Page last updated: 2024-12-04

clobenpropit

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

Description

clobenpropit: histamine H3 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

clobenpropit : An imidothiocarbamic ester that consists of isothiourea bearing S-3-(imidazol-4-yl)propyl and N-4-chlorobenzyl substituents. An extremely potent histamine H3 antagonist/inverse agonist (pA2 = 9.93). Also displays partial agonist activity at H4 receptors; induces eosinophil shape change with an EC50 of 3 nM. [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]

Cross-References

ID SourceID
PubMed CID2790
CHEMBL ID14690
CHEBI ID64177
SCHEMBL ID49050
SCHEMBL ID8312286
SCHEMBL ID19733457
MeSH IDM0228304

Synonyms (49)

Synonym
HMS3394B07
BRD-K71430621-303-01-5
gtpl1223
n'-[(4-chlorophenyl)methyl]-1-[3-(3h-imidazol-4-yl)propylsulfanyl]methanimidamide
bdbm22541
n''''-[(4-chlorophenyl)methyl]{[3-(1h-imidazol-5-yl)propyl]sulfanyl}methanimidamide
NCGC00024770-01
tocris-0752
PDSP1_000537
PDSP2_000535
clobenpropit
NCGC00024770-02
vuf 9153
s-(3-(4(5)-imidazolyl))propyl-n-(4-chlorobenzyl)isothiourea
carbamimidothioic acid, ((4-chlorophenyl)methyl)-, 3-(1h-imidazol-4-yl)propyl ester
vuf-9153
3-(1h-imidazol-4-yl)propyl ((4-chlorophenyl)methyl)carbamimidothioate
HMS2052B07
L000192
L010032
CHEMBL14690
chebi:64177 ,
C17934
145231-45-4
3-(1h-imidazol-5-yl)propyl n'-(4-chlorobenzyl)carbamimidothioate
3-(1h-imidazol-5-yl)propyl n'-[(4-chlorophenyl)methyl]carbamimidothioate
smr000469632
MLS001424295
CCG-101167
rku631jf4h ,
unii-rku631jf4h
3-(1h-imidazol-4-yl)propyl n-(4-chlorobenzyl)carbamimidothioate
SCHEMBL49050
NC00417
carbamimidothioic acid, n-((4-chlorophenyl)methyl)-, 3-(1h-imidazol-5-yl)propyl ester
DTXSID3043738
SCHEMBL8312286
carbamimidothioic acid,n-[(4-chlorophenyl)methyl]-, 3-(1h-imidazol-5-yl)propyl ester
AKOS025405026
carbamimidothioic acid, n-[(4-chlorophenyl)methyl]-, 3-(1h-imidazol-5-yl)propyl ester
SCHEMBL19733457
3-(1h-imidazol-4-yl)propyl 4-chlorobenzylcarbamimidothioate
Q5134762
3-(1h-imidazol-5-yl)propyl 4-chlorobenzylcarbamimidothioate
bdbm50214615
A852459
AS-77937
HY-115447
CS-0086986

Research Excerpts

Actions

ExcerptReferenceRelevance
"Clobenpropit and histidine inhibit the revival of morphine-induced CPP in a dose dependent manner, indicating that endogenous histamine may inhibit relapse of morphine to some extent."( [Effects of clobenpropit and histidine on reinstatement of morphine-induced conditioned place preference].
Chen, Z; Gong, YX; Lu, M; Wang, HJ, 2009
)
2.17

Treatment

Pretreatment with clobenpropit was without any effect on control MBF and AP but significantly reduced most of RH responses.

ExcerptReferenceRelevance
"Pretreatment with clobenpropit ameliorated cell impairment induced by Abeta42."( The H3 receptor antagonist clobenpropit protects against Abeta42-induced neurotoxicity in differentiated rat PC12 cells.
Chen, Z; Dai, H; Fan, Y; Fu, Q; He, P; Hu, W; Zhang, W, 2010
)
0.98
"Pretreatment with clobenpropit was without any effect on control MBF and AP but significantly reduced most of RH responses."( Histamine H3 receptors modulate reactive hyperemia in rat gut.
Biernat, J; Brzozowski, T; Konturek, SJ; Obuchowicz, R; Pawlik, MW; Pawlik, WW; Sendur, R, 2004
)
0.65
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
H3-receptor antagonistA histamine antagonist that selectively binds to but does not activate histamine H3 receptors, thereby blocking the actions of endogenous histamine.
H4-receptor agonistA histamine agonist that binds to and activates H4-receptors.
[role 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]

Drug Classes (3)

