Page last updated: 2024-11-04

damnacanthal

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

Description

Damnacanthal is a natural product isolated from the roots of the plant *Damnacanthus indicus* It has shown potent anti-inflammatory activity in various studies, along with other potential benefits like anti-cancer and anti-microbial properties. The compound is known to inhibit the production of pro-inflammatory cytokines and chemokines, which play a significant role in inflammatory processes. Research on damnacanthal's synthesis focuses on developing efficient methods to produce this valuable compound, potentially for medicinal applications. The complexity of the compound's structure poses challenges for synthetic chemists, and several research groups have been investigating different synthetic routes.'

damnacanthal: structure given in first source; isolated from the stem bark and roots of Morinda lucida; a selective inhibitor of p56(lck) tyrosine kinase activity [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
MorindagenusA plant genus of the family RUBIACEAE. Members contain iridoid glycosides and ANTHRAQUINONES.[MeSH]RubiaceaeThe Madder plant family of the order Gentianales (formerly Rubiales), subclass Asteridae, class Magnoliopsida includes important medicinal plants that provide QUININE; IPECAC; and COFFEE. They have opposite leaves and interpetiolar stipules.[MeSH]

Cross-References

ID SourceID
PubMed CID2948
CHEMBL ID212948
CHEBI ID93633
SCHEMBL ID147246
MeSH IDM0211997

Synonyms (60)

Synonym
CBIOL_001879
3-hydroxy-1-methoxyanthraquinone-2-aldehyde
K00034
BRD-K93325701-001-03-0
3-hydroxy-1-methoxy-9,10-dioxo-anthracene-2-carbaldehyde
damnacanthal
3-hydroxy-1-methoxy-9,10-dioxo-9,10-dihydro-anthracene-2-carbaldehyde
477-84-9
IDI1_002078
BIO2_000803
BIO1_000654
BIO1_000165
BIO1_001143
BIO2_000323
BSPBIO_000985
BCBCMAP01_000230
BIOMOLKI_000022
QTL1_000028
BIOMOLKI2_000030
NCGC00163375-01
NCGC00163375-02
ccris 6443
2-anthraquinonecarboxaldehyde, 3-hydroxy-1-methoxy-
damnacantal
KBIO3_000650
KBIO2_002893
KBIO2_000325
KBIOGR_000325
KBIOSS_000325
KBIO3_000649
KBIO2_005461
NCGC00163375-03
HMS1990A07
CHEMBL212948
BMK1-C10
HMS1362A07
HMS1792A07
3-hydroxy-1-methoxy-9,10-dioxo-9,10-dihydroanthracene-2-carbaldehyde
FT-0665458
3-hydroxy-1-methoxy-9,10-dioxoanthracene-2-carbaldehyde
CCG-100626
bdbm50366492
unii-wuc3cb63cd
wuc3cb63cd ,
9,10-dihydro-3-hydroxy-1-methoxy-9,10-dioxo-2-anthracenecarboxaldehyde
SCHEMBL147246
9,10-dihydroxy-3-hydroxy-1-methoxy-9,10-dioxo-2-anthracenecarboxaldehyde
AKOS024456868
HMS3403A07
DTXSID10197253
CHEBI:93633
Q5212724
damnacanthal - cas 477-84-9
HY-108485
CS-0028962
1-methoxy-2-formyl-3-hydroxy-9,10-anthraquinone
A937064
MS-24004
2-anthraldehyde, 9,10-dihydro-3-hydroxy-1-methoxy-9,10-dioxo-
3-hydroxy-1-methoxy-9,10-dioxo-9,10-dihydro-2-anthracenecarbaldehyde

Research Excerpts

Overview

Damnacanthal is an anthraquinone derivative with anti-cancer pharmacological properties. It is a major constituent of Morinda citrifolia L. It has a potent inhibitory activity towards tyrosine kinases.

