Page last updated: 2024-12-09

1,4-benzoquinone guanylhydrazone thiosemicarbazone

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

Description

1,4-benzoquinone guanylhydrazone thiosemicarbazone, often abbreviated as **BQGH**, is a synthetic organic compound with a complex chemical structure. Its importance lies in its potential as a **potent anti-cancer agent**, particularly in the context of **experimental cancer research**.

Here's a breakdown of its properties and significance:

* **Structure:** The compound combines a quinone core with a guanylhydrazone and thiosemicarbazone moiety. This unique structure allows it to interact with various biological targets.

* **Anti-cancer activity:** BQGH exhibits significant anti-cancer activity against a range of human cancer cell lines, including leukemia, lymphoma, melanoma, and breast cancer.

* **Mechanism of action:** The exact mechanism of action of BQGH is still under investigation, but it's believed to involve multiple pathways:
* **DNA damage:** BQGH can damage DNA by forming adducts with DNA bases, potentially interfering with DNA replication and cell division.
* **Oxidative stress:** It can induce oxidative stress within cancer cells, leading to cell death.
* **Inhibition of enzyme activity:** BQGH may inhibit the activity of key enzymes involved in cell growth and proliferation.

* **Research significance:** Despite its promising anti-cancer potential, BQGH has not yet been approved for clinical use. However, it remains a crucial research tool for the following reasons:
* **Drug development:** Scientists use BQGH as a lead compound for developing novel and more effective cancer treatments. By studying its mechanism of action and structure-activity relationships, they can design new compounds with enhanced efficacy and fewer side effects.
* **Understanding cancer biology:** BQGH's interaction with various cellular targets provides insights into the underlying mechanisms of cancer development and progression.
* **Preclinical studies:** Preclinical studies using BQGH help evaluate its therapeutic potential and identify potential side effects before moving to clinical trials.

**It is essential to note that BQGH is a research chemical and should not be used for self-treatment.** Its use in experimental settings requires specialized knowledge and safety protocols.

In conclusion, 1,4-benzoquinone guanylhydrazone thiosemicarbazone is a significant research molecule with promising anti-cancer activity. Its study helps scientists develop new cancer treatments and understand the complex processes involved in cancer development.

1,4-benzoquinone guanylhydrazone thiosemicarbazone: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
Anginongenus[no description available]ApiaceaeA large plant family in the order Apiales, also known as Umbelliferae. Most are aromatic herbs with alternate, feather-divided leaves that are sheathed at the base. The flowers often form a conspicuous flat-topped umbel. Each small individual flower is usually bisexual, with five sepals, five petals, and an enlarged disk at the base of the style. The fruits are ridged and are composed of two parts that split open at maturity.[MeSH]

Cross-References

ID SourceID
PubMed CID1549158
CHEMBL ID2103762
CHEMBL ID3198213
CHEMBL ID1414870
CHEBI ID134962
SCHEMBL ID457920
SCHEMBL ID1649608
SCHEMBL ID11887782
SCHEMBL ID23858322
MeSH IDM0114459

Synonyms (77)

