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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL4422
Preferred Name Free fatty acid receptor 1
Synonyms FFAR1 | Free fatty acid receptor 1 | G-protein coupled receptor 40 | GPR40
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > small molecule receptor (family a gpcr) > lipid-like ligand receptor (family a gpcr) > free fatty acid receptor

Target Components

Component Description Relationship Accession
Free fatty acid receptor 1 SINGLE PROTEIN O14842

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1829174 FASIGLIFAM Free fatty acid receptor 1 positive allosteric modulator 3 PubMed PubMed
CHEMBL3545086 LY2881835 Free fatty acid receptor 1 agonist 1 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000126266
Ensembl ENSG00000126266
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:0005085 (guanyl-nucleotide exchange factor activity)
GO:0008289 (lipid binding)
GO:0045125 (bioactive lipid receptor activity)
GO Biological Process GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0030073 (insulin secretion)
GO:0032024 (positive regulation of insulin secretion)
GO:0042593 (glucose homeostasis)
GO:0043547 (positive regulation of GTPase activity)
GO:0051928 (positive regulation of calcium ion transport)
GO:0070542 (response to fatty acid)
Wikipedia Free_fatty_acid_receptor_1

Target Cross References - Protein

canSAR O14842
Human Protein Atlas ENSG00000126266
Guide to Pharmacology 225
Open Targets ENSG00000126266
PharmGKB PA28887
Pharos O14842 (Tchem)
Reactome R-HSA-381771 (Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1).)
R-HSA-400511 (Synthesis, secretion, and inactivation of Glucose-dependent Insulinotropic Polypeptide (GIP).)
R-HSA-416476 (G alpha (q) signalling events.)
R-HSA-434316 (Fatty Acids bound to GPR40 (FFAR1) regulate insulin secretion.)
R-HSA-444209 (Free fatty acid receptors.)
UniProt O14842 Q0VAS2 Q4VBL4

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR013312 (GPR40-rel_orph.)
IPR013313 (GPR40_recept_FA.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)

Target Cross References - Structure