General Information of Drug (ID: DM537OH)

Drug Name
Clobenpropit Drug Info
Synonyms
clobenpropit; 145231-45-4; Vuf-9153; Vuf 9153; UNII-RKU631JF4H; S-(3-(4(5)-Imidazolyl))propyl-N-(4-chlorobenzyl)isothiourea; CHEBI:64177; RKU631JF4H; 3-(1h-imidazol-5-yl)propyl n'-(4-chlorobenzyl)carbamimidothioate; 3-(1H-imidazol-4-yl)propyl ((4-chlorophenyl)methyl)carbamimidothioate; Carbamimidothioic acid, ((4-chlorophenyl)methyl)-, 3-(1H-imidazol-4-yl)propyl ester; 3-(1H-imidazol-4-yl)propyl N-(4-chlorobenzyl)carbamimidothioate; Carbamimidothioic acid,N-[(4-chlorophenyl)methyl]-, 3-(1H-imidazol-5-yl)propyl ester
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
2790
ChEBI ID
CHEMBL14690
CAS Number
CAS 145231-45-4
TTD Drug ID
DM537OH

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Approved Drug(s)
Drug(s) Targeting Histamine H4 receptor (H4R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
PF-3893787 DMC2FAL Atopic dermatitis EA80 Phase 2 [6]
JNJ-38518168 DM9UMIO Plaque psoriasis EA90.0 Phase 2 [7]
UR-63325 DME6X27 Allergic rhinitis CA08.0 Phase 2 [8]
Thioperamide DM8S593 Cognitive impairment 6D71 Terminated [9]
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole DMZVBPG Discovery agent N.A. Investigative [10]
impromidine DMTDRPM Discovery agent N.A. Investigative [11]
burimamide DMZ2VYG Discovery agent N.A. Investigative [12]
Imetit DMMJ6NS Discovery agent N.A. Investigative [13]
[125I]iodophenpropit DMN4ABU Discovery agent N.A. Investigative [14]
(R)-alpha-methylhistamine DMKAW4P Discovery agent N.A. Investigative [15]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Histamine H3 receptor (H3R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pitolisant DM8RFNJ Excessive daytime sleepiness MG42 Approved [16]
SUVN-G3031 DM3BO8G Cognitive impairment 6D71 Phase 3 [17]
JNJ-17216498 DM1GRCU Narcolepsy 7A20 Phase 2 [18]
GSK239512 DMBJMZC Alzheimer disease 8A20 Phase 2 [19]
JNJ-39220675 DM0WY3H Alcohol dependence 6C40.2 Phase 2 [20]
AZD-5213 DMOZ04X Alzheimer disease 8A20 Phase 2 [21]
Bavisant DM6CVZ5 Attention deficit hyperactivity disorder 6A05.Z Phase 2 [22]
ABT-288 DM7X54F Alzheimer disease 8A20 Phase 2 [23]
SAR-110894 DMCLEXM Alzheimer disease 8A20 Phase 2 [21]
ABT-652 DMLEO2Z Diabetic neuropathy 8C0Z Phase 2 [24]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By C-C motif chemokine 2 (CCL2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [25]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [26]
Gefitinib DM15F0X Colon adenocarcinoma Approved [27]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [28]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [29]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [30]
TECFIDERA DM2OVDT Multiple sclerosis 8A40 Approved [31]
Methotrexate DM2TEOL Anterior urethra cancer Approved [32]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [33]
Quercetin DM3NC4M Obesity 5B81 Approved [34]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Pro-interleukin-16 (IL16)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [32]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [35]
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [5]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [36]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [37]
Ethanol DMDRQZU Chronic pain MG30 Approved [38]
Menthol DMG2KW7 Back pain ME84.Z Approved [39]
Sodium lauryl sulfate DMLJ634 Constipation DD91.1 Approved [40]
Melphalan DMOLNHF Hematologic disease 3C0Z Approved [41]
Gemcitabine DMSE3I7 Anterior urethra cancer Approved [42]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H3 receptor (H3R) TT9JNIC HRH3_HUMAN Antagonist [2]
Histamine H4 receptor (H4R) TTXJ178 HRH4_HUMAN Agonist [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
C-C motif chemokine 2 (CCL2) OTAD2HEL CCL2_HUMAN Gene/Protein Processing [4]
Pro-interleukin-16 (IL16) OTZ2MO6B IL16_HUMAN Gene/Protein Processing [5]

