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Assay Detail

CHEMBL3868427

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

Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
4
Total Activities
4
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

Free fatty acid receptor 1 (CHEMBL4422)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space.
Chen C, Li H, Long YQ.
Bioorg Med Chem Lett (2016) 26 : 5603 -5612
PubMed 27825762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.80 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3927519 1 6.92
CHEMBL3958983 1 6.84
CHEMBL3955132 1 6.82
CHEMBL3915620 LY2881835 1.0 1 6.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3927519 EC50 = 119.0 nM 6.92
CHEMBL3958983 EC50 = 146.0 nM 6.84
CHEMBL3955132 EC50 = 152.0 nM 6.82
CHEMBL3915620 LY2881835 EC50 = 233.0 nM 6.63