ExcerptReferenceRelevance
"Damnacanthal is an anthraquinone derivative with anti-cancer pharmacological properties."( Damnacanthal isolated from morinda species inhibited ovarian cancer cell proliferation and migration through activating autophagy.
Han, B; Jiang, W; Lan, J; Li, H; Li, R; Lin, X; Liu, F; Su, B; Xu, H; Yang, D; Yang, M, 2022
)
2.89
"Damnacanthal is a major constituent of Morinda citrifolia L. "( Damnacanthal inhibits the NF-κB/RIP-2/caspase-1 signal pathway by inhibiting p56lck tyrosine kinase.
Jeong, HJ; Kim, MH, 2014
)
3.29
"Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia L. "( Damnacanthal and its nanoformulation exhibit anti-cancer activity via cyclin D1 down-regulation.
Baek, SJ; Gritsanapan, W; Rojanapanthu, P; Silva, G; Sukamporn, P; Zhang, X, 2016
)
3.32
"Damnacanthal is an anthraquinone compound isolated from the root of Morinda citrifolia and was reported to have a potent inhibitory activity towards tyrosine kinases such as Lck, Src, Lyn and EGF receptor. "( Stimulation of ultraviolet-induced apoptosis of human fibroblast UVr-1 cells by tyrosine kinase inhibitors.
Arase, Y; Chen, Z; Hiwasa, T; Ito, H; Kita, K; Suzuki, N; Umezawa, K, 1999
)
1.75
"Damnacanthal is a potent and selective inhibitor of p56(lck) tyrosine kinase in a variety of tissues. "( Mechanism of damnacanthal-induced [Ca(2+)](i) elevation in human dermal fibroblasts.
Aoki, K; Parent, A; Zhang, J, 2000
)
2.12

Effects

ExcerptReferenceRelevance
"Damnacanthal has low water solubility and low bioavailability."( Development of biodegradable sustained-release damnacanthal nanocapsules for potential application in in-vitro breast cancer studies.
Abdul Latif, AZ; Ariff, TM; Mohamad, N; Mohamed, A; Mohd, MR; Suffian, IFM; Wan Nik, WMN, 2019
)
1.49

Actions

ExcerptReferenceRelevance
"Damnacanthal was shown to inhibit the oncogene Ras, p56lck tyrosine kinase, NF-KB pathway and induce apoptosis in vitro."( Damnacanthal: a promising compound as a medicinal anthraquinone.
Abu, N; Ali, NM; Alitheen, NB; Aziz, MY; Ho, WY; Yeap, SK, 2014
)
2.57

Dosage Studied

ExcerptRelevanceReference
" Various formulations of damnacanthal would be developed to enable the selection of a dosage form that could offer the provision of the anti-cancer bioactive substance with suitable sustained- or controlled release properties."( Development of biodegradable sustained-release damnacanthal nanocapsules for potential application in in-vitro breast cancer studies.
Abdul Latif, AZ; Ariff, TM; Mohamad, N; Mohamed, A; Mohd, MR; Suffian, IFM; Wan Nik, WMN, 2019
)
1.07
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
monohydroxyanthraquinoneAn anthraquinone in which the anthraquinone moiety is substituted by a single hydroxy group.
aldehydeA compound RC(=O)H, in which a carbonyl group is bonded to one hydrogen atom and to one R group.
[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 (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency30.30015.623417.292931.6228AID485281
phosphopantetheinyl transferaseBacillus subtilisPotency70.79460.141337.9142100.0000AID1490
TDP1 proteinHomo sapiens (human)Potency41.71260.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency16.85570.180013.557439.8107AID1460; AID1468
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency7.38410.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency18.12770.531815.435837.6858AID504845
alpha-galactosidaseHomo sapiens (human)Potency79.43284.466818.391635.4813AID2107
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.39740.035520.977089.1251AID504332
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency8.53980.354828.065989.1251AID504847
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency50.11870.010039.53711,122.0200AID1479
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency28.18380.251215.843239.8107AID504327
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Tyrosine-protein kinase LckHomo sapiens (human)IC50 (µMol)0.31850.00021.317310.0000AID325529; AID325530
LIM domain kinase 1Homo sapiens (human)IC50 (µMol)0.80000.00240.32451.7783AID1197750; AID1856822
LIM domain kinase 2Homo sapiens (human)IC50 (µMol)1.53000.00801.25137.9433AID1856823
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (44)

