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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL1985
Preferred Name Glucagon receptor
Synonyms GCGR | GL-R | Glucagon receptor
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family b g protein-coupled receptor > peptide receptor (family b gpcr) > glucagon-like receptor > glucagon receptor

Target Components

Component Description Relationship Accession
Glucagon receptor SINGLE PROTEIN P47871

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL266481 GLUCAGON Glucagon receptor agonist 4 PubMed
CHEMBL1201508 GLUCAGON HYDROCHLORIDE RECOMBINANT Glucagon receptor agonist 4 PubMed
CHEMBL1201618 GLUCAGON HYDROCHLORIDE Glucagon receptor agonist 4 PubMed
CHEMBL1933349 MK-0893 Glucagon receptor antagonist 2 PubMed
CHEMBL3544946 PF-06291874 Glucagon receptor antagonist 2
CHEMBL3545219 LY2409021 Glucagon receptor antagonist 2 PubMed
CHEMBL3545269 SAR425899 Glucagon receptor agonist 1 Other

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000215644
Ensembl ENSG00000215644
GO Cellular Component GO:0005768 (endosome)
GO:0005887 (integral component of plasma membrane)
GO:0016021 (integral component of membrane)
GO:0005886 (plasma membrane)
GO Molecular Function GO:0004967 (glucagon receptor activity)
GO:0005085 (guanyl-nucleotide exchange factor activity)
GO:0017046 (peptide hormone binding)
GO Biological Process GO:0070873 (regulation of glycogen metabolic process)
GO:0042593 (glucose homeostasis)
GO:0044281 (small molecule metabolic process)
GO:0042594 (response to starvation)
GO:0006887 (exocytosis)
GO:0007188 (adenylate cyclase-modulating G-protein coupled receptor signaling pathway)
GO:0007189 (adenylate cyclase-activating G-protein coupled receptor signaling pathway)
GO:0008217 (regulation of blood pressure)
GO:0007584 (response to nutrient)
GO:0006112 (energy reserve metabolic process)
GO:0009755 (hormone-mediated signaling pathway)
GO:0043547 (positive regulation of GTPase activity)
GO:0007166 (cell surface receptor signaling pathway)
GO:0071377 (cellular response to glucagon stimulus)
GO:0006091 (generation of precursor metabolites and energy)
Wikipedia Glucagon_receptor

Target Cross References - Protein

canSAR P47871
Human Protein Atlas ENSG00000215644
IntAct P47871
Guide to Pharmacology 251 (glucagon)
PharmGKB PA28607
UniProt Q2M3M5 P47871

Target Cross References - Domain

InterPro IPR003291 (GPCR_2_glucagon_rcpt.)
IPR003290 (GPCR_2_GLP1/glucagon_rcpt.)
IPR001879 (GPCR_2_extracellular_dom.)
IPR017983 (GPCR_2_secretin-like_CS.)
IPR000832 (GPCR_2_secretin-like.)
IPR017981 (GPCR_2-like.)
Pfam PF02793 (HRM)
PF00002 (7tm_2)

Target Cross References - Structure

PDBe 2A83 4L6R 4ERS 3CZF 4LF3