glucagon [Ligand Id: 1136] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL266481 (Glucagon, Glucagon Emergency Kit, Glucagon Recombinant, Glucagen Hypokit)
  • Glucagon-like peptide 1 receptor in Macaca fascicularis [ChEMBL: CHEMBL4295545] [UniProtKB: F8V479]
  • 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 Mouse [ChEMBL: CHEMBL1075290] [GtoPdb: 249] [UniProtKB: O35659]
  • This target only has 1 pki data point
1 CHEMBL266481_lig_chart_1 Glucagon-like peptide 1 receptor Macaca fascicularisHumanMouse
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  • glucagon receptor/Glucagon receptor in Human [ChEMBL: CHEMBL1985] [GtoPdb: 251] [UniProtKB: P47871]
  • glucagon receptor/Glucagon receptor in Mouse [ChEMBL: CHEMBL4773] [GtoPdb: 251] [UniProtKB: Q61606]
  • glucagon receptor/Glucagon receptor in Rat [ChEMBL: CHEMBL4720] [GtoPdb: 251] [UniProtKB: P30082]
  • This target only has 0 pki data point
2 CHEMBL266481_lig_chart_2 Glucagon receptor HumanMouseRat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Glucagon-like peptide 1 receptor in Macaca fascicularis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295545] [UniProtKB: F8V479]
ChEMBL Agonist activity at monkey GLP1R expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay B 10.51 pEC50 0.03 nM EC50 J Med Chem (2018) 61: 5580-5593 [PMID:29879354]
GLP-1 receptor/Glucagon-like peptide 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220]
GtoPdb - - 7 pKi - - - Mol. Endocrinol. (2005) 19: 812-23 [PMID:15528268]
ChEMBL Agonist activity at human GLP1 receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assay F 7.39 pEC50 41 nM EC50 Bioorg Med Chem (2018) 26: 2873-2881 [PMID:29153547]
ChEMBL Agonist activity at full length human GLP1R expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay F 8.11 pEC50 7.7 nM EC50 Eur J Med Chem (2017) 138: 1158-1169 [PMID:28772236]
ChEMBL Agonist activity at human GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay B 8.43 pEC50 3.74 nM EC50 J Med Chem (2017) 60: 4293-4303 [PMID:28448133]
ChEMBL Agonist activity at GLP1R expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay F 8.48 pEC50 3.3 nM EC50 Nat. Chem. Biol. (2009) 5: 749-757 [PMID:19597507]
ChEMBL Agonist activity at human GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay B 10.36 pEC50 0.04 nM EC50 J Med Chem (2017) 60: 4293-4303 [PMID:28448133]
ChEMBL Agonist activity at human GLP1R expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay F 10.36 pEC50 0.04 nM EC50 J Med Chem (2018) 61: 5580-5593 [PMID:29879354]
GLP-1 receptor/Glucagon-like peptide 1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075290] [GtoPdb: 249] [UniProtKB: O35659]
ChEMBL Agonist activity at mouse GLP1 receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assay F 8.59 pEC50 2.6 nM EC50 Bioorg Med Chem (2018) 26: 2873-2881 [PMID:29153547]
ChEMBL Agonist activity at mouse GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay B 10.36 pEC50 0.04 nM EC50 J Med Chem (2017) 60: 4293-4303 [PMID:28448133]
glucagon receptor/Glucagon receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1985] [GtoPdb: 251] [UniProtKB: P47871]
GtoPdb - - 9 pEC50 - - - Science (1969) 164: 566-7 [PMID:4305077]
ChEMBL Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay F 9.01 pEC50 0.97 nM EC50 Eur J Med Chem (2017) 138: 1158-1169 [PMID:28772236]
ChEMBL Agonist activity at human GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assay F 9.3 pEC50 0.5 nM EC50 Bioorg Med Chem (2018) 26: 2873-2881 [PMID:29153547]
ChEMBL Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay F 10.15 pEC50 0.07 nM EC50 Nat. Chem. Biol. (2009) 5: 749-757 [PMID:19597507]
ChEMBL Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay B 10.22 pEC50 0.06 nM EC50 J Med Chem (2017) 60: 4293-4303 [PMID:28448133]
glucagon receptor/Glucagon receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4773] [GtoPdb: 251] [UniProtKB: Q61606]
ChEMBL Agonist activity at mouse GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assay F 10.7 pEC50 0.02 nM EC50 Bioorg Med Chem (2018) 26: 2873-2881 [PMID:29153547]
glucagon receptor/Glucagon receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4720] [GtoPdb: 251] [UniProtKB: P30082]
ChEMBL Compound was tested for its ability to displace [125I]glucagon from the glucagon receptor B 8.82 pIC50 1.5 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1849-1852
ChEMBL Glucagon receptor binding measured as 50% inhibitory concentration B 8.82 pIC50 1.5 nM IC50 J. Med. Chem. (2001) 44: 3109-3116 [PMID:11543679]
ChEMBL Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon B 8.82 pIC50 1.5 nM IC50 J. Med. Chem. (1997) 40: 2555-2562 [PMID:9258362]
ChEMBL In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay B 8.82 pIC50 1.5 nM IC50 J. Med. Chem. (2000) 43: 1714-1722 [PMID:10794689]
ChEMBL inhibition of [125]glucagon specific binding. B 8.82 pIC50 1.5 nM IC50 J. Med. Chem. (2001) 44: 1372-1379 [PMID:11311060]
ChEMBL cAMP accumulation in rat hepatocytes in the presence rolipram F 8.1 pEC50 8 nM EC50 J. Med. Chem. (1997) 40: 2555-2562 [PMID:9258362]
ChEMBL In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay B 8.3 pEC50 5 nM EC50 J. Med. Chem. (2000) 43: 1714-1722 [PMID:10794689]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]