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Assay Detail

CHEMBL4132520

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

Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
28
Total Activities
28
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

A novel glucagon-like peptide-1/glucagon receptor dual agonist exhibits weight-lowering and diabetes-protective effects.
Zhou J, Cai X, Huang X, Dai Y, Sun L, Zhang B, Yang B, Lin H, Huang W, Qian H.
Eur J Med Chem (2017) 138 : 1158 -1169
PubMed 28772236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 8.57 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4163714 1 9.34
CHEMBL4170727 1 9.12
CHEMBL4174154 1 9.07
CHEMBL4166241 1 9.05
CHEMBL5314341 GLUCAGON 4.0 1 9.01
CHEMBL4098545 1 8.91
CHEMBL4167331 1 8.90
CHEMBL4162383 1 8.89
CHEMBL4160347 1 8.85
CHEMBL4159256 1 8.85
CHEMBL4167169 1 8.85
CHEMBL4173061 1 8.80
CHEMBL4175452 1 8.78
CHEMBL4169653 1 8.62
CHEMBL4163731 1 8.55
CHEMBL4174404 1 8.55
CHEMBL4177064 1 8.52
CHEMBL4172444 1 8.47
CHEMBL4174382 1 8.41
CHEMBL4165144 1 8.36
CHEMBL4159003 1 8.35
CHEMBL4160365 1 8.32
CHEMBL4159426 1 8.28
CHEMBL4161800 1 8.16
CHEMBL4159275 1 7.84
CHEMBL4170976 1 7.73
CHEMBL4162789 1 6.91
CHEMBL428139 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4163714 EC50 = 0.46 nM 9.34
CHEMBL4170727 EC50 = 0.75 nM 9.12
CHEMBL4174154 EC50 = 0.86 nM 9.07
CHEMBL4166241 EC50 = 0.9 nM 9.05
CHEMBL5314341 GLUCAGON EC50 = 0.97 nM 9.01
CHEMBL4098545 EC50 = 1.23 nM 8.91
CHEMBL4167331 EC50 = 1.27 nM 8.90
CHEMBL4162383 EC50 = 1.29 nM 8.89
CHEMBL4160347 EC50 = 1.41 nM 8.85
CHEMBL4159256 EC50 = 1.41 nM 8.85
CHEMBL4167169 EC50 = 1.43 nM 8.85
CHEMBL4173061 EC50 = 1.57 nM 8.80
CHEMBL4175452 EC50 = 1.68 nM 8.78
CHEMBL4169653 EC50 = 2.4 nM 8.62
CHEMBL4163731 EC50 = 2.84 nM 8.55
CHEMBL4174404 EC50 = 2.81 nM 8.55
CHEMBL4177064 EC50 = 2.99 nM 8.52
CHEMBL4172444 EC50 = 3.36 nM 8.47
CHEMBL4174382 EC50 = 3.88 nM 8.41
CHEMBL4165144 EC50 = 4.37 nM 8.36
CHEMBL4159003 EC50 = 4.49 nM 8.35
CHEMBL4160365 EC50 = 4.78 nM 8.32
CHEMBL4159426 EC50 = 5.3 nM 8.28
CHEMBL4161800 EC50 = 6.99 nM 8.16
CHEMBL4159275 EC50 = 14.6 nM 7.84
CHEMBL4170976 EC50 = 18.64 nM 7.73
CHEMBL4162789 EC50 = 122.57 nM 6.91
CHEMBL428139 EC50 - -