Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4220182

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

Functional
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
14
Total Activities
14
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

Optimization of peptide-based polyagonists for treatment of diabetes and obesity.
Knerr PJ, Finan B, Gelfanov V, Perez-Tilve D, Tschöp MH, DiMarchi RD.
Bioorg Med Chem (2018) 26 : 2873 -2881
PubMed 29153547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 10.12 10.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4226451 1 10.80
CHEMBL4226514 1 10.55
CHEMBL4227045 1 10.52
CHEMBL4226613 1 10.51
CHEMBL4225340 1 10.39
CHEMBL4227861 1 9.82
CHEMBL4225594 1 8.28
CHEMBL4229251 1 -
CHEMBL4224701 1 -
CHEMBL4225795 1 -
CHEMBL4224968 1 -
CHEMBL4226185 1 -
CHEMBL4227180 1 -
CHEMBL4226634 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4226451 EC50 = 0.016 nM 10.80
CHEMBL4226514 EC50 = 0.028 nM 10.55
CHEMBL4227045 EC50 = 0.03 nM 10.52
CHEMBL4226613 EC50 = 0.031 nM 10.51
CHEMBL4225340 EC50 = 0.041 nM 10.39
CHEMBL4227861 EC50 = 0.15 nM 9.82
CHEMBL4225594 EC50 = 5.225 nM 8.28
CHEMBL4229251 EC50 = 0.003 nM -
CHEMBL4224701 EC50 = 0.005 nM -
CHEMBL4225795 EC50 = 0.006 nM -
CHEMBL4224968 EC50 = 0.005 nM -
CHEMBL4226185 EC50 = 0.009 nM -
CHEMBL4227180 EC50 = 0.004 nM -
CHEMBL4226634 EC50 = 0.007 nM -