Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM5TDEW)

• Drug Name: A-846714 Drug Info
• Synonyms: JMC516547 Compound 2; A-846714; 2-Aminopyrimidine analog., 4; SCHEMBL2166660; CHEMBL494678; BDBM26229

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 25130235
  TTD Drug ID: DM5TDEW

Molecule-Related Drug Atlas

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	[2]
JNJ-38518168	DM9UMIO	Plaque psoriasis	EA90.0	Phase 2	[3]
UR-63325	DME6X27	Allergic rhinitis	CA08.0	Phase 2	[4]
Thioperamide	DM8S593	Cognitive impairment	6D71	Terminated	[5]
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole	DMZVBPG	Discovery agent	N.A.	Investigative	[6]
impromidine	DMTDRPM	Discovery agent	N.A.	Investigative	[7]
burimamide	DMZ2VYG	Discovery agent	N.A.	Investigative	[8]
Imetit	DMMJ6NS	Discovery agent	N.A.	Investigative	[9]
[125I]iodophenpropit	DMN4ABU	Discovery agent	N.A.	Investigative	[10]
(R)-alpha-methylhistamine	DMKAW4P	Discovery agent	N.A.	Investigative	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H4 receptor (H4R)	TTXJ178	HRH4_HUMAN	Inhibitor	[1]

References

• [1] Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and... J Med Chem. 2008 Oct 23;51(20):6547-57.
• [2] 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.
• [3] The histamine H4 receptor: from orphan to the clinic. Front Pharmacol. 2015; 6: 65.
• [4] Azines as histamine H4 receptor antagonists. Front Biosci (Schol Ed). 2012 Jan 1;4:967-87.
• [5] Role of histamine in short- and long-term effects of methamphetamine on the developing mouse brain. J Neurochem. 2008 Nov;107(4):976-86.
• [6] 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.
• [7] 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.
• [8] 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.
• [9] Histamine excites neonatal rat sympathetic preganglionic neurons in vitro via activation of H1 receptors. J Neurophysiol. 2006 Apr;95(4):2492-500.
• [10] 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.
• [11] Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.