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) |
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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 33:
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]
