Page last updated: 2024-12-10

kavain

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Description

kavain: RN given refers to cpd without isomeric designation; see also kavaform; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID45934481
CHEBI ID174183
MeSH IDM0058522
PubMed CID5281565
CHEMBL ID578607
CHEBI ID6117
CHEBI ID92164
SCHEMBL ID515202
MeSH IDM0058522
PubMed CID5369129
CHEMBL ID1482039
CHEBI ID156288
CHEBI ID91863
SCHEMBL ID515203
MeSH IDM0058522

Synonyms (151)

Synonym
4-methoxy-2-[(z)-2-phenylethenyl]-2,3-dihydropyran-6-one
CHEBI:174183
(r)-kawain
kavain
2h-pyran-2-one, 5,6-dihydro-4-methoxy-6-styryl-, (r)- (van)
5,6-dihydro-4-methoxy-6-styryl-(+)-2h-pyran-2-one
unii-w1es06373m
w1es06373m ,
MLS002154236
smr001233508
BRD-K09497549-001-03-6
kavaine
(r)-5,6-dihydro-4-methoxy-6-styryl-2h-pyran-2-one
einecs 207-907-2
d-kawain
(r-(e))-5,6-dihydro-4-methoxy-6-styryl-2h-pyran-2-one
2h-pyran-2-one, 5,6-dihydro-4-methoxy-6-styryl-, (+)-
2h-pyran-2-one, 5,6-dihydro-4-methoxy-6-styryl-, (r)-
2h-pyran-2-one, 5,6-dihydro-4-methoxy-6-(2-phenylethenyl)-, (r-(e))-
nsc 112162
5-hydroxy-3-methoxy-7-phenyl-2,6-heptadienoic acid gamma-lactone
4-methoxy-6-(beta-phenylvinyl)-5,6-dihydro-alpha-pyrone
cas-500-64-1
PRESTWICK3_000207
BSPBIO_000193
PRESTWICK2_000207
BPBIO1_000213
nsc112162
2h-pyran-2-one,6-dihydro-4-methoxy-6-styryl-, (+)-
2h-pyran-2-one,6-dihydro-4-methoxy-6-styryl-, (r)-
2h-pyran-2-one,6-dihydro-4-methoxy-6-(2-phenylethenyl)-, [r-(e)]-
gonosan
(+)-kavain
kawain
nsc-112162
kavain, dl-
NCGC00091905-01
AB00513818
C09947
(6r)-4-methoxy-6-[(e)-2-phenylvinyl]-5,6-dihydro-2h-pyran-2-one
NCGC00091905-02
D08096
kavaform (tn)
CHEMBL578607
chebi:6117 ,
kawaih
HMS1568J15
NCGC00091905-03
HMS2095J15
tox21_200907
dtxcid3013595
NCGC00258461-01
dtxsid5033595 ,
HMS2230N15
S9409
kawain [mi]
kawain [usp-rs]
2h-pyran-2-one, 5,6-dihydro-4-methoxy-6-((1e)-2-phenylethenyl)-, (6r)-
kawain [who-dd]
(+)-kawain
SCHEMBL515202
l-kawain
XEAQIWGXBXCYFX-GUOLPTJISA-N
2h-pyran-2-one, 5,6-dihydro-4-methoxy-6-(2-phenylethenyl)-, [r-(e)]-
AC-35093
Q-100559
(2r)-4-methoxy-2-[(e)-styryl]-2,3-dihydropyran-6-one
CHEBI:92164
NCGC00091905-05
AKOS030631732
Q3194310
HY-B1671
CS-0013634
(r,e)-4-methoxy-6-styryl-5,6-dihydro-2h-pyran-2-one
HMS3887G03
CCG-266792
MS-23309
kawain (usp-rs)
MLS001148390
BRD-A75455249-001-02-0
4-methoxy-6-styryl-5,6-dihydro-pyran-2-one
MLS000069449 ,
dl-kawain
2h-pyran-2-one, 5,6-dihydro-4-methoxy-6-styryl-
neuronica
2h-pyran-2-one, 5,6-dihydro-4-methoxy-6-(2-phenylethenyl)-
2,6-heptadienoic acid, 5-hydroxy-3-methoxy-7-phenyl-, delta-lactone
cavain
PRESTWICK_556
1635-33-2
BSPBIO_001184
IDI1_002187
500-64-1
3155-48-4
NCGC00089781-02
smr000059008
NCGC00089781-03
HMS1990L05
CHEBI:156288
d,l-kawain
(+-)-kavain
(+-)-kawain
dl-kavain
trans-5,6-dihydro-4-methoxy-6-(2-phenylethenyl)-2h-pyran-2-one
HMS1362L05
HMS1792L05
4-methoxy-2-[(e)-2-phenylethenyl]-2,3-dihydropyran-6-one
NCGC00018126-02
NCGC00018126-03
NCGC00018126-04
d,l-kawin
kawain, dl-
unii-5l1ni60tgb
ccris 9373
5l1ni60tgb ,
2h-pyran-2-one, 5,6-dihydro-4-methoxy-6-(2-phenylethenyl)-, (e)-(+-)-
kawain (+-)-form
HMS2232L23
(+/-)-kavain
CHEMBL1482039
AKOS015903213
2h-pyran-2-one, 5,6-dihydro-4-methoxy-6-((1e)-2-phenylethenyl)-
kawain (+/-)-form [mi]
kawain, (+/-)-
(+/-)-kawain
CCG-208228
SCHEMBL515203
XEAQIWGXBXCYFX-BQYQJAHWSA-N
HMS3403L05
OPERA_ID_1395
mfcd00270446
4-methoxy-6-styryl-5,6-dihydro-2h-pyran-2-one
CHEBI:91863
dl-kavain, analytical standard
dl-kavain, primary pharmaceutical reference standard
sr-01000003014
SR-01000003014-4
J-018461
(e)-4-methoxy-6-styryl-5,6-dihydro-2h-pyran-2-one
4-methoxy-6-[(e)-2-phenylethenyl]-5,6-dihydropyran-2-one
HY-N2096
CS-0018617
kavain (+/-)
DTXSID00904756
rac-kavain
BRD-A75455249-001-12-9
2h-pyran-2-one, 5,6-dihydro-4-methoxy-6-[(1e)-2-phenylethenyl]-
Q27262508
AS-75955
4-methoxy-6-[(1e)-2-phenylethenyl]-5,6-dihydro-2h-pyran-2-one
trans-5,6-dihydro-4-methoxy-6-(2-phenylethenyl)-2h-pyran-2-one, dl-kawain

