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Assay Detail

CHEMBL4385324

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Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
10
Total Activities
10
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

Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.
Huang H, Meegalla SK, Lanter JC, Winters MP, Zhao S, Littrell J, Qi J, Rady B, Lee PS, Liu J, Martin T, Lam WW, Xu F, Lim HK, Wilde T, Silva J, Otieno M, Pocai A, Player MR.
ACS Med Chem Lett (2019) 10 : 16 -21
PubMed 30655940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 8.67 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4541658 1 9.96
CHEMBL4463571 1 9.70
CHEMBL4457303 1 9.60
CHEMBL4591657 1 9.03
CHEMBL4534836 1 8.96
CHEMBL4513748 1 8.66
CHEMBL4464769 1 8.21
CHEMBL4459220 1 7.80
CHEMBL1829174 FASIGLIFAM 3.0 1 7.51
CHEMBL4443853 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4541658 EC50 = 0.11 nM 9.96
CHEMBL4463571 EC50 = 0.2 nM 9.70
CHEMBL4457303 EC50 = 0.25 nM 9.60
CHEMBL4591657 EC50 = 0.94 nM 9.03
CHEMBL4534836 EC50 = 1.1 nM 8.96
CHEMBL4513748 EC50 = 2.2 nM 8.66
CHEMBL4464769 EC50 = 6.1 nM 8.21
CHEMBL4459220 EC50 = 16.0 nM 7.80
CHEMBL1829174 FASIGLIFAM EC50 = 31.0 nM 7.51
CHEMBL4443853 EC50 = 54.0 nM 7.27