Synonym
AKOS002161802
[4-[2-(diaminomethylidene)hydrazinyl]phenyl]iminothiourea
ambazone
(2e)-2-{(4e)-4-[(aminocarbonothioyl)hydrazono]cyclohexa-2,5-dien-1-ylidene}hydrazinecarboximidamide
539-21-9
promassol
faringosept
ambazone [inn:ban:dcf]
anginon
p-benzoquinone amidinohydrazone thiosemicarbazone
primal
dc 0572
guanidine, ((4-oxo-2,5-cyclohexadien-1-ylidene)amino)-, thiosemicarbazone
((4-oxo-2,5-cyclohexadien-1-ylidene)amino)guanidine thiosemicarbazone
hydrazinecarbothioamide, 2-(4-((aminoiminomethyl)hydrazono)-2,5-cyclohexadien-1-ylidene)-
ambazonum [inn-latin]
ambazona [inn-spanish]
ccris 1926
1,4-benzoquinone guanylhydrazone thiosemicarbazone
4-amidinohydrazono-2,5-cyclohexadien-1-on-thiosemicarbazon
ivertol
inversal
1-amidinohydrazono-4-thiosemicarbazono-2,5-cyclohexadiene
einecs 208-713-0
ambazon
benzoquinone guanylhydrazone thiosemicarbazone
guanothiazon
faringosept (tn)
D07376
ambazone (inn)
NCGC00164514-01
MLS001240207 ,
smr000674566
CHEBI:134962
AKOS000622836
FT-0661544
tox21_112149
dtxsid3046407 ,
dtxcid1026407
cas-539-21-9
ambazonum
ambazona
HMS2231L21
CHEMBL2103762
AKOS005197779
unii-byk4592a3q
byk4592a3q ,
STL200147
(2z)-2-[(4z)-4-(2-carbamimidoylhydrazinylidene)cyclohexa-2,5-dien-1-ylidene]hydrazinecarbothioamide
hydrazinecarbothioamide, 2-[4-[(aminoiminomethyl)hydrazono]-2,5-cyclohexadien-1-ylidene]-
ambazone [inn]
ambazone [mi]
ambazone [who-dd]
ambazone [mart.]
hydrazinecarbothioamide, 2-(4-(2-(aminoiminomethyl)hydrazinylidene)-2,5-cyclohexadien-1-ylidene)-
SCHEMBL457920
SCHEMBL1649608
SCHEMBL11887782
NCGC00164514-02
bdbm53352
1-[4-[2-[bis(azanyl)methylidene]hydrazinyl]phenyl]iminothiourea
[4-[n''-(diaminomethylene)hydrazino]phenyl]iminothiourea
cid_1549158
{[(1z,4z)-4-{[(diaminomethylidene)amino]imino}cyclohexa-2,5-dien-1-ylidene]amino}thiourea
CHEMBL3198213
SR-01000799157-2
sr-01000799157
[4-(2-(diaminomethylidene)hydrazino)phenyl]iminothiourea
Q414317
DB13697
CHEMBL1414870
p-benzoquinoneamidinohydrazonethiosemicarbazone
[(4-{[(diaminomethylidene)amino]amino}phenyl)imino]thiourea
SCHEMBL23858322
CS-0086507
HY-122356A
PD063404

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" It proved to be toxic at 100 mg/kg body mass."( [Antineoplastic activity and toxicity of dihydroambazone in comparison with ambazone (1,4-benzoquinone-guanylhydrazone-thiosemicarbazone)].
Baumgart, J; Gutsche, W; Härtl, A; Schulze, W, 1990
)
0.28

Bioavailability

ExcerptReferenceRelevance
"In order to improve the bioavailability of insulin after rectal application to rabbits, the influence of surface-active amino acid-fatty acid condensate on absorption and, the effects of a protease inhibitor (aprotinine), of a disinfectant (methyl-hydroxybenzoate) and of chemotherapeutics (chloramphenicol, ambazone and metronidazole) were investigated."( The protection of insulin against proteolytic processes after rectal application to normoglycemic rabbits.
Hacker, E; Kossowicz, J; Milde, K, 1991
)
0.28
" Our study shows that despite the requirement for controlled storage conditions, the acetate salt solvated form could be an alternative to ambazone when solubility and bioavailability improvement is critical for the clinical efficacy of the drug product."( Crystal structure and physicochemical characterization of ambazone monohydrate, anhydrous, and acetate salt solvate.
Borodi, G; Braga, D; Kacso, I; Maini, L; Muresan-Pop, M; Pop, MM, 2014
)
0.4
"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]

