Compounds > khellinone
Page last updated: 2024-12-06

khellinone

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

Description

Khellinone is a naturally occurring coumarin derivative found in the fruit of Ammi visnaga, an herb native to the Mediterranean region. It exhibits a variety of pharmacological activities, including antispasmodic, bronchodilator, and anti-inflammatory effects. Khellinone is particularly known for its ability to relax smooth muscle, making it a potential therapeutic agent for conditions such as asthma and angina. Its mechanism of action involves inhibiting the activity of phosphodiesterase enzymes, which regulate the levels of cyclic adenosine monophosphate (cAMP) in cells. Increased cAMP levels lead to smooth muscle relaxation. Khellinone has been studied for its potential to treat other conditions, including cancer and Alzheimer's disease, but further research is needed to confirm its efficacy and safety.'

khellinone: a Kv1.3 potassium channel blocker [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68086
CHEMBL ID78293
SCHEMBL ID3189671
MeSH IDM0496749

Synonyms (37)

Synonym
CHEMBL78293 ,
EU-0040671
MAYBRIDGE1_002164
SR-01000455056-2
bdbm50145066
1-(6-hydroxy-4,7-dimethoxy-benzofuran-5-yl)-ethanone
1-(6-hydroxy-4,7-dimethoxybenzofuran-5-yl)ethanone
HMS547K08
1-(6-hydroxy-4,7-dimethoxy-1-benzofuran-5-yl)ethanone
484-51-5
AKOS001631881
6-hydroxy-4,7-dimethoxybenzofuran-5-yl methyl ketone
unii-vj1360ywr9
vj1360ywr9 ,
khellinone
einecs 207-607-1
CCG-46379
FT-0619935
STL377843
5-acetyl-6-hydroxy-4,7-dimethoxybenzofuran
4,7-dimethoxy-5-acetyl-6-hydroxybenzofuran
6-hydroxy-4,7-dimethoxy-5-benzofuranyl methyl ketone
SCHEMBL3189671
BBL028032
5-acetyl-4,7-dimethoxy-6-benzofuranol
ethanone, 1-(6-hydroxy-4,7-dimethoxy-5-benzofuranyl)-
DTXSID70197512
SR-01000455056-1
sr-01000455056
5-acetyl-6-hydroxybenzofuran-4.7-dione
3-bromobutyricacid
1-(6-hydroxy-4,7-dimethoxy-1-benzofuran-5-yl)ethan-1-one
VS-08650
5-acetyl-6-hydroxy-4,7-dimethoxybenzo[b]furan
BRD-K35673046-001-01-2
1-(6-hydroxy-4,7-dimethoxybenzofuran-5-yl)ethan-1-one
CS-0317734
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (6)

Processvia Protein(s)Taxonomy
potassium ion transportPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
optic nerve developmentPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
corpus callosum developmentPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
protein homooligomerizationPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
action potentialPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
voltage-gated monoatomic ion channel activityPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
outward rectifier potassium channel activityPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
plasma membranePotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
presynaptic membranePotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
calyx of HeldPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
membrane raftPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
postsynaptic membranePotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
glutamatergic synapsePotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
axonPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
membranePotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID261016Effect on blockade of mouse Kv1.3 channel expressed in L929 cells2006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
A new class of blockers of the voltage-gated potassium channel Kv1.3 via modification of the 4- or 7-position of khellinone.
AID217629Dissociation constant for the blockage of voltage-gated potassium channel subunit Kv1.3 in human lymphocytes2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Khellinone derivatives as blockers of the voltage-gated potassium channel Kv1.3: synthesis and immunosuppressive activity.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (44.44)29.6817
2010's3 (33.33)24.3611
2020's2 (22.22)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.16

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 Index12.16 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.16)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
4-aminopyridine
[no description available]		2.0210aminopyridine;
aromatic amine		avicide;
orphan drug;
potassium channel blocker
benzofurans
Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.		3.1750
ConditionIndicatedRelationship StrengthStudiesTrials
Plasmodium falciparum Malaria
[description not available]		02.110
Malaria, Falciparum
Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.		02.110
Anemia, Fanconi
[description not available]		02.1310
Fanconi Anemia
Congenital disorder affecting all bone marrow elements, resulting in ANEMIA; LEUKOPENIA; and THROMBOPENIA, and associated with cardiac, renal, and limb malformations as well as dermal pigmentary changes. Spontaneous CHROMOSOME BREAKAGE is a feature of this disease along with predisposition to LEUKEMIA. There are at least 7 complementation groups in Fanconi anemia: FANCA, FANCB, FANCC, FANCD1, FANCD2, FANCE, FANCF, FANCG, and FANCL. (from Online Mendelian Inheritance in Man, http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227650, August 20, 2004)		02.1310