ClassDescription
imidazolesA five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
imidothiocarbamic ester
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
[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 (33)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
USP1 protein, partialHomo sapiens (human)Potency14.12540.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency25.49570.000811.382244.6684AID686978; AID686979
glucocerebrosidaseHomo sapiens (human)Potency39.81070.01268.156944.6684AID2101
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency12.58930.00207.533739.8107AID891
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency19.95260.316212.443531.6228AID902
cytochrome P450 2C19 precursorHomo sapiens (human)Potency15.84890.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency12.58930.00636.904339.8107AID883
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency39.81070.354828.065989.1251AID504847
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency1.58490.031610.279239.8107AID884; AID885
lethal factor (plasmid)Bacillus anthracis str. A2012Potency15.84890.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency3.98110.316212.765731.6228AID881
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency9.14600.00638.235039.8107AID881; AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
[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 H3 receptorMus musculus (house mouse)IC50 (µMol)0.00100.00100.00100.0010AID525895
Histamine H3 receptorMus musculus (house mouse)Ki0.00060.00060.01810.0680AID426166
Histamine H4 receptorMus musculus (house mouse)Ki0.14080.00260.69785.1250AID1649748; AID1649760
Histamine H4 receptorHomo sapiens (human)Ki0.02580.00060.478710.0000AID1649747; AID1649753; AID1649754; AID1649755; AID1649756; AID1649757; AID1649758; AID1798265; AID404336; AID425225; AID468419; AID597171; AID632452; AID632453; AID632454; AID632455; AID632456; AID632457; AID632458
Histamine H3 receptorRattus norvegicus (Norway rat)Ki0.00080.00010.29638.5110AID89558; AID89562
Histamine H3 receptorHomo sapiens (human)IC50 (µMol)0.00110.00050.46685.9000AID1729985; AID1755234; AID525896; AID781268
Histamine H3 receptorHomo sapiens (human)Ki0.00160.00010.33998.5110AID1649746; AID1649749; AID1649750; AID1649752; AID1798209; AID1798266; AID1829881; AID1829899; AID238933; AID408541; AID425224; AID468415; AID597172; AID632451; AID86456; AID86458; AID86466
[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 H3 receptorMus musculus (house mouse)EC50 (µMol)0.00170.00170.00630.0110AID426159
Histamine H4 receptorMus musculus (house mouse)EC50 (µMol)0.85110.00242.07168.7096AID1540382
Histamine H4 receptorHomo sapiens (human)EC50 (µMol)0.02240.00740.601610.0000AID1540381
Histamine H4 receptorHomo sapiens (human)Kd0.03090.00400.01940.0702AID1912433
Histamine H3 receptorHomo sapiens (human)Kd0.02930.00010.01380.0631AID1912432; AID781268
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H3 receptorHomo sapiens (human)Kb0.00020.00020.20972.0000AID1728990
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (30)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo 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 (11)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo 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 (11)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
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 (109)

