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Assay Detail

CHEMBL4713470

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Functional
Agonist activity at rat GLP-1R expressed in HEK293 cells assessed as stimulation of cAMP accumulation by FRET assay
2
Total Activities
2
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-like peptide 1 receptor (CHEMBL5862)
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 2 9.62 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4749279 1 9.92
CHEMBL4751466 1 9.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4749279 EC50 = 0.12 nM 9.92
CHEMBL4751466 EC50 = 0.48 nM 9.32