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

General Information of Drug (ID: DMROD7Q)

Drug Name

A-943931 Drug Info

Synonyms

UNII-Q598HK01AO; A-943931; Q598HK01AO; 1027330-97-7; SCHEMBL602812; CHEMBL502347; BDBM26396; MolPort-035-936-414; SDTRYHWIXVHTLM-GFCCVEGCSA-N; ZINC40977166; NCGC00370827-02; 5H-Benzo(6,7)cyclohepta(1,2-d)pyrimidin-2-amine, 4-((3R)-3-amino-1-pyrrolidinyl)-6,7-dihydro-; 2,4-diamino-5,6-disubstituted pyrimidine, 10; 6-[(3R)-3-aminopyrrolidin-1-yl]-3,5-diazatricyclo[9.4.0.0^{2,7}]pentadeca-1(15),2(7),3,5,11,13-hexaen-4-amine

Indication

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

Cross-matching ID

PubChem CID: 25068753
CAS Number: CAS 1027330-97-7
TTD Drug ID: DMROD7Q

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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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]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

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

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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.