Assay IDTitleYearJournalArticle
AID1912433Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
AID88633In vivo Histamine H3 receptor antagonism, dose required to increase in N-t-methylhistamine levels in Swiss mice brains 90 min after p.o. administration2000Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20
Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
AID425225Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting2009Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.
AID426159Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.
AID86283Displacement of [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortex2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE.
AID86631In vivo Histamine H3 receptor antagonistic activity as increase in N'-methylhistamine levels in Swiss mice after peroral administration1998Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15
General construction pattern of histamine H3-receptor antagonists: change of a paradigm.
AID1912439Binding affinity to NLuc-tagged human H3R expressed in HEK293T cell homogenates at 1 uM using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min in presence of clobenpropit by NanoBRET saturation binding assay
AID1829881Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assay2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H
AID468416Selectivity, ratio of Ki for human histaminee H4 receptor to Ki for human histamine H3 receptor2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
AID132754In vivo antagonistic activity against Histamine H3 receptor in mouse after peroral administration was assessed from the brain histamine turnover1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
Novel carbamates as potent histamine H3 receptor antagonists with high in vitro and oral in vivo activity.
AID632458Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
AID89886Ratio of binding affinity of rat histamine H3 receptor to that of human histamine H3 receptor; 1:22001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Different antagonist binding properties of human and rat histamine H3 receptors.
AID632455Displacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
AID89716In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex2000Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20
Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
AID426169Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay relative to basal level2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.
AID1540382Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
AID426166Displacement of 3-([1,1,1-3H]methyl)-2-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone from mouse histamine H3 receptor expressed in HEK293 cells2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.
AID1729985Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
AID468415Displacement of [3H]iodoproxyfan from human histamine H3 receptor expressed in CHO-K1 cells2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
AID525896Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Investigation of 4-piperidinols as novel H3 antagonists.
AID597172Displacement of [125I]iodoproxyfan from human full-length histamine H3 receptor expressed in HEK293 cells after 60 mins2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.
AID781268Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Synthesis and evaluation of N-alkyl-S-[3-(piperidin-1-yl)propyl]isothioureas: high affinity and human/rat species-selective histamine H(3) receptor antagonists.
AID425226Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay2009Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.
AID86458Inhibition of [125I]iodoproxyfan binding to human histamine H3 receptor of CHO-K1 cells2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Different antagonist binding properties of human and rat histamine H3 receptors.
AID404336Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.
AID597168Antagonist activity at histamine H3 receptor in po dosed 24 hrs fasted Swiss mouse brain assessed as N-methylhistamine level after 90 mins by radioimmunoassay2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.
AID86456Antagonist potency against human histamine H3 receptor expressed in CHO cells was determined by GTPgamma-S-assay2004Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.
AID1649753Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
AID1649758Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
AID86466Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressing CHO cells2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.
AID1755236Inhibition of amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 20 uM incubated for 24 hrs by Thioflavin T based fluorometric assay relative to control
AID1649755Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
AID86633In vivo antagonist activity at Histamine H3 receptor was screened by measuring the effect on brain histamine turnover after oral application to mice.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity.
AID1912441Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates at 1 uM using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min in presence of clobenpropit by NanoBRET saturation binding assay
AID1649757Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
AID238933Antagonist potency against human H3 receptor in GTPgamma-S-Assay2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.
AID597171Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.
AID1829899Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assay2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H
AID1912432Binding affinity to NLuc-tagged human H3R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
AID89712In vitro antagonistic activity against Histamine H3 receptor on Synaptosomes of rat cerebral cortex.1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
Novel carbamates as potent histamine H3 receptor antagonists with high in vitro and oral in vivo activity.
AID1540381Agonist activity at human H4R by [35S]-GTPgammaS-binding assay
AID1649760Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
AID89711In vitro antagonist potency at Histamine H3 receptor measured as K+-evoked [3H]histamine release from synaptosomes of rat cerebral cortex.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity.
AID632456Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
AID89571Effect at histamine H3 receptors (in vitro) on synaptosomes of rat cerebral cortex assayed by functional H3-receptor assay.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Development of chiral N-alkylcarbamates as new leads for potent and selective H3-receptor antagonists: synthesis, capillary electrophoresis, and in vitro and oral in vivo activity.
AID86630Compound was tested for its effect at histamine H3 receptors (in vivo) on mice by central H3-receptor test.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Development of chiral N-alkylcarbamates as new leads for potent and selective H3-receptor antagonists: synthesis, capillary electrophoresis, and in vitro and oral in vivo activity.
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
AID86629Histamine H3 receptor antagonist potency in vivo in mice after peroral administration2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Novel histamine H(3)-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds.
AID632451Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
AID89709In vitro Histamine H3 receptor antagonist activity in an assay with K+-evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex1998Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15
General construction pattern of histamine H3-receptor antagonists: change of a paradigm.
AID408542Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as reduction of forskolin-stimulated cAMP production at 10 uM relative to control2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.
AID89562Inhibition of [125I]iodoproxyfan from rat histamine H3 receptor expressed in CHO-K1 cells2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Different antagonist binding properties of human and rat histamine H3 receptors.
AID408541Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.
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
AID1755237Antioxidant activity assessed as trolox equivalent antioxidant capacity
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
AID468419Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
AID632452Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
