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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL1941
Preferred Name Histamine H2 receptor
Synonyms Gastric receptor I | H2R | HH2R | HRH2 | Histamine H2 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 H2 receptor SINGLE PROTEIN P25021

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL30 CIMETIDINE Histamine H2 receptor antagonist 4 ISBN
CHEMBL653 NIZATIDINE Histamine H2 receptor antagonist 4 DailyMed
CHEMBL902 FAMOTIDINE Histamine H2 receptor antagonist 4 DailyMed
CHEMBL1689 TOLAZOLINE HYDROCHLORIDE Histamine H2 receptor agonist 4 DailyMed DailyMed ISBN PubMed PubMed
CHEMBL1200949 BETAZOLE HYDROCHLORIDE Histamine H2 receptor agonist 4 ISBN PubMed
CHEMBL1200988 METHANTHELINE BROMIDE Histamine H2 receptor antagonist 4 PubMed
CHEMBL1201051 CIMETIDINE HYDROCHLORIDE Histamine H2 receptor antagonist 4 ISBN
CHEMBL2110372 RANITIDINE HYDROCHLORIDE Histamine H2 receptor antagonist 4 DailyMed FDA
CHEMBL2111286 RANITIDINE BISMUTH CITRATE Histamine H2 receptor antagonist 4 DailyMed FDA

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000113749
Ensembl ENSG00000113749
GO Cellular Component 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:0001696 (gastric acid secretion)
GO:0001697 (histamine-induced gastric acid secretion)
GO:0001698 (gastrin-induced gastric acid secretion)
GO:0003382 (epithelial cell morphogenesis)
GO:0006955 (immune response)
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:0007613 (memory)
GO:0008542 (visual learning)
GO:0045907 (positive regulation of vasoconstriction)
GO:0048167 (regulation of synaptic plasticity)
GO:0048565 (digestive tract development)
GO:0048732 (gland development)
GO:1901998 (toxin transport)
Wikipedia Histamine_H2_receptor

Target Cross References - Protein

canSAR P25021
Human Protein Atlas ENSG00000113749
Guide to Pharmacology 263
Open Targets ENSG00000113749
PharmGKB PA29457
Pharos P25021 (Tclin)
Reactome R-HSA-390650 (Histamine receptors.)
R-HSA-418555 (G alpha (s) signalling events.)
UniProt B5BUP7 P25021 Q14464 Q7Z5R9

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR000503 (Histamine_H2_rcpt.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)