Page last updated: 2024-11-12

trans-delta-tocotrienoloic acid

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

Description

tocotrienoloic acid: from leaves of Tovomitopsis psychotriifolia; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10455173
CHEMBL ID4463788
CHEBI ID190931
MeSH IDM0249385

Synonyms (13)

Synonym
(2e,6e,10e)-13-[(2r)-6-hydroxy-2,8-dimethyl-3,4-dihydrochromen-2-yl]-2,6,10-trimethyltrideca-2,6,10-trienoic acid
CHEBI:190931
trans-delta-tocotrienoloic acid
CHEMBL4463788 ,
garcinoic acid, >=90% (lc/ms-elsd)
NCGC00385362-01
garcinoicacid
gtpl10734
tocotrienoloic acid
bdbm50527521
CS-0179237
HY-N9454
AKOS040734096

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 (1)

ClassDescription
tocotrienolA tocol in which the hydrocarbon chain at position 2 contains three double bonds.
[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 (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC50 (µMol)0.20300.00011.68479.3200AID1703351; AID1703353; AID1777220; AID1777222
[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)
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC50 (µMol)1.30000.00203.519610.0000AID1605742
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)Kd0.33000.33000.33000.3300AID1605747
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (43)

Processvia Protein(s)Taxonomy
negative regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
signal transductionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
steroid metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of gene expressionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic catabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic transportNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
cell differentiationNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
negative regulation of endothelial cell proliferationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte chemotaxis involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte migration involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
humoral immune responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of bone mineralizationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
dendritic cell migrationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
glucose homeostasisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
long-chain fatty acid biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of fat cell differentiationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of insulin secretionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of vascular wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory response to woundingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cytokine production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cellular response to oxidative stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene A4 biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of sprouting angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of leukocyte adhesion to arterial endothelial cellPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxin biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
RNA polymerase II transcription regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
protein bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
arachidonate 5-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 12(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
iron ion bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
protein bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
hydrolase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
nucleoplasmNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
transcription regulator complexNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear bodyNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intermediate filament cytoskeletonNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
chromatinNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nucleusNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
extracellular regionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
extracellular spacePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelope lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nucleoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
cytosolPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear matrixPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear membranePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
secretory granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
perinuclear region of cytoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
ficolin-1-rich granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (118)

