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Assay Detail

CHEMBL5349699

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

Binding
Agonist activity at human GPR40/Galpha-16 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GPR40-Galpha16 (CHEMBL5482994)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of orally effective and safe GPR40 agonists by incorporating a chiral, rigid and polar sulfoxide into β-position to the carboxylic acid.
Chen C, Guo SM, Sun Y, Li H, Hu N, Yao K, Ni H, Xia Z, Xu B, Xie X, Long YQ.
Eur J Med Chem (2023) 251 : 115267 -115267
PubMed 36933395 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.76 7.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5422928 1 7.56
CHEMBL1829174 FASIGLIFAM 3.0 1 7.45
CHEMBL2151289 1 7.03
CHEMBL267476 LINOLEIC ACID 2.0 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5422928 EC50 = 27.4 nM 7.56
CHEMBL1829174 FASIGLIFAM EC50 = 35.8 nM 7.45
CHEMBL2151289 EC50 = 93.3 nM 7.03
CHEMBL267476 LINOLEIC ACID EC50 = 10100.0 nM 5.00