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Assay Detail

CHEMBL4052169

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

Functional
Agonist activity at human GLP-1 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-like peptide 1 receptor (CHEMBL1784)
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 10.60 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4090347 1 10.82
CHEMBL4065846 1 10.76
CHEMBL4069307 1 10.76
CHEMBL4098545 1 10.68
CHEMBL4101203 1 10.65
CHEMBL4098061 1 10.65
CHEMBL4060629 1 10.60
CHEMBL4082505 1 10.50
CHEMBL5314341 GLUCAGON 4.0 1 10.36
CHEMBL4074468 1 10.25
CHEMBL414357 EXENATIDE 4.0 1 -
CHEMBL410972 1 -
CHEMBL4524066 1 -
CHEMBL4093458 1 -
CHEMBL4100420 1 -
CHEMBL4076828 1 -
CHEMBL4080035 1 -
CHEMBL4072029 1 -
CHEMBL4086979 1 -
CHEMBL4065550 1 -
CHEMBL4095024 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4090347 EC50 = 0.0153 nM 10.82
CHEMBL4065846 EC50 = 0.0174 nM 10.76
CHEMBL4069307 EC50 = 0.0172 nM 10.76
CHEMBL4098545 EC50 = 0.0209 nM 10.68
CHEMBL4101203 EC50 = 0.0222 nM 10.65
CHEMBL4098061 EC50 = 0.0222 nM 10.65
CHEMBL4060629 EC50 = 0.0254 nM 10.60
CHEMBL4082505 EC50 = 0.0313 nM 10.50
CHEMBL5314341 GLUCAGON EC50 = 0.0439 nM 10.36
CHEMBL4074468 EC50 = 0.0558 nM 10.25
CHEMBL414357 EXENATIDE EC50 = 0.0004 nM -
CHEMBL410972 EC50 = 0.0009 nM -
CHEMBL4524066 EC50 = 0.0064 nM -
CHEMBL4093458 EC50 = 0.0018 nM -
CHEMBL4100420 EC50 = 0.0012 nM -
CHEMBL4076828 EC50 = 0.0007 nM -
CHEMBL4080035 EC50 = 0.0082 nM -
CHEMBL4072029 EC50 = 0.0022 nM -
CHEMBL4086979 EC50 = 0.0039 nM -
CHEMBL4065550 EC50 = 0.0052 nM -
CHEMBL4095024 EC50 = 0.0058 nM -