Processvia Protein(s)Taxonomy
protein phosphorylationTyrosine-protein kinase LckHomo sapiens (human)
intracellular zinc ion homeostasisTyrosine-protein kinase LckHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTyrosine-protein kinase LckHomo sapiens (human)
response to xenobiotic stimulusTyrosine-protein kinase LckHomo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase LckHomo sapiens (human)
hemopoiesisTyrosine-protein kinase LckHomo sapiens (human)
platelet activationTyrosine-protein kinase LckHomo sapiens (human)
T cell differentiationTyrosine-protein kinase LckHomo sapiens (human)
T cell costimulationTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of heterotypic cell-cell adhesionTyrosine-protein kinase LckHomo sapiens (human)
intracellular signal transductionTyrosine-protein kinase LckHomo sapiens (human)
peptidyl-tyrosine autophosphorylationTyrosine-protein kinase LckHomo sapiens (human)
Fc-gamma receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of T cell receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of T cell activationTyrosine-protein kinase LckHomo sapiens (human)
leukocyte migrationTyrosine-protein kinase LckHomo sapiens (human)
release of sequestered calcium ion into cytosolTyrosine-protein kinase LckHomo sapiens (human)
regulation of lymphocyte activationTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of leukocyte cell-cell adhesionTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
innate immune responseTyrosine-protein kinase LckHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
B cell receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
protein phosphorylationLIM domain kinase 1Homo sapiens (human)
signal transductionLIM domain kinase 1Homo sapiens (human)
Rho protein signal transductionLIM domain kinase 1Homo sapiens (human)
nervous system developmentLIM domain kinase 1Homo sapiens (human)
positive regulation of actin filament bundle assemblyLIM domain kinase 1Homo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisLIM domain kinase 1Homo sapiens (human)
stress fiber assemblyLIM domain kinase 1Homo sapiens (human)
positive regulation of axon extensionLIM domain kinase 1Homo sapiens (human)
axon extensionLIM domain kinase 1Homo sapiens (human)
negative regulation of ubiquitin-protein transferase activityLIM domain kinase 1Homo sapiens (human)
positive regulation of stress fiber assemblyLIM domain kinase 1Homo sapiens (human)
actin cytoskeleton organizationLIM domain kinase 1Homo sapiens (human)
positive regulation of protein phosphorylationLIM domain kinase 2Homo sapiens (human)
protein phosphorylationLIM domain kinase 2Homo sapiens (human)
spermatogenesisLIM domain kinase 2Homo sapiens (human)
phosphorylationLIM domain kinase 2Homo sapiens (human)
astral microtubule organizationLIM domain kinase 2Homo sapiens (human)
establishment of vesicle localizationLIM domain kinase 2Homo sapiens (human)
head developmentLIM domain kinase 2Homo sapiens (human)
cornea development in camera-type eyeLIM domain kinase 2Homo sapiens (human)
positive regulation of protein localization to nucleusLIM domain kinase 2Homo sapiens (human)
negative regulation of cilium assemblyLIM domain kinase 2Homo sapiens (human)
actin cytoskeleton organizationLIM domain kinase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
phosphotyrosine residue bindingTyrosine-protein kinase LckHomo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase LckHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase LckHomo sapiens (human)