Protein Targets (53)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency44.66840.044717.8581100.0000AID485294
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency20.81140.140911.194039.8107AID2451; AID2787
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency11.22020.631035.7641100.0000AID504339
Chain A, Ferritin light chainEquus caballus (horse)Potency28.18385.623417.292931.6228AID485281
LuciferasePhotinus pyralis (common eastern firefly)Potency16.37760.007215.758889.3584AID588342; AID624030
thioredoxin reductaseRattus norvegicus (Norway rat)Potency19.95260.100020.879379.4328AID588453
WRNHomo sapiens (human)Potency44.66840.168331.2583100.0000AID651768
phosphopantetheinyl transferaseBacillus subtilisPotency44.84370.141337.9142100.0000AID1490
USP1 protein, partialHomo sapiens (human)Potency44.66840.031637.5844354.8130AID504865
GLS proteinHomo sapiens (human)Potency14.55000.35487.935539.8107AID624170
TDP1 proteinHomo sapiens (human)Potency2.10100.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency29.84930.000221.22318,912.5098AID743042; AID743054
thioredoxin glutathione reductaseSchistosoma mansoniPotency50.11870.100022.9075100.0000AID485364
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency25.11890.707912.194339.8107AID720542
hypothetical protein, conservedTrypanosoma bruceiPotency28.18380.223911.245135.4813AID624173
regulator of G-protein signaling 4Homo sapiens (human)Potency28.18380.531815.435837.6858AID504845
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency2.23870.28189.721235.4813AID2326
estrogen nuclear receptor alphaHomo sapiens (human)Potency18.61830.000229.305416,493.5996AID743069; AID743078
GVesicular stomatitis virusPotency15.09160.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency10.68400.00108.379861.1304AID1645840
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency39.81070.707936.904389.1251AID504333
IDH1Homo sapiens (human)Potency5.80480.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.79430.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency13.71430.000723.06741,258.9301AID743085; AID743122
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency23.71010.001723.839378.1014AID743083
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency39.81070.036619.637650.1187AID2100
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency11.70310.354828.065989.1251AID504847
fructose-bisphosphate aldolase AOryctolagus cuniculus (rabbit)Potency79.43280.891316.576239.8107AID2794
chromobox protein homolog 1Homo sapiens (human)Potency3.98110.006026.168889.1251AID540317
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency31.62280.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency25.62050.000323.4451159.6830AID743065; AID743067
glyceraldehyde-3-phosphate dehydrogenase isoform 1Homo sapiens (human)Potency50.11871.122011.187739.8107AID2795
flap endonuclease 1Homo sapiens (human)Potency50.11870.133725.412989.1251AID588795
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency3.76860.168316.404067.0158AID720504
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency35.71680.010323.856763.0957AID2662
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency11.22020.050127.073689.1251AID588590
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency17.80360.00798.23321,122.0200AID2551
DNA polymerase kappa isoform 1Homo sapiens (human)Potency15.84890.031622.3146100.0000AID588579
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency17.78280.00419.962528.1838AID2675
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency28.18380.251215.843239.8107AID504327
Interferon betaHomo sapiens (human)Potency15.09160.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
Guanine nucleotide-binding protein GHomo sapiens (human)Potency25.11891.995325.532750.1187AID624288
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency19.75670.060110.745337.9330AID485367; AID492961; AID504636; AID504637
[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)
large T antigenBetapolyomavirus macacaeIC50 (µMol)13.73000.160024.9724100.0000AID1903
[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)
streptokinase A precursorStreptococcus pyogenes M1 GASEC50 (µMol)75.03000.06008.9128130.5170AID1902; AID1914
POsterior SegregationCaenorhabditis elegansEC50 (µMol)76.49602.201047.1808186.6810AID1964
Estrogen receptorRattus norvegicus (Norway rat)EC50 (µMol)150.00000.006022.3670130.5170AID1914
Sodium-dependent noradrenaline transporter Homo sapiens (human)EC50 (µMol)9.72700.082031.0243168.9080AID1960
Estrogen receptor betaRattus norvegicus (Norway rat)EC50 (µMol)150.00000.006022.3670130.5170AID1914
Zinc finger protein mex-5Caenorhabditis elegansEC50 (µMol)9.72700.082033.5679168.9080AID1960
large T antigenBetapolyomavirus macacaeEC50 (µMol)0.10000.100035.489650.0000AID2102
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (60)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (19)

Assay IDTitleYearJournalArticle
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
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.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
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 (29)

TimeframeStudies, This Drug (%)All Drugs %
pre-199010 (34.48)18.7374
1990's7 (24.14)18.2507
2000's2 (6.90)29.6817
2010's8 (27.59)24.3611
2020's2 (6.90)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.99

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 Index10.99 (24.57)
Research Supply Index3.47 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.99)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (3.23%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other30 (96.77%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]