exendin-4 [Ligand Id: 1135] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL414357 (AC-2993A, LY-2148568, AC-2993LAR, Exenatide, AC-002993, AC002993, DA-3091, Bydureon bcise, EXENDIN-4, AC-2993, AC2993A, ITCA-650, LY2148568, Byetta, AC 2993, Exenatide Synthetic, AC2993, Bydureon pen, Bydureon, Exenatide synthetic)
  • GLP-1 receptor/Glucagon-like peptide 1 receptor in Human [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220]
  • GLP-1 receptor/Glucagon-like peptide 1 receptor in Rat [ChEMBL: CHEMBL5862] [GtoPdb: 249] [UniProtKB: P32301]
  • This target only has 1 pki data point
  • 0
1 CHEMBL414357_lig_chart_1 Glucagon-like peptide 1 receptor HumanRat
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  • glucagon receptor/Glucagon receptor in Mouse [ChEMBL: CHEMBL4773] [GtoPdb: 251] [UniProtKB: Q61606]
  • This target only has 0 pki data point
  • 0
2 CHEMBL414357_lig_chart_2 Glucagon receptor Mouse
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GLP-1 receptor/Glucagon-like peptide 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220]
GtoPdb - - 9 pKi 1 nM Ki Mol Endocrinol (2005) 19: 812-23 [PMID:15528268]
GtoPdb Displacement of GLP-1 from hGLP-1 receptor expressed in CHOK1 cells by exendin-4 - 9.18 pIC50 0.66 nM IC50 J Med Chem (2008) 51: 2758-65 [PMID:18412318]
ChEMBL Displacement of [125I]GLP1 from human GLP1R expressed in CHOK1 cells B 9.18 pIC50 0.66 nM IC50 J. Med. Chem. (2008) 51: 2758-2765 [PMID:18412318]
ChEMBL Agonist activity at human GLP-1 receptor expressed in CHO cells assessed as increase in cAMP production F 10 pEC50 0.1 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 4631-4634 [PMID:20576431]
GLP-1 receptor/Glucagon-like peptide 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5862] [GtoPdb: 249] [UniProtKB: P32301]
ChEMBL Displacement of [125I]exendin-4 from GLP1 receptor in rat RINm5F cells after 2 hrs by gamma counting B 9.85 pIC50 0.14 nM IC50 J. Med. Chem. (2009) 52: 6889-6896 [PMID:19827752]
glucagon receptor/Glucagon receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4773] [GtoPdb: 251] [UniProtKB: Q61606]
ChEMBL Agonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay B 5 pEC50 >10000 nM EC50 J Med Chem (2017) 60: 4293-4303 [PMID:28448133]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]