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"To examine the bioavailability of kavalactones in vitro and the possible differences in their bioavailability because of variations in either chemical structure or the method of extraction used."( Permeability studies of Kavalactones using a Caco-2 cell monolayer model.
Blanchfield, JT; Bone, KM; Lehmann, RP; Matthias, A; Penman, KG; Toth, I, 2007
)
0.34
"Caco-2 cell monolayers were used to determine the potential bioavailability of kavalactones."( Permeability studies of Kavalactones using a Caco-2 cell monolayer model.
Blanchfield, JT; Bone, KM; Lehmann, RP; Matthias, A; Penman, KG; Toth, I, 2007
)
0.34
" Not all differences in their bioavailability can be related to kavalactone structural differences as it appears that bioavailability may also be affected by co-extracted compounds."( Permeability studies of Kavalactones using a Caco-2 cell monolayer model.
Blanchfield, JT; Bone, KM; Lehmann, RP; Matthias, A; Penman, KG; Toth, I, 2007
)
0.34
"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

Dosage Studied

ExcerptRelevanceReference
" The lower dosages of (+/-)-kavain (50 and 100 mg/kg) showed only a nonsignificant attenuation of MPTP-induced dopamine depletion, but a high dosage of (+/-)-kavain (200 mg/kg) significantly antagonized the dopamine depletion to 58."( Neuroprotective effects of (+/-)-kavain in the MPTP mouse model of Parkinson's disease.
Ferger, B; Schmidt, N, 2001
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
glycine receptor antagonistAn antagonist that blocks glycine receptors.
[role 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]

Drug Classes (3)