Assay IDTitleYearJournalArticle
AID1347387Cytotoxicity qHTS for assessment of Hepg2 cells membrane integrity screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347401Redox Reaction Profiling qHTS: Assay Interference Panel against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347379qHTS for Inflammasome Signaling Inhibitors: IL-1-beta AlphaLISA screen against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347345OV-KATE Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID134737610-beta competent E. coli microbial cell viability qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347373qHTS for Constitutive Androstane Receptor (CAR) Agonist screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347347UWB1.289 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347368G06 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347375qHTS for Hypoxia signaling pathway (HIF-1) agonists against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347356HPAF-II 24hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347358HPAF-II 12hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347372qHTS for Constitutive Androstane Receptor (CAR) Antagonist screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347396qHTS for inhibitors of Wild type Zika virus screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347402qHTS for inhibitors of Rabies Virus screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347389qHTS assay for small molecule disruptors of mitochondrial membrane potential screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347361HEK293 12hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347349Panc-1005 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347362Diaphorse counterscreen qHTS: Assay Interference Panel against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347348OV-SAHO Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347352COV-362 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347394Vero-766 cells viability qHTS against the NCATS CANVASS Library: Counterscreen for Zika virus inhibition assay2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347400Viability qHTS for inhibitors of the SERCaMP assay screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347363Firefly luciferase counterscreen qHTS: Assay Interference Panel against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347374qHTS for Hypoxia signaling pathway (HIF-1) antagonists against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347390Secretion counterscreen for inhibitors of the SERCaMP assay screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
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.
AID1347365SDT Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347353A2780 Cisplatin Sensitive Ovarian Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347367qHTS for ATAD5 Agonist screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347381Inflammasome Signaling qHTS Counterscreen: IL-1-beta AlphaLISA counterscreen against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347371J3T Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347393qHTS for inhibitors of ER calcium dysfunction: SERCaMP assay screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347357HEK293 18hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347377DH5-alpha competent E. coli microbial cell viability qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347364KB-8-5-11 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347370qHTS for ATAD5 Antagonist screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347359HEK293 24hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347366KB-3-1 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347392qHTS for activators of dead-cell proteases activity screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347354UWB1.289-WTBRCA1 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347346HPAF-II Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347378qHTS for H2AX Agonists against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347388qHTS for Activators of p53 Stress Response Pathway screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347355HEK-293 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347350SW1088 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347391qHTS for activators of Nrf2/ARE signaling pathway screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347351U-118MG Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347369MCF7 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347360HPAF-II 18hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347380qHTS for Antimalaria activity screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1605773Toxicity in C57BL/6 mouse assessed as induction of organ damage at <=25 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605778Induction of PXR-dependent CYP3A11 protein expression in C57BL/6 mouse intestine at 5 to 25 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605765Agonist activity at PXR in human HT29 cells assessed as increase in CYP3A4 protein expression at 1 to 25 uM incubated for 24 hrs by immunoblot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605750Agonist activity at PXR in human HepG2 cells assessed as increase in CYP3A4 protein expression at 1 to 25 uM incubated for 24 hrs by immunoblot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605759Agonist activity at PXR in human HepaRG cells assessed as reversion of PXR antagonist sulforaphane-induced suppression of PXR expression at 10 uM incubated for 24 hrs by immunoblot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605743Agonist activity at His-tagged PXR-LBD/SRC-1p (unknown origin) expressed in Escherichia coli BL21(DE3) by coactivator recruitment based Alpha-screen assay relative to T09013172020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1777222Inhibition of 5-LOX in human PMNL assessed as reduction in 5-LOX product formation preincubated for 10 mins before addition of AA and A23187 and measured after 10 mins by RP-HPLC method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation.
AID1703353Inhibition of 5-LO in human PMNL cells assessed as reduction in LTB4, 5-H(P)ETE, 12-HETE and 15-HETE products formation using arachidonic acid as substrate preincubated for 10 mins followed by addition of substrate and measured after 10 mins by RP-HPLC me2020European journal of medicinal chemistry, Sep-15, Volume: 202Structure-based design, semi-synthesis and anti-inflammatory activity of tocotrienolic amides as 5-lipoxygenase inhibitors.
AID1605758Agonist activity at PXR in human HepaRG cells assessed as reversion of PXR binding at 10 uM incubated for 24 hrs by immunoblot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605763Agonist activity at PXR in human HepG2 cells assessed as stimulation of CYP450-mediated alpha-tocopherol metabolites efflux at 25 uM2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605769Toxicity in C57BL/6 mouse assessed as mortality at 50 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605762Agonist activity at PXR in human HepG2 cells assessed as stimulation of CYP450-mediated alpha-tocopherol metabolites production at 25 uM2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1696173Antibacterial activity against Streptococcus sobrinus 6715 assessed as reduction in bacterial growth incubated for 24 hrs by INT dye based broth dilution method2020Journal of natural products, 07-24, Volume: 83, Issue:7
Garcinoic Acids and a Benzophenone Derivative from the Seeds of
