Page last updated: 2024-11-09

jnj-5207852

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

Cross-References

ID SourceID
PubMed CID2766326
CHEMBL ID129542
SCHEMBL ID3577334
MeSH IDM0483777

Synonyms (44)

Synonym
jnj 5207852
gtpl1256
smr000550361
MLS001166116
1-[4-(3-piperidinopropoxy)benzyl]piperidine
L021228
jnj-5207852
CHEMBL129542 ,
1-[4-(3-hexahydro-1-pyridinylpropoxy)benzyl]hexahydropyridine
1-(4-(3-(piperidin-1-yl)propoxy)benzyl)piperidine
1-(3-(4-(piperidin-1-ylmethyl)phenoxy)propyl)piperidine
1-[3-(4-hexahydro-1-pyridinylmethylphenoxy)propyl]hexahydropyridine
bdbm50159110
AKOS005076686
1-[3-[4-(piperidin-1-ylmethyl)phenoxy]propyl]piperidine
HMS2852B03
1-(3-(4-((piperidin-1-yl)methyl)phenoxy)propyl)piperidine
unii-4i9ovb1g7d
piperidine, 1-(3-(4-(1-piperidinylmethyl)phenoxy)propyl)-
4i9ovb1g7d ,
398473-34-2
1-[3-(4-piperidin-1-ylmethyl-phenoxy)-propyl]-piperidine
PTKHFRNHJULJKT-UHFFFAOYSA-N
10X-0933
1-(3-{4-[(piperidin-1-yl)methyl]phenoxy}propyl)piperidine
SCHEMBL3577334
DTXSID70377579
1-[3-[4-(1-piperidinylmethyl)phenoxy]propyl]piperidine
jnj 5207852 dihydrochloride
3-({n-[(benzyloxy)carbonyl]-l-valyl}amino)-5-fluoro-4-oxopentanoic acid
J-690293
EX-A763
1-({4-[3-(piperidin-1-yl)propoxy]phenyl} methyl)piperidine
mfcd05974930
NCGC00371012-01
BCP16434
jnj-5207852 dihydrochloride
Q6108574
FT-0700304
jnj5207852
HY-12190
CS-0003148
YQA47334
AC-36816

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency37.90830.01237.983543.2770AID1645841
[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)
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)3.20000.00000.933210.0000AID323564
Histamine H3 receptorRattus norvegicus (Norway rat)Ki0.00080.00010.29638.5110AID1140781; AID260990; AID715208; AID89869
Histamine H3 receptorHomo sapiens (human)IC50 (µMol)0.00050.00050.46685.9000AID323565
Histamine H3 receptorHomo sapiens (human)Ki0.00090.00010.33998.5110AID1115514; AID1140780; AID1729009; AID1829881; AID1829888; AID1829899; AID1833219; AID238933; AID260989; AID290795; AID300627; AID305748; AID315075; AID349186; AID353208; AID375418; AID465708; AID478551; AID526118; AID599203; AID616620; AID692494; AID715202; AID86618
[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)
Muscarinic acetylcholine receptor M2Sus scrofa (pig)Kd0.00010.00010.02190.0437AID239867
Histamine H3 receptorHomo sapiens (human)Kd0.00030.00010.01380.0631AID239867; AID260991; AID290797; AID599205; AID86475
[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)
DNA repair protein RAD52 homolog isoform aHomo sapiens (human)AC5010.26000.150012.066235.2100AID652116
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo 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 (13)

Processvia Protein(s)Taxonomy
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo 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 (15)

Processvia Protein(s)Taxonomy
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo 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 (78)

