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Assay Detail

CHEMBL4052170

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucagon receptor (CHEMBL1985)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of Novel Exendin-Based Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists.
Evers A, Haack T, Lorenz M, Bossart M, Elvert R, Henkel B, Stengelin S, Kurz M, Glien M, Dudda A, Lorenz K, Kadereit D, Wagner M.
J Med Chem (2017) 60 : 4293 -4303
PubMed 28448133 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 9.58 10.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4069307 1 10.81
CHEMBL4098061 1 10.58
CHEMBL4076828 1 8.95
CHEMBL4072029 1 8.91
CHEMBL4060629 1 8.63
CHEMBL5314341 GLUCAGON 4.0 1 -
CHEMBL414357 EXENATIDE 4.0 1 -
CHEMBL410972 1 -
CHEMBL4524066 1 -
CHEMBL4093458 1 -
CHEMBL4065846 1 -
CHEMBL4101203 1 -
CHEMBL4074468 1 -
CHEMBL4100420 1 -
CHEMBL4080035 1 -
CHEMBL4090347 1 -
CHEMBL4086979 1 -
CHEMBL4065550 1 -
CHEMBL4095024 1 -
CHEMBL4098545 1 -
CHEMBL4082505 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4069307 EC50 = 0.0156 nM 10.81
CHEMBL4098061 EC50 = 0.0264 nM 10.58
CHEMBL4076828 EC50 = 1.12 nM 8.95
CHEMBL4072029 EC50 = 1.24 nM 8.91
CHEMBL4060629 EC50 = 2.32 nM 8.63
CHEMBL5314341 GLUCAGON EC50 = 0.0004 nM -
CHEMBL414357 EXENATIDE EC50 > 1.0 10'8pM -
CHEMBL410972 EC50 > 0.001 nM -
CHEMBL4524066 EC50 > 0.001 nM -
CHEMBL4093458 EC50 = 5.8 10'7pM -
CHEMBL4065846 EC50 = 5.7 10'6pM -
CHEMBL4101203 EC50 = 1.0 10'7pM -
CHEMBL4074468 EC50 = 4.2 10'7pM -
CHEMBL4100420 EC50 > 1.0 10'8pM -
CHEMBL4080035 EC50 = 0.0019 nM -
CHEMBL4090347 EC50 = 0.0089 nM -
CHEMBL4086979 EC50 = 0.0007 nM -
CHEMBL4065550 EC50 = 0.0062 nM -
CHEMBL4095024 EC50 = 0.0063 nM -
CHEMBL4098545 EC50 = 0.008 nM -
CHEMBL4082505 EC50 = 1.7 10'5pM -