protein serine/threonine phosphatase activityTyrosine-protein kinase LckHomo sapiens (human)
protein bindingTyrosine-protein kinase LckHomo sapiens (human)
ATP bindingTyrosine-protein kinase LckHomo sapiens (human)
phospholipase activator activityTyrosine-protein kinase LckHomo sapiens (human)
protein kinase bindingTyrosine-protein kinase LckHomo sapiens (human)
protein phosphatase bindingTyrosine-protein kinase LckHomo sapiens (human)
SH2 domain bindingTyrosine-protein kinase LckHomo sapiens (human)
T cell receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
CD4 receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
CD8 receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
identical protein bindingTyrosine-protein kinase LckHomo sapiens (human)
phospholipase bindingTyrosine-protein kinase LckHomo sapiens (human)
phosphatidylinositol 3-kinase bindingTyrosine-protein kinase LckHomo sapiens (human)
ATPase bindingTyrosine-protein kinase LckHomo sapiens (human)
signaling receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
protein kinase activityLIM domain kinase 1Homo sapiens (human)
protein serine/threonine kinase activityLIM domain kinase 1Homo sapiens (human)
protein bindingLIM domain kinase 1Homo sapiens (human)
ATP bindingLIM domain kinase 1Homo sapiens (human)
heat shock protein bindingLIM domain kinase 1Homo sapiens (human)
metal ion bindingLIM domain kinase 1Homo sapiens (human)
protein serine kinase activityLIM domain kinase 1Homo sapiens (human)
protein serine/threonine kinase activityLIM domain kinase 2Homo sapiens (human)
protein bindingLIM domain kinase 2Homo sapiens (human)
ATP bindingLIM domain kinase 2Homo sapiens (human)
metal ion bindingLIM domain kinase 2Homo sapiens (human)
protein serine kinase activityLIM domain kinase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
pericentriolar materialTyrosine-protein kinase LckHomo sapiens (human)
immunological synapseTyrosine-protein kinase LckHomo sapiens (human)
cytosolTyrosine-protein kinase LckHomo sapiens (human)
plasma membraneTyrosine-protein kinase LckHomo sapiens (human)
membrane raftTyrosine-protein kinase LckHomo sapiens (human)
extracellular exosomeTyrosine-protein kinase LckHomo sapiens (human)
plasma membraneTyrosine-protein kinase LckHomo sapiens (human)
postsynapseLIM domain kinase 1Homo sapiens (human)
glutamatergic synapseLIM domain kinase 1Homo sapiens (human)
male germ cell nucleusLIM domain kinase 1Homo sapiens (human)
cytoplasmLIM domain kinase 1Homo sapiens (human)
cytosolLIM domain kinase 1Homo sapiens (human)
cytoskeletonLIM domain kinase 1Homo sapiens (human)
focal adhesionLIM domain kinase 1Homo sapiens (human)
membraneLIM domain kinase 1Homo sapiens (human)
nuclear speckLIM domain kinase 1Homo sapiens (human)
lamellipodiumLIM domain kinase 1Homo sapiens (human)
neuron projectionLIM domain kinase 1Homo sapiens (human)
nucleusLIM domain kinase 1Homo sapiens (human)
neuron projectionLIM domain kinase 1Homo sapiens (human)
cytoplasmLIM domain kinase 1Homo sapiens (human)
nucleusLIM domain kinase 2Homo sapiens (human)
cytoplasmLIM domain kinase 2Homo sapiens (human)
cis-Golgi networkLIM domain kinase 2Homo sapiens (human)
centrosomeLIM domain kinase 2Homo sapiens (human)
perinuclear region of cytoplasmLIM domain kinase 2Homo sapiens (human)
mitotic spindleLIM domain kinase 2Homo sapiens (human)
nucleusLIM domain kinase 2Homo sapiens (human)
cytoplasmLIM domain kinase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (42)