ClassDescription
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
2-pyranonesA pyranone based on the structure of 2H-pyran-2-one and its substituted derivatives.
2-pyranonesA pyranone based on the structure of 2H-pyran-2-one and its substituted derivatives.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
racemateA racemate is an equimolar mixture of a pair of enantiomers.
[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 (27)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency0.35480.044717.8581100.0000AID485294
pregnane X receptorRattus norvegicus (Norway rat)Potency50.11870.025127.9203501.1870AID651751
RAR-related orphan receptor gammaMus musculus (house mouse)Potency27.69520.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency24.89300.173734.304761.8120AID1346859
ATAD5 protein, partialHomo sapiens (human)Potency18.47060.004110.890331.5287AID504466; AID504467
SMAD family member 3Homo sapiens (human)Potency24.89300.173734.304761.8120AID1346859
GLI family zinc finger 3Homo sapiens (human)Potency39.17650.000714.592883.7951AID1259368; AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency35.20380.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743042; AID743054
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency12.58930.011212.4002100.0000AID1030
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency3.78660.001022.650876.6163AID1224838; AID1224839; AID1224893
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency20.81610.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency2.23870.000817.505159.3239AID588544
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency16.11850.001530.607315,848.9004AID1224841; AID1224842; AID1259401
pregnane X nuclear receptorHomo sapiens (human)Potency24.68340.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency21.18200.000229.305416,493.5996AID743075; AID743079
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency31.62280.001024.504861.6448AID588534
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency7.80560.001723.839378.1014AID743083
histone deacetylase 9 isoform 3Homo sapiens (human)Potency28.48680.037617.082361.1927AID1259364; AID1259388
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency24.60100.000627.21521,122.0200AID651741; AID743219
gemininHomo sapiens (human)Potency1.12200.004611.374133.4983AID624297
Nuclear receptor ROR-gammaHomo sapiens (human)Potency33.49150.026622.448266.8242AID651802
TAR DNA-binding protein 43Homo sapiens (human)Potency4.46681.778316.208135.4813AID652104
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
ATAD5 protein, partialHomo sapiens (human)Potency23.10930.004110.890331.5287AID504467
Microtubule-associated protein tauHomo sapiens (human)Potency19.09190.180013.557439.8107AID1460
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency89.12510.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.38720.035520.977089.1251AID504332
survival motor neuron protein isoform dHomo sapiens (human)Potency3.16230.125912.234435.4813AID1458
TAR DNA-binding protein 43Homo sapiens (human)Potency10.00001.778316.208135.4813AID652104
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (31)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
xenobiotic metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of glucose metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of steroid metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor ROR-gammaHomo sapiens (human)
circadian regulation of gene expressionNuclear receptor ROR-gammaHomo sapiens (human)
cellular response to sterolNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of circadian rhythmNuclear receptor ROR-gammaHomo sapiens (human)
regulation of fat cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor ROR-gammaHomo sapiens (human)
adipose tissue developmentNuclear receptor ROR-gammaHomo sapiens (human)
T-helper 17 cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
protein bindingNuclear receptor ROR-gammaHomo sapiens (human)
oxysterol bindingNuclear receptor ROR-gammaHomo sapiens (human)
zinc ion bindingNuclear receptor ROR-gammaHomo sapiens (human)
ligand-activated transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
nuclear receptor activityNuclear receptor ROR-gammaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
nucleoplasmNuclear receptor ROR-gammaHomo sapiens (human)
nuclear bodyNuclear receptor ROR-gammaHomo sapiens (human)
chromatinNuclear receptor ROR-gammaHomo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (77)

