Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

HRH1 (P35367) - Overview - Molecular Target Synopsis

Protein


HRH1, Histamine H1 receptor
UniProt P35367

Also Known as HRH1_HUMAN, HRH1

In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.

3RZE deposition date (2011-05-11)
STRUCTURE OF THE HUMAN HISTAMINE H1 RECEPTOR IN COMPLEX WITH DOXEPIN
RCSB/PDB
Inspect Structure
See all 3D Structures for HRH1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
487P35367-1
19ENSG00000196639ENST00000413416ENSP00000392383

Drugs


HRH1 is targeted by Approved Drugs Olopatadine, Diphenylpyraline, Desloratadine, Histamine, Emedastine, Chlorpheniramine, Pyrilamine, Cyclizine, Buclizine, Cetirizine, Cyproheptadine, Promethazine, Dimenhydrinate, Dexchlorpheniramine, Methdilazine, Bromodiphenhydramine, Triprolidine, Ketotifen, Methylpromazine, Mesoridazine, Acetophenazine, Mirtazapine, Carphenazine, Chlorpromazine, Antazoline, Loratadine, Carbinoxamine, Pheniramine, Astemizole, Azatadine, Hydroxyzine Pamoate, Dexbrompheniramine, Tripelennamine, Fexofenadine, Acrivastine, Meclizine, Azelastine, Alcaftadine, Hydroxyzine Hydrochloride, Quetiapine, Brompheniramine, Olanzapine, Diphenhydramine, Clemastine, Doxylamine. (see details)
Olopatadine
Diphenylpyraline
Desloratadine
Histamine
Emedastine
Chlorpheniramine
Pyrilamine
Cyclizine
Buclizine
Cetirizine
Cyproheptadine
Promethazine
Dimenhydrinate
Dexchlorpheniramine
Methdilazine
Bromodiphenhydramine
Triprolidine
Ketotifen
Methylpromazine
Mesoridazine
Acetophenazine
Mirtazapine
Carphenazine
Chlorpromazine
Antazoline
Loratadine
Carbinoxamine
Pheniramine
Astemizole
Azatadine
Hydroxyzine Pamoate
Dexbrompheniramine
Tripelennamine
Fexofenadine
Acrivastine
Meclizine
Azelastine
Alcaftadine
Hydroxyzine Hydrochloride
Quetiapine
Brompheniramine
Olanzapine
Diphenhydramine
Clemastine
Doxylamine

Sub-cellular localization


UniProt: HRH1 is active in the following subcellular-locations: cell membrane.
GO terms: HRH1 is active in the following subcellular-locations: cytosol, integral component of plasma membrane, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project HRH1 has gain in 4 cell-lines, loss in 3 cell-lines and no signal in 997 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SF_539, BT_549, HOP_62

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, NCI-H441, PK-59

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: NHLF, AG445, HUVEC

(see details)

RNA Interference


HRH1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: . (see details)

3D Structures


For HRH1 there are:
1 structures (1 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


HRH1 has been screened with 3164 compounds (4856 bioactivities), 852 compounds have bioactivities that show binding affinity of <= 500nM (1201 bioactivities). (see details)