References

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2 The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20.
3 Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR s... Bioorg Med Chem. 2009 Jun 1;17(11):3987-94.
4 Histamine downregulates monocyte CCL2 production through the histamine H4 receptor. J Allergy Clin Immunol. 2007 Aug;120(2):300-7. doi: 10.1016/j.jaci.2007.03.024. Epub 2007 May 15.
5 Histamine h(4) and h(2) receptors control histamine-induced interleukin-16 release from human CD8(+) T cells. J Pharmacol Exp Ther. 2002 Oct;303(1):300-7. doi: 10.1124/jpet.102.036939.
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9 Role of histamine in short- and long-term effects of methamphetamine on the developing mouse brain. J Neurochem. 2008 Nov;107(4):976-86.
10 Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor. Bioorg Med Chem. 2010 Jul 15;18(14):5441-8.
11 Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first pote... J Pharmacol Exp Ther. 2005 Sep;314(3):1310-21.
12 Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. J Pharmacol Exp Ther. 2001 Oct;299(1):121-30.
13 Histamine excites neonatal rat sympathetic preganglionic neurons in vitro via activation of H1 receptors. J Neurophysiol. 2006 Apr;95(4):2492-500.
14 Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening. J Med Chem. 2008 Jun 12;51(11):3145-53.
15 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
16 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
17 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
18 Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61.
19 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
20 JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats. Psychopharmacology (Berl). 2011 Apr;214(4):829-41.
21 SAR110894, a potent histamine H receptor antagonist, displays procognitive effects in rodents. Pharmacol Biochem Behav. 2012 Aug;102(2):203-14.
22 Randomized clinical study of a histamine H3 receptor antagonist for the treatment of adults with attention-deficit hyperactivity disorder. CNS Drugs. 2012 May 1;26(5):421-34.
23 A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia.J Alzheimers Dis.2014;42(3):959-71.
24 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032225)
25 Some HIV antiretrovirals increase oxidative stress and alter chemokine, cytokine or adiponectin production in human adipocytes and macrophages. Antivir Ther. 2007;12(4):489-500.
26 Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
27 Crosstalk between alveolar macrophages and alveolar epithelial cells/fibroblasts contributes to the pulmonary toxicity of gefitinib. Toxicol Lett. 2021 Mar 1;338:1-9. doi: 10.1016/j.toxlet.2020.11.011. Epub 2020 Nov 25.
28 Oxidative Stress Alters miRNA and Gene Expression Profiles in Villous First Trimester Trophoblasts. Biomed Res Int. 2015;2015:257090. doi: 10.1155/2015/257090. Epub 2015 Aug 3.
29 Cannabidiol selectively modulates interleukin (IL)-1 and IL-6 production in toll-like receptor activated human peripheral blood monocytes. Toxicology. 2021 Dec;464:153016. doi: 10.1016/j.tox.2021.153016. Epub 2021 Nov 2.
30 Monitoring of deiodinase deficiency based on transcriptomic responses in SH-SY5Y cells. Arch Toxicol. 2013 Jun;87(6):1103-13. doi: 10.1007/s00204-013-1018-4. Epub 2013 Feb 10.
31 Dimethyl Fumarate Inhibits the Nuclear Factor B Pathway in Breast Cancer Cells by Covalent Modification of p65 Protein. J Biol Chem. 2016 Feb 12;291(7):3639-47. doi: 10.1074/jbc.M115.679704. Epub 2015 Dec 18.
32 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
33 Simvastatin reduces expression of cytokines interleukin-6, interleukin-8, and monocyte chemoattractant protein-1 in circulating monocytes from hypercholesterolemic patients. Arterioscler Thromb Vasc Biol. 2002 Jul 1;22(7):1194-9. doi: 10.1161/01.atv.0000022694.16328.cc.
34 Plant polyphenols differentially modulate inflammatory responses of human keratinocytes by interfering with activation of transcription factors NFB and AhR and EGFR-ERK pathway. Toxicol Appl Pharmacol. 2011 Sep 1;255(2):138-49.
35 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
36 Identification of vitamin D3 target genes in human breast cancer tissue. J Steroid Biochem Mol Biol. 2016 Nov;164:90-97.
37 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
38 Alcohol and Cannabinoids Differentially Affect HIV Infection and Function of Human Monocyte-Derived Dendritic Cells (MDDC). Front Microbiol. 2015 Dec 22;6:1452. doi: 10.3389/fmicb.2015.01452. eCollection 2015.
39 Repurposing L-menthol for systems medicine and cancer therapeutics? L-menthol induces apoptosis through caspase 10 and by suppressing HSP90. OMICS. 2016 Jan;20(1):53-64.
40 The THP-1 cell toolbox: a new concept integrating the key events of skin sensitization. Arch Toxicol. 2019 Apr;93(4):941-951.
41 Bone marrow osteoblast damage by chemotherapeutic agents. PLoS One. 2012;7(2):e30758. doi: 10.1371/journal.pone.0030758. Epub 2012 Feb 17.
42 Metronomic gemcitabine suppresses tumour growth, improves perfusion, and reduces hypoxia in human pancreatic ductal adenocarcinoma. Br J Cancer. 2010 Jun 29;103(1):52-60.