Protein detail

HRH1

Histamine H1 receptor (H1-R) (H1R) (HH1R)

Entry name HRH1	UniProt ID P35367	EVMP confidence score 0.63
Supporting publications (n) 6	Transmembrane count 7	Protein classification FDA approved drug targetsG-protein coupled receptorsPredicted intracellular proteinsPredicted membrane proteins

EVMP confidence score

Annotation confidence score; open for threshold definitions.

Extremely high >= 0.85High >= 0.70Medium >= 0.55Low >= 0.40

Basic Information12

Protein Names

Histamine H1 receptor (H1-R) (H1R) (HH1R)

Protein Class (4)

FDA approved drug targetsG-protein coupled receptorsPredicted intracellular proteinsPredicted membrane proteins

Protein Function (3)

FDA approved drug targets:Small molecule drugs
Predicted intracellular proteins
G-protein coupled receptors:GPCRs excl olfactory receptors

Transmembrane

30..50; Helical; Name=1; 65..89; Helical; Name=2; 98..123; Helical; Name=3; 145..164; Helical; Name=4; 189..211; Helical; Name=5; 417..440; Helical; Name=6; 447..469; Helical; Name=7

Transmembrane Count

Ensembl

ENSG00000196639

Entrez Gene Symbol

HRH1

Gene Description

Histamine receptor H1

Chromosome

Position

11137093-11263557

Supporting publications (n)

EVMP confidence score

0.63

Fluorescence & Localization1

Function & Pathway7

Protein Function (3)

FDA approved drug targets:Small molecule drugs
Predicted intracellular proteins
G-protein coupled receptors:GPCRs excl olfactory receptors

Cellular Component (4)

Molecular Function

GO:0004969 histamine receptor activity

Biological Process (3)

KEGG (4)

Reactome (5)

Mediation Categories (2)

Clinical-translation mediationReceptor-signaling mediation

Relations & Evidence78

Enzyme-Mediated Modification (14)

14 records.

Substrate Gene Symbol	Enzyme Gene Symbol	Enzyme UniProt ID	Residue Type	Residue Offset	Modification	Database	References
HRH1	PRKACA	P17612	S	396	phosphorylation	SIGNOR_ProtMapperSIGNORProtMapper	ProtMapper:15328002 SIGNOR:15328002
HRH1	PRKACA	P17612	S	398	phosphorylation	phosphoELM_MIMPPhosphoSite_MIMPMIMPSIGNORProtMapperSIGNOR_ProtMapperPhosphoSitePhosphoSite_ProtMapper	ProtMapper:15328002 SIGNOR:15328002
HRH1	PRKX	P51817	S	398	phosphorylation	MIMPphosphoELM_MIMPPhosphoSite_MIMP
HRH1	PRKY	O43930	S	398	phosphorylation	MIMPphosphoELM_MIMPPhosphoSite_MIMP

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Ligand-Receptor Signaling (48)

48 records.

Category	Parent	Database	Transmitter	Receiver	Secreted	Plasma Membrane (Transmembrane)	Plasma Membrane (Peripheral)
extracellular	extracellular	OmniPath	No	No	No	Yes	No
intracellular	intracellular	ComPPI	No	No	No	Yes	No
intracellular	intracellular	GO_Intercell	No	No	No	Yes	No
intracellular	intracellular	OmniPath	No	No	No	Yes	No
transmembrane	transmembrane	UniProt_location	No	No	No	Yes	No
transmembrane	transmembrane	UniProt_topology	No	No	No	Yes	No
transmembrane	transmembrane	UniProt_keyword	No	No	No	Yes	No
transmembrane	transmembrane	GO_Intercell	No	No	No	Yes	No
transmembrane	transmembrane	CellPhoneDB	No	No	No	Yes	No
transmembrane	transmembrane	TopDB	No	No	No	Yes	No

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Regulatory Interaction Network (15)

15 records.

