Page last updated: 2024-11-12

jnj 10191584

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

Description

JNJ 10191584: histamine H4 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10446295
CHEMBL ID185951
CHEBI ID92272
SCHEMBL ID602043
SCHEMBL ID16939347
MeSH IDM0493745

Synonyms (32)

Synonym
BRD-K15086322-103-01-0
vuf 6002
gtpl1277
(6-chloro-1h-benzimidazol-2-yl)-(4-methylpiperazin-1-yl)methanone
jnj 10191584
CHEMBL185951 ,
jnj-10191584
(5-chloro-1h-benzoimidazol-2-yl)-(4-methyl-piperazin-1-yl)-methanone
(5-chloro-1h-benzoimidazol-2-yl)(4-methylpiperazin-1-yl)methanone
bdbm50179335
AKOS015994569
(6-chloro-1h-benzoimidazol-2-yl)-(4-methyl-piperazin-1-yl)-methanone
piperazine, 1-[(5-chloro-1h-benzimidazol-2-yl)carbonyl]-4-methyl-
73903-17-0
SCHEMBL602043
7ee5t3wl8p ,
piperazine, 1-((5-chloro-1h-benzimidazol-2-yl)carbonyl)-4-methyl-
unii-7ee5t3wl8p
(5-chloro-1h-benzimidazol-2-yl)(4-methylpiperazin-1-yl)methanone
vuf-6002
methanone, (6-chloro-1h-benzimidazol-2-yl)(4-methyl-1-piperazinyl)-
ES-0014
SCHEMBL16939347
CHEBI:92272
jnj10191584
Q7907646
jnj 10191584 (maleate)
6-chloro-2-(4-methylpiperazine-1-carbonyl)-1h-1,3-benzodiazole
CS-0082926
HY-123532
DTXSID801170826
E98838

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Treatment with JNJ 10191584 (10-100 mg/kg p.o., b.i.d.) caused a dose-dependent reduction in macroscopic damage, inhibition of the TNBS-provoked elevation of both colonic myeloperoxidase and tumour necrosis factor-alpha (TNF-alpha), and a reduction in the histologically assessed increase in mucosal and submucosal thickness and neutrophil infiltration."( Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat.
Berko, A; Dunford, PJ; Horvath, K; Thurmond, RL; Varga, C; Whittle, BJ, 2005
)
0.67
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzimidazolesAn organic heterocyclic compound containing a benzene ring fused to an imidazole ring.
[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 (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H4 receptorHomo sapiens (human)IC50 (µMol)0.33400.00070.630510.0000AID256876; AID256877
Histamine H4 receptorHomo sapiens (human)Ki0.03910.00060.478710.0000AID1127886; AID239984; AID256865; AID594143; AID630911; AID630917; AID638337; AID640808; AID640809
Histamine H3 receptorHomo sapiens (human)Ki12.67800.00010.33998.5110AID239983; AID256878; AID640810
[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 H4 receptorHomo sapiens (human)Kd0.02000.00400.01940.0702AID256866
Histamine H3 receptorHomo sapiens (human)EC50 (µMol)3.16230.00000.09473.1623AID243150
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
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 (3)

Processvia Protein(s)Taxonomy
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 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 (33)

Assay IDTitleYearJournalArticle
AID244406Intrinsic activity against human histamine H3 receptor2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
AID640808Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Synthesis of novel histamine H4 receptor antagonists.
AID630911Antagonist activity at human histamine H4 receptor by functional assay2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).
AID256874Oral bioavailability in rat administered with 10 mg/kg, po2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID256877Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptor2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID256871Maximum concentration in rat administered with 10 mg/kg, po2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID1127886Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists.
AID640814Clearance in rat at 10 mg/kg, sc2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Synthesis of novel histamine H4 receptor antagonists.
AID256878Binding affinity to histamine H3 receptor2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID640817Half life in rat at 10 mg/kg, sc2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Synthesis of novel histamine H4 receptor antagonists.
AID256869In vitro half life in rat liver microsomes2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID256868In vitro half life in human S9 fraction2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID256876Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID640811Metabolic stability in human liver microsomes2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Synthesis of novel histamine H4 receptor antagonists.
AID243150Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
AID256873Area under curve in rat administered with 10 mg/kg, po2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID256870In vitro half life in rat S9 fraction2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID256866Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID256867In vitro half life in human liver microsomes2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID594143Displacement of [3H]histamine from human histamine H4 receptor2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Triamino pyrimidines and pyridines as histamine H(4) receptor modulators.
AID256865Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID640820Volume of distribution in rat at 10 mg/kg, sc2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Synthesis of novel histamine H4 receptor antagonists.
AID239984Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
AID1693533Antagonist activity at human histamine 4 receptor transfected in human HEK293T cells assessed as reduction in histamine-induced activity at 10 uM incubated for 30 mins followed by histamine stimulation and measured immediately by BRET assay
AID630917Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).
AID239983Binding affinity towards human histamine H3 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
AID638590Displacement of [3H]histamine from human H4R assessed as binding half life2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics.
AID638337Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics.
AID256872Half life in rat administered with 10 mg/kg, po2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
AID640812Metabolic stability in rat liver microsomes2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Synthesis of novel histamine H4 receptor antagonists.
AID640810Binding affinity to human histamine H3 receptor2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Synthesis of novel histamine H4 receptor antagonists.
AID640809Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Synthesis of novel histamine H4 receptor antagonists.
AID1346055Human H4 receptor (Histamine receptors)2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (33.33)29.6817
2010's12 (57.14)24.3611
2020's2 (9.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.61

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 Index11.61 (24.57)
Research Supply Index3.09 (2.92)
Research Growth Index4.71 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.76%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other20 (95.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]