exendin-4   Click here for help

GtoPdb Ligand ID: 1135

Synonyms: AC 2993 | AC002993 | AC2993A | Bydureon® | Byetta®
Approved drug
exendin-4 is an approved drug (FDA (2005), EMA (2006))
Comment: This peptide is found in the venom of the Gila monster Heloderma suspectum. Exenatide is the synthetic form of the peptide used in clinical practice. Exendin-4 is a GLP-1 analogue/mimetic [1]. There is some ambiguity surrounding the exact stereochemistry of exendin-4. Representations of the peptide's full chemical structure can be accessed using the PubChem, ChEMBL and ChEBI links that we provide in the Database Links table.
Click here for help
IUPHAR Pharmacology Education Project (PEP) logo

View more information in the IUPHAR Pharmacology Education Project: exenatide

Bioactivity Comments
Binds to the GLP-1 receptor.
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
GLP-1 receptor Primary target of this compound Hs Agonist Full agonist 8.7 – 9.0 pKi - 2
pKi 8.7 – 9.0 (Ki 1.99x10-9 – 1x10-9 M) [2]
GLP-1 receptor Primary target of this compound Hs Agonist Agonist 9.2 pIC50 - 3
pIC50 9.2 (IC50 6.6x10-10 M) [3]
Description: Displacement of GLP-1 from hGLP-1 receptor expressed in CHOK1 cells by exendin-4