Source Protein Symbol	Source UniProt ID	Target Protein Symbol	Target UniProt ID	Is Directed	Is Stimulation	Is Inhibition	Database	References
HRH1	P35367	GNAL	P38405	Yes	Yes	No	SIGNOR	SIGNOR:31160049
KGP1	Q13976	HRH1	P35367	Yes	No	Yes	phosphoELM_MIMPPhosphoSite_MIMPMIMPiPTMnetPhosphoPointSIGNORProtMapperPhosphoSite_KEAKEAphosphoELMSIGNOR_ProtMapperPhosphoSite_ProtMapper	SIGNOR:10101032 ProtMapper:10101032 KEA:15107581 phosphoELM:15107581 SIGNOR:15107581 ProtMapper:15107581 KEA:10101032
KCC2A	Q9UQM7	HRH1	P35367	Yes	No	Yes	phosphoELM_MIMPPhosphoSite_MIMPMIMPPhosphoSite_norefPhosphoPointSIGNORProtMapperiPTMnetPhosphoSite_KEAKEAphosphoELM_KEAphosphoELMSIGNOR_ProtMapperPhosphoSite_ProtMapper	KEA:15107581 phosphoELM:15107581 SIGNOR:15107581 ProtMapper:15107581 KEA:10101032
HRH1	P35367	GNAI3	P08754	Yes	Yes	No	SIGNOR	SIGNOR:31160049
HRH1	P35367	GNAS3	O95467	Yes	Yes	No	SIGNOR	SIGNOR:31160049
HRH1	P35367	ALEX	P84996	Yes	Yes	No	SIGNOR	SIGNOR:31160049
HRH1	P35367	GNAS2	P63092	Yes	Yes	No	SIGNOR	SIGNOR:31160049
HRH1	P35367	GNAS1	Q5JWF2	Yes	Yes	No	SIGNOR	SIGNOR:31160049
KAPCA	P17612	HRH1	P35367	Yes	No	Yes	phosphoELM_MIMPPhosphoSite_MIMPMIMPiPTMnetSIGNORProtMapperSIGNOR_ProtMapperPhosphoSite_ProtMapper	ProtMapper:15328002 SIGNOR:15328002
HRH1	P35367	GNAO	P09471	Yes	Yes	No	SIGNOR	SIGNOR:31160049

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Isolation & Detection Technology (1)

1 record.

EV Isolation Method	Detection Method	Number of References	References
Differential UltracentrifugationSize Exclusion Chromatography	R SequencingMass spectrometry	2	38343172 40222457

Sequence, Structure & Domains11

Sequences

Length

487

Mass

55,784

Sequence

MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLRPENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKLYCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSRTDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFKRILHIRS

3D Structural Models

Helix

29..54; 62..78; 80..89; 97..130; 132..137; 141..155; 156..158; 159..163; 165..168; 169..171; 183..185; 188..198; 200..224; 411..441; 447..471; 473..484

Beta Strand

55..57; 90..92; 177..180; 442..444

3D Structure

Electron microscopy (2); X-ray crystallography (1)

Domain & Motif Annotations

Compositional Bias

238..261; Basic and acidic residues; 353..369; Polar residues

Domain (CC)

Histamine activates the receptor by forming hydrogen bonds with transmembrane domains 3 and 6, squashing the ligand-binding pocket on the extracellular side and opening the cavity for G-protein engagement on the intracellular side.

Region

107..112; Important for agonist binding; 238..291; Disordered; 345..379; Disordered; 424..428; Important for agonist binding

Protein Families

G-protein coupled receptor 1 family

Sequence Similarities

Belongs to the G-protein coupled receptor 1 family.

Clinical Relevance4

Disease Involvement

FDA approved drug targets

Drug Targets

FDA approved drug targets

Drugs (125)

