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Assay Detail

CHEMBL4124800

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Functional
Agonist activity at human GLP1R expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
16
Total Activities
16
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

Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists Specifically Optimized for Multidose Formulations.
Evers A, Bossart M, Pfeiffer-Marek S, Elvert R, Schreuder H, Kurz M, Stengelin S, Lorenz M, Herling A, Konkar A, Lukasczyk U, Pfenninger A, Lorenz K, Haack T, Kadereit D, Wagner M.
J Med Chem (2018) 61 : 5580 -5593
PubMed 29879354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 10.32 10.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5314341 GLUCAGON 4.0 1 10.36
CHEMBL4130044 1 10.28
CHEMBL414357 EXENATIDE 4.0 1 -
CHEMBL4128125 1 -
CHEMBL4128276 1 -
CHEMBL4524066 1 -
CHEMBL4127525 1 -
CHEMBL4129347 1 -
CHEMBL4126027 1 -
CHEMBL4126953 1 -
CHEMBL4130225 1 -
CHEMBL4128194 1 -
CHEMBL4126812 1 -
CHEMBL4130148 1 -
CHEMBL4128112 1 -
CHEMBL4126738 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5314341 GLUCAGON EC50 = 0.0439 nM 10.36
CHEMBL4130044 EC50 = 0.0525 nM 10.28
CHEMBL414357 EXENATIDE EC50 = 0.0004 nM -
CHEMBL4128125 EC50 = 0.0039 nM -
CHEMBL4128276 EC50 = 0.0009 nM -
CHEMBL4524066 EC50 = 0.0064 nM -
CHEMBL4127525 EC50 = 0.0025 nM -
CHEMBL4129347 EC50 = 0.0014 nM -
CHEMBL4126027 EC50 = 0.0064 nM -
CHEMBL4126953 EC50 = 0.0022 nM -
CHEMBL4130225 EC50 = 0.0022 nM -
CHEMBL4128194 EC50 = 0.0048 nM -
CHEMBL4126812 EC50 = 0.0053 nM -
CHEMBL4130148 EC50 = 0.008 nM -
CHEMBL4128112 EC50 > 1.0 10'8pM -
CHEMBL4126738 EC50 = 0.0018 nM -