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

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ChEMBL ligand: CHEMBL266481 (Baqsimi, Glucagen Hypokit, Glucagon, Glucagon Emergency Kit, Glucagon recombinant, Gvoke hypopen, Gvoke pfs)
  • 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]
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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]
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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 F 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 F 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 F 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 F 10.22 pEC50 0.06 nM EC50 J Med Chem (2017) 60: 4293-4303 [PMID:28448133]
ChEMBL Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting F 10.67 pEC50 0.02 nM EC50 J Med Chem (2016) 59: 8061-8067 [PMID:27509198]
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]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL Activation of human GCCR expressed in human HEK293 cells assessed as luminescence signal incubated for 16 hrs at 37C measured by CRE-driven luciferase reporter assay B 10.52 pEC50 0.03 nM EC50 J Med Chem (2021) 64: 13893-13901 [PMID:34506138]
ChEMBL Activation of human GCCR expressed in human CHO-K1 cell lines assessed as intracellular cAMP generation incubated for 30 mins measured by HTRF assay B 10.7 pEC50 0.02 nM EC50 J Med Chem (2021) 64: 13893-13901 [PMID:34506138]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]