens (human)
protein bindingOrexin receptor type 2Homo sapiens (human)
neuropeptide receptor activityOrexin receptor type 2Homo sapiens (human)
orexin receptor activityOrexin receptor type 2Homo sapiens (human)
peptide hormone bindingOrexin receptor type 2Homo sapiens (human)
peptide bindingOrexin receptor type 2Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via GsD(1A) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1A) dopamine receptorHomo sapiens (human)
protein bindingD(1A) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine bindingD(1A) dopamine receptorHomo sapiens (human)
arrestin family protein bindingD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1A) dopamine receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
plasma membraneOrexin receptor type 1Homo sapiens (human)
synapseOrexin receptor type 1Homo sapiens (human)
plasma membraneOrexin receptor type 1Homo sapiens (human)
plasma membraneOrexin receptor type 2Homo sapiens (human)
synapseOrexin receptor type 2Homo sapiens (human)
plasma membraneOrexin receptor type 2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
nucleusD(1A) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
ciliumD(1A) dopamine receptorHomo sapiens (human)
presynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
dendritic spineD(1A) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
ciliary membraneD(1A) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1A) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(1A) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (42)

Assay IDTitleYearJournalArticle
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID765089Binding affinity to orexin receptor 1 (unknown origin)2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective orexin receptor antagonists.
AID765084Binding affinity to 5HT2B receptor (unknown origin)2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective orexin receptor antagonists.
AID765085Binding affinity to dopamine D1 receptor (unknown origin)2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective orexin receptor antagonists.
AID1582240Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX2 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liqu2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
AID1582239Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX1 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liqu2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
AID765090Binding affinity to orexin receptor 2 (unknown origin)2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective orexin receptor antagonists.
AID347748Selectivity for OX1 receptor over OX2 receptor2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.
AID347747Binding affinity to OX1 receptor2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.
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.
AID1346381Human OX1 receptor (Orexin receptors)2004British journal of pharmacology, Jan, Volume: 141, Issue:2
Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
AID1346381Human OX1 receptor (Orexin receptors)2009Molecular pharmacology, Sep, Volume: 76, Issue:3
Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.
AID1346418Human OX2 receptor (Orexin receptors)2009Molecular pharmacology, Sep, Volume: 76, Issue:3
Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.
AID1346418Human OX2 receptor (Orexin receptors)2004British journal of pharmacology, Jan, Volume: 141, Issue:2
Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (12.90)29.6817
2010's20 (64.52)24.3611
2020's7 (22.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.78

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index16.78 (24.57)
Research Supply Index3.47 (2.92)
Research Growth Index5.06 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.78)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (6.45%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other29 (93.55%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]