Page last updated: 2024-11-04

histamine dihydrochloride

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Description

Ceplene: Tradename for histamine dihydrochloride. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID120160
CHEMBL ID535166
SCHEMBL ID887606
SCHEMBL ID17377087
MeSH IDM0010392
PubMed CID5818
CHEMBL ID1533310
SCHEMBL ID58710
SCHEMBL ID16778301
MeSH IDM0010392

Synonyms (179)

Synonym
MLS000069448 ,
smr000059063
histamine hydrochloride
histamine, monohydrochloride
chlorhydrate d'histamine [french]
imidazole, 4-aminoethyl-, hydrochloride
1h-imidazole-4-ethanamine, monohydrochloride
SGCUT00129
TO_000059
wln: t5m cnj d2z &gh 2
nsc257873
histamine dichloride
histamine chloride
CHEMBL535166
2-(1h-imidazol-5-yl)ethanamine hydrochloride
ai3-52154
23758-34-1
1h-imidazole-4-ethanamine, hydrochloride
nsc-757057
pharmakon1600-01500331
nsc757057
histamine monohydrochloride
unii-f9i23ac4pq
chlorhydrate d'histamine
55-36-7
f9i23ac4pq ,
histamine hcl
1h-imidazole-5-ethanamine, hydrochloride (1:1)
SCHEMBL887606
AKOS022902450
IVCJGQQPPHYHBS-UHFFFAOYSA-N
histamine chlorhydrate
OPERA_ID_1544
SCHEMBL17377087
AS-66105
2-(1h-imidazol-4-yl)ethan-1-amine hydrochloride
2-(3h-imidazol-4-yl)ethanamine hydrochloride
mfcd00044557
Q27277851
2-(1h-imidazol-5-yl)ethanamine;hydrochloride
D97233
2-(1h-imidazol-5-yl)ethan-1-amine--hydrogen chloride (1/1)
DTXSID70946542
2-(1h-imidazol-4-yl)ethanamine hydrochloride
AC-7507
histamine dihydrochloride
EU-0100595
histamine dihydrochloride, >=99% (tlc), powder
bichlorhydrate d'histamine [french]
ai3-24394
histamine dihydrochloride [usan]
einecs 200-298-4
2-(1h-imidazol-4-yl)ethanamine dihydrochloride
2-(1h-imidazol-4-yl)ethylamine dihydrochloride
2-imidazol-4-ylethylamine dihydrochloride
nsc 257873
c5h9n3.2hcl
ceplene
ceplene (tn)
histamine dihydrochloride (usan)
D04444
56-92-8
histamine, dihydrochloride
nsc-257873
4-(2-aminoethyl)imidazole dihydrochloride
histaminedium dichloride
1h-imidazole-4-ethanamine, dihydrochloride
NCGC00093973-03
NCGC00093973-02
SPECTRUM1500331
NCGC00093973-01
H-2250
H-2255
H 7250
1h-imidazole-4-ethanamine dihydrochloride
H0146
HMS1920D11
2-(1h-imidazol-5-yl)ethanamine dihydrochloride
2-(4-imidazolyl)ethylamine dihydrochloride; 2-(1h-imidazol-4-yl)ethylamine dihydrochloride;histamine 2hcl
A831236
2-(1h-imidazol-4-yl)ethan-1-amine dihydrochloride
EN300-75558
2-(4-imidazolyl)ethylamine dihydrochloride
histaminum hydrochloricum
S4118
histamine 2hcl
CCG-38567
unii-3poa0q644u
1h-imidazole-5-ethanamine, hydrochloride (1:2)
bichlorhydrate d'histamine
3poa0q644u ,
BP-12001
FT-0627074
2-(1h-imidazol-5-yl)ethan-1-amine dihydrochloride
BS-3141
LP00595
AKOS015894236
histamine dihydrocloride
CHEMBL1533310
AKOS016353223
histamine hydrochloride [mart.]
histamine dihydrochloride [ep monograph]
histamine hydrochloride [who-dd]
histaminum hydrochloricum [hpus]
histamine dihydrochloride [mi]
histamine dihydrochloride [usp-rs]
histamine dihydrochloride [ema epar]
SCHEMBL58710
4-(2-aminoethyl)imidazole dihydorchloride
PPZMYIBUHIPZOS-UHFFFAOYSA-N
KS-5310
tox21_500595
2-(4-imidazolyl)ethylaminedihydrochloride
NCGC00261280-01
histaminedihydrochloride
DTXSID1058767
STR02021
4-(2-aminoethyl)-1h-imidazole dihydrochloride
CS-W020699
histamine (dihydrochloride)
HB2803
mfcd00012703
F2191-0277
SCHEMBL16778301
Z1267773750
SR-01000075270-1
sr-01000075270
histamine dihydrochloride, >=99.0% (at)
histamine dihydrochloride, saj special grade, >=98.0%
histamine dihydrochloride, united states pharmacopeia (usp) reference standard
histamine dihydrochloride, tested according to ph eur
2-(1h-imidazol-5-yl)ethanamine dihydrochloride, aldrichcpr
histamine dihydrochloride, european pharmacopoeia (ep) reference standard
bichlorhydrated'histamine
histamine dihcl ,
histamine dihydrochloride, vetec(tm) reagent grade, 98%
histamine dihydrochloride; 2-(1h-imidazol-4-yl)ethanamine dihydrochloride
SR-01000075270-7
SY012860
SW219552-1
histamine dichlorhydrate
BCP16313
Q5772985
HY-B0722
histamine dihydrochloride 100 microg/ml in acetonitrile/water
2-(1h-imidazol-5-yl)ethanamine;dihydrochloride
mfcd08060928
1h-imidazole-4-ethanamine, chloride (1:1)
timtec-bb sbb003722
2-(1h-imidazol-5-yl)ethanamine hydrochloride (1:1)
edihydrochlorideavailablefrom1kgto100kg.
histaminum 30c allergy relief
allergen scratch extract positive control'torii' histamine dihydrochloride
muscleshok back pain
histaminum hydrochloricum 6c
hand and wrist pain cream
histamine phenolic
cvs arthritis pain relief
histamine dihydrochloride .025%
dr. freds miracle rub
histamine dihydrochloride (usp-rs)
ropana pain relief cream
havasu hemp soothing pain relief rub
histamine dihydrochloride (ep monograph)
mancore muscle mend roll-on pain reliever
bakers best arthritis pain relief cream with hemp and lavender
2-(1-h-imidazol-4-yl) ethylamine dihydrochloride
glucosamine cream extra strength
amino active topical analgesic cream
histamine6x
walgreens arthritis pain relief cream
histamine1522
histaminum hydrochloricum200ck
muscleshok sport
histaminum hydrocloricum
australian dream back pain
maxamine
pain relieving arthritis
bakers best arthritis pain relief
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency89.12510.044717.8581100.0000AID485294
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency12.58930.707912.194339.8107AID720542
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency89.12510.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency1.25890.035520.977089.1251AID504332
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency19.95260.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency2.99420.004611.374133.4983AID624296; AID624297
survival motor neuron protein isoform dHomo sapiens (human)Potency1.99530.125912.234435.4813AID1458
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency35.48130.003245.467312,589.2998AID1705
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency28.76730.001530.607315,848.9004AID1224819; AID1224820; AID1224821
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00010.540617.639296.1227AID2364; AID2528
[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)
Histamine H4 receptorMus musculus (house mouse)Ki1.31960.00260.69785.1250AID1649748; AID1649760
Histamine H4 receptorHomo sapiens (human)Ki0.07810.00060.478710.0000AID1649703; AID1649705; AID1649747; AID1649753; AID1649754; AID1649755; AID1649756; AID1649757; AID1649758; AID271661
Histamine H3 receptorHomo sapiens (human)Ki0.17120.00010.33998.5110AID1649704; AID1649746; AID1649749; AID1649750; AID1649752
[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)
Histamine H2 receptorHomo sapiens (human)EC50 (µMol)1.25890.11481.77695.4954AID697893
Histamine H2 receptorCavia porcellus (domestic guinea pig)EC50 (µMol)1.20230.00030.57191.2023AID697896
Histamine H4 receptorMus musculus (house mouse)EC50 (µMol)1.21570.00242.07168.7096AID1649713; AID1649719
Histamine H4 receptorHomo sapiens (human)EC50 (µMol)0.02540.00740.601610.0000AID1649698; AID1649715
Histamine H3 receptorHomo sapiens (human)EC50 (µMol)0.00330.00000.09473.1623AID1649710
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (12)

