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Assay Detail

CHEMBL4018830

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

Functional
Agonist activity at human GLP1 receptor expressed in HEK293 cells harboring mCerulean and mCitrine fused Epac protein assessed as increase in cAMP level up to 30 mins by fluorescence assay
9
Total Activities
9
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-like peptide 1 receptor (CHEMBL1784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Peptide Half-Life Extension: Divalent, Small-Molecule Albumin Interactions Direct the Systemic Properties of Glucagon-Like Peptide 1 (GLP-1) Analogues.
Bech EM, Martos-Maldonado MC, Wismann P, Sørensen KK, van Witteloostuijn SB, Thygesen MB, Vrang N, Jelsing J, Pedersen SL, Jensen KJ.
J Med Chem (2017) 60 : 7434 -7446
PubMed 28771355 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 9.92 10.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3616711 1 10.64
CHEMBL410972 1 10.36
CHEMBL4524066 1 10.17
CHEMBL4073765 1 10.17
CHEMBL4083273 1 9.93
CHEMBL4062410 1 9.83
CHEMBL4100575 1 9.66
CHEMBL4103967 1 9.28
CHEMBL4079706 1 9.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3616711 EC50 = 0.023 nM 10.64
CHEMBL410972 EC50 = 0.044 nM 10.36
CHEMBL4524066 EC50 = 0.067 nM 10.17
CHEMBL4073765 EC50 = 0.068 nM 10.17
CHEMBL4083273 EC50 = 0.118 nM 9.93
CHEMBL4062410 EC50 = 0.148 nM 9.83
CHEMBL4100575 EC50 = 0.221 nM 9.66
CHEMBL4103967 EC50 = 0.522 nM 9.28
CHEMBL4079706 EC50 = 0.547 nM 9.26