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.
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.
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
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID315086Displacement of [3H]tiotidine from human H2 receptor expressed in monkey COS7 cells at 10 uM2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.
AID465708Displacement of [125I]Iodoproxyfan from human histamine H3 receptor expressed in HEK293 cells after 60 mins by scintillation counting2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Acidic elements in histamine H(3) receptor antagonists.
AID1115514Binding affinity to Homo sapiens (human) H3 receptor2013Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, Aug, Volume: 22, Issue:8
Non-imidazole histamine H
AID290795Binding affinity to human histamine H3 receptor2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
A new class of histamine H3 receptor antagonists derived from ligand based design.
AID315084Displacement of [3H]histamine from human H4 receptor expressed in monkey COS7 cells at 1 uM2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.
AID86475Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor2003Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
AID260989Displacement of N-[3H]methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells2006Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
Aplysamine-1 and related analogs as histamine H3 receptor antagonists.
AID349186Displacement of [125I]iodoproxyfan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
2-Aryloxymethylmorpholine histamine H(3) antagonists.
AID715208Binding affinity to rat histamine H3 receptor2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Radiofluorinated histamine H₃ receptor antagonist as a potential probe for in vivo PET imaging: radiosynthesis and pharmacological evaluation.
AID315082Displacement of [3H]pyrilamine from human H1 receptor expressed in monkey COS7 cells at 1 uM2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.
AID478551Binding affinity to human histamine H3 receptor2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.
AID28405Apparent permeability in Caco-2 cells was determined2003Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
AID1140781Binding affinity to rat histamine H3 receptor2014Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
Benzylpiperidine variations on histamine H3 receptor ligands for improved drug-likeness.
AID353209In vivo histamine H3 receptor potency in po dosed Swiss mouse assessed as N'-methylhistamine level2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Fluorinated non-imidazole histamine H3 receptor antagonists.
AID315083Displacement of [3H]tiotidine from human H2 receptor expressed in monkey COS7 cells at 1 uM2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.
AID315076Displacement of [3H]N-alpha-methylhistamine from histamine H3 receptor in rat striatal membrane2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.
AID1833219Antagonist activity at human histamine H3 receptor2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Histamine H
AID616616Tmax in Swiss mouse brain at 10 mg/kg, po by LC-MS/MS2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series.
AID1140780Binding affinity to human histamine H3 receptor2014Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
Benzylpiperidine variations on histamine H3 receptor ligands for improved drug-likeness.
AID1729009Binding affinity to human H3R2021European journal of medicinal chemistry, Mar-05, Volume: 213Structural modifications in the distal, regulatory region of histamine H
AID692499Half life in rat2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Histamine H3 receptor as a drug discovery target.
AID315075Displacement of [3H]N-alpha-methylhistamine from human cloned histamine H3 receptor expressed in monkey COS7 cells2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.
AID599205Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.
AID692494Binding affinity to human histamine H3 receptor2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Histamine H3 receptor as a drug discovery target.
AID715202Binding affinity to human recombinant histamine H3 receptor2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Radiofluorinated histamine H₃ receptor antagonist as a potential probe for in vivo PET imaging: radiosynthesis and pharmacological evaluation.
AID616618Tmax in Swiss mouse plasma at 10 mg/kg, po by LC-MS/MS2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series.
AID300627Binding affinity to human histamine H3 receptor2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.
AID526118Displacement of [125I]iodoproxyfan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells after 1 hr by fluid scintillation counting2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Indole- and benzothiophene-based histamine H3 antagonists.
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
AID260990Displacement of N-[3H]methylhistamine from rat histamine H3 receptor in rat cortical hemispheres2006Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
Aplysamine-1 and related analogs as histamine H3 receptor antagonists.
AID616621Ratio of AUC (0 to 3 hrs) in Swiss mouse brain to AUC (0 to 3 hrs) in Swiss mouse plasma at 10 mg/kg, po by LC-MS/MS2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series.
AID1829887Displacement of [3H]UR-DE25 from human H2R receptor expressed in HEK293 cells by radioligand competition 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
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
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.
AID599203Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.
AID86618In vitro binding affinity for human Histamine H3 receptor by displacing N-[3H]-methylhistamine in SK-N-MC cells was determined2003Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
AID7595Human plasma protein binding activity was determined2003Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
AID353208Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in HEL293 cells2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Fluorinated non-imidazole histamine H3 receptor antagonists.
AID315087Displacement of [3H]histamine from human H4 receptor expressed in monkey COS7 cells at 10 uM2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.
AID616620Inverse agonist activity at human histamine H3 receptor expressed in SK-N-MC cells2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series.
AID1829888Displacement of [3H]UR-P1294 from human H3R receptor expressed in HEK293 cells by radioligand competition 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
AID315085Displacement of [3H]pyrilamine from human H1 receptor expressed in monkey COS7 cells at 10 uM2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.
AID1829890Inhibition of human H3R expressed in HEK293-A cells assessed as inhibition of imetit-induced Gi2 activation by BRET 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
AID323564Inhibition of AChE2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling.
AID375418Binding affinity to histamine H3 receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.
AID323565Inhibition of histamine H3 receptor2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling.
AID616615AUC (0 to 3 hrs) in Swiss mouse brain at 10 mg/kg, po by LC-MS/MS2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series.
AID89869In vitro binding affinity for rat Histamine H3 receptor by displacing N-[3H]-methylhistamine in SK-N-MC cells was determined2003Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
AID1829886Displacement of [3H]mepyramine from human H1R receptor expressed in HEK293 cells by radioligand competition 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
AID305748Displacement of [3H]N-alpha-methylhistamine from human cloned histamine H3 receptor expressed in C6 cells2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.
AID692509Volume of distribution in rat2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Histamine H3 receptor as a drug discovery target.
AID616617AUC (0 to 3 hrs) in Swiss mouse plasma at 10 mg/kg, po by LC-MS/MS2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series.
AID30949stabilit in human liver microsome expressed as Half life2003Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
AID715201Binding affinity to rat cerebral cortex histamine H3 receptor assessed as per mg of protein2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Radiofluorinated histamine H₃ receptor antagonist as a potential probe for in vivo PET imaging: radiosynthesis and pharmacological evaluation.
AID1829889Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells by radioligand competition 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
AID239867Mean functional activity against human H3 receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists.
AID290797Antagonist activity at human histamine H3 receptor2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
A new class of histamine H3 receptor antagonists derived from ligand based design.
AID260991Activity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cells2006Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
Aplysamine-1 and related analogs as histamine H3 receptor antagonists.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1346107Human H3 receptor (Histamine receptors)2003Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
AID493017Wombat Data for BeliefDocking2003Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (32)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's14 (43.75)29.6817
2010's12 (37.50)24.3611
2020's6 (18.75)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 Index3.50 (2.92)
Research Growth Index4.48 (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 (3.13%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other31 (96.88%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]