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Assay Detail

CHEMBL3868432

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Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
3
Total Activities
3
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

Free fatty acid receptor 1 (CHEMBL1795180)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 3 7.87 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3923877 1 9.40
CHEMBL3927863 1 8.00
CHEMBL3954105 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3923877 EC50 = 0.4 nM 9.40
CHEMBL3927863 EC50 = 10.0 nM 8.00
CHEMBL3954105 EC50 = 630.0 nM 6.20