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Assay Detail

CHEMBL4432349

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

Functional
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
11
Total Activities
11
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

Pyridyl-alanine as a Hydrophilic, Aromatic Element in Peptide Structural Optimization.
Mroz PA, Perez-Tilve D, Liu F, Gelfanov V, DiMarchi RD, Mayer JP.
J Med Chem (2016) 59 : 8061 -8067
PubMed 27509198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 10.28 10.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4453136 1 10.77
CHEMBL5314341 GLUCAGON 4.0 1 10.67
CHEMBL4469604 1 10.57
CHEMBL4466715 1 10.51
CHEMBL4571762 1 10.47
CHEMBL4458230 1 10.44
CHEMBL4586269 1 10.42
CHEMBL4578443 1 10.40
CHEMBL4444485 1 10.15
CHEMBL4437733 1 10.07
CHEMBL4466856 1 8.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4453136 EC50 = 0.017 nM 10.77
CHEMBL5314341 GLUCAGON EC50 = 0.0212 nM 10.67
CHEMBL4469604 EC50 = 0.0268 nM 10.57
CHEMBL4466715 EC50 = 0.0309 nM 10.51
CHEMBL4571762 EC50 = 0.0339 nM 10.47
CHEMBL4458230 EC50 = 0.0359 nM 10.44
CHEMBL4586269 EC50 = 0.0379 nM 10.42
CHEMBL4578443 EC50 = 0.0399 nM 10.40
CHEMBL4444485 EC50 = 0.0714 nM 10.15
CHEMBL4437733 EC50 = 0.0843 nM 10.07
CHEMBL4466856 EC50 = 2.325 nM 8.63