Assay IDTitleYearJournalArticle
AID325537Selectivity for p56lck over p60src2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
AID336956Inhibition of TPA-induced EBV-early antigen activation in human Raji cells at 10 molar ratio after 48 hrs by indirect immunofluorescence technique relative to TPA
AID325534Selectivity for p56lck over c-ErbB22007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
AID336959Cytotoxicity against human Raji cells assessed as cell viability at 100 molar ratio
AID325530Inhibition of p56lck-mediated exogenous peptide phosphorylation2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
AID1328320Cytotoxicity against human MDA-MB-231 cells after 72 hrs by alamar blue assay2016Journal of natural products, 09-23, Volume: 79, Issue:9
Naphthalene Derivatives from the Roots of Pentas parvifolia and Pentas bussei.
AID270273Antifungal activity against Trichophyton mentagrophytes2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Antifungal anthraquinones from Saprosma fragrans.
AID325538Selectivity for p56lck over p59fyn2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
AID325533Selectivity for p56lck over EGFR2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
AID1630227Inhibition of c-myc and His6-tagged full length HIV1 NL4-3 Vpr transfected in human TREx-HeLa cells assessed as cell proliferation at 2.5 uM after 48 hrs in presence of tetracycline by WST-8 assay (Rvb = 100 +/- 1%)2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Quassinoids: Viral protein R inhibitors from Picrasma javanica bark collected in Myanmar for HIV infection.
AID1856823Inhibition of his6 tagged LIMK2 (unknown origin) expressed in baculovirus-infected Sf9 cells measured after 1 hr in presence of ATP by fluorescence based analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID336954Inhibition of TPA-induced EBV-early antigen activation in human Raji cells at 500 molar ratio after 48 hrs by indirect immunofluorescence technique relative to TPA
AID336960Cytotoxicity against human Raji cells assessed as cell viability at 10 molar ratio
AID270274Antifungal activity against Aspergillus fumigatus2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Antifungal anthraquinones from Saprosma fragrans.
AID336955Inhibition of TPA-induced EBV-early antigen activation in human Raji cells at 100 molar ratio after 48 hrs by indirect immunofluorescence technique relative to TPA
AID1197750Inhibition of Limk1 (unknown origin)2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.
AID270272Antifungal activity against Sporothrix schenckii2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Antifungal anthraquinones from Saprosma fragrans.
AID336957Cytotoxicity against human Raji cells assessed as cell viability at 1000 molar ratio
AID1856822Inhibition of his6 tagged LIMK1 (unknown origin) expressed in baculovirus-infected Sf9 cells measured after 1 hr in presence of ATP by fluorescence based analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID270271Antifungal activity against Cryptococcus neoformans2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Antifungal anthraquinones from Saprosma fragrans.
AID325531Selectivity for p56lck over PKA2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
AID270270Antifungal activity against Candida albicans2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Antifungal anthraquinones from Saprosma fragrans.
AID1630228Inhibition of c-myc and His6-tagged full length HIV1 NL4-3 Vpr transfected in human TREx-HeLa cells assessed as cell proliferation at 5 uM after 48 hrs in presence of tetracycline by WST-8 assay (Rvb = 100 +/- 1%)2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Quassinoids: Viral protein R inhibitors from Picrasma javanica bark collected in Myanmar for HIV infection.
AID1630230Cytotoxicity against human TREx-HeLa cells assessed as cell viability at 2.5 uM after 48 hrs by WST-8 assay2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Quassinoids: Viral protein R inhibitors from Picrasma javanica bark collected in Myanmar for HIV infection.
AID1290518Selectivity index, ratio of CC50 for human THP1 cells to IC50 for Trypanosoma cruzi Tulahuen2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi.
AID325536Selectivity for p56lck over PDGFR2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
AID336953Inhibition of TPA-induced EBV-early antigen activation in human Raji cells at 1000 molar ratio after 48 hrs by indirect immunofluorescence technique relative to TPA
AID1630226Inhibition of c-myc and His6-tagged full length HIV1 NL4-3 Vpr transfected in human TREx-HeLa cells assessed as cell proliferation at 1.25 uM after 48 hrs in presence of tetracycline by WST-8 assay (Rvb = 100 +/- 1%)2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Quassinoids: Viral protein R inhibitors from Picrasma javanica bark collected in Myanmar for HIV infection.
AID325529Inhibition of p56lck autophosphorylation2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
AID354878Induction of morphological changes in rat NRK cells expressing K-ras-ts proto-oncogene assessed as flat morphology1996Journal of natural products, Jul, Volume: 59, Issue:7
Cyclopentabenzofuran lignan protein synthesis inhibitors from Aglaia odorata.
AID1290516Cytotoxicity against human THP1 cells assessed as cell viability after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi.
AID336958Cytotoxicity against human Raji cells assessed as cell viability at 500 molar ratio
AID354877Induction of morphological changes in rat NRK cells expressing K-ras assessed as flat morphology1996Journal of natural products, Jul, Volume: 59, Issue:7
Cyclopentabenzofuran lignan protein synthesis inhibitors from Aglaia odorata.
AID1290514Antiprotozoan activity against intracellular amastigote stage of Trypanosoma cruzi Tulahuen infected in human THP1 cells assessed as reduction in parasite viability after 48 hrs by microplate based assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi.
AID472448Inhibition of autotaxin at 10 uM2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Pharmacophore development and application toward the identification of novel, small-molecule autotaxin inhibitors.
AID1287499Inhibition of -c-myc-His6 tagged HIV1 NL4-3 Vpr expressed in human TREx-HeLa-Vpr cells assessed as cell viability at 5 uM after 48 hrs in presence of tetracycline by WST8 assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Isopimarane diterpenoids from Kaempferia pulchra rhizomes collected in Myanmar and their Vpr inhibitory activity.
AID325535Selectivity for p56lck over insulin receptor kinase2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
AID325532Selectivity for p56lck over PKC2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
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.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (54)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (3.70)18.7374
1990's6 (11.11)18.2507
2000's13 (24.07)29.6817
2010's28 (51.85)24.3611
2020's5 (9.26)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 30.80

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index30.80 (24.57)
Research Supply Index4.03 (2.92)
Research Growth Index5.15 (4.65)
Search Engine Demand Index39.34 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (30.80)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (3.64%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other53 (96.36%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]