ChEMBL logo


ChEMBL Statistics
  Loading Statistics...

Target Report Card

Target Name and Classification

Target ID CHEMBL264
Preferred Name Histamine H3 receptor
Synonyms G-protein coupled receptor 97 | GPCR97 | H3R | HH3R | HRH3 | Histamine H3 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 H3 receptor SINGLE PROTEIN Q9Y5N1

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111378 Histamine receptor (H3 and H4) SELECTIVITY GROUP

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL24441 BETAHISTINE Histamine H3 receptor antagonist 4 PubMed PubMed PubMed PubMed PubMed PubMed
CHEMBL462605 PITOLISANT Histamine H3 receptor inverse agonist 4 PubMed PubMed
CHEMBL517140 GSK189254 Histamine H3 receptor antagonist 2 PubMed
CHEMBL476323 MK-0249 Histamine H3 receptor inverse agonist 2 PubMed PubMed
CHEMBL2103862 BAVISANT Histamine H3 receptor antagonist 2 PubMed
CHEMBL2151197 PF-03654746 Histamine H3 receptor antagonist 2 PubMed PubMed
CHEMBL2206292 PF-03654764 Histamine H3 receptor antagonist 2 PubMed
CHEMBL3092650 GSK239512 Histamine H3 receptor antagonist 2 PubMed
CHEMBL3545029 ABT-288 Histamine H3 receptor antagonist 2 PubMed
CHEMBL3545030 JNJ-17216498 Histamine H3 receptor antagonist 2 PubMed
CHEMBL1829335 IRDABISANT Histamine H3 receptor antagonist 1 PubMed PubMed
CHEMBL2106003 CIPRALISANT MALEATE Histamine H3 receptor agonist 1 PubMed PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000101180
Ensembl ENSG00000101180
GO Cellular Component GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0045202 (synapse)
GO:0098793 (presynapse)
GO Molecular Function GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0004969 (histamine receptor activity)
GO Biological Process GO:0001505 (regulation of neurotransmitter levels)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007187 (G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger)
GO:0007194 (negative regulation of adenylate cyclase activity)
GO:0007269 (neurotransmitter secretion)
GO:0014050 (negative regulation of glutamate secretion)
GO:0014061 (regulation of norepinephrine secretion)
GO:0014063 (negative regulation of serotonin secretion)
GO:0050890 (cognition)
Wikipedia Histamine_H3_receptor

Target Cross References - Protein

canSAR Q9Y5N1
Human Protein Atlas ENSG00000101180
IntAct Q9Y5N1
Guide to Pharmacology 264
MICAD NBK23693 (Histamine H3 receptor)
Open Targets ENSG00000101180
PharmGKB PA29458
Pharos Q9Y5N1 (Tclin)
Reactome R-HSA-390650 (Histamine receptors.)
R-HSA-418594 (G alpha (i) signalling events.)
UniProt Q4QRI7 Q9GZX2 Q9H4K8 Q9Y5N1

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR003980 (Histamine_H3_rcpt.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)