Processvia Protein(s)Taxonomy
gastric acid secretionHistamine H2 receptorHomo sapiens (human)
immune responseHistamine H2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H2 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H2 receptorHomo sapiens (human)
inflammatory responseHistamine H4 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationHistamine H4 receptorHomo sapiens (human)
biological_processHistamine H4 receptorHomo sapiens (human)
regulation of MAPK cascadeHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H4 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H4 receptorHomo sapiens (human)
neurotransmitter secretionHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H3 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H3 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
histamine receptor activityHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H2 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H2 receptorHomo sapiens (human)
histamine receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H4 receptorHomo sapiens (human)
histamine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membraneHistamine H2 receptorHomo sapiens (human)
synapseHistamine H2 receptorHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
dendriteHistamine H2 receptorHomo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
dendriteHistamine H4 receptorHomo sapiens (human)
synapseHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
presynapseHistamine H3 receptorHomo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
synapseHistamine H3 receptorHomo sapiens (human)
dendriteHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (61)

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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1649752Displacement of [3H]-N-alpha-methylhistamine from human recombinant H3R expressed in human SK-N-MC cell membranes
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID697896Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H₂ receptor agonists.
AID1649705Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
AID1649709Selectivity ratio of Ki for displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes to Ki for displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled huma
AID1649704Displacement of [3H]-N-alpha-methylhistamine from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
AID1649715Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
AID1649750Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H3R expressed in HEK293T cells by Nano-BRET assay
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1649746Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
AID697899Selectivity index, ratio of EC50 for human H2R-Gsalphas to EC50 for guinea pig H2R-Gsalphas by by steady state GTPase activity assay2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H₂ receptor agonists.
AID1649749Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS4 measured after 60 mins by microbeta scintillation counting method
AID1649760Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
AID1649754Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
AID697900Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H₂ receptor agonists.
AID1649755Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1649713Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
AID1649756Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
AID697893Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H₂ receptor agonists.
AID1649698Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1649703Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
AID1649753Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
AID1649710Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
AID1649719Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
AID1649758Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
AID1649747Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
AID271661Displacement of [3H]histamine from human histamine H4 receptor2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.
AID1649748Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1649757Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
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.
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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (17.65)29.6817
2010's11 (64.71)24.3611
2020's3 (17.65)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 35.46

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index35.46 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index66.93 (26.88)
Search Engine Supply Index2.97 (0.95)

This Compound (35.46)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Reviews1 (9.09%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
Other10 (90.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]