Compounds > palinurin
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palinurin

Description

palinurin: an NSAID with antibacterial activity; isolated from Ircinia species; structure in firs t source [MeSH]

Cross-References

ID SourceID
PubMed CID54726684
CHEMBL ID464381
MeSH IDM0537966

Synonyms (2)

Synonym
CHEMBL464381
palinurin

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Cyclin-dependent kinase 1Homo sapiens (human)IC50100.0000AID722956
Casein kinase II subunit alpha'Homo sapiens (human)IC50100.0000AID722949
Glycogen synthase kinase-3 alphaHomo sapiens (human)IC501.6109AID722958
Glycogen synthase kinase-3 betaHomo sapiens (human)IC502.9960AID718830; AID722955; AID729991
Casein kinase II subunit betaHomo sapiens (human)IC50100.0000AID722949
Casein kinase II subunit alphaHomo sapiens (human)IC50100.0000AID722949
Cyclin-dependent-like kinase 5 Homo sapiens (human)IC5025.0594AID722957

Bioassays (25)

Assay IDTitleYearJournalArticle
AID722947Selectivity ratio of IC50 for human recombinant CDK1 to IC50 for human recombinant GSK3alpha2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722944Selectivity ratio of IC50 for human recombinant CDK5 to IC50 for human recombinant GSK3beta2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722954Inhibition of GSK-3beta in human SH-SY5Y cells assessed as reduction of tau phosphorylation at 15 to 200 uM after 18 hrs by ELISA sandwich method2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722955Inhibition of human recombinant GSK-3beta using GS2 peptide as substrate and [gamma33P]-ATP after 30 mins by scintillation counting2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722948Selectivity ratio of IC50 for human recombinant CDK5 to IC50 for human recombinant GSK3alpha2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722957Inhibition of human recombinant CDK5 using histone H1 as substrate and [gamma33P]-ATP after 20 mins by scintillation counting2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722951Non-competitive inhibition of human recombinant GSK-3beta using fixed concentration of [gamma33P]-ATP and GS2 peptide as substrate by double reciprocal plot analysis2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722952Non-competitive inhibition of human recombinant GSK-3beta using [gamma33P]-ATP and fixed concentration of GS2 peptide as substrate by double reciprocal plot analysis2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722958Inhibition of human recombinant GSK-3alpha using GS2 peptide as substrate and [gamma33P]-ATP after 12 mins by scintillation counting2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID729991Inhibition of GSK3beta (unknown origin)2013European journal of medicinal chemistry, Mar, Volume: 61ISSN: 1768-3254Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β).
AID722941Selectivity ratio of IC50 for human recombinant CK2 to IC50 for human recombinant GSK3beta2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID403324Cytotoxicity against human SK-MEL-2 cells2004Journal of natural products, Jul, Volume: 67, Issue:7
ISSN: 0163-3864		Cytotoxic furanosesterterpenes from a marine sponge Psammocinia sp.
AID722956Inhibition of human recombinant CDK1 using histone H1 as substrate and [gamma33P]-ATP after 15 mins by scintillation counting2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722942Selectivity ratio of IC50 for human recombinant MAPK to IC50 for human recombinant GSK3beta2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722949Inhibition of human recombinant CK2 using GS2 peptide as substrate and [gamma33P]-ATP after 30 mins by scintillation counting2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722943Selectivity ratio of IC50 for human recombinant CDK1 to IC50 for human recombinant GSK3beta2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722950Inhibition of human recombinant MAPK using myelin binding protein as substrate and [gamma33P]-ATP after 15 mins by scintillation counting2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID403323Cytotoxicity against human SKOV3 cells2004Journal of natural products, Jul, Volume: 67, Issue:7
ISSN: 0163-3864		Cytotoxic furanosesterterpenes from a marine sponge Psammocinia sp.
AID718830Non-ATP competitive inhibition of GSK3beta2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
ISSN: 1464-3405		Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening.
AID403322Cytotoxicity against human A549 cells2004Journal of natural products, Jul, Volume: 67, Issue:7
ISSN: 0163-3864		Cytotoxic furanosesterterpenes from a marine sponge Psammocinia sp.
AID722946Selectivity ratio of IC50 for human recombinant CK2 to IC50 for human recombinant GSK3alpha2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID403326Cytotoxicity against human HCT15 cells2004Journal of natural products, Jul, Volume: 67, Issue:7
ISSN: 0163-3864		Cytotoxic furanosesterterpenes from a marine sponge Psammocinia sp.
AID403325Cytotoxicity against human XF498 cells2004Journal of natural products, Jul, Volume: 67, Issue:7
ISSN: 0163-3864		Cytotoxic furanosesterterpenes from a marine sponge Psammocinia sp.
AID722953Cytotoxicity against human SH-SY5Y cells assessed as intracellular LDH level after 18 hrs2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.
AID722945Selectivity ratio of IC50 for human recombinant MAPK to IC50 for human recombinant GSK3alpha2013European journal of medicinal chemistry, Feb, Volume: 60ISSN: 1768-3254Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (33.33)29.6817
2010's4 (66.67)24.3611
2020's0 (0.00)2.80

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%
Other6 (100.00%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
pd 173074
2
aromatic amine;
biaryl;
dimethoxybenzene;
pyridopyrimidine;
tertiary amino compound;
ureas		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist		2012201311.5medium000020
dasatinib
2
1,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor		2012201311.5medium000020
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
2
benzenes;
thiadiazolidine		anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
neuroprotective agent		2012201311.5medium000020
su 11248
2
monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist		2012201311.5medium000020
manzamine a
1
alkaloid;
beta-carbolines;
isoquinolines		animal metabolite;
anti-HSV-1 agent;
antimalarial;
antineoplastic agent;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
marine metabolite		2012201212.0low000010
bibw 2992
2
aromatic ether;
enamide;
furans;
monochlorobenzenes;
organofluorine compound;
quinazolines;
secondary carboxamide;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor		2012201311.5medium000020
ascorbic acid
1
ascorbic acid;
vitamin C		coenzyme;
cofactor;
flour treatment agent;
food antioxidant;
food colour retention agent;
geroprotector;
plant metabolite;
skin lightening agent		2013201311.0low000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
4-butyrolactone
3
butan-4-olidemetabolite;
neurotoxin		2009201313.0medium000120
furan
1
furans;
mancude organic heteromonocyclic parent;
monocyclic heteroarene		carcinogenic agent;
hepatotoxic agent;
Maillard reaction product		2009200915.0low000100
phosphine
1
mononuclear parent hydride;
phosphanes;
phosphine		carcinogenic agent;
fumigant insecticide		2009200915.0low000100
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Acute Confusional Senile Dementia0
1
2011201113.0high000010
Alzheimer Disease0
1
2011201113.0high000010