AID1605772Toxicity in C57BL/6 mouse assessed as induction of liver damage at <=25 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605767Agonist activity at PXR in human HT29-MTX cells assessed as increase in CYP3A4 protein expression at 1 to 25 uM incubated for 24 hrs by immunoblot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605760Agonist activity at PXR in human HepaRG cells assessed as reversion of PXR antagonist sulforaphane-induced suppression of CYP3A4 expression at 10 uM incubated for 24 hrs by immunoblot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605776Induction of PXR mRNA expression in C57BL/6 mouse intestine at 5 to 25 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605741Agonist activity at His-tagged PXR-LBD/SRC-1p (unknown origin) expressed in Escherichia coli BL21(DE3) at 10 uM by coactivator recruitment based Alpha-screen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605768Toxicity in C57BL/6 mouse assessed as mortality at 100 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605753Agonist activity at PXR in human HepG2 cells assessed as increase recombinant human Pgp in a cell membrane fraction by Pgp-Glo assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605752Agonist activity at PXR in human HepG2 cells assessed as increase in MDR1 mRNA expression at 1 to 50 uM incubated for 24 hrs2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605749Agonist activity at PXR in human HepG2 cells assessed as increase in PXR protein expression at 1 to 25 uM incubated for 24 hrs by immunoblot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605751Agonist activity at PXR in human HepG2 cells assessed as increase in CYP3A4 mRNA expression at 1 to 50 uM incubated for 24 hrs2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605770Toxicity in C57BL/6 mouse assessed as effect on gross appearance at <=25 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605785Induction of PXR protein expression in C57BL/6 mouse intestine assessed as induction of localization of PXR protein at brush border of enterocytes at 10 mg dosed as oral gavage as single bolus and measured after 24 hrs by IHC analysis relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605754Agonist activity at PXR in human HepaRG cells assessed as increase in PXR protein expression at 1 to 25 uM incubated for 24 hrs by immunoblot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1703351Inhibition of recombinant human 5-LO expressed in Escherichia coli BL21(DE3) assessed as reduction in LTB4 and 5-H(P)ETE formation using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 12020European journal of medicinal chemistry, Sep-15, Volume: 202Structure-based design, semi-synthesis and anti-inflammatory activity of tocotrienolic amides as 5-lipoxygenase inhibitors.
AID1605774Induction of PXR protein expression in C57BL/6 mouse liver at 5 to 25 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605781Induction of PXR protein expression in C57BL/6 mouse hepatic parenchyma assessed as induction of localization of PXR protein at hepatocytes around centro-lobular veins at 25 mg dosed as oral gavage as single bolus and measured after 24 hrs by IHC analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1777221Inhibition of recombinant human 5-LOX expressed in Escherichia coli BL21 (DE3) cells assessed as residual activity at 1 uM preincubated for 10 mins followed by arachidonic acid addition and measured after 10 mins by RP-HPLC method relative to control2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation.
AID1605744Agonist activity at LXR-beta (unknown origin) at 10 uM by coactivator recruitment based Alpha-screen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605777Induction of PXR protein expression in C57BL/6 mouse intestine at 5 to 25 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605764Agonist activity at PXR in human HT29 cells assessed as increase in PXR protein expression at 1 to 25 uM incubated for 24 hrs by immunoblot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605780Induction of PXR protein expression in C57BL/6 mouse hepatic parenchyma assessed as induction of localization of PXR protein at sinusoidal endothelial cells at 5 to 25 mg dosed as oral gavage as single bolus and measured after 24 hrs by IHC analysis relat2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1696172Bactericidal activity against Porphyromonas gingivalis ATCC 33277 assessed as reduction in bacterial growth incubated for 48 hrs by INT dye based broth dilution method2020Journal of natural products, 07-24, Volume: 83, Issue:7
Garcinoic Acids and a Benzophenone Derivative from the Seeds of
AID1696171Antibacterial activity against Porphyromonas gingivalis ATCC 33277 assessed as reduction in bacterial growth incubated for 24 hrs by INT dye based broth dilution method2020Journal of natural products, 07-24, Volume: 83, Issue:7
Garcinoic Acids and a Benzophenone Derivative from the Seeds of
AID1605745Agonist activity at PXR in human HepG2 cells transfected with PXR siRNA at 10 to 50 uM incubated for 24 hrs2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605779Induction of PXR-dependent CYP3A11 protein expression in C57BL/6 mouse liver at 5 to 25 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605782Induction of PXR protein expression in C57BL/6 mouse hepatic parenchyma assessed as induction of localization of PXR protein at hepatocytes around lobular midzonal area at 25 mg dosed as oral gavage as single bolus and measured after 24 hrs by IHC analysi2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605775Induction of PXR mRNA expression in C57BL/6 mouse liver at 5 to 25 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605747Binding affinity to His-tagged PXR-LBD (unknown origin) expressed in Escherichia coli BL21 Gold by ITC analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1777223Inhibition of 5-LOX in human PMNL assessed as residual activity by measuring reduction in 5-LOX product formation at 3 uM preincubated for 10 mins before addition of AA and A23187 and measured after 10 mins by RP-HPLC method relative to control2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation.
AID1777220Inhibition of recombinant human 5-LOX expressed in Escherichia coli BL21 (DE3) cells preincubated for 10 mins followed by arachidonic acid addition and measured after 10 mins by RP-HPLC method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation.
AID1605761Effect on alpha-tocopherol level in human HepG2 cells at 25 uM2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605742Agonist activity at His-tagged PXR-LBD/SRC-1p (unknown origin) expressed in Escherichia coli BL21(DE3) by coactivator recruitment based Alpha-screen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605746Agonist activity at PXR in human HepG2 cells transfected with PXR siRNA assessed as induction of CYP3A4 expression at 10 to 50 uM incubated for 24 hrs2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605784Induction of PXR protein expression in C57BL/6 mouse intestine assessed as induction of localization of PXR protein at glandular epithelium of crypts at base of mucosa epithelium at 5 to 25 mg dosed as oral gavage as single bolus and measured after 24 hrs2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605766Agonist activity at PXR in human HT29-MTX cells assessed as increase in PXR protein expression at 1 to 25 uM incubated for 24 hrs by immunoblot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605771Toxicity in C57BL/6 mouse assessed as effect on animal behavior at <=25 mg dosed as oral gavage as single bolus and measured after 24 hrs relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1696174Bactericidal activity against Streptococcus sobrinus 6715 assessed as reduction in bacterial growth incubated for 48 hrs by INT dye based broth dilution method2020Journal of natural products, 07-24, Volume: 83, Issue:7
Garcinoic Acids and a Benzophenone Derivative from the Seeds of
AID1605755Agonist activity at PXR in human HepaRG cells assessed as increase in CYP3A4 protein expression at 1 to 25 uM incubated for 24 hrs by immunoblot analysis2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1605783Induction of PXR protein expression in C57BL/6 mouse intestine assessed as induction of localization of PXR protein at villous epithelium at 5 to 25 mg dosed as oral gavage as single bolus and measured after 24 hrs by IHC analysis relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1347164384 well plate NINDS Rhodamine confirmatory 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.
AID1347152Confirmatory screen NINDS 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.
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.
AID1347167Vero cells viability 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.
AID1347158ZIKV-mCherry secondary 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.
AID1347169Tertiary RLuc qRT-PCR qHTS assay 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.
AID1347157Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS2020Proceedings 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.
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.
AID1347161Confirmatory 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.
AID1347149Furin counterscreen 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.
AID1347163384 well plate NINDS AMC confirmatory 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.
AID1347156DAPI mCherry counterscreen 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.
AID1347168HepG2 cells viability 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.
AID1347153Confirmatory 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (16.67)18.2507
2000's1 (8.33)29.6817
2010's2 (16.67)24.3611
2020's7 (58.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]