DGIdb - HRH4 Gene Record

HRH4 59340 Druggable Genome

Alternate Names:

59340
HISTAMINE RECEPTOR H4
HRH4
AXOR35
BG26
GPCR105
GPRv53
H4
H4R
HH4R
606792
17383
ENSG00000134489
OTTHUMG00000131945
265
H<sub>4</sub> receptor
Q9H3N8
NP_067637
NM_021624
HRH4_HUMAN
BE0000146
HISTAMINE H4 RECEPTOR (HH4R) (GPRV53) (G-PROTEIN COUPLED RECEPTOR 105) (GPCR105) (SP9144) (AXOR35). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9H3N8]
SP9144
Pfi-013
G-protein coupled receptor 105
Histamine H4 receptor
PA134982275
T26500

Gene Info:

GuideToPharmacology Gene Category Name	Histamine receptors
GuideToPharmacology Gene Category ID	33
GuideToPharmacology Gene Type	gpcr
Target Main Class	Receptors
Target Subclass	GPCR
Transmembrane Helix Count	7
Target Subclass	Rhodopsin
Human Readable Name	DRUGGABLE GENOME
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Uniprot Evidence	1: Evidence at protein level
Interpro Name	GPCR, rhodopsin-like, 7TM
Uniprot Status	Swiss-Prot
Interpro Acc	IPR000276
Interpro Short Name	7TM_GPCR_Rhodpsn
Interpro Type	Family
Target Class	Receptors
Gene Biotype	PROTEIN_CODING

(12 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Blaya et al., 2010, Histamine and histamine receptor antagonists in cancer biology., Inflamm Allergy Drug Targets
Cowden et al., 2010, Histamine H4 receptor antagonism diminishes existing airway inflammation and dysfunction via modulation of Th2 cytokines., Respir. Res.
Yu et al., 2010, Copy number variations of the human histamine H4 receptor gene are associated with systemic lupus erythematosus., Br. J. Dermatol.
Smits RA et al., 2008, Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach., J Med Chem
Smits RA et al., 2010, Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists., J Med Chem
Nguyen et al., 2001, Discovery of a novel member of the histamine receptor family., Mol. Pharmacol.
Thurmond RL, 2015, The histamine H4 receptor: from orphan to the clinic., Front Pharmacol
Mowbray CE et al., 2011, 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
Wei Z et al., 2013, Histamine H4 receptor polymorphism: a potential predictor of risperidone efficacy., J Clin Psychopharmacol
Lim et al., 2005, Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist., J. Pharmacol. Exp. Ther.
Smits et al., 2006, Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives., J. Med. Chem.
Sugata et al., 2007, Histamine H4 receptor agonists have more activities than H4 agonism in antigen-specific human T-cell responses., Immunology
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Adachi et al., 2006, Suppression of ischemia/reperfusion liver injury by histamine H4 receptor stimulation in rats., Eur. J. Pharmacol.
Connelly WM et al., 2009, The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS., Br J Pharmacol
Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)
Wade L et al., 2012, Ophthalmic antihistamines and H1-H4 receptors., Curr Opin Allergy Clin Immunol
de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

TOREFORANT HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H4 receptor antagonist

Direct Interaction? False

Publications:

Thurmond RL, 2015, The histamine H4 receptor: from orphan to the clinic., Front Pharmacol

THIOPERAMIDE HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Details of Interaction Selective for H3/H4 compared to H1 and H3.

Endogenous Drug? False

Publications:

Smits RA et al., 2010, Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists., J Med Chem

Smits RA et al., 2008, Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach., J Med Chem

PF-03893787 HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:

Mowbray CE et al., 2011, 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
CLOBENPROPIT HRH4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? False

Publications:
PITOLISANT HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:
chembl:CHEMBL185951 HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
IMETIT HRH4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
4-METHYLHISTAMINE HRH4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? False

Publications:
BURIMAMIDE HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
METHIMEPIP HRH4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Publications:
CONESSINE HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:
2-METHYLHISTAMINE HRH4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
IMPROGAN HRH4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
IMMEPIP HRH4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
N-METHYLHISTAMINE HRH4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Publications:
CIPROXIFAN HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:
UR-63325 HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H4 receptor antagonist

Direct Interaction yes

Publications:
MK-0249 HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:
IMPROMIDINE HRH4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Publications:
IODOPHENPROPIT HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
DIMAPRIT HRH4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:

HISTAMINE HRH4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? True

Publications:

Blaya et al., 2010, Histamine and histamine receptor antagonists in cancer biology., Inflamm Allergy Drug Targets

Cowden et al., 2010, Histamine H4 receptor antagonism diminishes existing airway inflammation and dysfunction via modulation of Th2 cytokines., Respir. Res.

Yu et al., 2010, Copy number variations of the human histamine H4 receptor gene are associated with systemic lupus erythematosus., Br. J. Dermatol.

CHLORPROMAZINE HRH4

Interaction Types & Directionality:

binder

Interaction Info:

Publications:

Nguyen et al., 2001, Discovery of a novel member of the histamine receptor family., Mol. Pharmacol.

