General Information of Drug (ID: DMZVBPG)

Drug Name
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole Drug Info
Synonyms 4-(2-(4-tert-butylphenylthio)ethyl)-1H-imidazole; 4-(2-(40-tert-butylphenylthio)ethyl)-1H-imidazole
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
46222048
TTD Drug ID
DMZVBPG

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
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 [4]
JNJ-38518168 DM9UMIO Plaque psoriasis EA90.0 Phase 2 [5]
UR-63325 DME6X27 Allergic rhinitis CA08.0 Phase 2 [6]
Thioperamide DM8S593 Cognitive impairment 6D71 Terminated [7]
impromidine DMTDRPM Discovery agent N.A. Investigative [8]
burimamide DMZ2VYG Discovery agent N.A. Investigative [9]
Imetit DMMJ6NS Discovery agent N.A. Investigative [10]
[125I]iodophenpropit DMN4ABU Discovery agent N.A. Investigative [11]
(R)-alpha-methylhistamine DMKAW4P Discovery agent N.A. Investigative [12]
N-[3H]alpha-methylhistamine DMWDCV1 Discovery agent N.A. Investigative [13]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Curcumin DMQPH29 Solid tumour/cancer 2A00-2F9Z Phase 3 [14]
PMX-53 DMZUAJ4 Atopic dermatitis EA80 Phase 2 [15]
BMS-536924 DMXJB4N Discovery agent N.A. Investigative [16]
Heme DMGC287 Discovery agent N.A. Investigative [17]
ML-3163 DM3S5UC Discovery agent N.A. Investigative [18]
6-(3-Hydroxy-phenyl)-naphthalen-2-ol DMH8WA2 Discovery agent N.A. Investigative [19]
ML-3375 DMXJY6W Discovery agent N.A. Investigative [18]
ML-3403 DMTQWI8 Discovery agent N.A. Investigative [18]
4-[5-(3-Hydroxyphenyl)-3-thienyl]-2-methylphenol DM7ERYJ Discovery agent N.A. Investigative [20]
2-Fluoro-4-[5-(3-hydroxyphenyl)-2-thienyl]phenol DMUGAT8 Discovery agent N.A. Investigative [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glutethimide DMGE0CW Insomnia 7A00-7A0Z Approved [21]
ISOQUINE DMR17YI Malaria 1F40-1F45 Phase 1 [22]
ICI-199441 DMEWZ80 Discovery agent N.A. Investigative [23]
ML-3163 DM3S5UC Discovery agent N.A. Investigative [18]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide DM0XDG6 Discovery agent N.A. Investigative [24]
4-[5-(3-Hydroxyphenyl)-3-thienyl]-2-methylphenol DM7ERYJ Discovery agent N.A. Investigative [20]
2-Fluoro-4-[5-(3-hydroxyphenyl)-2-thienyl]phenol DMUGAT8 Discovery agent N.A. Investigative [20]
4-[5-(3-Hydroxyphenyl)-2-thienyl)-2-methyl]phenol DMK4ICB Discovery agent N.A. Investigative [20]
4-[2-(4-Imidazol-1-yl-phenoxy)-ethyl]-morpholine DM9UGO0 Discovery agent N.A. Investigative [25]
DIHYDROCUBEBIN DMZL7R6 Discovery agent N.A. Investigative [26]
⏷ 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 [27]
SUVN-G3031 DM3BO8G Cognitive impairment 6D71 Phase 3 [28]
JNJ-17216498 DM1GRCU Narcolepsy 7A20 Phase 2 [29]
GSK239512 DMBJMZC Alzheimer disease 8A20 Phase 2 [30]
JNJ-39220675 DM0WY3H Alcohol dependence 6C40.2 Phase 2 [31]
AZD-5213 DMOZ04X Alzheimer disease 8A20 Phase 2 [32]
Bavisant DM6CVZ5 Attention deficit hyperactivity disorder 6A05.Z Phase 2 [33]
ABT-288 DM7X54F Alzheimer disease 8A20 Phase 2 [34]
SAR-110894 DMCLEXM Alzheimer disease 8A20 Phase 2 [32]
ABT-652 DMLEO2Z Diabetic neuropathy 8C0Z Phase 2 [35]
⏷ 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
Albendazole monooxygenase (CYP3A4) TTXV4FI CP3A4_HUMAN Inhibitor [2]
Debrisoquine 4-hydroxylase (CYP2D6) TTVG215 CP2D6_HUMAN Inhibitor [2]
Histamine H3 receptor (H3R) TT9JNIC HRH3_HUMAN Inhibitor [1]
Histamine H4 receptor (H4R) TTXJ178 HRH4_HUMAN Inhibitor [3]

References

1 Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain. J Med Chem. 2010 Sep 9;53(17):6445-56.
2 Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active hi... J Med Chem. 2010 May 13;53(9):3840-4.
3 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.
4 Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6596-602.
5 The histamine H4 receptor: from orphan to the clinic. Front Pharmacol. 2015; 6: 65.
6 Azines as histamine H4 receptor antagonists. Front Biosci (Schol Ed). 2012 Jan 1;4:967-87.
7 Role of histamine in short- and long-term effects of methamphetamine on the developing mouse brain. J Neurochem. 2008 Nov;107(4):976-86.
8 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.
9 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.
10 Histamine excites neonatal rat sympathetic preganglionic neurons in vitro via activation of H1 receptors. J Neurophysiol. 2006 Apr;95(4):2492-500.
11 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.
12 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
13 Histamine induces cytoskeletal changes in human eosinophils via the H(4) receptor. Br J Pharmacol. 2003 Nov;140(6):1117-27.
14 Structure-activity relationships for the inhibition of recombinant human cytochromes P450 by curcumin analogues. Eur J Med Chem. 2008 Aug;43(8):1621-31.
15 Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92.
16 Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)py... J Med Chem. 2008 Oct 9;51(19):5897-900.
17 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
18 Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J Med Chem. 2003 Jul 17;46(15):3230-44.
19 Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors... J Med Chem. 2008 Apr 10;51(7):2158-69.
20 New insights into the SAR and binding modes of bis(hydroxyphenyl)thiophenes and -benzenes: influence of additional substituents on 17beta-hydroxyst... J Med Chem. 2009 Nov 12;52(21):6724-43.
21 A study of the effects of large doses of glutethimide that were used for self-poisoning during pregnancy on human fetuses. Toxicol Ind Health. 2008 Feb-Mar;24(1-2):69-78.
22 Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for ... J Med Chem. 2009 Mar 12;52(5):1408-15.
23 Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity. Bioorg Med Chem Lett. 2005 May 16;15(10):2647-52.
24 Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) b... J Med Chem. 2009 Sep 24;52(18):5685-702.
25 Imidazole derivatives as new potent and selective 20-HETE synthase inhibitors. Bioorg Med Chem Lett. 2004 Jan 19;14(2):333-6.
26 Potent CYP3A4 inhibitory constituents of Piper cubeba. J Nat Prod. 2005 Jan;68(1):64-8.
27 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
28 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
29 Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61.
30 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
31 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.
32 SAR110894, a potent histamine H receptor antagonist, displays procognitive effects in rodents. Pharmacol Biochem Behav. 2012 Aug;102(2):203-14.
33 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.
34 A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia.J Alzheimers Dis.2014;42(3):959-71.
35 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032225)