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Target Report Card

Target Name and Classification

Target ID CHEMBL231
Target Type SINGLE PROTEIN
Preferred Name Histamine H1 receptor
Synonyms H1R | HH1R | HRH1 | Histamine H1 receptor
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > small molecule receptor (family a gpcr) > monoamine receptor > histamine receptor

Target Components

Component Description Relationship Accession
Histamine H1 receptor SINGLE PROTEIN P35367

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL296419 ASTEMIZOLE Histamine H1 receptor antagonist 4 PubMed
CHEMBL998 LORATADINE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1172 DESLORATADINE Histamine H1 receptor antagonist 4 DailyMed
CHEMBL1224 ACRIVASTINE Histamine H1 receptor antagonist 4 DailyMed
CHEMBL1564 DIPHENYLPYRALINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1620 DIPHENHYDRAMINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 PubMed PubMed
CHEMBL1633 KETOTIFEN FUMARATE Histamine H1 receptor antagonist 4 ISBN
CHEMBL1653 PHENIRAMINE MALEATE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1659 CHLORPHENIRAMINE MALEATE Histamine H1 receptor antagonist 4 PubMed PubMed
CHEMBL1689 TOLAZOLINE HYDROCHLORIDE Histamine H1 receptor agonist 4 DailyMed DailyMed ISBN PubMed PubMed
CHEMBL1716 CYPROHEPTADINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 ISBN
CHEMBL1719 OLOPATADINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 DailyMed
CHEMBL1200392 DOXYLAMINE SUCCINATE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200395 ORPHENADRINE CITRATE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200403 BUCLIZINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 KEGG PubMed
CHEMBL1200406 DIMENHYDRINATE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200446 TRIPELENNAMINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200450 TRIPROLIDINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200467 HYDROXYZINE PAMOATE Histamine H1 receptor antagonist 4 ISBN PubMed
CHEMBL1200491 EPINASTINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 DailyMed FDA
CHEMBL1200497 CYCLIZINE LACTATE Histamine H1 receptor antagonist 4 Other PubMed
CHEMBL1200532 METHDILAZINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200550 ANTAZOLINE PHOSPHATE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200590 MECLIZINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 DailyMed PubMed
CHEMBL1200618 FEXOFENADINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 DailyMed
CHEMBL1200638 DEXBROMPHENIRAMINE MALEATE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200750 PROMETHAZINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 DailyMed
CHEMBL1200769 TRIPELENNAMINE CITRATE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200795 CLEMASTINE FUMARATE Histamine H1 receptor antagonist 4 ISBN
CHEMBL1200801 HISTAMINE PHOSPHATE Histamine H1 receptor agonist 4 DailyMed
CHEMBL1200809 AZELASTINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 DailyMed FDA
CHEMBL1200927 DEXCHLORPHENIRAMINE MALEATE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200948 TRIMIPRAMINE MALEATE Histamine H1 receptor antagonist 4 ISBN
CHEMBL1200959 METHDILAZINE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200961 BROMPHENIRAMINE MALEATE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1200967 BROMODIPHENHYDRAMINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 PubMed PubMed
CHEMBL1200974 CARBINOXAMINE MALEATE Histamine H1 receptor antagonist 4 DailyMed FDA
CHEMBL1201006 PYRILAMINE MALEATE Histamine H1 receptor antagonist 4 PubMed
CHEMBL1201007 HYDROXYZINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 ISBN PubMed
CHEMBL1201023 ORPHENADRINE (CHLORIDE) Histamine H1 receptor antagonist 4 PubMed
CHEMBL1201068 PROPIOMAZINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 ISBN
CHEMBL1201089 DIPHENHYDRAMINE CITRATE Histamine H1 receptor antagonist 4 PubMed PubMed
CHEMBL1201113 CETIRIZINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 FDA
CHEMBL1201190 LEVOCETIRIZINE DIHYDROCHLORIDE Histamine H1 receptor antagonist 4 DailyMed
CHEMBL1201659 CHLORPHENIRAMINE POLISTIREX Histamine H1 receptor antagonist 4 PubMed PubMed
CHEMBL1201747 ALCAFTADINE Histamine H1 receptor antagonist 4 DailyMed
CHEMBL1201759 BEPOTASTINE BESYLATE Histamine H1 receptor antagonist 4 DailyMed FDA
CHEMBL1237102 LEVOCABASTINE HYDROCHLORIDE Histamine H1 receptor antagonist 4 DailyMed
CHEMBL1713082 TRIMEPRAZINE TARTRATE Histamine H1 receptor antagonist 4 PubMed PubMed
CHEMBL2103739 EMEDASTINE DIFUMARATE Histamine H1 receptor antagonist 4 DailyMed
CHEMBL3544908 AZATADINE MALEATE Histamine H1 receptor antagonist 4 PubMed
CHEMBL2107339 ESMIRTAZAPINE MALEATE Histamine H1 receptor antagonist 3 PubMed PubMed
CHEMBL539843 VAPITADINE DIHYDROCHLORIDE Histamine H1 receptor antagonist 2 Other
CHEMBL3545287 LY2624803 Histamine H1 receptor antagonist 2 Other PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000196639
Ensembl ENSG00000196639
GO Cellular Component GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO Molecular Function GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0004969 (histamine receptor activity)
GO Biological Process GO:0006954 (inflammatory response)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007200 (phospholipase C-activating G-protein coupled receptor signaling pathway)
GO:0007613 (memory)
GO:0008542 (visual learning)
GO:0019229 (regulation of vasoconstriction)
GO:0032962 (positive regulation of inositol trisphosphate biosynthetic process)
GO:0043114 (regulation of vascular permeability)
GO:0045907 (positive regulation of vasoconstriction)
GO:0048016 (inositol phosphate-mediated signaling)
GO:0048167 (regulation of synaptic plasticity)
GO:0048245 (eosinophil chemotaxis)
GO:0050804 (modulation of synaptic transmission)
GO:0071420 (cellular response to histamine)
Wikipedia Histamine_H1_receptor

Target Cross References - Protein

canSAR P35367
Human Protein Atlas ENSG00000196639
IntAct P35367
Guide to Pharmacology 262
Open Targets ENSG00000196639
PharmGKB PA29456
Pharos P35367 (Tclin)
Reactome R-HSA-390650 (Histamine receptors.)
R-HSA-416476 (G alpha (q) signalling events.)
UniProt A8K047 P35367 Q6P9E5

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR000921 (Histamine_H1_rcpt.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)

Target Cross References - Structure

PDBe 3RZE
CREDO 3RZE
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