AMOXAPINE HRH4

Interaction Types & Directionality:

binder

Interaction Info:

Publications:

Lim et al., 2005, Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist., J. Pharmacol. Exp. Ther.

CLOZAPINE HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Trial Name -

Publications:

Smits et al., 2006, Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives., J. Med. Chem.

Sugata et al., 2007, Histamine H4 receptor agonists have more activities than H4 agonism in antigen-specific human T-cell responses., Immunology

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

AMITRIPTYLINE HRH4

Interaction Types & Directionality:

binder

Interaction Info:

Publications:

Nguyen et al., 2001, Discovery of a novel member of the histamine receptor family., Mol. Pharmacol.

Connelly WM et al., 2009, The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS., Br J Pharmacol

OLANZAPINE HRH4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)
PHENIRAMINE HRH4

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Publications:

Wade L et al., 2012, Ophthalmic antihistamines and H1-H4 receptors., Curr Opin Allergy Clin Immunol
ARIPIPRAZOLE HRH4

Interaction Types & Directionality:

ligand

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
DOXEPIN HRH4

Interaction Types & Directionality:

binder

Interaction Info:

Publications:
MIANSERIN HRH4

Interaction Types & Directionality:

binder

Interaction Info:

Publications:
LOXAPINE HRH4

Interaction Types & Directionality:

binder

Interaction Info:

Publications:
JNJ-7777120 HRH4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Mowbray CE et al., 2011, 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
RISPERIDONE HRH4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Wei Z et al., 2013, Histamine H4 receptor polymorphism: a potential predictor of risperidone efficacy., J Clin Psychopharmacol
chembl:CHEMBL452847 HRH4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Smits RA et al., 2008, Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach., J Med Chem
chembl:CHEMBL454890 HRH4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Smits RA et al., 2008, Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach., J Med Chem
chembl:CHEMBL502347 HRH4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL494678 HRH4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ensembl: ENSG00000134489
- Version: 101_38
Alternate Names:

HRH4 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:

RussLampel: ENSG00000134489

Version: 26-July-2011

Alternate Names:

ENSG00000134489 Ensembl Gene Id

HISTAMINE H4 RECEPTOR (HH4R) (GPRV53) (G-PROTEIN COUPLED RECEPTOR 105) (GPCR105) (SP9144) (AXOR35). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9H3N8] Description

HRH4 Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

TEND: Q9H3N8
- Version: 01-August-2011
Alternate Names:

59340 Entrez Gene Id

Q9H3N8 Uniprot Accession

HRH4_HUMAN Uniprot Id

Gene Info:

Target Main Class Receptors

Target Subclass GPCR

Transmembrane Helix Count 7

Publications:
GuideToPharmacologyGenes: 265
- Version: 4-March-2015
Alternate Names:

histamine receptor H4 HUGO Gene Name

17383 HUGO Gene ID

HRH4 Gene Symbol

Gene Info:

GuideToPharmacology Gene Category Name Histamine receptors

GuideToPharmacology Gene Category ID 33

GuideToPharmacology Gene Type gpcr

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
HopkinsGroom: Q9H3N8
- Version: 11-September-2012
Alternate Names:

Q9H3N8 Uniprot Accession

HISTAMINE H4 RECEPTOR Uniprot Protein Name

59340 Entrez Gene Id

Gene Info:

Human Readable Name G PROTEIN COUPLED RECEPTOR

Uniprot Evidence 1: Evidence at protein level

Human Readable Name DRUGGABLE GENOME

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: Q9H3N8
- Version: January-2014
Alternate Names:

HRH4 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
PharmGKB: HRH4
- Version: 18-August-2020
Alternate Names:

PA134982275 PharmGKB ID

Gene Info:

Publications:

Wei Z et al., 2013, Histamine H4 receptor polymorphism: a potential predictor of risperidone efficacy., J Clin Psychopharmacol
TTD: Histamine H4 receptor
- Version: 2020.06.01
Alternate Names:

H4R TTD Gene Abbreviation

T26500 TTD Target ID

Gene Info:

Publications:

Thurmond RL, 2015, The histamine H4 receptor: from orphan to the clinic., Front Pharmacol

DrugBank: BE0000146

Version: 5.1.7

Alternate Names:

HRH4 DrugBank Gene Name

Q9H3N8 UniProt Accession

59340 Entrez Gene Id

Gene Info:

Publications:

Sugata et al., 2007, Histamine H4 receptor agonists have more activities than H4 agonism in antigen-specific human T-cell responses., Immunology

Adachi et al., 2006, Suppression of ischemia/reperfusion liver injury by histamine H4 receptor stimulation in rats., Eur. J. Pharmacol.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

DTC: HRH4

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Smits RA et al., 2010, Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists., J Med Chem

Smits RA et al., 2008, Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach., J Med Chem

Mowbray CE et al., 2011, 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

ChemblInteractions: GPCR105
- Version: chembl_23
Alternate Names:

