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Assay Detail

CHEMBL4671906

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

Functional
Agonist activity at human GLP-1 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
11
Total Activities
11
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

Automated Design of Macrocycles for Therapeutic Applications: From Small Molecules to Peptides and Proteins.
Sindhikara D,Wagner M,Gkeka P,Güssregen S,Tiwari G,Hessler G,Yapici E,Li Z,Evers A
J Med Chem (2020) 63 : 12100 -12115
PubMed 33017535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 10.39 10.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4755815 1 10.83
CHEMBL4098061 1 10.74
CHEMBL4761047 1 10.60
CHEMBL4745985 1 10.32
CHEMBL4745235 1 10.12
CHEMBL4762061 1 9.71
CHEMBL4751319 1 -
CHEMBL4758415 1 -
CHEMBL4756489 1 -
CHEMBL4757675 1 -
CHEMBL4741348 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4755815 EC50 = 0.0147 nM 10.83
CHEMBL4098061 EC50 = 0.0183 nM 10.74
CHEMBL4761047 EC50 = 0.0249 nM 10.60
CHEMBL4745985 EC50 = 0.0475 nM 10.32
CHEMBL4745235 EC50 = 0.0754 nM 10.12
CHEMBL4762061 EC50 = 0.194 nM 9.71
CHEMBL4751319 EC50 = 0.00813 nM -
CHEMBL4758415 EC50 = 0.0064 nM -
CHEMBL4756489 EC50 = 0.0012 nM -
CHEMBL4757675 EC50 = 0.0004 nM -
CHEMBL4741348 EC50 = 0.0074 nM -