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Assay Detail

CHEMBL4713467

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Functional
Agonist activity at rat glucagon receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation by FRET assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucagon receptor (CHEMBL4720)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design and Evaluation of Peptide Dual-Agonists of GLP-1 and NPY2 Receptors for Glucoregulation and Weight Loss with Mitigated Nausea and Emesis.
Milliken BT,Elfers C,Chepurny OG,Chichura KS,Sweet IR,Borner T,Hayes MR,De Jonghe BC,Holz GG,Roth CL,Doyle RP
J Med Chem (2021) 64 : 1127 -1138
PubMed 33449689 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.52 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4749279 1 7.52
CHEMBL439904 1 -
CHEMBL414357 EXENATIDE 4.0 1 -
CHEMBL4796216 1 -
CHEMBL4748874 1 -
CHEMBL4741000 1 -
CHEMBL4759334 1 -
CHEMBL4752195 1 -
CHEMBL4751466 1 -
CHEMBL4281479 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4749279 EC50 = 30.0 nM 7.52
CHEMBL439904 EC50 - -
CHEMBL414357 EXENATIDE EC50 - -
CHEMBL4796216 EC50 - -
CHEMBL4748874 EC50 - -
CHEMBL4741000 EC50 > 3000.0 nM -
CHEMBL4759334 EC50 > 3000.0 nM -
CHEMBL4752195 EC50 > 3000.0 nM -
CHEMBL4751466 EC50 > 3000.0 nM -
CHEMBL4281479 EC50 - -