GPCR105 GENE_SYMBOL

HRH4 GENE_SYMBOL

Histamine H4 receptor UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000134489
- Version: 31-May-2017
Alternate Names:

ENSG00000134489 Gene Symbol

HRH4 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
GuideToPharmacologyInteractions: ENSG00000134489
- Version: 20-July-2020
Alternate Names:

H4 receptor GuideToPharmacology Name

Q9H3N8 UniProtKB ID

Gene Info:

Publications:
Pharos: HRH4
- Version: 03-September-2020
Alternate Names:

Histamine H4 receptor Gene Name

Q9H3N8 UniProt ID

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
GO: HRH4
- Version: 05-September-2020
Alternate Names:

GPCR105 GO Gene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
dGene: HRH4
- Version: 27-Jun-2013
Alternate Names:

59340 Gene ID

AXOR35 dGene Synonym

BG26 dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

Direct Interaction	yes
Mechanism of Interaction	Histamine H4 receptor antagonist
Direct Interaction?	False

Specific Action of the Ligand	Antagonist
Details of Interaction	Selective for H<sub>3</sub>/H<sub>4</sub> compared to H<sub>1</sub> and H<sub>3</sub>.
Endogenous Drug?	False

Specific Action of the Ligand	Partial agonist
Endogenous Drug?	False
Direct Interaction?	False

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False

ENSG00000134489	Ensembl Gene Id
HISTAMINE H4 RECEPTOR (HH4R) (GPRV53) (G-PROTEIN COUPLED RECEPTOR 105) (GPCR105) (SP9144) (AXOR35). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9H3N8]	Description
HRH4	Display Id

59340	Entrez Gene Id
Q9H3N8	Uniprot Accession
HRH4_HUMAN	Uniprot Id

histamine receptor H4	HUGO Gene Name
17383	HUGO Gene ID
HRH4	Gene Symbol

HRH4	DrugBank Gene Name
Q9H3N8	UniProt Accession
59340	Entrez Gene Id

GPCR105	GENE_SYMBOL
HRH4	GENE_SYMBOL
Histamine H4 receptor	UNIPROT

H<sub>4</sub> receptor	GuideToPharmacology Name
Q9H3N8	UniProtKB ID

HRH4 Gene Record

HRH4 59340 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Histamine H4 receptor antagonist Direct Interaction? False

Publications: Thurmond RL, 2015, The histamine H4 receptor: from orphan to the clinic., Front Pharmacol

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Details of Interaction Selective for H<sub>3</sub>/H<sub>4</sub> compared to H<sub>1</sub> and H<sub>3</sub>. Endogenous Drug? False

Publications: Smits RA et al., 2010, Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists., J Med Chem Smits RA et al., 2008, Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach., J Med Chem

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

Publications: Mowbray CE et al., 2011, 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

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Partial agonist Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Full agonist

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Full agonist

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H4 receptor antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Partial agonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? True

Interaction Types & Directionality: binder

Interaction Info:

Publications: Nguyen et al., 2001, Discovery of a novel member of the histamine receptor family., Mol. Pharmacol.

Interaction Types & Directionality: binder

Interaction Info:

Publications: Lim et al., 2005, Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Antagonist Trial Name -

Interaction Types & Directionality: binder

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H4 receptor antagonist

Direct Interaction? False

Publications:

Thurmond RL, 2015, The histamine H4 receptor: from orphan to the clinic., Front Pharmacol

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Details of Interaction Selective for H<sub>3</sub>/H<sub>4</sub> compared to H<sub>1</sub> and H<sub>3</sub>.

Endogenous Drug? False

Publications:

Smits RA et al., 2010, Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists., J Med Chem

Smits RA et al., 2008, Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach., J Med Chem

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:

Mowbray CE et al., 2011, 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

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H4 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? True

Interaction Types & Directionality:

binder

Publications:

Nguyen et al., 2001, Discovery of a novel member of the histamine receptor family., Mol. Pharmacol.

Interaction Types & Directionality:

binder

Publications:

Lim et al., 2005, Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Trial Name -

Interaction Types & Directionality:

binder

Publications:

Nguyen et al., 2001, Discovery of a novel member of the histamine receptor family., Mol. Pharmacol.

Connelly WM et al., 2009, The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS., Br J Pharmacol

Interaction Types & Directionality:

antagonist (inhibitory)

Publications:

Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)

Interaction Types & Directionality:

inverse agonist (inhibitory)

Publications:

Wade L et al., 2012, Ophthalmic antihistamines and H1-H4 receptors., Curr Opin Allergy Clin Immunol

Interaction Types & Directionality:

ligand

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

binder

Interaction Types & Directionality:

binder

Interaction Types & Directionality:

binder

Interaction Types & Directionality:

n/a

Publications:

Mowbray CE et al., 2011, 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

Interaction Types & Directionality:

n/a

Publications:

Wei Z et al., 2013, Histamine H4 receptor polymorphism: a potential predictor of risperidone efficacy., J Clin Psychopharmacol

Interaction Types & Directionality:

n/a

Publications:

Smits RA et al., 2008, Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Smits RA et al., 2008, Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach., J Med Chem