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Assay Detail

CHEMBL3868447

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Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM 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 CHO
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 7.94 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3944424 1 9.52
CHEMBL3931755 1 7.89
CHEMBL3900797 1 6.42
CHEMBL3928769 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3944424 EC50 = 0.3 nM 9.52
CHEMBL3931755 EC50 = 13.0 nM 7.89
CHEMBL3900797 EC50 = 380.0 nM 6.42
CHEMBL3928769 EC50 < 300.0 nM -