AID89872Affinity for histamine H3 receptor in rat cerebral cortex.1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-Amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives.
AID1540386Antagonist activity at rat H4R by [35S]-GTPgammaS-binding assay
AID1649750Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H3R expressed in HEK293T cells by Nano-BRET assay
AID632457Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
AID86627In vivo effects in mice against H3 receptor on N6-methylhistamine levels in brain (following oral dosing of compound)2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.
AID632459Selectivity ratio of pKi for human histamine H4 receptor N457Y to pki for wild type human histamine H4 receptor2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
AID1728992Antagonist activity at recombinant human H3R expressed in CHO-K1 cells assessed as induction of calcium mobilization measured for 20 secs by aequorin-reporter gene based luminescence assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Structural modifications in the distal, regulatory region of histamine H
AID1728990Antagonist activity at recombinant human H3R expressed in CHO-K1 cells assessed as reduction in histamine-induced calcium mobilization preincubated for 15 mins followed by histamine addition and measured for 20 secs by aequorin-reporter gene based lumines2021European journal of medicinal chemistry, Mar-05, Volume: 213Structural modifications in the distal, regulatory region of histamine H
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
AID632454Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
AID632453Displacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
AID1755234Antagonist activity at human H3 receptor by TR-FRET assay
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
AID425224Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells by liquid scintillation counting2009Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.
AID525895Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Investigation of 4-piperidinols as novel H3 antagonists.
AID1755235Inhibition of amyloid beta (1 to 42) (unknown origin) self-induced aggregation incubated for 24 hrs by Thioflavin T based fluorometric assay
AID1649752Displacement of [3H]-N-alpha-methylhistamine from human recombinant H3R expressed in human SK-N-MC cell membranes
AID89573Effect on histamine H3 receptors in vitro, on synaptosomes of rat cerebral cortex for the release of [3H]histamine2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Novel histamine H(3)-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds.
AID89558Inhibition of [3H]- N-alpha-methylhistamine from histamine H3 receptor1998Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10
New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
AID89866Compound was tested for its ability to displace [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortex2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE.
AID1649756Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
AID781265Increase of histamine release in Wistar rat hypothalamus at 10 uM administered through dialysis membrane by HPLC-fluorometric based microdialysis relative to control2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Synthesis and evaluation of N-alkyl-S-[3-(piperidin-1-yl)propyl]isothioureas: high affinity and human/rat species-selective histamine H(3) receptor antagonists.
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.
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.
AID1346017Rat H3 receptor (Histamine receptors)2000British journal of pharmacology, Dec, Volume: 131, Issue:7
Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
AID1346017Rat H3 receptor (Histamine receptors)2001Biochemical and biophysical research communications, Jan-12, Volume: 280, Issue:1
The rat H3 receptor: gene organization and multiple isoforms.
AID1346044Mouse H4 receptor (Histamine receptors)2001The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1
Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
AID1346095Human H2 receptor (Histamine receptors)2003The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
AID1346055Human H4 receptor (Histamine receptors)2005The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
AID1346055Human H4 receptor (Histamine receptors)2001The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3
Cloning and characterization of a novel human histamine receptor.
AID1346017Rat H3 receptor (Histamine receptors)2000The Journal of pharmacology and experimental therapeutics, Jun, Volume: 293, Issue:3
Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
AID1346088Mouse H3 receptor (Histamine receptors)2003European journal of pharmacology, Apr-25, Volume: 467, Issue:1-3
Molecular and pharmacological characterization of the mouse histamine H3 receptor.
AID1346037Human H1 receptor (Histamine receptors)2003The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
AID1346017Rat H3 receptor (Histamine receptors)2003The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
AID1346055Human H4 receptor (Histamine receptors)2001The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1
Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
AID1346017Rat H3 receptor (Histamine receptors)2001The Journal of pharmacology and experimental therapeutics, Dec, Volume: 299, Issue:3
Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
AID1346107Human H3 receptor (Histamine receptors)2000The Journal of pharmacology and experimental therapeutics, Jun, Volume: 293, Issue:3
Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
AID1346107Human H3 receptor (Histamine receptors)2003The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
AID1346028Rat H4 receptor (Histamine receptors)2001The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1
Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
AID1346055Human H4 receptor (Histamine receptors)2003The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
AID1346107Human H3 receptor (Histamine receptors)2000British journal of pharmacology, Dec, Volume: 131, Issue:7
Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
AID1346107Human H3 receptor (Histamine receptors)2002European journal of pharmacology, Oct-18, Volume: 453, Issue:1
Characteristics of recombinantly expressed rat and human histamine H3 receptors.
AID1346055Human H4 receptor (Histamine receptors)2001Molecular pharmacology, Mar, Volume: 59, Issue:3
Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
AID1346017Rat H3 receptor (Histamine receptors)2002European journal of pharmacology, Oct-18, Volume: 453, Issue:1
Characteristics of recombinantly expressed rat and human histamine H3 receptors.
AID1346107Human H3 receptor (Histamine receptors)2001The Biochemical journal, Apr-15, Volume: 355, Issue:Pt 2
Genomic organization and characterization of splice variants of the human histamine H3 receptor.
AID1346107Human H3 receptor (Histamine receptors)2001Molecular pharmacology, Mar, Volume: 59, Issue:3
Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
AID1346107Human H3 receptor (Histamine receptors)2001The Journal of pharmacology and experimental therapeutics, Dec, Volume: 299, Issue:3
Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
AID1798209H3R Radioligand Binding Assay from Article 10.1021/jm7014149: \\4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.\\2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.
AID1798266H3R Radioligand Binding Assay from Article 10.1124/jpet.105.087965: \\Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.\\2005The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
AID1798265H4R Radioligand Binding Assay from Article 10.1124/jpet.105.087965: \\Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.\\2005The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
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 (147)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's29 (19.73)18.2507
2000's79 (53.74)29.6817
2010's28 (19.05)24.3611
2020's11 (7.48)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 34.20

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 Index34.20 (24.57)
Research Supply Index5.00 (2.92)
Research Growth Index4.59 (4.65)
Search Engine Demand Index45.89 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (34.20)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (2.72%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other143 (97.28%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]