Assay IDTitleYearJournalArticle
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
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.
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.
AID1347160Primary screen NINDS Rhodamine 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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
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.
AID1090312Antifungal activity against Fusarium solani assessed as growth inhibition at 10 ppm after 4 days relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090310Antifungal activity against Fusarium oxysporum assessed as growth inhibition at 10 ppm after 4 days relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090304Herbicidal activity against Lactuca sativa cv. Great Lakes 366 (lettuce) assessed as inhibition of shoot length at 1 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090311Antifungal activity against Fusarium solani assessed as growth inhibition at 50 ppm after 4 days relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID447711Inhibition of TNF-alpha-induced NF-kappaB expressed in human A549 cells treated 1 hr after TNFalpha challenge measured after 6 hrs by luciferase reporter gene assay2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Identification of methysticin as a potent and non-toxic NF-kappaB inhibitor from kava, potentially responsible for kava's chemopreventive activity.
AID1090300Herbicidal activity against Echinochloa crus-galli (barnyard grass) assessed as inhibition of germination at 1 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090299Herbicidal activity against Echinochloa crus-galli (barnyard grass) assessed as inhibition of germination at 10 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID481211Induction of HO-1 protein expression in rat PC12 cells at 10 uM after 24 hrs by Western blot analysis2010Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
A novel kavalactone derivative protects against H2O2-induced PC12 cell death via Nrf2/ARE activation.
AID1090316Herbicidal activity against Echinochloa crus-galli (barnyard grass) assessed as inhibition of root length at 1 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID447716Hepatotoxicity against mouse Hepa-1c1c7 cells after 48 hrs by celltiter blue assay2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Identification of methysticin as a potent and non-toxic NF-kappaB inhibitor from kava, potentially responsible for kava's chemopreventive activity.
AID1090313Antifungal activity against Colletotrichum gloeosporioides assessed as growth inhibition at 50 ppm after 4 days relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090317Herbicidal activity against Echinochloa crus-galli (barnyard grass) assessed as inhibition of shoot length at 10 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID666151Inhibition of PA endonuclease at 1 uM2011PloS one, , Volume: 6, Issue:5
Anti-influenza activity of marchantins, macrocyclic bisbibenzyls contained in liverworts.
AID1090314Antifungal activity against Colletotrichum gloeosporioides assessed as growth inhibition at 10 ppm after 4 days relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090298Herbicidal activity against Echinochloa crus-galli (barnyard grass) assessed as inhibition of shoot length at 1 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090302Herbicidal activity against Lactuca sativa cv. Great Lakes 366 (lettuce) assessed as inhibition of root length at 1 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090307Antifungal activity against Hypocrea rufa assessed as growth inhibition at 10 ppm after 4 days relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090315Herbicidal activity against Echinochloa crus-galli (barnyard grass) assessed as inhibition of root length at 10 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090306Herbicidal activity against Lactuca sativa cv. Great Lakes 366 (lettuce) assessed as inhibition of germination at 1 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090301Herbicidal activity against Lactuca sativa cv. Great Lakes 366 (lettuce) assessed as inhibition of root length at 10 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090305Herbicidal activity against Lactuca sativa cv. Great Lakes 366 (lettuce) assessed as inhibition of germination at 10 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1090309Antifungal activity against Fusarium oxysporum assessed as growth inhibition at 50 ppm after 4 days relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID666150Inhibition of PA endonuclease at 10 uM2011PloS one, , Volume: 6, Issue:5
Anti-influenza activity of marchantins, macrocyclic bisbibenzyls contained in liverworts.
AID1090303Herbicidal activity against Lactuca sativa cv. Great Lakes 366 (lettuce) assessed as inhibition of shoot length at 10 ppm relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID1396185Antiperiodontic activity in mouse bone marrow macrophages assessed as reduction in Porphyromonas gingivalis-induced TNFalpha levels at 100 ug/ml after 4 hrs by ELISA2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
Kava analogues as agents for treatment of periodontal diseases: Synthesis and initial biological evaluation.
AID1090308Antifungal activity against Hypocrea rufa assessed as growth inhibition at 50 ppm after 4 days relative to untreated control2006Journal of agricultural and food chemistry, Feb-08, Volume: 54, Issue:3
Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).
AID481210Activation of Nrf2 in rat PC12 cells at 10 uM after 24 hrs by antioxidant response element-driven luciferase reporter gene assay2010Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
A novel kavalactone derivative protects against H2O2-induced PC12 cell death via Nrf2/ARE activation.
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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
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.
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.
AID697853Inhibition of horse BChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID697852Inhibition of electric eel AChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (98)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (5.10)18.7374
1990's21 (21.43)18.2507
2000's31 (31.63)29.6817
2010's26 (26.53)24.3611
2020's15 (15.31)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 39.87

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

MetricThis Compound (vs All)
Research Demand Index39.87 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index4.48 (4.65)
Search Engine Demand Index56.46 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (39.87)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (4.82%)5.53%
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Reviews0 (0.00%)6.00%
Reviews0 (0.00%)6.00%
Case Studies1 (1.20%)4.05%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other78 (93.98%)84.16%
Other16 (100.00%)84.16%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]