HISTAMINE VAPITADINE MEQUITAZINE DESLORATADINE PYRILAMINE MALEATE TRIPELENNAMINE HYDROCHLORIDE AZATADINE MALEATE BUCLIZINE HYDROCHLORIDE DIMENHYDRINATE PROCHLORPERAZINE PEMIROLAST NULL BETAHISTINE MECLIZINE DIMETHINDENE GSK-1004723 DOXEPIN HYDROCHLORIDE BROMPHENIRAMINE METHOTRIMEPRAZINE KETOTIFEN FUMARATE BUCLIZINE DOXYLAMINE CETIRIZINE HYDROCHLORIDE DIPHENYLPYRALINE BENZQUINAMIDE THIETHYLPERAZINE ALCAFTADINE CHLORPHENIRAMINE POLISTIREX EMEDASTINE DIFUMARATE ACEPROMETAZINE HYDROXYZINE PYRILAMINE TRIPROLIDINE HYDROCHLORIDE DIPHENHYDRAMINE CITRATE TRAZODONE CHLORPHENIRAMINE MALEATE QUETIAPINE FUMARATE TERFENADINE ORPHENADRINE ACRIVASTINE CINNARIZINE PHENIRAMINE MALEATE HYDROXYZINE HYDROCHLORIDE NOBERASTINE OLANZAPINE DIPHENHYDRAMINE TRIPELENNAMINE TRIPROLIDINE BROMODIPHENHYDRAMINE MIZOLASTINE PROPIOMAZINE HYDROCHLORIDE ESMIRTAZAPINE MALEATE THENALIDINE AZELASTINE EPINASTINE HYDROCHLORIDE CHLOPHEDIANOL CYPROHEPTADINE HYDROCHLORIDE EBASTINE BEPOTASTINE BESILATE LEVOCETIRIZINE FLUNARIZINE METHDILAZINE BROMPHENIRAMINE MALEATE PROMETHAZINE HYDROCHLORIDE TRIMEPRAZINE TARTRATE TRIPELENNAMINE CITRATE TRIMIPRAMINE MALEATE EPINASTINE LY2624803 PROPIOMAZINE BIPERIDEN CLEMASTINE MIANSERIN TRIMEPRAZINE ANTAZOLINE ORPHENADRINE CITRATE AZELASTINE HYDROCHLORIDE MECLIZINE HYDROCHLORIDE DIPHENHYDRAMINE HYDROCHLORIDE OXATOMIDE PHENINDAMINE BILASTINE OLOPATADINE CYCLIZINE LEVOCABASTINE METHDILAZINE HYDROCHLORIDE RUPATADINE ASTEMIZOLE CLOZAPINE HYDROXYZINE PAMOATE DIBENZEPIN EMEDASTINE METHAPYRILENE HYDROCHLORIDE ASENAPINE FEXOFENADINE HYDROCHLORIDE PROMAZINE CHLORPROTHIXENE PHENIRAMINE DEXCHLORPHENIRAMINE MALEATE PROFENAMINE AZATADINE CARBINOXAMINE MALEATE CARBINOXAMINE METHAPYRILENE FUMARATE LORATADINE BROMODIPHENHYDRAMINE HYDROCHLORIDE DESIPRAMINE DOXYLAMINE SUCCINATE LEVOCABASTINE HYDROCHLORIDE CLEMASTINE FUMARATE CAREBASTINE CYCLIZINE LACTATE VAPITADINE DIHYDROCHLORIDE ANTAZOLINE PHOSPHATE ZIPRASIDONE CHLORPHENOXAMINE LY-2624803 CHEMBL:CHEMBL1923521 ORPHENADRINE HYDROCHLORIDE TOLAZOLINE HYDROCHLORIDE DIPHENYLPYRALINE HYDROCHLORIDE DEXBROMPHENIRAMINE MALEATE HISTAMINE PHOSPHATE TRANILAST ILOPERIDONE

Antibody

HPA029740

Supporting Publications6

PMID	Title	Abstract
31508500	Proteomic profiling of extracellular vesicles allows for human breast cancer subtyping.	No abstract available
31685984	Tumour exosomal CEMIP protein promotes cancer cell colonization in brain metastasis.	Proteomic analysis identified cell migration-inducing and hyaluronan-binding protein (CEMIP) as elevated in exosomes from brain metastatic but not lung or bone metastatic cells.
32795414	Extracellular Vesicle and Particle Biomarkers Define Multiple Human Cancers.	Among traditional exosome markers, CD9, HSPA8, ALIX, and HSP90AB1 represent pan-EVP markers, while ACTB, MSN, and RAP1B are novel pan-EVP markers.
40091455	Potential Role of Menstrual Fluid-Derived Small Extracellular Vesicle Proteins in Endometriosis Pathogenesiss.	No abstract available
40098346	Toward Identification of Markers for Brain-Derived Extracellular Vesicles in Cerebrospinal Fluid: A Large-Scale, Unbiased Analysis Using Proximity Extension Assays.	No abstract available
40784529	Serum-derived exosome proteomics unveils the distinct and adjustable nature of the dampness constitution in traditional Chinese medicine.	No abstract available