Protein detail

HRH1

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

Protein symbol HRH1	UniProt ID P35367	EVMP score 0.63
Frequency 6	Transmembrane count 7	Protein classification FDA approved drug targetsG-protein coupled receptorsPredicted intracellular proteinsPredicted membrane proteins

Basic Information

Protein Names

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

Protein Class

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

Protein Function

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

Frequency

EVMP Score

0.63

Fluorescence & Localization

Function & Pathway

Protein Function

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

Cellular Component

Molecular Function

GO:0004969 histamine receptor activity

Biological Process

KEGG

Reactome

Mediation Categories

Clinical-translation mediationReceptor-signaling mediation

Relations & Evidence

Enzyme-Mediated Modification

14 records.

Substrate Gene Symbol	Enzyme Gene Symbol	Enzyme UniProt ID	Residue Type	Residue Offset	Modification	Database	References
HRH1	PRKG1	Q13976	S	398	phosphorylation	phosphoELM_MIMPPhosphoSite_MIMPMIMPSIGNORProtMapperKEAphosphoELMSIGNOR_ProtMapperPhosphoSitePhosphoSite_ProtMapper	SIGNOR:10101032 ProtMapper:10101032 KEA:15107581 phosphoELM:15107581 SIGNOR:15107581 ProtMapper:15107581 KEA:10101032
HRH1	PRKG1	Q13976	S	396	phosphorylation	phosphoELM_MIMPPhosphoSite_MIMPMIMPProtMapperKEAphosphoELMPhosphoSitePhosphoSite_ProtMapper	KEA:15107581 phosphoELM:15107581
HRH1	PRKCA	P17252	S	398	phosphorylation	BEL-Large-Corpus_ProtMapperphosphoELM_MIMPPhosphoSite_MIMPMIMPSIGNORProtMapperKEAphosphoELMSIGNOR_ProtMapperPhosphoSitePhosphoSite_ProtMapper	SIGNOR:10101032 ProtMapper:15212693 ProtMapper:10101032 KEA:15107581 phosphoELM:15107581 SIGNOR:15107581 ProtMapper:15107581 phosphoELM:10101032 KEA:10101032
HRH1	PRKCA	P17252	S	396	phosphorylation	phosphoELM_MIMPPhosphoSite_MIMPMIMPProtMapperKEAphosphoELMPhosphoSitePhosphoSite_ProtMapper	KEA:15107581 phosphoELM:15107581
HRH1	PRKCA	P17252	T	478	phosphorylation	PhosphoNetworksphosphoELM_MIMPPhosphoSite_MIMPMIMPSIGNORProtMapperKEAphosphoELMSIGNOR_ProtMapperPhosphoSitePhosphoSite_ProtMapper	SIGNOR:15107581 ProtMapper:15107581 KEA:15107581 phosphoELM:15107581
HRH1	GRK2	P25098	S	398	phosphorylation	phosphoELM_MIMPPhosphoSite_MIMPMIMPProtMapperKEAphosphoELMPhosphoSitePhosphoSite_ProtMapper	KEA:15107581 phosphoELM:15107581 KEA:10101032
HRH1	CAMK2A	Q9UQM7	S	398	phosphorylation	phosphoELM_MIMPPhosphoSite_MIMPMIMPSIGNORProtMapperKEAphosphoELMSIGNOR_ProtMapperPhosphoSitePhosphoSite_ProtMapper	KEA:15107581 phosphoELM:15107581 SIGNOR:15107581 ProtMapper:15107581 KEA:10101032
HRH1	CAMK2A	Q9UQM7	S	396	phosphorylation	phosphoELM_MIMPPhosphoSite_MIMPMIMPProtMapperKEAphosphoELMPhosphoSitePhosphoSite_ProtMapper	KEA:15107581 phosphoELM:15107581
HRH1	CAMK2A	Q9UQM7	T	140	phosphorylation	phosphoELM_MIMPPhosphoSite_MIMPMIMPSIGNORProtMapperKEAphosphoELMSIGNOR_ProtMapperPhosphoSitePhosphoSite_ProtMapper	SIGNOR:15107581 ProtMapper:15107581 KEA:15107581 phosphoELM:15107581
HRH1	CAMK2A	Q9UQM7	T	142	phosphorylation	phosphoELM_MIMPPhosphoSite_MIMPMIMPProtMapperKEAphosphoELMPhosphoSitePhosphoSite_ProtMapper	KEA:15107581 phosphoELM:15107581

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Ligand-Receptor Signaling

48 records.

Category	Parent	Database	Transmitter	Receiver	Secreted	Plasma Membrane (Transmembrane)	Plasma Membrane (Peripheral)
seven_transmembrane_7tm	receptor	HPMR	No	Yes	No	Yes	No
7tm_a	receptor	HPMR	No	Yes	No	Yes	No
histamine_7tm_a	receptor	HPMR	No	Yes	No	Yes	No
rhodopsin	receptor	Surfaceome	No	Yes	No	Yes	No
gpcr	receptor	Surfaceome	No	Yes	No	Yes	No
class_a_rhodopsin	receptor	GPCRdb	No	Yes	No	Yes	No
class_a_rhodopsin_aminergic	receptor	GPCRdb	No	Yes	No	Yes	No
class_a_rhodopsin_aminergic_histamine	receptor	GPCRdb	No	Yes	No	Yes	No
receptor	receptor	OmniPath	No	Yes	No	Yes	No
extracellular	extracellular	HPMR	No	No	No	Yes	No

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Regulatory Interaction Network

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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Protein Complex Composition

0 records.

Isolation & Detection Technology

1 record.

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

Sequence, Structure & Domains

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 Relevance

Disease Involvement

FDA approved drug targets

Drug Targets

FDA approved drug targets

Drugs

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