glucagon [Ligand Id: 1136] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL266481 (Glucagen Hypokit, Glucagon, Glucagon Emergency Kit) |
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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 | - | - | 7 | pKi | - | - | - | Mol Endocrinol (2005) 19: 812-23 [PMID:15528268] |
| ChEMBL | Agonist activity at human GLP-1R expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay | F | 8.42 | pEC50 | 3.8 | nM | EC50 | Eur J Med Chem (2021) 212: 113118-113118 [PMID:33422984] |
| 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 human GLP1R expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay | F | 10.24 | pEC50 | 0.06 | nM | EC50 | ACS Med Chem Lett (2022) 13: 1248-1254 [PMID:35978682] |
| 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] |
| 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 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 incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay | F | 10.1 | pEC50 | 0.08 | nM | EC50 | Eur J Med Chem (2021) 212: 113118-113118 [PMID:33422984] |
| 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] |
| glucagon receptor/Glucagon receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4773] [GtoPdb: 251] [UniProtKB: Q61606] | ||||||||
| ChEMBL | Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation | B | 9.47 | pEC50 | 0.34 | nM | EC50 | Eur J Med Chem (2020) 203: 112496-112496 [PMID:32682196] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
